Academic literature on the topic 'Drugs – Solubility – Testing'
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Journal articles on the topic "Drugs – Solubility – Testing"
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D’Souza, Malcolm J., Ghada J. AlAbed, Melissa Earley, Natalia Roberts, and Fady J. Gerges. "Manipulating In-House Designed Drug Databases For The Prediction Of pH-Dependent Aqueous Drug Solubility." American Journal of Health Sciences (AJHS) 4, no. 3 (August 14, 2013): 137–50. http://dx.doi.org/10.19030/ajhs.v4i3.8010.
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Chemical, pharmacokinetic, and pharmacodynamics properties are available in the package inserts of every Food and Drug Administration (FDA) approved prescription drug, including all available chemotherapy drugs. These inserts follow a specific format imposed by the FDA. Whether chemotherapy drugs are administered via the parenteral route or alimentary tract, a significant factor affecting their bioavailability, elimination, and consequently, the drug’s effectiveness and potency, is its state of aqueous solubility. Water solubility has always lent itself poorly to the different predictive and experimental measures employed in the determination of a useful quantitative assessment. In this project, we first built a chemical structure-based searchable database for 85 FDA approved chemotherapy drugs and then used Bio-Rad’s KnowItAll® Informatics suite to focus on the drugs pH-dependent water solubility prediction. We compared the predicted values for water solubility to the available values reported in the drug inserts, testing the practical utility and the predictive ability of our model in reporting such a clinically relevant, underreported pharmacokinetic parameter. A relational cancer drug database (MySQL) was created to further facilitate analysis and/or prediction of a chemotherapy compound’s missing pharmacokinetic properties.
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de Vos, Dick, Rudolph Willem, Marcel Gielen, Kyra E. van Wingerden, and Kees Nooter. "The Development of Novel Organotin Anti-Tumor Drugs: Structure and Activity." Metal-Based Drugs 5, no. 4 (January 1, 1998): 179–88. http://dx.doi.org/10.1155/mbd.1998.179.
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An overview of the development of anti-tumor organotin derivatives in selected classes of compounds is presented and discussed. High to very high in vitro activity has been found, sometimes equaling that of doxorubicin. Solubility in water is an important issue, dominating the in vivo testing of compounds with promising in vitro properties. The cytotoxicity of the compounds was increased by the presence of a bulky group, an active substituent or one or more polar substituents. Polar substituents may also improve the water solubility. Although organotin derivatives constitute a separate class of compounds, the comparison with cisplatin is inevitable. Among the observed toxicities, neurotoxicity, known from platinum cytostatics, and gastrointestinal toxicity, typical for many oncology drugs, have been detected. Further research to develop novel, useful organotin anti-tumor compounds should be carried out.
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Grimberg, Dominic C., Ankeet Shah, Wei Phin Tan, Wiguins Etienne, Ivan Spasojevic, and Brant A. Inman. "Hyperthermia Improves Solubility of Intravesical Chemotherapeutic Agents." Bladder Cancer 6, no. 4 (December 14, 2020): 461–70. http://dx.doi.org/10.3233/blc-200350.
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BACKGROUND: Nearly 70% of all new cases of bladder cancer are non-muscle invasive disease, the treatment for which includes transurethral resection followed by intravesical therapy. Unfortunately, recurrence rates approach 50% in part due to poor intravesical drug delivery. Hyperthermia is frequently used as an adjunct to intravesical chemotherapy to improve drug delivery and response to treatment. OBJECTIVE: To assess the solubility profile of intravesical chemotherapies under varying conditions of pH and temperature. METHODS: Using microplate laser nephelometry we measured the solubility of three intravesical chemotherapy agents (mitomycin C, gemcitabine, and cisplatin) at varying physical conditions. Drugs were assessed at room temperature (23°C), body temperature (37°C), and 43°C, the temperature used for hyperthermic intravesical treatments. To account for variations in urine pH, solubility was also investigated at pH 4.00, 6.00, and 8.00. RESULTS: Heat incrementally increased the solubility of all three drugs studied. Conversely, pH largely did not impact solubility aside for gemcitabine which showed slightly reduced solubility at pH 8.00 versus 6.00 or 4.00. Mitomycin C at the commonly used 2.0 mg/mL was insoluble at room temperature, but soluble at both 37 and 43°C. CONCLUSIONS: Hyperthermia as an adjunct to intravesical treatment would improve drug solubility, and likely drug delivery as some current regimens are insoluble without heat. Improvements in solubility also allow for testing of alternative administration regimens to improve drug delivery or tolerability. Further studies are needed to confirm that improvements in solubility result in increased drug delivery.
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Sopyan, Iyan, Dolih Gozali, and Eka Paramudya. "Formulation and Stability Testing of Microemulsion Griseovulfin." Indonesian Journal of Pharmaceutics 2, no. 2 (June 17, 2020): 32. http://dx.doi.org/10.24198/idjp.v2i2.27574.
