Journal articles on the topic 'In vitro release kinetic models'
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Costa, André Lima de Oliveira, Paula Cristina Rezende Enéas, Tiago Assis Miranda, Sueli Aparecida Mingoti, Cristina Duarte Vianna Soares, and Gerson Antônio Pianetti. "In vitro dissolution kinetic for mycophenolic acid derivatives tablets." Brazilian Journal of Pharmaceutical Sciences 49, no. 2 (June 2013): 311–19. http://dx.doi.org/10.1590/s1984-82502013000200013.
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Mycophenolate mofetil (MMF) and mycophenolate sodium (MPS) are an ester and a salt of mycophenolic acid. They have different kinetic in vivo characteristics due to differences in molecular structures, physicochemical properties and formulations administered. In this study, dissolution profiles of reference products were tested in different media to evaluate the effect of pH, kinetic dissolution and the best statistical model that can be used to predict the release of both drugs. The drug release was determined by using a validated ultraviolet spectrophotometry method, λ 250 nm. The method showed to be selective, linear, precise and accurate for MMF in 0.1 M HCl and MPS in sodium phosphate buffer pH 6.8. Dissolution kinetics models of zero order, first order, Higuchi, Hixson-Crowell and Weibull were applied to data in order to select the best fit by linear regression. The regression parameters were estimated and the models were evaluated with the results of residuals and coefficient of determination. The residuals obtained from dissolution kinetics models were random, uncorrelated, and normally distributed with constant variance. The R² values (74.7% for MMF and 95.8% for MPS) demonstrated good ability of the Weibull regression to explain the variability and to predict the drugs' release.
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Quintal Martínez, Juan Pablo, Jorge Carlos Ruiz Ruiz, and Maira Rubí Segura Campos. "Release Kinetic Studies of Stevia rebaudiana Extract Capsules from Sodium Alginate and Inulin by Ionotropic Gelation." Advances in Materials Science and Engineering 2018 (July 11, 2018): 1–8. http://dx.doi.org/10.1155/2018/6354924.
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This study was oriented towards encapsulation of S. rebaudiana extract and the study of its release kinetics. The desired encapsulation was achieved by the ionotropic gelation method using sodium alginate and inulin of polymeric constituents. Characterization of the capsules was performed by micrometric properties, encapsulation efficiency, in vitro extract release analysis, and biological activity of released extract. The in vitro release profiles from different capsules were applied on different kinetic models. The prepared capsules were found spherical in shape with diameters ranging from 2.07 to 2.63 mm, having the encapsulation efficiencies of 43.77% and 56.53% for phenolic compounds and steviol glycosides, respectively. The best-fit model with the highest correlation coefficient was observed in the Ritger–Peppas model, indicating diffusion controlled principle. The release exponent n value obtained from the Korsmeyer–Peppas model varied between 0.2273 and 1.1719, confirming that the mechanism of S. rebaudiana extract bioactive compounds release was diffusion controlled.
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Kumar, B., and G. Jeyabalan. "Development of Anti-diabetic Niosomes Formulation Containing Metformin and Gliclazide." Indian Journal of Pharmaceutical and Biological Research 5, no. 02 (June 30, 2017): 24–28. http://dx.doi.org/10.30750/ijpbr.5.2.5.
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Metformin/Gliclazide niosomes were formulated with span 60 by ether injection method. Three batches MG1-MG3 were prepared in order to study influence of drug polymer ratio on the niosomes formation and in vitro drug release. The formulated niosomes were characterized by drug entrapment, vesicle size determination, and in vitro drug release. Optimized concentration of span 60 and cholesterol was found to be 1:1. In the in-vitro study, niosomes formulation of MG1 showed high percentage of drug release, 40.18 to 45.75% for about 8 hrs. This indicated that this batch of niosomes formulation exhibit sustained drug release pattern as the niosomes act as reservoir system for continuous delivery of drug. The quantity of Metformin/Gliclazide present in the niosomes and the release medium were estimated by a validated HPLC method. The formulated niosomes had acceptable physicochemical characters and released the drug over 6-8 h. The data obtained from in vitro release studies were fitted with various kinetic models and was found to follow Higuchi kinetics.
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Dewan, Irin, Md Maynul Islam, Maksud Al-Hasan, Joydeb Nath, Sefat Sultana, and Md Sohel Rana. "Surface Deposition and Coalescence and Coacervation Phase Separation Methods: In Vitro Study and Compatibility Analysis of Eudragit RS30D, Eudragit RL30D, and Carbopol-PLA Loaded Metronidazole Microspheres." Journal of Pharmaceutics 2015 (November 16, 2015): 1–10. http://dx.doi.org/10.1155/2015/254930.
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Metronidazole (MTZ) has extremely broad spectrum of protozoal and antimicrobial activity and is clinically effective in trichomoniasis, amoebic colitis, and giardiasis. This study was performed to formulate and evaluate the MTZ loaded microspheres by coacervation phase separation and surface deposition and coalescence methods using different polymers like Gelatin, Carbopol 934P, Polylactic Acid (PLA), Eudragit RS30D, and Eudragit RL30D to acquire sustained release of drug. In vitro dissolution studies were carried out in phosphate buffer (pH 7.4) for 8 hours according to USP paddle method. The maximum and minimum release of MTZ from microspheres observed were 84.81% and 76.6% for coacervation and 95.07% and 80.07% for surface deposition method, respectively, after 8 hours. Release kinetics was studied in different mathematical release models. The SEM and FTIR studies confirm good spheres and smooth surface as well as interaction between drug and polymers. Though release kinetic is uncertain, the best fit was obtained with the Korsmeyer kinetic model with release exponent (n) lying between 0.45 and 0.89. In vitro studies showed that MTZ microspheres with different polymers might be a good candidate as sustained drug delivery system to treat bacterial infections.
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Hurtado, M. González, J. Rieumont Briones, Laura M. Castro González, E. Ortiz Islas, and Inti Zumeta Dube. "Kinetic studies of the release profiles of antiepileptic drug released from a nanostructured TiO2 matrix." JOURNAL OF ADVANCES IN CHEMISTRY 12, no. 4 (December 16, 2016): 4365–73. http://dx.doi.org/10.24297/jac.v12i4.2176.
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In this paper is reported the “in vitro” release kinetic studies of antiepileptic drugs released from an inorganic, titanium oxide (TiO2) porous matrix. In order to determine the drug release mechanism, the experimental values were fitted to different mathematical models: zero-order, firs-order, Higuchi, Hixson-Crowel and Peppas. TiO2 was prepared by the sol-gel method adding valproic acid (VPA) or phenytoine (DHP) during the titanium n-butoxide hydrolysis step. The drug-TiO2 systems were observed by scanning electron microscopy. The “in vitro” release experiments were performed at laboratory scale following the United States Pharmacopeia (USP) standards. The obtained materials have a morphology of nanoparticle agglomerates. The particles have different sizes with some roughness and spherical shape. Peppas model suggests for both systems, that the release mechanism is controlled by two parallel processes. The first one is by diffusion of the drug through the matrix and the second is related to a gradient of constant diffusion by ingress of the solvent in the matrix.
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Iovanov, Rareș Iuliu, Ioan Tomuță, and Sorin Emilian Leucuța. "Development of a reservoir type prolonged release system with felodipine via simplex methodology." Medicine and Pharmacy Reports 89, no. 1 (September 28, 2015): 128–36. http://dx.doi.org/10.15386/cjmed-526.
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Background and aims. Felodipine is a dihydropyridine calcium antagonist that presents good characteristics to be formulated as prolonged release preparations. The aim of the study was the formulation and in vitro characterization of a reservoir type prolonged release system with felodipine, over a 12 hours period using the Simplex method.Methods. The first step of the Simplex method was to study the influence of the granules coating method on the felodipine release. Furthermore the influence of the coating polymer type, the percent of the coating polymer and the percent of pore forming agent in the coating on the felodipine release were studied. Afterwards these two steps of the experimental design the percent of Surelease applied on the felodipine loaded granules and the percent of pore former in the polymeric coating formulation variables were studied. The in vitro dissolution of model drug was performed in phosphate buffer solution (pH 6.5) with 1% sodium lauryl sulfate. The released drug quantification was done using an HPLC method. The release kinetics of felodipine from the final granules was assessed using different mathematical models.Results. A 12 hours release was achieved using granules with the size between 315 – 500 µm coated with 45% Surelease with different pore former ratios in the coating via the top-spray method.Conclusion. We have prepared prolonged release coated granules with felodipine using a fluid bed system based on the Simplex method. The API from the studied final formulations was released over a 12 hours period and the release kinetics of the model drug substance from the optimized preparations fitted best the Higuchi and Peppas kinetic models.
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Gönüllü, Ü., P. Gürpınar, and M. Üner. "Double-layer Tablets of Lornoxicam: Validation of Quantification Method, In vitro Dissolution and Kinetic Modelling." Tropical Journal of Pharmaceutical Research 14, no. 9 (October 12, 2015): 1659–66. http://dx.doi.org/10.4314/tjpr.v14i9.16.
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Purpose: To formulate double-layer tablets of lornoxicam (LRX) prepared by direct compression method and evaluate their physical and drug release characteristics.Methods: The outer layer of tablets, composed of microcrystalline cellulose (MCC), starch and lactose, incorporated tan initial or prompt dose of the drug (4 mg) for immediate release. Hydroxypropyl methylcellulose (HPMC), polyvinylpyrrolidone (PVP K90) and carbomer, in varying concentrations, were used to prepare the tablet cores for sustained drug delivery. Weight variation, dimensions, hardness, tensile strength, friability and disintegration time of the tablets were evaluated. Drug release from double-layer tablets as well as kinetic models of drug release were determined after validating the method used for the quantification of the drug. The analytical method for quantification of LRX by UV spectroscopy was validated and verified for linearity, intra-day and inter-day precision, accuracy, recovery and specifity.Results: Tablet cores based on HPMC and HPMC:PVP K90 mixture displayed better compression and flow properties (good and fair to passable) than those formulated with PVP K90 and carbomer (poor). Satisfactory results were obtained from all the tablet formulations met compendial requirements. The slowest drug release rate was obtained with tablet cores based on PVP K90 (1.21 mg%.h-1). Drug release followed Higuchi kinetic model and the tablet cores released drug by diffusion/polymer relaxation or diffusion/erosion.Conclusion: Double-layer tablet formulation of lornoxicam based on HPMC or HPMC-PVP mixture is suitable for the treatment of inflammatory and painful conditions.Keywords: Lornoxicam, Controlled release, Double-layer tablets, Non-steroidal antiinflammatory drug, Oral delivery
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Haroun, Ahmed, Ali Osman, Sayed Ahmed, and Ahmed H. Elghandour. "Synthesis and Characterization of Ibuprofen Delivery System Based on β-cyclodextrin/Itaconic Acid Copolymer." Trends in Sciences 19, no. 19 (August 31, 2022): 5825. http://dx.doi.org/10.48048/tis.2022.5825.
