Relevant bibliographies by topics / Long-acting release kinetics

Academic literature on the topic 'Long-acting release kinetics'

Author: Grafiati
Published: 10 December 2022
Last updated: 28 January 2023

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Journal articles on the topic "Long-acting release kinetics"

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Verma, Malvika, Jacqueline N. Chu, John A. F. Salama, Mohammed T. Faiz, Feyisope Eweje, Declan Gwynne, Aaron Lopes, et al. "Development of a long-acting direct-acting antiviral system for hepatitis C virus treatment in swine." Proceedings of the National Academy of Sciences 117, no. 22 (May 18, 2020): 11987–94. http://dx.doi.org/10.1073/pnas.2004746117.

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Chronic hepatitis C virus (HCV) infection is a leading cause of cirrhosis worldwide and kills more Americans than 59 other infections, including HIV and tuberculosis, combined. While direct-acting antiviral (DAA) treatments are effective, limited uptake of therapy, particularly in high-risk groups, remains a substantial barrier to eliminating HCV. We developed a long-acting DAA system (LA-DAAS) capable of prolonged dosing and explored its cost-effectiveness. We designed a retrievable coil-shaped LA-DAAS compatible with nasogastric tube administration and the capacity to encapsulate and release gram levels of drugs while resident in the stomach. We formulated DAAs in drug–polymer pills and studied the release kinetics for 1 mo in vitro and in vivo in a swine model. The LA-DAAS was equipped with ethanol and temperature sensors linked via Bluetooth to a phone application to provide patient engagement. We then performed a cost-effectiveness analysis comparing LA-DAAS to DAA alone in various patient groups, including people who inject drugs. Tunable release kinetics of DAAs was enabled for 1 mo with drug–polymer pills in vitro, and the LA-DAAS safely and successfully provided at least month-long release of sofosbuvir in vivo. Temperature and alcohol sensors could interface with external sources for at least 1 mo. The LA-DAAS was cost-effective compared to DAA therapy alone in all groups considered (base case incremental cost-effectiveness ratio $39,800). We believe that the LA-DAA system can provide a cost-effective and patient-centric method for HCV treatment, including in high-risk populations who are currently undertreated.
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Cortez, John M., Rafaela Quintero, John A. Moss, Martin Beliveau, Thomas J. Smith, and Marc M. Baum. "Pharmacokinetics of Injectable, Long-Acting Nevirapine for HIV Prophylaxis in Breastfeeding Infants." Antimicrobial Agents and Chemotherapy 59, no. 1 (October 13, 2014): 59–66. http://dx.doi.org/10.1128/aac.03906-14.

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ABSTRACTMother-to-child transmission (MTCT) of HIV-1 remains a global health problem. The World Health Organization (WHO) recommendations advise the administration of a once-daily, oral, prophylactic regimen of the nonnucleoside reverse transcriptase inhibitor nevirapine (NVP) from birth until 4 to 6 weeks of age for infants born to HIV-infected mothers in regions without access to safe and nutritionally adequate alternatives to breast milk. A critical factor driving the successful implementation of the WHO guidelines involves sustaining high adherence to the frequent dosing. With these challenges in mind, we have developed the first injectable, sustained-release NVP formulations with the goal of providing, for 6 weeks or longer, preventative plasma drug levels from a single subcutaneous administration at birth. The long-acting NVP consists of large (>50 μm), monodisperse NVP particles coated with biocompatible polymers that control the drug release kinetics. Two lead formulations exhibiting burst-free, sustained-release kinetics for up to 75 daysin vitrowere developed. Subsequentin vivostudies in rats demonstrated no toxicity related to the formulations. Rat plasma NVP concentrations were above the analytical assay's limit of quantification for up to 28 days. Pharmacokinetic analysis of the rat plasma NVP concentration-time data allowed absorption rate constants to be calculated. These data then were used to simulate infant NVP exposure from a single injected dose (<200 mg) of our long-acting formulations, demonstrating preliminary feasibility of the technology to maintain safe, preventative NVP plasma levels (0.2 to 3.0 μg ml−1) for 6 weeks or longer.
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Comets, Emmanuelle, France Mentré, Ryosei Kawai, Fritz Nimmerfall, Peter Marbach, and Jacky Vonderscher. "Modeling the Kinetics of Release of Octreotide from Long‐Acting Formulations Injected Intramuscularly in Rabbits." Journal of Pharmaceutical Sciences 89, no. 9 (September 2000): 1123–33. http://dx.doi.org/10.1002/1520-6017(200009)89:9<1123::aid-jps4>3.0.co;2-k.

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Yan, Xieguo, Shiqiang Wang, and Kaoxiang Sun. "Long-Acting Risperidone Dual Control System: Preparation, Characterization and Evaluation In Vitro and In Vivo." Pharmaceutics 13, no. 8 (August 5, 2021): 1210. http://dx.doi.org/10.3390/pharmaceutics13081210.