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The use of drugs that are less soluble in water will become clinically less efficient, this is caused by the low penetration of the drug into the body. A microemulsion is a dispersion system such as an emulsion that can increase the solubility of drugs that are sometimes difficult to dissolve in water. Microemulsions have long-term stability, clear, transparent, and good penetration capabilities. In this study, a microemulsion formulation with active ingredients griseofulvin and virgin coconut oil was conducted as an oil phase. The resulting microemulsion evaluates physical stability during 35 storage days. The results showed that the microemulsion preparation remained stable during storage time without changes in color, odor, and consistency, while the pH and dosage viscosity experienced less significant changes. The consequences of the centrifugation test at 3700 rpm for 5 hours and freezing tests for 24 days showed stable preparation and cannot be separated. The diffusion test results obtained by FG2 had the largest permeation percentages of 3.6136%, FG3 2.8724%, and the smallest FG1 2.0477%.Keywords: microemulsion, griseofulvin, stability, diffusion test
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Viviane Annisa, Teuku Nanda Saifullah Sulaiman, and Agung Endro Nugroho. "Biorelevant dissolution models to assess precipitation of weak base drug." International Journal of Research in Pharmaceutical Sciences 11, SPL4 (December 21, 2020): 2165–72. http://dx.doi.org/10.26452/ijrps.v11ispl4.4438.
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The impact of precipitation can affect the amount of drug absorbed, thereby affecting the amount of drug in the systemic body. The precipitation process is preceded by a supersaturation phase, caused by decreased drug solubility in the gastrointestinal tract. This precipitation occurs for weak base drugs with low solubility. When the drug entering the small intestine, the solubility of weak base drugs decrease, then occurs supersaturation, which leads to precipitation, so that drug precipitation is one of a challenge for the pharmaceutical industry in drug development. Precipitation testing of water-soluble weak base drugs can be carried out by the pH shift method to describe the gastrointestinal pH gradient from gastric to small intestine. This pH change can cause supersaturation and then trigger precipitation, especially for weak base drugs. The methods that can used to assess precipitation drug is modification of the USP dissolution which are two compartment and multi compartment model. The choice of dissolution medium play an important role in the test results. The use of bio relevant medium can produce closer in vitro and in vivo correlations than the use of buffers. Generally, the medium used to simulate the weakly condition in the small intestine is FaSSIF (Fasted State Simulated Intestinal Fluid) or FeSSIF (Fed State Stimulate Intestinal Fluid) medium. The medium used to simulate the acidic condition in the stomach is FaSSGF (Fasted state simulated gastric fluid) or FeSSGF (Fed state simulated gastric fluid) medium.
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Shin, Hey-Won, Joo-Eun Kim, and Young-Joon Park. "Nanoporous Silica Entrapped Lipid-Drug Complexes for the Solubilization and Absorption Enhancement of Poorly Soluble Drugs." Pharmaceutics 13, no. 1 (January 6, 2021): 63. http://dx.doi.org/10.3390/pharmaceutics13010063.
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This study aims to examine the contribution of nanoporous silica entrapped lipid-drug complexes (NSCs) in improving the solubility and bioavailability of dutasteride (DUT). An NSC was loaded with DUT (dissolved in lipids) and dispersed at a nanoscale level using an entrapment technique. NSC microemulsion formation was confirmed using a ternary phase diagram, while the presence of DUT and lipid entrapment in NSC was confirmed using scanning electron microscopy. Differential scanning calorimetry and X-ray diffraction revealed the amorphous properties of NSC. The prepared all NSC had excellent flowability and enhanced DUT solubility but showed no significant difference in drug content homogeneity. An increase in the lipid content of NSC led to an increase in the DUT solubility. Further the NSC were formulated as tablets using D-α tocopheryl polyethylene glycol 1000 succinate, glyceryl caprylate/caprate, and Neusilin®. The NSC tablets showed a high dissolution rate of 99.6% at 30 min. Furthermore, NSC stored for 4 weeks at 60 °C was stable during dissolution testing. Pharmacokinetic studies performed in beagle dogs revealed enhanced DUT bioavailability when administered as NSC tablets. NSC can be used as a platform to develop methods to overcome the technical and commercial limitations of lipid-based preparations of poorly soluble drugs.
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Hopkinson, Desirée, Peter Scheiner, and Frank A. Barile. "In Vitro Cytotoxicity Testing of Potentially Active Anti-HIV Drugs with Cultured Cells." Alternatives to Laboratory Animals 24, no. 3 (June 1996): 413–18. http://dx.doi.org/10.1177/026119299602400316.
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This study compared the ability of two continuous cell lines to predict the cytotoxicity of potentially active anti-HIV drugs. Human fetal lung fibroblasts (HFL1) and CD4+ T-lymphocytes (CEM-IW) were incubated in the absence or presence of increasing concentrations of 12 antiviral compounds. These six-membered unsaturated nucleoside analogues were stereospecifically synthesised in our laboratories, and were evaluated for cytotoxicity as well as for antiviral activity. Cells were incubated for six days and mitochondrial activity (XTT and MTT assays) was used to assess cytotoxicity. IC50 values were derived from concentration–effect curves after linear regression analysis. Comparison of the two sets of cytotoxicity data suggests that the experimental IC50 values from HFL1 cells correlate well with the values obtained in lymphocyte studies performed at the National Cancer Institute laboratories (r value = 0.93). For the 12 antiviral chemicals, and those we have tested previously, these methods probably detect basal cytotoxicity, i.e. the toxicity of a chemical to basic cellular functions and structures common to all mammalian specialised cells. However, as with any testing procedure, some chemicals may elude the cytotoxicity screen, as a result of false negatives due to solubility, miscibility and organ-specific effects, and could be mislabelled as having low toxic potential. It is therefore conceivable that tests involving continuous differentiated cell lines of various origins could be developed to cover a large percentage of toxic effects, thereby reducing the need to introduce many laborious assay systems with freshly-isolated primary cultures.