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This study aims at preparation and characterization of drug delivery system based on grafted beta-cyclodextrin (β-CD) with itaconic acid (IA) using free-radical copolymerization technique, in the presence of N, N'-methylene bisacrylamide (BIS) and ammonium persulphate (APS) as a crosslinker and an initiator, respectively. The obtained copolymer (CD-PIA) was characterized using Fourier transform infrared spectroscopy (FT-IR), thermogravimetric analysis (TGA), X-ray diffraction patterns (XRD), transmission and scanning electron microscopes (TEM and SEM). Ibuprofen (IBU), as an anti-inflammatory drug model, was loaded during the preparation. The kinetic of the copolymerization was investigated in terms of grafting yield (GY %), grafting efficiency (GE %) and monomer conversion (%). Moreover, in vitro IBU release and kinetic of released using the different mathematical models (0-order, first-order and Higushi) were carried out in simulated gastric and intestinal fluids (SGF and SIF at pH 1.2 and 7.4, respectively) at 37 °. The results proved the successful preparation of the target copolymer with irregular spherical-like shape and particle size around 14 - 27.7 nm. After IBU loading, the copolymer exhibited thermal stability with crystalline nature. Also, the study showed that the synthesized copolymer, especially which high IA content is controlled the release of IBU after 4 h. Besides, it could be used as a potential IBU delivery system with sustained-release followed the first-order kinetic over 24 h.
HIGHLIGHTS
The nanogels drug carriers used for nonsteroidal anti-inflammatory drugs to overcome the unfavorable release in the stomach due to unforeseen pH alterations
The polymeric grafted β-CD derivatives using IA represent a unique class of the host materials with tunable inclusion properties and high affinity for Ibuprofen release
In vitro kinetic of IBU released showed the best fit with first-order model
GRAPHICAL ABSTRACT
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Khalid, Ikrima, Mahmood Ahmad, Muhammad Usman Minhas, and Muhammad Sohail. "Formulation and in vitro evaluation of mucoadhesive controlled release matrix tablets of flurbiprofen using response surface methodology." Brazilian Journal of Pharmaceutical Sciences 50, no. 3 (September 2014): 493–504. http://dx.doi.org/10.1590/s1984-82502014000300007.
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The objective of the current study was to formulate mucoadhesive controlled release matrix tablets of flurbiprofen and to optimize its drug release profile and bioadhesion using response surface methodology. Tablets were prepared via a direct compression technique and evaluated for in vitro dissolution parameters and bioadhesive strength. A central composite design for two factors at five levels each was employed for the study. Carbopol 934 and sodium carboxymethylcellulose were taken as independent variables. Fourier transform infrared (FTIR) spectroscopy studies were performed to observe the stability of the drug during direct compression and to check for a drug-polymer interaction. Various kinetic models were applied to evaluate drug release from the polymers. Contour and response surface plots were also drawn to portray the relationship between the independent and response variables. Mucoadhesive tablets of flurbiprofen exhibited non-Fickian drug release kinetics extending towards zero-order, with some formulations (F3, F8, and F9) reaching super case II transport, as the value of the release rate exponent (n) varied between 0.584 and 1.104. Polynomial mathematical models, generated for various response variables, were found to be statistically significant (P<0.05). The study also helped to find the drug's optimum formulation with excellent bioadhesive strength. Suitable combinations of two polymers provided adequate release profile, while carbopol 934 produced more bioadhesion.
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Narissara Kulpreechanan and Feuangthit Niyamissara Sorasitthiyanukarn. "Evaluation of in vitro release kinetics of Capsaicin-loaded chitosan nanoparticles using DDSolver." International Journal of Research in Pharmaceutical Sciences 11, no. 3 (July 31, 2020): 4555–59. http://dx.doi.org/10.26452/ijrps.v11i3.2685.
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The present aim is to evaluate the release profile and its release kinetics of encapsulated capsaicin from chitosan nanoparticles using the software DDSolver. The release study was performed by using a dialysis technique in PBS solutions with different pHs (1.2, 6.8 and 7.4) to mimics the different gastrointestinal tract and circulatory system pH ranges as a releasing medium. The nanoparticles were prepared using o/w emulsification and ionotropic gelation technique under optimal condition obtained from response surface methodology (RSM) design as described in our previous study. These nanoparticles were around 180 nm in average hydrodynamic size and encapsulation efficiency percentage around 70%, respectively. In vitro drug release study suggested that the chitosan nanoparticles can potentially use to controlled and sustained release of capsaicin over at least 96. The kinetic release analysis results by DDSolver software indicated that Weibull model was suggested to be the best dynamic models with highest R2adjusted and model selection criteria (MSC) and lowest Akaike information criterion (AIC), respectively, for capsaicin loaded chitosan nanoparticles. The release mechanism of capsaicin from nanoparticles was found to be Fickian diffusion. The results suggest that the chitosan nanoparticles can be applied for the controlled and sustained release of capsaicin in the gastrointestinal tract and circulatory system.
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Alsamman, Aseel, and Mohammad Othman. "PREPARATION AND IN VITRO EVALUATION OF FAST RELEASE DIAZEPAM SUPPOSITORIES FOR FEBRILE SEIZURES." Asian Journal of Pharmaceutical and Clinical Research 10, no. 9 (September 1, 2017): 224. http://dx.doi.org/10.22159/ajpcr.2017.v10i9.19264.
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Objective: The objective of this study was to optimize the best formula for fast release suppositories of diazepam.Methods: Suppositories were prepared by fusion method using Witepsol H15 as oleaginous base, polyethylene glycol as water-soluble polymer and poloxamer 188 as water miscible base. All suppositories were evaluated for physical characteristics, in vitro drug release and kinetic models. The effects of incorporating Tween 80 as a nonionic surfactant, propylene glycol as a cosolvent, and effervescent pair on the release rate of diazepam from suppositories were investigated. Differential scanning calorimetry and Fourier transform infrared spectrometry were used to characterize physical mixtures of diazepam and the different used bases.Results: Fast release of diazepam has been obtained from suppositories containing the effervescent pair. Many formulations of diazepam have been prepared and in vitro evaluated. PEG suppositories released diazepam more efficiently than poloxamer and Witepsol suppositories. The including of an effervescent pair in the formulation of suppositories greatly enhanced the release of diazepam. The addition of Tween 80 to Witepsol suppositories, PG to poloxamer suppositories, increased the rate and extent of diazepam release.Conclusion: Fast release of diazepam has been obtained from suppositories containing the effervescent pair (formula F3), which also have good physical properties.
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Alsamman, Aseel, and Mohammad Othman. "PREPARATION AND IN VITRO EVALUATION OF FAST RELEASE DIAZEPAM SUPPOSITORIES FOR FEBRILE SEIZURES." Asian Journal of Pharmaceutical and Clinical Research 10, no. 9 (September 1, 2017): 365. http://dx.doi.org/10.22159/ajpcr.2017.v10i9.20162.
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Objective: The objective of this study was to optimize the best formula for fast release suppositories of diazepam.Methods: Suppositories were prepared by fusion method using Witepsol H15 as oleaginous base, polyethylene glycol as a water-soluble polymer, and Poloxamer 188 as water miscible base. All suppositories were evaluated for physical characteristics, in vitro drug release and kinetic models. The effects of incorporating Tween 80 as a non-ionic surfactant, propylene glycol as a cosolvent, and effervescent pair on the release rate of diazepam from suppositories were investigated. Differential scanning calorimetry and Fourier transform infrared spectrometry were used to characterize physical mixtures of diazepam and the different used bases.Results: Many formulations of diazepam have been prepared and in vitro evaluated. PEG suppositories released diazepam more efficiently than poloxamer and witepsol suppositories. The including of an effervescent pair in the formulation of suppositories greatly enhanced the release of diazepam. The addition of tween 80 to witepsol suppositories, PG to poloxamer suppositories, increased the rate and extent of diazepam release.Conclusion: Fast release of diazepam has been obtained from suppositories containing the effervescent pair (formula F3), which also have good physical properties.
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Chourasiya, Vibha, Sarvesh Bohrey, and Archna Pandey. "Formulation, optimization, and characterization of amlodipine besylate loaded polymeric nanoparticles." Polymers and Polymer Composites 29, no. 9_suppl (November 2021): S1555—S1568. http://dx.doi.org/10.1177/09673911211056154.
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The objectives of this work were to formulate and optimize amlodipine besylate loaded polymeric nanoparticles by using factorial design. The emulsion solvent evaporation method was employed successfully to produce the drug loaded polymeric nanoparticles and the optimization was done by the help of the 24 factorial design. The effect of the main preparation variables on the dependent variables such as nanoparticle size and % drug entrapment efficiency was studied for the optimization of the nanoparticles. The characterization of these nanoparticles was done by the different parameters such as interaction between the excipients, size, morphology, zeta potential, % drug entrapment efficiency, % process yield, and in-vitro drug release behavior. FTIR, DLS, TEM, AFM, zeta potential studies, and dialysis bag method were performed for this purpose. The in vitro drug release data were analyzed by different kinetic models to know the release mechanism. The optimized nanoparticles were spherical in shape and showed particle size 91.5 ± 4.3 nm, PDI 0.368 ± 0.014, zeta potential −17.5 mV, % drug entrapment efficiency 74.06 ± 2.1%, and % process yield 78.51 ± 1.8%. The release kinetics studies revealed that drug release from the nanoparticles follow the Korsmeyer–Peppas model.
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Islam, Asraful, Shimul Halder, and Sitesh Chandra Bachar. "Formulation and in vitro Evaluation of Betahistine Dihydrochloride Twice Daily Controlled Release Matrix Tablet." Dhaka University Journal of Pharmaceutical Sciences 10, no. 2 (September 3, 2012): 93–100. http://dx.doi.org/10.3329/dujps.v10i2.11786.