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Schizophrenia, a psychiatric disorder, requires long-term treatment; however, large fluctuations in blood drug concentration increase the risk of adverse reactions. We prepared a long-term risperidone (RIS) implantation system that can stabilize RIS release and established in-vitro and in-vivo evaluation systems. Cumulative release, drug loading, and entrapment efficiency were used as evaluation indicators to evaluate the effects of different pore formers, polymer ratios, porogen concentrations, and oil–water ratios on a RIS implant (RIS-IM). We also built a mathematical model to identify the optimized formulation by stepwise regression. We also assessed the crystalline changes, residual solvents, solubility and stability after sterilization, in-vivo polymer degradation, pharmacokinetics, and tissue inflammation in the case of the optimized formulation. The surface of the optimized RIS microspheres was small and hollow with 134.4 ± 3.5 µm particle size, 1.60 SPAN, 46.7% ± 2.3% implant drug loading, and 93.4% entrapment efficiency. The in-vitro dissolution behavior of RIS-IM had zero-order kinetics and stable blood concentration; no lag time was released for over three months. Furthermore, the RIS-IM was not only non-irritating to tissues but also had good biocompatibility and product stability. Long-acting RIS-IMs with microspheres and film coatings can provide a new avenue for treating schizophrenia.
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Gohn, Anne M., Amy Nolte, Ethan Ravotti, Seth P. Forster, Morgan Giles, Nathan Rudd, and Gamini Mendis. "Dissolution from Ethylene Vinyl Acetate Copolymer Long-Acting Implants: Effect of Model Active Ingredient Size and Shape." Pharmaceutics 14, no. 6 (May 27, 2022): 1139. http://dx.doi.org/10.3390/pharmaceutics14061139.

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In recent pharmaceutical applications, an active pharmaceutical ingredient (API) can be mixed with a polymer material to yield a composite long-acting drug-delivery device. These devices boast higher patient compliance, localized drug delivery, and lower dosage concentrations, which can increase patient safety. As a laboratory-safe option, calcium carbonate (CaCO3) was used as a drug surrogate to mimic the release kinetics of a low-solubility API. The release of CaCO3 from a poly(ethylene vinyl acetate) (EVA) polymer matrix was studied in ultra-high-purity water. The geometry of CaCO3, along with the manufacturing technique, was manipulated to study the implications on surrogate drug release. It was found that injection molding proved to yield higher burst release, due to higher pressures achievable during manufacturing. The extrusion process can affect the surface concentration of the pharmaceutical ingredient when extruded through a water bath, resulting in a lower initial burst concentration. Regarding CaCO3 geometry, the particle size was more critical than the surface area in terms of CaCO3 release. Larger particles showed a higher release rate, though they also displayed higher variability in release. These data can be used to engineer specific release profiles when designing composite formulations and manufacturing methods for pharmaceutical-drug-delivery applications.
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Wojcik-Pastuszka, Dorota, Justyna Krzak, Bartosz Macikowski, Ryszard Berkowski, Bogdan Osiński, and Witold Musiał. "Evaluation of the Release Kinetics of a Pharmacologically Active Substance from Model Intra-Articular Implants Replacing the Cruciate Ligaments of the Knee." Materials 12, no. 8 (April 12, 2019): 1202. http://dx.doi.org/10.3390/ma12081202.

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Implants are readily applied as a convenient method of therapy. There is great interest in the prolonged release of active substances from implants. The objective of this work was to evaluate the dissolution kinetics of steroidal anti-inflammatory preparation (SAP) released from novel implants, and to test the influence of the technology on SAP release kinetics. The proposed long-acting preparations may overcome difficulties resulting from repeated injections and often visits to ambulatory clinic, as the stabilizing function of the artificial ligament would be enriched with pharmacological activity. The potential advantages provided by the new coatings of knee implants include the continuous, sustained, and prolonged release of an active substance. The study was carried out using a modified United States Pharmacopoeia (USP) apparatus 4. The amount of SAP was measured spectroscopically. It was revealed that the transport of the drug was mainly a diffusion process. The drug release kinetics was analyzed using zero-, first-, and second-order kinetics as well as Korsmeyer-Peppas, Higuchi, and Hixon-Crowell models. The highest values of the release rate constants were k0 = (7.49 ± 0.05) × 10−5 mg × min−1, k1 = (6.93 ± 0.05) × 10−6 min−1, and k2 = (7.70 ± 0.05) × 10−7 mg−1 × min−1 as calculated according to zero-, first-, and second-order kinetics equations, respectively. The values of the rate constants obtained for the slowest process were k0 = (3.63 ± 0.06) × 10−5 mg × min−1, k1 = (2.50 ± 0.03) × 10−6 min−1, and k2 = (2.80 ± 0.03) × 10−7 mg−1 × min−1. They may suggest the possibility of sustained release of betamethasone from the system. Due to the statistical analysis, differences were observed between most of the studied implants. Incubation, temperature, time of stabilization of layers, and the method of SAP deposition on the matrix affected the drug release.
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Gao, Ge Fiona, Mukul Ashtikar, Ryo Kojima, Takatsune Yoshida, Masanori Kaihara, Tomokazu Tajiri, Saeed Shanehsazzadeh, Harshvardhan Modh, and Matthias G. Wacker. "Predicting drug release and degradation kinetics of long-acting microsphere formulations of tacrolimus for subcutaneous injection." Journal of Controlled Release 329 (January 2021): 372–84. http://dx.doi.org/10.1016/j.jconrel.2020.11.055.