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In order to reduce dosing frequency, a sustained release dosage form of betahistine dihydrochloride was developed as a twice daily controlled release tablet formulation that could be used to decrease vertigo resulted in Meniere's disease for a prolonged time. Six formulations were developed by using Methocel K4M CR, Methocel K15M CR and Methocel K 100 LVCR as single and combinations in different percentage. The tablets were prepared by wet granulation method. Physical properties of betahistine dihydrochloride granules and betahistine dihydrochloride matrix tablets were evaluated. The tablets were characterized for Betahistine Dihydrochloride release in both gastric simulated fluid (0.1 N HCl, pH 1.3) and simulated intestinal fluid (buffer solution pH 6.8). The data were subjected to different models in order to evaluate their release kinetics and mechanisms. The results of the in vitro dissolution study indicate that most of the formulations showed above 80% of drug release in 12 hours but formulations (F-2 and F-4) met the official specification of release profile. Dissolution data were fitted to zero order equation, Higuchi square root law, Korsmeyer-Peppas model and Hixson-Crowell cube root law as these plots showed the highest value of linearity to evaluate kinetic data. The release of betahistine dihydrochloride was prolonged for 12 hours indicating the usefulness of the formulations for twice daily dosage forms, leading to improve efficacy, controlling the release and better patient compliance. DOI: http://dx.doi.org/10.3329/dujps.v10i2.11786 Dhaka Univ. J. Pharm. Sci. 10(2): 93-100, 2011 (December)
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Mikušová, Veronika, Jarmila Ferková, Dominika Žigrayová, Daniel Krchňák, and Peter Mikuš. "Comparative Study of Polysaccharide-Based Hydrogels: Rheological and Texture Properties and Ibuprofen Release." Gels 8, no. 3 (March 7, 2022): 168. http://dx.doi.org/10.3390/gels8030168.
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Polysaccharides are attractive gelling agents in pharmacy due to their safety, biocompatibility, biodegradability, relatively easy way of preparation, and low price. Due to their variable physical-chemical properties, polysaccharides have potentialities to be used for designing new drug delivery systems for controlled drug release. In this comparative study, rheological and texture properties as well as the in vitro release of model drug ibuprofen (IBU) with 11 polysaccharide-based hydrogels were investigated. The in vitro release of IBU significantly differed between (i) neutral (hydroxy/alkylcelluloses), (ii) anionic (carboxyalkylcellulose and its sodium salt, tragacanth, carrageenan, xanthan gum), and (iii) cationic (chitosans) hydrogels due to different contribution of provided interactions and viscosity within the hydrogel groups. The drug release kinetics of each hydrogel system was evaluated for five kinetic models. Several combinations of cationic hydrogels with neutral or anionic ones were performed to illustrate possibilities of providing modified IBU release profiles. In this context, chitosan was presented as an effective modifier of diffusion profiles for negatively charged drugs formulated into combined polymeric systems, providing their prolonged release. The most appropriate hydrogel for the topical application (i.e., providing favorable rheological and texture properties along with the highest drug release) was selected from a studied series of polysaccharide-based hydrogels.
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Vieira, Italo Rennan Sousa, Gisele dos Santos Miranda, Eduardo Ricci-Júnior, and Marcia Cerqueira Delpech. "Waterborne poly(urethane-urea)s films as a sustained release system for ketoconazole." e-Polymers 19, no. 1 (May 29, 2019): 168–80. http://dx.doi.org/10.1515/epoly-2019-0018.
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AbstractKetoconazole (KTZ) was incorporated in waterborne poly(urethane-urea)s dispersions (WPUU), aiming at the production of films for drug sustained release. Dispersions based on poly(ethylene glycol-block-propylene glycol) (PEG-b-PPG) (four monomers with different contents of PEG hydrophilic segments), poly(propylene glycol), isophorone diisocyanate, dime-thylolpropionic acid and hydrazine were produced and characterized by apparent viscosity and average particle size (APS). Cast films-drug interaction was investigated by Fourier-Transform infrared spectrometry (FTIR). In vitro dissolution assays were performed in simulated gastrointestinal juices, followed by application of kinetic models. Stable pseudoplastic dispersions, with APS between 27 to 320 nm were obtained. FTIR from KTZ-loaded films indicated interactions between polymer and drug. In vitro release of KTZ was achieved above 80%, notably influenced by PEG-based segments content up to 2 h, followed by sustained release for 8 h. Higuchi’s and first-order equations described the drug kinetic profile, as diffusion of the drug and erosion of the swollen polymer, respectively.
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Zhang, Shuang, Xinxin Fan, Guojing Zhang, Weidong Wang, and Lei Yan. "Preparation, characterization, and in vitro release kinetics of doxorubicin-loaded magnetosomes." Journal of Biomaterials Applications 36, no. 8 (November 30, 2021): 1469–83. http://dx.doi.org/10.1177/08853282211060544.
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The doxorubicin (DOX) was successfully coupled to the magnetosomes from Acidithiobacillus ferrooxidans ( At. ferrooxidans) by genipin bridging. The parameters (magnetosome concentration, DOX concentration, genipin concentration-, and cross-link time) expected for temperature significantly influenced the coupling rate. Bacterial magnetosome-doxorubicin complexes (BMDCs) were characterized by transmission electron microscope (TEM), particle size analyzer and Fourier transform infrared spectroscopy. Results indicated that BMDCs exhibited a mean particle size of 83.98 mm and displayed a negative charge. The chemical reaction occurring between CO and NH group and the physical adsorption predominated by electrostatic interaction were found to involve in coupling. BMDCs can release 40% of DOX in simulated gastrointestinal conditions within 38 h. Kinetic models including Higuchi, Korsmeyer–Peppas, Zero order, First order, Hixon-Crowell, Baker-Lonsdale, and Weibull and Gompertz were utilized to explore the release mechanism of DOX from BMDCs. All models were found to fit well (r2 ≥ 0.8144) with the release data and the Gompertz was the best fit model (r2 = 0.9742), implying that the complex mechanisms involving Fickian and Gompertz diffusion contributed to the release. These findings suggested that magnetosomes from At. ferrooxidans have great potential applications in biomedical and clinical fields as the carrier of target drug delivery systems in the future.
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Naik, Santoshi, Prasiddhi Raikar, and Mohammed Gulzar Ahmed. "Formulation and evaluation of chitosan films containing sparfloxacin for the treatment of periodontitis." Journal of Drug Delivery and Therapeutics 9, no. 1 (January 15, 2019): 38–45. http://dx.doi.org/10.22270/jddt.v9i1.2245.
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In the present study an attempt has been made to formulate and evaluate a sustained release periodontal film of Sparfloxacin with biodegradable, cost effective polymer Chitosan. The objective of the study was to formulate intra-pocket periodontal films, which could be easily placed into the periodontal pocket, and thus be capable of delivering therapeutic concentrations of drug. Sparfloxacin is an antibiotic, showing wide spectrum antibacterial activity against a number of periodontal pathogens. Hence Sparfloxacin is selected as model for site specific delivery, i.e., into periodontal pocket for the treatment of periodontitis. In the present investigation Chitosan films containing Sparfloxacin were prepared by solution casting method using acetic acid. The copolymers HPMC K4M, Sodium CMC and Eudragit RL 100 in the concentrations of 10%, 20% and 30% w/w of Chitosan were added into the polymeric solution. Propylene glycol was used as plasticizer. FT-IR and UV spectroscopic methods revealed no interaction between Sparfloxacin and polymers. The drug loaded films were evaluated for their thickness, weight variation, content uniformity, tensile strength, percent elongation, percentage moisture loss, surface pH, folding endurance, in- vitro drug release studies, in - vitro antibacterial activity and stability studies. Periodontal films showed initial burst release of drug on 1st day and then the release was sustained for a period of 8 days. In – vitro antibacterial activity was carried out on staphylococcus aureus and the antibacterial activity was retained for 96 hours. In - vitro release from periodontal films was fit to kinetic models to reveal drug release kinetics.
Keywords: Periodontitis, Sparfloxacin, Bio-adhesive polymers.
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Atara, Samir A., and Moinuddin M. Soniwala. "FORMULATION AND EVALUATION OF PECTIN-CALCIUM CHLORIDE BEADS OF AZATHIOPRINE FOR COLON TARGETED DRUG DELIVERY SYSTEM." International Journal of Pharmacy and Pharmaceutical Sciences 10, no. 1 (January 1, 2018): 172. http://dx.doi.org/10.22159/ijpps.2018v10i1.23175.
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Objective: Calcium pectinate is an insoluble hydrophilic material used for sustained release delivery. The objective of the study was formulation and evaluation pectin-calcium chloride beads of azathioprine.Methods: Calibration curves of azathioprine were prepared in 0.1N HCl solution (pH-1.2) and phosphate buffer (pH-6.8 and pH-7.4). Fourier transform infrared spectroscopy and differential scanning calorimetry was used to determine compatibility between azathioprine and excipients. Formulation and optimization of calcium-pectinate beads were performed. The coating of the optimized batch was performed with eudragit S100. Micrometric properties, scanning electron microscopy, in vitro azathioprine release, and stability study was performed. Dissolution kinetic study was assessed for various kinetics models of the optimized batch. The Wilcoxon test followed by the Dunnett’s multiple comparison tests were performed between uncoated and coated beads in vitro dissolution profile of optimized batch in 0.1N HCl after 2 h.Results: Fourier transform infrared spectroscopy and differential scanning calorimetry had identical peaks with that of pure azathioprine in compatibility study. Scanning electron microscopy of an uncoated optimized batch of beads indicated the smooth and uniform surface of prepared beads. Eudragit S100 coating was decreased release of azathioprine release in 0.1N HCl after 2 h (p = 0.049, q = 3.533). Korsmeyer/Peppa's model was applied with release exponent higher than 1. In vitro percentage cumulative azathioprine release was identical before and after stability study.Conclusion: Calcium pectinate beads of azathioprine, a multi-particulate dosage form using pH-dependent approaches were prepared.
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Chaturvedi, Prateek Kumar, Rajesh Gour, Janki Prasad Rai, and Akhlesh Kumar Singhai. "Development and Evaluation of Losartan Potassium Floating Matrix Tablet." Journal of Drug Delivery and Therapeutics 12, no. 3-S (June 15, 2022): 106–14. http://dx.doi.org/10.22270/jddt.v12i3-s.5388.
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The present study was aimed towards the development of controlled release formulations of Losartan Potassium based on designed to enhance the bioavailability by prolonging its duration in the stomach via the floating dosage forms with controlled release. This study was intended to evaluate the influence of formulation variables like levels of polymer, amount of mannitol concentrations, and coating solution ratios of semi permeable membrane on the drug release from the developed formulations. Thus, there is a strong clinical need and market potential for a dosage form that will deliver Losartan Potassium in a controlled manner to a patient needing this therapy, thereby resulting in a better patient compliance. This study was designed to enhance the bioavailability of drug by prolonging its duration in the stomach via the floating dosage forms with controlled release. Floating matrix tablets of Losartan Potassium were prepared by the direct compression method, using locust bean gum and HPMC K 15M as polymers and Sodium bicarbonate as floating agent. The effect of the nature of polymers was studied by preparing various formulations of tablets. In all these formulations, a constant amount of drug (100 mg) was maintained. The blend was initially characterized for pre-compression and post- compression parameters. Pre-compression characterization was done for angle of repose, bulk density, tapped density, Carr’s index, and Hausner’s ratio. The results of pre-compression characterization were indicated good to excellent flow characteristics. Post-compression characterization includes thickness, hardness, friability, weight variation, drug content, buoyancy lag time, floating time and in-vitro drug release. All the results were satisfactory as per the guideline of pharmacopoeia. The in vitro drug release studies found that formulations LPFT4 showed best sustained release profile in 24 hrs. Among the nine formulations (LPFT1 to LPFT9) prepared formulations LPFT4 was found to be the best formulations in terms of sustained drug release. Drug release kinetics was performed by using various kinetic models such as Zero order, First order, Korsmeyer- Peppas and Higuchi’s equation and followed supercase II transport diffusion kinetic models.
Keywords: Oral drug delivery system, Gastroretentive technology, losartan potassium, floating tablet, matrix tablet
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Castillo-Henríquez, Luis, Pablo Sanabria-Espinoza, Brayan Murillo-Castillo, Gabriela Montes de Oca-Vásquez, Diego Batista-Menezes, Briner Calvo-Guzmán, Nils Ramírez-Arguedas, and José Vega-Baudrit. "Topical Chitosan-Based Thermo-Responsive Scaffold Provides Dexketoprofen Trometamol Controlled Release for 24 h Use." Pharmaceutics 13, no. 12 (December 6, 2021): 2100. http://dx.doi.org/10.3390/pharmaceutics13122100.
Full textAbstract:
Chronic and non-healing wounds demand personalized and more effective therapies for treating complications and improving patient compliance. Concerning that, this work aims to develop a suitable chitosan-based thermo-responsive scaffold to provide 24 h controlled release of Dexketoprofen trometamol (DKT). Three formulation prototypes were developed using chitosan (F1), 2:1 chitosan: PVA (F2), and 1:1 chitosan:gelatin (F3). Compatibility tests were done by DSC, TG, and FT-IR. SEM was employed to examine the morphology of the surface and inner layers from the scaffolds. In vitro release studies were performed at 32 °C and 38 °C, and the profiles were later adjusted to different kinetic models for the best formulation. F3 showed the most controlled release of DKT at 32 °C for 24 h (77.75 ± 2.72%) and reduced the burst release in the initial 6 h (40.18 ± 1.00%). The formulation exhibited a lower critical solution temperature (LCST) at 34.96 °C, and due to this phase transition, an increased release was observed at 38 °C (88.52 ± 2.07% at 12 h). The release profile for this formulation fits with Hixson–Crowell and Korsmeyer–Peppas kinetic models at both temperatures. Therefore, the developed scaffold for DKT delivery performs adequate controlled release, thereby; it can potentially overcome adherence issues and complications in wound healing applications.
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Kabir, Abul Kalam Lutful, Shimul Halder, Madhabi Lata Shuma, and Abu Shara Shamsur Rouf. "Formulation Development and in vitro Evaluation of Drug Release Kinetics from Sustained Release Aceclofenac Matrix Tablets using Hydroxypropyl Methyl Cellulose." Dhaka University Journal of Pharmaceutical Sciences 11, no. 1 (November 4, 2012): 37–43. http://dx.doi.org/10.3329/dujps.v11i1.12485.
Full textAbstract:
The objective of the present study was to develop a once-daily sustained release matrix tablet of Aceclofenac using hydroxypropyl methyl cellulose (Methocel K 100M CR) as release controlling factor and to evaluate drug release parameters as per various release kinetic models. The tablets were prepared by direct compression method. The powder blends were evaluated for angle of repose, loose bulk density, tapped bulk density, compressibility index, total porosity and drug content etc. The tablets were subjected to thickness, weight variation test, drug content, hardness, friability and in vitro release studies. The in vitro dissolution study was carried out for 24 hours using United States Pharmacopoeia (USP) 22 paddle-type dissolution apparatus in phosphate buffer (pH 7.4). The powder blends showed satisfactory flow properties, compressibility index and drug content etc. All the tablet formulations showed acceptable pharmacotechnical properties and complied with pharmacopoeial specifications. The results of dissolution studies indicated that the formulation F-3 (40% Methocel K100M CR of total weight of tablet) could extend the drug release up to 24 hours and the total release pattern was very close to the theoretical release profile. By comparing the dissolution profiles with the originator brand of Arrestin SR, the formulation F-3 exhibited drug release profile like originator brand. From this study, a decrease in release kinetics of the drug was observed by increasing the polymer concentration. Kinetic modeling of in vitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport, which was only dependent on the type and amount of polymer used. The drug release followed both diffusion and erosion mechanism in all cases. The drug release from the formulation (F-3) was satisfactory after 3 months storage in 400C and 75% RH. Besides, this study explored both of the optimum concentration and effect of polymer(s) on Aceclofenac release pattern from the tablet matrix for 24 hour period. The matrix tablet of Aceclofenac using HPMC with molecular weight of K100M controlled the drug release effectively for 24 hours; hence the formulation can be considered as a once daily sustained release tablet of Aceclofenac in order to improve patient compliance. DOI: http://dx.doi.org/10.3329/dujps.v11i1.12485 Dhaka Univ. J. Pharm. Sci. 11(1): 37-43, 2012 (June)
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Kar, Ayan Kumar, and Banhishikha Kar. "In-Vitro Comparative Dissolution Study of Commercially Available Paracetamol Tablet." Journal of Drug Delivery and Therapeutics 10, no. 1 (January 15, 2020): 18–23. http://dx.doi.org/10.22270/jddt.v10i1.3817.
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Quality is the most important issue in the pharmaceutical field due to the presence of a drug which is considered as safe and therapeutically active agent. In-vitro evaluation ensures their quality, bioavailability as well as optimum therapeutic activity. Paracetamol (acetaminophen) which are the active metabolites of phenacetin is commonly used for the relief of headaches and pains, and is a major ingredient in numerous cold and flu remedies. Paracetamols are available in different brands in Indian market. The main objective of the present study was to conduct the comparative in-vitro dissolution studies of various brands collected from the local market to determine whether all the formulations used were equivalent or significantly different. The calibration curve was constructed covering the concentration range of 1 to 10 mcg/ml at 268 nm by UV spectrophotometer (UV 2203 Double beam spectrophotometer, Shimadzu). Five different brands of Paracetamol of 500 mg conventional tablets from different manufacturers were selected in the study and dissolution testing in Phosphate buffer at pH 7.4 was conducted from each brands for 90 mins by using dissolution testing apparatus USP type-II. The dissolution rate was subjected to various mathematical models like zero order, first order, Higuchi and Hixson-Crowell equations to elucidate the kinetic behavior of drug release from the test samples. Different release kinetics model of all the selected brands was assuring the quality standard of manufacturing.
Keywords: Paracetamol, Marketed Tablet, In-Vitro dissolution study, Release profile.
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Bashir, Irfan, Ayesha Sethi, Muhammad Zaman, Junaid Qureshi, Rai M. Sarfraz, Asif Mahmood, Muhammad I. Sajid, Talha Jamshaid, and Muhammad A. Akram. "Formulation and in-vitro bioequivalence evaluation of verapamil hydrochloride matrix tablets with Calan R." International Current Pharmaceutical Journal 3, no. 6 (May 3, 2014): 286–90. http://dx.doi.org/10.3329/icpj.v3i6.18761.
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The purpose of the current work was to formulate Verapamil Hydrochloride (VH) sustained release matrix tablets by using natural polymers and comparison with leading national brand Calan SR of Searle Pharmaceuticals. Tragacanth and pectin were used in various concentrations. Pre compression studies i.e. angle of repose, bulk density, tapped density, Carrs compressibility index and Hausners ratio were also performed and found within the Pharmacopoeial limits. Eight formulations (F1-F8) of (VH) were prepared by direct compression method. Post compression studies i.e. Thickness, Hardness, Diameter, Friability and Dissolution studies were conducted. Different kinetic models i.e. zero order, first order, Highuchi model and Korsmeyer Peppas were applied to study release patterns and similarity index was calculated. Dissolution studies were carried out in phosphate buffer of pH 6.8 showed that formulations (F4 and F8) formulated with higher polymers concentration showed comparatively better drug retardation. F5 was the most comparable with the reference product. Verapamil hydrochloride released was observed non-fickian as diffusion following Higuchi model.DOI: http://dx.doi.org/10.3329/icpj.v3i6.18761 International Current Pharmaceutical Journal, May 2014, 3(6): 286-290
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Patel, Anand J., Deep R. Naik, and Jignesh P. Raval. "Sustain Release Formulation and Evaluation of Ofloxacin Floating Delivery System." International Letters of Chemistry, Physics and Astronomy 31 (March 2014): 69–83. http://dx.doi.org/10.18052/www.scipress.com/ilcpa.31.69.