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Chrysafi, Iouliana, Stavroula Nanaki, Alexandra Zamboulis, Margaritis Kostoglou, Eleni Pavlidou, and Dimitrios N. Bikiaris. "Poly(Lactic Acid) Block Copolymers with Poly(Hexylene Succinate) as Microparticles for Long-Acting Injectables of Risperidone Drug." Polymers 14, no. 19 (September 30, 2022): 4111. http://dx.doi.org/10.3390/polym14194111.

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In the present work, Risperidone microparticles from poly(lactic acid)/poly(hexylene succinate) (PLA-b-PHSu) block copolymers in different ratios, 95/05, 90/10 and 80/20 w/w, were examined as long-acting injectable formulations. Nuclear magnetic resonance (NMR) was used to verify the successful synthesis of copolymers. Enzymatic hydrolysis showed an increase in weight loss as the content of PHSu increased, while the cytotoxicity studies confirmed the biocompatibility of the copolymers. The polyesters were further used to encapsulate Risperidone by spray drying. The drug-loaded microparticles were studied by Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM) and X-ray diffraction (XRD). SEM microphotographs confirmed that spherically shaped microparticles were prepared with sizes about 5–12 μm, while XRD and differential scanning calorimetry (DSC) studies evidenced that Risperidone was encapsulated in amorphous form. The drug loading and the entrapment efficiency of Risperidone were studied as well as the in vitro release from the prepared microparticles. As the content of PHSu increased, a higher release of Risperidone was observed, with PLA-b-PHSu 80/20 w/w succeeding to release 100% of RIS within 12 days. According to theoretical modeling, the kinetics of RIS release from PLA-b-PHSu microparticles is complex, governed by both diffusion and polymer erosion.
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Nanaki, Stavroula, Panagiotis Barmpalexis, Alexandros Iatrou, Evi Christodoulou, Margaritis Kostoglou, and Dimitrios Bikiaris. "Risperidone Controlled Release Microspheres Based on Poly(Lactic Acid)-Poly(Propylene Adipate) Novel Polymer Blends Appropriate for Long Acting Injectable Formulations." Pharmaceutics 10, no. 3 (August 13, 2018): 130. http://dx.doi.org/10.3390/pharmaceutics10030130.

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The present study evaluates the preparation of risperidone controlled release microspheres as appropriate long-acting injectable formulations based on a series of novel biodegradable and biocompatible poly(lactic acid)–poly(propylene adipate) (PLA/PPAd) polymer blends. Initially, PPAd was synthesized using a two-stage melt polycondensation method (esterification and polycondensation) and characterized by 1H-NMR, differential scanning calorimetry (DSC), and powder X-ray diffraction (XRD) analyses. DSC and XRD results for PLA/PPAd blends (prepared by the solvent evaporation method) showed that these are immiscible, while enzymatic hydrolysis studies performed at 37 °C showed increased mass loss for PPAd compared to PLA. Risperidone-polyester microparticles prepared by the oil–water emulsification/solvent evaporation method showed smooth spherical surface with particle sizes from 1 to 15 μm. DSC, XRD, and Fourier-transformed infrared (FTIR) analyses showed that the active pharmaceutical ingredient (API) was dispersed in the amorphous phase within the polymer matrices, whereas in vitro drug release studies showed risperidone controlled release rates in all PLA/PPAd blend formulations. Finally, statistical moment analysis showed that polyester hydrolysis had a major impact on API release kinetics, while in PLA/PPAd blends with high PLA content, drug release was mainly controlled by diffusion.
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Sonam, ,., Nilesh Jain, and Jitendra Banveer. "Formulation, Development and Evaluation of Gastroretentive Sustained Release Tablets of Lansoprazole Using Natural Polymer." Journal of Drug Delivery and Therapeutics 11, no. 5-S (November 21, 2021): 108–12. http://dx.doi.org/10.22270/jddt.v11i5-s.5087.