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Floating tablets has been accepted as a process to achieve controlled drug delivery by prolonging the residence time of the dosage form at the site of absorption, thereby improving and enhancing the bioavailability of drug. The objective of present study outlines the development and characterization the floating drug delivery system of Ofloxacin to enhance its bioavailability and therapeutic efficacy, using different grades of polymer along with effervescent agent sodium bicarbonate and citric acid. Ofloxacin is a synthetic chemotherapeutic second-generation antibiotic of the fluoroquinolone class. Different tablet formulations were formulated by wet granulation technique and were evaluated for physical parameters like Tablet Thickness, Hardness, % Friability, Weight variation, Content uniformity, In vitro buoyancy, Swelling index, In vitro dissolution study and drug release mechanisms. As the concentration of the polymer in the formulations increased the release of drug decreased. Hence it was considered as suitable candidate for formulation as floating drug delivery system. Different kinetic models were applied to drug release data in order to evaluate release mechanisms and kinetics. The optimized formula F4 showed better sustained drug release with good floating properties and fitted best to be Korsmeyer-Peppas model with R2 value of 0.9575. As the n value for the Korsmeyer- Peppas model was found be more than 0.5 it follows Non-Fickian diffusion mechanism. FTIR result showed that there is no drug excipients interaction.
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Patel, Anand J., Deep R. Naik, and Jignesh P. Raval. "Sustain Release Formulation and Evaluation of Ofloxacin Floating Delivery System." International Letters of Chemistry, Physics and Astronomy 31 (March 28, 2014): 69–83. http://dx.doi.org/10.56431/p-77x959.
Full textAbstract:
Floating tablets has been accepted as a process to achieve controlled drug delivery by prolonging the residence time of the dosage form at the site of absorption, thereby improving and enhancing the bioavailability of drug. The objective of present study outlines the development and characterization the floating drug delivery system of Ofloxacin to enhance its bioavailability and therapeutic efficacy, using different grades of polymer along with effervescent agent sodium bicarbonate and citric acid. Ofloxacin is a synthetic chemotherapeutic second-generation antibiotic of the fluoroquinolone class. Different tablet formulations were formulated by wet granulation technique and were evaluated for physical parameters like Tablet Thickness, Hardness, % Friability, Weight variation, Content uniformity, In vitro buoyancy, Swelling index, In vitro dissolution study and drug release mechanisms. As the concentration of the polymer in the formulations increased the release of drug decreased. Hence it was considered as suitable candidate for formulation as floating drug delivery system. Different kinetic models were applied to drug release data in order to evaluate release mechanisms and kinetics. The optimized formula F4 showed better sustained drug release with good floating properties and fitted best to be Korsmeyer-Peppas model with R2 value of 0.9575. As the n value for the Korsmeyer- Peppas model was found be more than 0.5 it follows Non-Fickian diffusion mechanism. FTIR result showed that there is no drug excipients interaction.
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Alam, Md Shamsul, Jakir Ahmed Chowdhury, Sams Mohammad Anowar Sadat, and Md Selim Reza. "Development and Evaluation of Salbutamol Sulphate Loaded Ethyl Cellulose Microcapsules using Emulsion Solvent Evaporation Technique." Bangladesh Pharmaceutical Journal 18, no. 2 (July 26, 2015): 132–36. http://dx.doi.org/10.3329/bpj.v18i2.24311.
Full textAbstract:
Ethyl cellulose (EC) microcapsules containing Salbutamol sulphate (SS) were prepared through emulsion-solvent evaporation technique. Microcapsules were compressed and in-vitro release profiles were studied from both microcapsules and their compressed matrix tablets. Different amounts of drug were added in order to obtain various drugs to polymer ratios and it was found that the size of microcapsules reduced with the increase in core loading. In the preparation of formulations, Tween 80 was used as an emulsifying or dispersing agent and light liquid paraffin (LLP) was used as oil phase. The in-vitro release of EC microcapsules was studied in distilled water at 37º ± 0.5°C. A biphasic release behavior of SS from microcapsules was observed. In case of microcapsules, an immediate release was observed but for their compressed tablet form, initially a burst effect and then slow release were observed which was extended for 8 hours. In order to further investigate the type of drug release mechanism, the dissolution data were plotted according to the different kinetic models. In-vitro dissolution studies showed that zero-order and square-root of time (Higuchi model) release characteristics were exhibited.Bangladesh Pharmaceutical Journal 18(2): 132-136, 2015
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Prajapati, Shailesh T., Charmi G. Patel, and Chhagan N. Patel. "Formulation and Evaluation of Transdermal Patch of Repaglinide." ISRN Pharmaceutics 2011 (July 20, 2011): 1–9. http://dx.doi.org/10.5402/2011/651909.
Full textAbstract:
Repaglinide has the half life of 1 hour, and bioavailability in the body is 56% due to first-pass metabolism. The total daily dose of Repaglinide is 16 mg (e.g., 4 mg four times daily depending on meal patterns); hence, it required frequent dosing. Transdermal patch of Repaglinide was prepared to sustain the release and improve bioavailability of drug and patient compliance. Different formulations were prepared by varying the grades of HPMC and concentration of PVP K30 by solvent casting method. The prepared formulations were evaluated for various parameters like thickness, tensile strength, folding endurance, % elongation, % moisture content, % moisture uptake, % drug content, in vitro drug release, in vitro permeation, and drug excipient compatibility. A 32 full factorial design was applied to check the effect of varying the grades of HPMC (X1) and PVP concentration (X2) on the responses, that is, tensile strength, percentage drug released in 1 hr (Q1), 9 hr (Q9), and diffusion coefficient as a dependent variables. In vitro release data were fitted to various models to ascertain kinetic of drug release. Regression analysis and analysis of variance were performed for dependent variables. The results of the F2 statistics between factorial design batches and theoretical profile were used to select optimized batch. Batch F6 was considered optimum batch which contained HPMC K100 and PVP (1.5%), showed release 92.343% up to 12 hr, and was more similar to the theoretical predicted dissolution profile (f2=69.187).
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Betala, Surendranath, M. Mohan Varma, and K. Abbulu. "Formulation and evaluation of polymeric nanoparticles of an antihypetensive drug labetalol." Journal of Drug Delivery and Therapeutics 8, no. 6-s (December 15, 2018): 187–91. http://dx.doi.org/10.22270/jddt.v8i6-s.2109.
Full textAbstract:
Labetalol is an adrenergic receptor blocking agent used in the treatment of hypertension and characterized by high solubility and high permeability which corresponds to BCS class I drug. Plasma half life ranges from 6 & bioavailability is 25%. Ethyl cellulose was used as a rate controlling polymer. Effects of addition of ethyl cellulose on in vitro dissolution were studied. Nanoparticles were formulated using different polymer ratios. In vitro drug release was carried out by using USP Type II at 50 rpm in 900 ml of acidic dissolution medium (pH 1.2) for 2 hours, followed by 900 ml alkaline dissolution medium (pH7.4) for 12 hours. Mean dissolution time is used to characterize drug release rate from a dosage form. Several kinetic models were applied to the dissolution profiles to determine the drug release kinetics. Excipients are selected by FTIR studies. Finally the nanoparticles were evaluated for various characteristics like encapsulation efficiency, percentage yield, partial size and the In vitro release for 12 hrs. The nanoparticles were found to be discrete, spherical, and free-flowing. The nanoparticles were uniform in size, and the microencapsulation efficiency was in the range of 52.5-81.7%. The surface morphology of prepared Labetalol nanoparticles was observed under scanning electron Microscopy. Nanoparticles had good spherical geometry. The stability study was performed at 40ºC ± 2ºC and 75 ± 5% RH for 6 months.
Keywords: Nanoparticles; Labetalol, Hypertension, Ethyl Cellulose, Dissolution, entrapment efficiency.
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Song, Jianfei, Navideh Abbasnezhad, Mathieu Specklin, Mohammadali Shirinbayan, Smaine Kouidri, and Farid Bakir. "Numerical prediction of drug release from polyurethane samples combining kinetic model developed by experimental data." E3S Web of Conferences 321 (2021): 03012. http://dx.doi.org/10.1051/e3sconf/202132103012.
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With the aim of optimizing Drug Eluting Stents (DES), particular attention has been laid on computational methods of controlling the drug release profile among researchers. Consequently, various models and simulations are available in the literature. Nevertheless, validations based on biorelevant in-vitro trials are lacking. In the present study, a comparison of drug release from polyurethane samples between calculated results and experimental-data has been carried out. The calculation results are from a numerical simulation and a newly established mathematical model for reproducing the liberation kinetic. Different fluid flow rates and initial drug concentrations in polymer have been taken into account.
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Chowdhury, Sonia, Mandava Nithin Babu, K. Ankitha, B. Shirisha, Madhurika Sirigadi, and Esarapu Kavya. "A comparative study on effect of polymers on release kinetics glimepiride matrix tablet." Pharmaceutical and Biological Evaluations 4, no. 2 (April 2, 2017): 103. http://dx.doi.org/10.26510/2394-0859.pbe.2017.16.
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Objective: The Present investigation was performed to find out the effect of synthetic and natural polymers on the release properties of glimepiride matrix tablet. Glimepiride is a first third generation sulphonyl urea agent for the treatment of type- II diabetes mellitus. Methocel K15M, Olibanum Gum were used as key release modifying polymers.Methods: Nine formulations were prepared taking different concentration of natural and synthetic polymers, The drug excipient mixtures were subjected to pre-compression studies. The tablets were prepared by direct compression method; all formulations were subjected to physicochemical studies, in- vitro drug release, kinetic studies and stability studies. The physicochemical results were found within the limits.Results: FTIR study interpretation did not show any drug–excipient interaction The drug release from the optimized formulation F-7 was extended for a period of 12 hours. The release kinetics of F-7 formulation showed that the release of drug follows zero order models. The optimized formulations were subjected to stability studies and shown there were no significant changes in drug content, physicochemical parameters and release pattern.Conclusions: Results of the present study indicated the suitability of the above mentioned polymers in the preparation of sustained release formulation of Glimepiride for the management of type-II diabetes mellitus effectively.
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Costa, Antonio O., Claure N. Lunardi, and Anderson J. Gomes. "Kinetic Evaluation of Anti-tumor Chlorambucil Release from O-stearoyl Mannose PLGA Nanoparticles." Current Nanomedicine 10, no. 1 (April 22, 2020): 63–75. http://dx.doi.org/10.2174/2468187309666190823153341.
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Purpose: This study assesses the kinetics of the anti-tumor drug chlorambucil (CLB) incorporated into PLGA nanoparticles (NP-CLB) with and without the presence of the O-stearoyl mannose (OEM) functionalizing agent (NP-CLBMAN). Methods: OEM was synthesized and used in the NP-CLB-MAN formulation. The nanoparticles were characterized by dynamic light scattering, electrophoretic light scattering, scanning electron microscopy, and Fourier-transform infrared spectroscopy. Results: The nanoparticles presented an encapsulation efficiency greater than 61% and a PdI between 0.186–0.217. The mean size was 185 nm for NP-CLB and 220 nm for NPCLB- MAN, and the zeta potential values were -17.7 mV for NP-CLB and -14.2 mV for NP- CLB-MAN. Scanning electron microscopy showed that NPs with OEM have a surface with a different shape, and FTIR analyses showed binding of CLB to the drug delivery system, as well as functionalization with OEM. In vitro release studies showed a biphasic release profile for both systems, and they were analyzed considering the mathematical Korsmeyer-Peppas, first-order, and Fick diffusion models, and the combination of the first-order and Fick diffusion models. Conclusion: The experimental results obtained for the release of CLB were better described using a combination of the first order and Fick diffusion mathematical models.
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Pathak, Sudhakar, Harish Pandey, and Sunil Kumar Shah. "Formulation and Evaluation of Floating Matrix Tablets of Sacubitril and Valsartan." Journal of Drug Delivery and Therapeutics 9, no. 4-s (August 15, 2019): 298–309. http://dx.doi.org/10.22270/jddt.v9i4-s.3322.
Full textAbstract:
Floating Drug Delivery Systems (FDDS) have a bulk density lower than gastric fluids and thus remain buoyant in the stomach for a prolonged period of time, without affecting the gastric emptying rate. While the system is floating on the gastric contents, the drug is released slowly at a desired rate from the system. These floating tablets mainly prepared for reduction of lag time and release the drug up to 12 hours and may also increase the bioavailability of the drugs by utilizing the drug to full extent avoiding unnecessary frequency of dosing. The purpose of this research was to develop and evaluated floating matrix tablets of sacubitril and valsartan. The floating matrix tablets of sacubitril and valsartan were prepared by direct compression method using altered concentrations of HPMC K4M, HPMC K100M, sodium alginate as polymers and sodium bicarbonate, citric acid as gas generating agent. FTIR, DSC studies conformed that there was no incompatibility between the polymers and the drug. Tablet preformulation parameters were within the pharmacopoeias limit. Tablets were evaluated by different parameters such as weight uniformity, content uniformity, thickness, hardness, in vitro release studies, buoyancy determination and kinetic analysis of dissolution data. The varying concentration of gas generating agent and polymers was found to affect on in-vitro drug release and floating lag time. Tablet showed ≤ 1min lag time, continuance of buoyancy for >12 h. The in-vitro drug release pattern of sacubitril and valsartan optimized floating tablets (F16) was fitted to different kinetic models which showed highest regression (r2 = 0.9838) for Higuchi model. The Optimized formulation (F16) showed no significant change in physical appearance, drug content, floating lag time, in vitro dissolution studies after 75%±5% RH at 40±20C relative humidity for 6 months. Prepared floating tablets of sacubitril and valsartan may prove to be a potential candidate for safe and effective controlled drug delivery over an extended period of time for gastro retentive drug delivery system.
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Bercea, Maria, Ioana-Alexandra Plugariu, Luiza Madalina Gradinaru, Mihaela Avadanei, Florica Doroftei, and Vasile Robert Gradinaru. "Hybrid Hydrogels for Neomycin Delivery: Synergistic Effects of Natural/Synthetic Polymers and Proteins." Polymers 15, no. 3 (January 26, 2023): 630. http://dx.doi.org/10.3390/polym15030630.
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This paper reports new physical hydrogels obtained by the freezing/thawing method. They include pullulan (PULL) and poly(vinyl alcohol) (PVA) as polymers, bovine serum albumin (BSA) as protein, and a tripeptide, reduced glutathione (GSH). In addition, a sample containing PULL/PVA and lysozyme was obtained in similar conditions. SEM analysis evidenced the formation of networks with porous structure. The average pore size was found to be between 15.7 mm and 24.5 mm. All samples exhibited viscoelastic behavior typical to networks, the hydrogel strength being influenced by the protein content. Infrared spectroscopy analysis revealed the presence of intermolecular hydrogen bonds and hydrophobic interactions (more pronounced for BSA content between 30% and 70%). The swelling kinetics investigated in buffer solution (pH = 7.4) at 37 °C evidenced a quasi-Fickian diffusion for all samples. The hydrogels were loaded with neomycin trisulfate salt hydrate (taken as a model drug), and the optimum formulations (samples containing 10–30% BSA or 2% lysozyme) have been proven to have a sustained drug release over 480 min in in simulated physiological conditions. The experimental data were analyzed using different kinetic models in order to investigate the drug release mechanism. Among them, the semi-empirical Korsmeyer–Peppas and Peppas–Sahlin models were suitable to describe in vitro drug release mechanism of neomycin sulfate from the investigated hybrid hydrogels. The structural, viscoelastic, and swelling properties of PULL/PVA/protein hybrid hydrogels are influenced by their composition and preparation conditions, and they represent important factors for in vitro drug release behavior.
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Dona, Anthony C., Guilhem Pages, Robert G. Gilbert, and Philip W. Kuchel. "Digestion of starch: In vivo and in vitro kinetic models used to characterise oligosaccharide or glucose release." Carbohydrate Polymers 80, no. 3 (May 5, 2010): 599–617. http://dx.doi.org/10.1016/j.carbpol.2010.01.002.
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Budz, J. A., M. Lore, and G. H. Nancollas. "Hydroxyapatite and Carbonated Apatite as Models for the Dissolution Behavior of Human Dental Enamel." Advances in Dental Research 1, no. 2 (December 1987): 314–21. http://dx.doi.org/10.1177/08959374870010022301.
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It is now well-established that kinetic aspects as well as considerations based solely on solubilities and thermodynamic driving forces should be taken into account while one is attempting to understand the mechanism of dental caries. In the present study, kinetic comparisons of the dissolution of hydroxyapatite, carbonated apatite, and ground human dental enamel have been made in order that the appropriateness of these synthetic phases as enamel dissolution models can be assessed. Specific additives used to form intact surface layers in vitro have also been investigated. An interesting phenomenon related to surface-controlled dissolution has been revealed. During Constant Composition experiments, the dissolution rates for all the systems decrease markedly as the reaction proceeds. Further tests with fresh crystals suggest that micro-impurities, in addition to microstructural changes of the dissolving surfaces, may play a role in the case of hydroxyapatite but do not influence the dissolution of carbonated apatite. Kinetic results for ground human enamel indicate the release of dissolution poisons. Nevertheless, the results confirm expectations that carbonated apatite may be a better model for enamel than near-stoichiometric synthetic hydroxyapatite.
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Bakliwal, A. A., D. S. Jat, S. G. Talele, and A. G. Jadhav. "FORMULATION AND EVALUATION OF NATEGLINIDE NANOSPONGES." INDIAN DRUGS 55, no. 02 (February 26, 2018): 27–35. http://dx.doi.org/10.53879/id.55.02.10717.
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The objective of the present study was to produce extended release nateglinide nanosponges for oral delivery. Preparation of nanosponges leads to solubility enhancement. Nateglinide is a BCS Class II drug, having low solubility. So, to increase the solubility of nateglinide it is formulated into nanosponges. Nanosponges using ethyl cellulose as a polymer and dichloromethane as a cross-linker were prepared successfully by ultra-sound assisted synthesis method. The effects of different drug: placebo ratios on the physical characteristics of the nanosponges as well as the drug content and in vitro drug release of the nanosponges were investigated. Particle size analysis and surface morphology of nanosponges were performed. The scanning and transmission electron microscopy of nanosponges showed that they were spongy in nature. The particle size was found to be in the range 46.37 - 97.23 nm out of which particle size of the optimized formulation was 51.79 nm and the drug content was found to 79.43 %. The optimized nanosponge formulations were selected for preparing nanosponge tablets for extended drug delivery by oral route. These tablets were prepared using xanthan gum and PVP K-30 and were evaluated by pre-compression and post-compression parameters. The nateglinide nanosponges tablet formulation were studied for different parameters using Design Expert Software. All formulations were evaluated for in vitro drug release analyzed according to various release kinetic models and it was found that it follows zero order release kinetics.
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AlMajed, Zeyad, Najla M. Salkho, Hana Sulieman, and Ghaleb A. Husseini. "Modeling of the In Vitro Release Kinetics of Sonosensitive Targeted Liposomes." Biomedicines 10, no. 12 (December 5, 2022): 3139. http://dx.doi.org/10.3390/biomedicines10123139.
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Targeted liposomes triggered by ultrasound are a promising drug delivery system as they potentially improve the clinical outcomes of chemotherapy while reducing associated side effects. In this work, a comprehensive model fitting was performed for a large dataset of liposomal release profiles with seven targeting moieties (albumin, cRGD, estrone, hyaluronic acid, Herceptin, lactobionic acid, and transferrin) in addition to the control liposomes under ultrasound release protocols. Two levels of ultrasound frequencies were tested: low frequency (20 kHz) at 6.2, 9, and 10 mW/cm2 as well as high frequencies (1.07 MHz and 3 MHz) at 10.5 and 173 W/cm2. At a low frequency, Hixson–Crowell, Korsmeyer–Peppas, Gompertz, Weibull, and Lu–Hagen showed good fits to our release profiles at all three power densities. At high frequencies, the former three models reflected the best fit. These models will aid in predicting drug release profiles for future in vitro studies.
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Zaman, M., RM Sarfraz, S. Adnan, A. Mahmood, M. Hanif, J. Qureshi, MT Chaudhary, MA Akram, and I. Bashir. "Development and in-vitro Evaluation of Once Daily Tablet Dosage Form of Loxoprofen Sodium." Tropical Journal of Pharmaceutical Research 14, no. 9 (October 9, 2015): 1557–63. http://dx.doi.org/10.4314/tjpr.v14i9.3.