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The goal of this study is to develop a long-acting Lansoprazole delivery system. Lansoprazole belongs to a class of antisecretory drugs known as substituted benzimidazoles, which decrease gastric acid secretion by inhibiting the (H+,K+)-ATPase enzyme system at the secretory membrane of the stomach parietal cell. Due to its mechanism of action, despite its short half-life of 1-5 hours, it can effectively block acid secretion for 24 hours. However, as his plasma concentration falls, the effect will diminish. Lansoprazole will be given as a sustained release tablet to avoid multiple dosing or to reduce the frequency of dose. Lansoprazole was produced and analysed utilizing natural and synthetic polymers such as Xanthan gum, Gellan gum, Carbopol 940 P, and Chitosan. Based on the findings of this experiment, it was determined that formulation F7 demonstrated sustained drug release for up to 12 hours in all developed formulations. Formulation (F1, F2, F3, F4, F5, and F6) were tested in vitro for drug release. For the improved formulation F7, the formulation and release kinetics were estimated. When the regression coefficient values of were evaluated, it was found that Peppas had the highest ‘r2' value, 0.952, indicating that drug release from formulations followed Peppas release kinetics. Key words: Lansoprazole, Sustain release tablets, Synthetic and Natural Polymers, formulation, evaluation
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Books on the topic "Long-acting release kinetics"

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Cavacuiti, Christopher. The Pharmacology of Opioids (DRAFT). Oxford University Press, 2018. http://dx.doi.org/10.1093/med/9780190265366.003.0008.

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This chapter focuses on the attributes of and component medications within the class of opioids, emphasizing kinetics, dynamics, and therapeutic and adverse effects. To help patients make informed decisions about opioid use, the clinicians prescribing these medications must be able to explain when opioids are likely to help and when they are likely to do harm. Subclasses of opioids include phenanthrenes, benzomorphans, phenylpiperidines, and diphenylheptanes; examples are given of each, with respective utilities and limitations. A discussion then follows of pharmacodynamics, pharmacokinetics, opioid receptor affinity, metabolism, and drug interactions. Tables and figures amplifying the text include: opioid class by synthetic method (Table 8.1); common physiological effects by opioid receptor subtypes (Table 8.2); opioid activity (Table 8.3); and a listing of figures and tables located in Appendix B (opioid receptor affinity, respiratory depression with opioids, adverse effects, metabolism, pharmacogenetics, extended release/long-acting opioids, abuse deterrent formulations). A text box provides supplemental resources.
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Conference papers on the topic "Long-acting release kinetics"

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Åman, Rafael, Pavel Ponomarev, Lauri O. Luostarinen, Heikki Handroos, Juha Pyrhönen, and Laurila Lasse. "Experimental Analysis of Electro-Hydraulic Hybrid Actuator System for Off-Highway Working Vehicles." In 8th FPNI Ph.D Symposium on Fluid Power. American Society of Mechanical Engineers, 2014. http://dx.doi.org/10.1115/fpni2014-7826.

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Electro-hydraulic hybrid power transmission system can save energy and thus reduce the pollution while maintaining the same performance in comparison to the conventional fluid power system in off-highway working vehicles. This paper introduces experimental analysis of an electro-hydraulic hybrid actuator system specially developed for the recuperation of the potential and kinetic energy in off-highway working vehicles. In this compact assembly all the components are located near each other to save space. Proposed hybrid actuator system can be controlled directly by an electrical frequency converter which allows the replacement of long lossy fluid power transmission lines with electrical cables. Integrated electro-hydraulic energy converter (IEHEC) is the principal component of the proposed hybrid actuator system. The energy converter consists of a fixed-displacement hydraulic pump-motor and an integrated electrical permanent magnet synchronous motor-generator. IEHEC unit can be driven in four quadrants to produce the mechanical power required for the hydraulic actuator, or to recover the energy released by the actuator mechanism and supply it back to electrical circuit. Suitable places for this application are all actuators that carry out work cycle in which the kinetic and potential energy is available for recovery, e.g. lifting cylinders in cranes, fork lift trucks, etc. The test rig allows the experimental analysis of behavior of real power transmission system in two modes while using simulated loads. The first mode is the work cycle mode using IEHEC as motor connected to the hydraulic pump. The other mode is the energy recovery mode while direction of operation is reversed. The real-time simulated loads, which are carried out by simulating typical work cycle of a mechanism, enable the loading in the work cycle and provide the recoverable energy in the recovery mode. The forces acting in actuator connection point are implemented in the test rig by a hydraulic cylinder which is controlled by bandwidth proportional cartridge valves and a dSpace Real-time Control system. The electro-hydraulic hybrid actuator system was simulated in a certain loading case using virtual simulation and also hardware-in-the-loop (HIL) simulation in the test rig. The responses were compared. Experimental analysis of the dynamic behaviour of a real electro-hydraulic hybrid actuator system has been carried out by using HIL simulation.
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