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Purpose: To formulate and characterize once daily controlled release tablet of loxoprofen sodium.Methods: Eudragit RS-100, hydroxylpropyl methylcellulose (HPMC) and pectin were used as release retarding polymers. All the formulations were prepared by direct compression method. Various precompression studies were carried out to determine Hausner’s ratio, Carr’s index, angle of repose, bulk density and tapped density Differential scanning calorimetry (DSC) studies and also post-compression studies to evaluate hardness, friability, weight variation, drug content, in-vitro drug release were conducted on the tablets. The drug release data were subjected to kinetic models, including zero order, first order, Hixon Crowell, Higuchi and Korsmeyer-Peppas.Results: Compressibility index (7.6 ± 1.32 - 12.5 ± 1.43%), Hausner’s ratio (1.08 ± 0.04 - 1.14 ± 0.03), angle of repose (27.78 ± 0.47 - 30.49 ± 0.46°), hardness (6.25 ± 0.27 - 7.21±0.21 kg/cm2), friability (0.14 ± 0.06 - 0.28 ± 0.0 %), weight variation (249.5 ± 2.09 - 251.35 ± 2.41 mg) and drug content (97.30 ± 0.28 - 103.70 ± 0.31 %) were within generally accepted limits for the pre-and post-compression formulations, respectively. The tablets having the maximum amount of among the three polymers tested as matrix materials, HPMC, represented by F3 tablets, exerted better sustained release properties after 12 h. Release pattern was more of Fickian diffusion followed by Higuchi mechanism.Conclusion: The release of the loxoprofen sodium was optimized up to 12 h.Keywords: Loxoprofen, Sustained release, hydroxypropyl methylcelluose, Pectin, Eudragit, Matrix tablets
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Patel, Bharat, Satyendra Kumar Tripathi, Sandhya Pathak, Sandeep Shukla, and Archna Pandey. "Synthesis and in vitro drug release of primaquine phosphate loaded PLGA nanoparticles." European Journal of Chemistry 12, no. 4 (December 31, 2021): 482–87. http://dx.doi.org/10.5155/eurjchem.12.4.482-487.2138.
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Plasmodium falciparum is one of the most common resistant Plasmodium species responsible for high rates of morbidity and mortality in malaria patients. Clinical guidelines for the management of Plasmodium falciparum include the use of a dose of primaquine phosphate resulting intolerable side effects. Therefore, the aim of this work was to formulate primaquine phosphate-loaded PLGA nanoparticles by using a nanoprecipitation method in order to increase its bioavailability to minimize drug intake. This leads to reduced toxicity and better therapeutic efficacy of the drug. The synthesized nanoparticles were characterized by using dynamic light scattering (DLS), transmission electron microscopy (TEM), scanning electron microscopy (SEM), atomic force microscopy (AFM), Fourier transformed infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and powder X-ray diffraction (XRD). TEM analysis revealed the presence of smooth spherical-shaped nanoparticles. The drug DLS analysis confirmed the presence of negatively charged nanoparticles with particle size in the range of 100-400 nm. The drug release study was performed to analyses different kinetic models like zero-order model, first-order model, Higuchi model, Hixson-Crowell model, and Korsmeyer-Peppas model.
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Chime, Salome. "Application of Cyperus esculentus oil in the development of sustained release diclofenac sodium-loaded nanostructured lipid carrier." Journal of Current Biomedical Research 2, no. 3, May-June (June 30, 2022): 145–59. http://dx.doi.org/10.54117/jcbr.v2i3.23.
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The aim of the work was to develop sustained release diclofenac sodium nanostructured lipid carrier (NLC) using tigernut oil (TNO), solid lipids and polyethylene glycol 4000 (PEG 4000) and to evaluate the properties of the formulations. Structured lipids containing tiger nut oil, Softisan®154 and Phospholipon® 90H at varying ratios were prepared by fusion and used as the lipid carrier in formulating the NLC. PEGylated lipid carriers were also employed and the physicochemical properties of these formulations were studied using standard methods including particle size and polydispersity index, encapsulation efficiency, loading capacity and drug release. The results revealed some monodispersed nano-sized formulations that were stable over time. Particle size ranged from 75.22 ± 22.72 nm to 78.11 ± 32.73 nm. High encapsulation efficiency of about 92 % was obtained confirming the suitability of the TNO based carrier. In vitro drug release in simulated intestinal fluid (pH 7.2) revealed that PEGylated diclofenac sodium-loaded NLC exhibited significantly higher sustained release properties than the non-PEGylated formulations (p <0.05). The results of the drug release kinetics models revealed that the NLC followed a mixed order release kinetic. Hence, the findings in this work showed that TNO could be used as a lipid carrier matrix in combination with other solid lipids for the development of sustained release diclofenac sodium-loaded nanostructured lipid carrier.
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B., Preethi G., and Prashanth Kunal. "DESIGN AND EVALUATION OF CONTROLLED-RELEASE OCULAR INSERTS OF BRIMONIDINE-TARTRATE AND TIMOLOL MALEATE." International Journal of Pharmacy and Pharmaceutical Sciences 9, no. 1 (December 31, 2016): 79. http://dx.doi.org/10.22159/ijpps.2017v9i1.15199.
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<p><strong>Objective: </strong>The current work was attempted to formulate and evaluate a controlled-release matrix-type ocular inserts containing a combination of brimonidine tartrate and timolol maleate, with a view to sustain the drug release in the cul-de-sac of the eye.<strong></strong></p><p><strong>Methods: </strong>Initially, the infrared studies were done to determine the drug–polymer interactions. Sodium alginate-loaded ocuserts were prepared by solvent casting technique. Varying the concentrations of polymer—sodium alginate, plasticizer—glycerine, and cross-linking agent—calcium chloride by keeping the drug concentration constant, made a total of nine formulations. These formulations were evaluated for its appearance, drug content, weight uniformity, thickness uniformity, percentage moisture loss, percentage moisture absorption, and <em>in vitro </em>release profile of the ocuserts. Finally, accelerated stability studies and the release kinetics were performed on the optimised formulation.<strong></strong></p><p><strong>Results: </strong>It was perceived that polymer, plasticizer, and calcium chloride had a significant influence on the drug release. The data obtained from the formulations showed that formulation—F9 was the optimised formulation, which exhibited better drug release. The release data of the optimised formulation tested on the kinetic models revealed that it exhibited first-order release kinetics. <strong></strong></p><p><strong>Conclusion: </strong>It can be concluded that a natural bioadhesive hydrophilic polymer such as sodium alginate can be used as a film former to load water soluble and hydrophilic drugs like brimonidine tartrate and timolol maleate. Among all formulations, F9 with 400 mg sodium alginate, 2% calcium chloride and 60 mg glycerin were found to be the most suitable insert in terms of appearance, ease of handling, thickness, <em>in vitro</em> drug release and stability.</p>
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Hasan, Ikramul, Shovan Paul, Sharmin Akhter, Navid Jubaer Ayon, and Md Selim Reza. "Evaluation and Optimization of Influence of Permeability Property and Concentration of Polymethacrylic Polymers on Microspheres of Metformin HCl." Dhaka University Journal of Pharmaceutical Sciences 12, no. 2 (January 12, 2014): 131–41. http://dx.doi.org/10.3329/dujps.v12i2.17611.
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Metformin HCl microspheres were prepared with the aim of increasing its bioavailability and decreasing gastrointestinal side effects by means of sustained action. Eudragit RSPO and Eudragit RLPO, polymers of different permeability characteristics were used to prepare different microspheres. Emulsification solvent evaporation technique using acetone as the internal phase and liquid paraffin as the external phase was the method of choice. Six formulations were prepared using two polymers. The effect of drug loading and polymeric property on the surface morphology, entrapment efficiency, particle size and release characteristics of the microspheres were examined. FTIR and DSC studies established compatibility of the drug with the polymers. SEM studies clearly revealed the effect of drug loading and polymeric nature on the surface morphology of the microspheres. Entrapment efficiencies were within 77.09-97.11% and particle size of all the batches were in the acceptable range. Release data were treated with different mathematical kinetic models. The drug release profile showed that Eudragit RSPO and Eudragit RLPO have opposite effect on drug release. On the other hand, increase in drug loading results in increased drug release. Kinetic modeling of in vitro dissolution profiles revealed that the drug release mechanism varies from diffusion controlled to anomalous type. Dhaka Univ. J. Pharm. Sci. 12(2): 131-141, 2013 (December) DOI: http://dx.doi.org/10.3329/dujps.v12i2.17611
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Malik, Prashant, Upendra Nagaich, Raj Kaur Malik, and Neha Gulati. "Pentoxifylline Loaded Floating Microballoons: Design, Development and Characterization." Journal of Pharmaceutics 2013 (May 9, 2013): 1–5. http://dx.doi.org/10.1155/2013/107291.
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The floating microballoons have been utilized to obtain prolonged and uniform release in the stomach. The objective of the present study involves design, development, and characterization of pentoxifylline loaded floating microballoons to prolong their gastric residence time. Pentoxifylline (trisubstituted xanthine derivative) loaded microballoons were prepared by the solvent evaporation technique using different concentrations of polymers like HPMC K4M and ethyl cellulose (EC) in ethyl alcohol and dichloromethane organic solvent system. Microballoons were characterized for their particle size, surface morphology, production yield, loading efficiency, buoyancy percentage, and in vitro drug release studies. From the characterization it was observed that increases in amount of polymers (HPMC K4M and EC) led to increased particle size, loading efficiency, and buoyancy percentage, and retarded drug release. The particle size, particle yield, loading efficiency, buoyancy percentage and in vitro drug release for optimized formulation (F3) were found to be 104.0±2.87 µm, 80.89±2.24%, 77.85±0.61%, 77.52±2.04%, and 82.21±1.29%, respectively. The data was fitted to different kinetic models to illustrate its anomalous (non-Fickian) diffusion. The in vitro result showed that formulations comprised of varying concentrations of ethyl cellulose in higher proportion exhibited much retarded drug release as compared to formulations comprised of higher proportion of varying concentrations of HPMC K4M.
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Concha, Luis, Ana Luiza Resende Pires, Angela Maria Moraes, Elizabeth Mas-Hernández, Stefan Berres, and Jacobo Hernandez-Montelongo. "Cost Function Analysis Applied to Different Kinetic Release Models of Arrabidaea chica Verlot Extract from Chitosan/Alginate Membranes." Polymers 14, no. 6 (March 10, 2022): 1109. http://dx.doi.org/10.3390/polym14061109.
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This work focuses on the mathematical analysis of the controlled release of a standardized extract of A. chica from chitosan/alginate (C/A) membranes, which can be used for the treatment of skin lesions. Four different types of C/A membranes were tested: a dense membrane (CA), a dense and flexible membrane (CAS), a porous membrane (CAP) and a porous and flexible membrane (CAPS). The Arrabidae chica extract release profiles were obtained experimentally in vitro using PBS at 37 °C and pH 7. Experimental data of release kinetics were analyzed using five classical models from the literature: Zero Order, First Order, Higuchi, Korsmeyer–Peppas and Weibull functions. Results for the Korsmeyer–Peppas model showed that the release of A. chica extract from four membrane formulations was by a diffusion through a partially swollen matrix and through a water filled network mesh; however, the Weibull model suggested that non-porous membranes (CA and CAS) had fractal geometry and that porous membranes (CAP and CAPS) have highly disorganized structures. Nevertheless, by applying an explicit optimization method that employs a cost function to determine the model parameters that best fit to experimental data, the results indicated that the Weibull model showed the best simulation for the release profiles from the four membranes: CA, CAS and CAP presented Fickian diffusion through a polymeric matrix of fractal geometry, and only the CAPS membrane showed a highly disordered matrix. The use of this cost function optimization had the significant advantage of higher fitting sensitivity.
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Hasan, Md Asif, Sabiha Sultana, Sabiha Sultana, Md Masud Kaisar Bhuiyan, Md Selim Reza, and Mohammad Salim Hossain. "Formulation and In vitro Characterization of Hydrochlorothiazide Gastroretentive Floating Drug Delivery System." Dhaka University Journal of Pharmaceutical Sciences 14, no. 2 (June 28, 2016): 163–70. http://dx.doi.org/10.3329/dujps.v14i2.28506.
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The purpose of the study was to develop and optimize floating bioadhesive gastroretentive drug delivery system (GRDDS) exhibiting a unique combination of floatation and bioadhesion to prolong residence in the stomach, using hydrochlorothiazide (HCTZ) as a model drug. Formulated matrix tablets were prepared by direct compression method with two different rate controlling polymer HPMC K4M and Carbopol 971. The formulated tablets were evaluated for physical characterization, floating lag time, swelling index and drug content uniformity. The drug release study was carried out in 0.1N HCl as the medium (pH 1.2) for 8 hours using USP type II dissolution apparatus and investigated the effects of polymers on the drug release profile. In vitro buoyancy study results found to be 1033 sec and >8 h, floating lag time and total floating time respectively. Simulated drug release pattern in different kinetic models of Korsmeyer-Peppas release suggests that the mechanism controlling of the drug release from all formulations was the anomalous non-Fickian or anomalous release. Polymer with lower viscosity (HMPC K4M) was found to be beneficial than higher viscosity polymer (Carbopol 971) in improving the release properties of gastric floating drug delivery system. Incorporation of Carbopol in formulation also helped in maintaining buoyancy of system with desirable drug release. Further study is necessary in case of in vitro- in vivo relationship, but this study will ready to lend a hand to future scientists working in this field to successfully exploit the potential of this drug delivery system for the advantage of mankind.Dhaka Univ. J. Pharm. Sci. 14(2): 163-170, 2015 (December)
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Hebbar, Srinivas, Akhilesh Dubey, Ravi G. S., and Shanon Ben Mascarenhas. "STUDIES ON CROSS-LINKED CHITOSAN HYDROGEL FOR MATRIX TABLETS OF MONTELUKAST SODIUM." International Journal of Applied Pharmaceutics 9, no. 4 (July 13, 2017): 22. http://dx.doi.org/10.22159/ijap.2017v9i4.17445.
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Objective: The aim of the present study was to prepare hydrogel matrix tablets for controlled release of an anti-asthma drug (Montelukast sodium) by modifying the applications of chitosan by crosslinking it with the different cross linking agent.Methods: The hydrogels were prepared by crosslinking chitosan using three different crosslinking agents namely, anhydrous dextrose (DXT), sodium tripolyphosphate (TPP) and glutaraldehyde (GL). Formulations were prepared by direct compression method and pre and post compression parameters were evaluated.Results: FTIR (Fourier transform infrared spectroscopy) studies of tablet formulation indicated that there is no drug-excipient interaction in the prepared formulations. The matrix tablets were capable of releasing the drug for 11 h depending upon the formulation variables. The tablets prepared by plain chitosan discharged the drug quickly, while those prepared by using GL crosslinked-hydrogel released the drug more slowly in a controlled manner. In general, the order of drug release from the crosslinked hydrogel matrix tablets on the basis of crosslinking agents, was found to be DXT>TPP>GL. The type of cross-linking agents affected the drug release rate and in the case of the tablets prepared with CHTPP (95 % to 83 %) it was slower than for the tablets prepared with CHDX (96 % to 88 %) at the end of 11th h. CHGL tablets showed more prolonged drug release profiles (86 % to 74 %) as compared to CHDX and CHTPP at the end of 11th h. In vitro release data was fitted into various release kinetic models to study the release mechanism and showed zero order kinetics and “n” value were found to be less than 0.5 indicated the release mechanism followed fickian diffusion due to swelling of gel matrix and high solubility of montelukast sodium.Conclusion: From the experimental results it can be concluded that hydrogels of chitosan were successfully prepared by using DXT, TPP and GL with different concentration.
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Bhardwaj, P., R. Singh, and A. Swarup. "DEVELOPMENT AND CHARACTERIZATION OF NOVEL SITE SPECIFIC FLOATING-MUCOADHESIVE TABLETS BEARING 5-FLOUROURACIL FOR STOMACH TARGETING." INDIAN DRUGS 51, no. 09 (September 28, 2014): 23–30. http://dx.doi.org/10.53879/id.51.09.10140.
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Object of present investigation was to develop and characterize such a gastroretentive tablet, which provides the synergism effect of adhesiveness and floating property for prolonged release of 5-flourouracil within the stomach. The floating mucoadhesive tablets were prepared by the wet granulation method using different ratios of hydroxy propyl methyl cellulose (HPMC K4MCR) and Carbopol 934P as polymers. The prepared floating-mucoadhesive tables were characterized for hardness, detachment stress, floating properties, swelling index and surface morphology by SEM. The in vitro drug release and floating behaviour were studied in simulated gastric fluid (SGF) at pH 1.2. Different kinetic models for drug release were as well applied. Formulations of T-9 batch were furthermore subjected to stability and in vivo radiographic studies.
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Hamdan, Lama, and Jamila Husian. "FORMULATION AND EVALUATION IN VITRO A MATRIX TYPE OF KETOTIFEN FUMARATE TRANSDERMAL PATCHES FOR ALLERGIC DISEASES." Asian Journal of Pharmaceutical and Clinical Research 10, no. 10 (September 1, 2017): 327. http://dx.doi.org/10.22159/ajpcr.2017.v10i10.20123.
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Objective: Transdermal patches of Ketotifen fumarate (KT) were developed for prolonged effect of the drug, and to protect the patient from allergic symptoms associated with asthma and other allergic diseases.Methods: Matrix type patches were prepared by solvent casting technique using different types of polymers: Hydroxy propyl methyl cellulose (HPMC K15M) and ethyl cellulose to formed the matrix of the patch in different ratios, emulsifying agents were added as a penetration enhancers (Span 60, Tween 60, Cremophor EL) in a ratio 0.025% w/v to the matrix, 10% v/v of glycerin was added as plasticizer to 10 ml of chloroform:methanol (1:1). The drug matrix film was casted on a polyvinyl alcohol backing membrane. All patches were evaluated for physical proprieties, thickness uniformity, folding endurance, moisture uptake, moisture content, drug content, uniformity of weight, content uniformity, in vitro drug release, and kinetic models. Differential scanning calorimetry was used to characterize physical mixtures of KT and the different used excipients.Results: The results showed that the prepared patches had acceptable physical properties. The drug substance was released well. Adding the penetration enhancers delayed the release of the drug from the matrix in all the prepared formulas, formula A2 that having no enhancer, showed maximum amounts of drugs release (90.06±0.9)% for 24 hrs. However, adding penetration enhancers decreased the amount of the drug release, formula B2 having Tween 60 as a penetration enhancer, showed the maximum release of the drug (87.78±0.88)%, and formula B3 having Cremophor EL showed the minimum release of the drug (79.13±1.58) at the end of 24 hrs dissolution study. The release of the drug from all formulations was followed by Korsmeyer-Peppas pattern with n>0.45 indicating that drug release from matrix was mainly happened by swallowed and diffusion (non- Fickian pattern).Conclusion: Optimized formula A2 containing the maximum amounts of HPMC K15M showed a controlled release of the drug over 12 hrs, and it identified as a successful formulation for this study.
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Ranjha, Nazar Mohammad, Muhammad Hanif, Zunaira Afzal, and Ghulam Abbas. "Diffusion coefficient, porosity measurement, dynamic and equilibrium swelling studies of Acrylic acid/Polyvinyl alcohol (AA/PVA) hydrogels." Pakistan Journal of Pharmaceutical Research 1, no. 2 (June 1, 2015): 48. http://dx.doi.org/10.22200/pjpr.2015248-57.
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Objective of the present work was to synthesize hydrogels of acrylic acid/polyvinyl alcohol (AA/PVA) by free radical polymerization by using glutaradehyde (GA) as crosslinkers. The hydrogels were evaluated for swelling, diffusion coefficient and network parameters like the average molecular weight between crosslink’s, polymer volume fraction in swollen state, number of repeating units between crosslinks and crosslinking density by using Flory-Huggins theory. It was found that the degree of swelling of AA/PVA hydrogels increases greatly within the pH range 5-7. The gel fraction and porosity increased by increasing the concentration of AA or PVA. Increase in degree of crosslinking, decreased the porosity and inverse was observed in gel fraction. Selected samples were loaded with metoprolol tartrate. Drug release was studied in USP hydrochloric acid solution of pH 1.2 and phosphate buffer solutions of pH 5.5 and 7.5. Various kinetics models like zero order, first order, Higuchi and Peppas model were used for in vitro kinetic studies. The results showed that the drug release followed concentration dependent effect (First order kinetics) with non-Fickian diffusion. FTIR and SEM used to study the structure, crystallinity, compatibility, thermal stability and morphology of prepared and drug loaded hydrogels respectively.