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Santhosh Raja M and Venkataramana K. "Formulation Characterization And Invitro, Invivo Evaluation Of Stabilized Rosuvastatin Calcium Nanosuspension." International Journal of Research in Pharmaceutical Sciences 11, no. 2 (June 13, 2020): 2657–64. http://dx.doi.org/10.26452/ijrps.v11i2.2280.
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Rosuvastatin calcium is a BCS class II drug which is used as hyper lipidemic. Many of BCS class II drugs offer the disadvantage of solubility, to overcome the issue of solubility nanoparticle preparation is an promisable approach. A simple and efficient technique for the preparation of nanoparticles is precipitation technique. Polymeric nano particles have been prepared by employing nano precipitation technique. The nanosuspensions were prepared by using PVP K30, HPMC K15M, Eudragit L100 in various ratios using precipitation technique. The compatibility between the drug and various ingredients are tested by DSC. The formed nanoparticles were evaluated for various testing parameters like particle size, zetapotential, drug content and dissolution testing. Among all the formulations the nanosuspension prepared with Eudragit L 100 showed better characteristics. The dissolution test showed the drug release for 12 hours. The best formulation showed the particle size of 100.5 ± 5.4 nm and zeta potential of -55.1 mv. The invivo studies on the wistar rats showed better pharmacokinetic parameters when compared to the pure drug. Nano precipitation method was successfully employed to prepare Rosuvastatin calcium nanosuspension to improve the dissolution as well as bioavailability.
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Viana, Olimpia Maria, Ramon Alves, Jennifer Jacon, Antonio Carlos Doriguetto, Magali Araújo, and Rudy Bonfilio. "Evaluation of the polymorphism effects in the dissolution of Carvedilol tablets." Acta Crystallographica Section A Foundations and Advances 70, a1 (August 5, 2014): C1577. http://dx.doi.org/10.1107/s2053273314084228.
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Polymorphism in solids is a common phenomenon in drugs, which occurs when an active pharmaceutical ingredient shows up in two or more crystalline forms. The polymorphism may influence the physical and chemical properties of pharmaceutical solids, particularly, solubility and dissolution rates which are very important properties because changes in these parameters may affect the absorption and consequently the bioavailability of drugs (especially those that have a low solubility). Carvedilol is an alpha and beta blocking agent that is used for the treatment of various cardiovascular disorders such as angina pectoris, congestive heart failure and hypertension. This work aims to prepare and characterize the forms II and III of Carvedilol drug and compare them in terms of solubility and dissolution rates. Carvedilol raw material was used as source of form II and Form III, and the last is a hemihydrate of Carvedilol that was obtained by a recrystallization process in ethanol/water 1:1 v/v. Both of the crystalline forms have been identified in this study by Powder X-Ray Diffraction experiments and attenuated total reflectance Fourier transform infrared spectroscopy studies demonstrated that the spectra of forms II and III of Carvedilol have no significant differences. The Thermal Analysis curves, as expected, allowed us to discriminate between the two forms due to a hydratation of Form III. In the solubility study, it was found that the polymorphic Form II is more soluble than Form III in certain conditions (pH 1.0 to 7.2). Dissolution studies have shown that polymorphism may influence the quality of Carvedilol tablets, since form III showed a higher drug release after 20 minutes of dissolution testing. Our results suggest that the identification of polymorphic phases should be a mandatory test for Carvedilol in an official compendium. Acknowledgments: We thank FAPEMIG, FINEP, CAPES and CNPq for their financial support.
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Tay, Erin, Tri-Hung Nguyen, Leigh Ford, Hywel D. Williams, Hassan Benameur, Peter J. Scammells, and Christopher J. H. Porter. "Ionic Liquid Forms of the Antimalarial Lumefantrine in Combination with LFCS Type IIIB Lipid-Based Formulations Preferentially Increase Lipid Solubility, In Vitro Solubilization Behavior and In Vivo Exposure." Pharmaceutics 12, no. 1 (December 22, 2019): 17. http://dx.doi.org/10.3390/pharmaceutics12010017.
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Lipid based formulations (LBFs) are commonly employed to enhance the absorption of highly lipophilic, poorly water-soluble drugs. However, the utility of LBFs can be limited by low drug solubility in the formulation. Isolation of ionizable drugs as low melting, lipophilic salts or ionic liquids (ILs) provides one means to enhance drug solubility in LBFs. However, whether different ILs benefit from formulation in different LBFs is largely unknown. In the current studies, lumefantrine was isolated as a number of different lipophilic salt/ionic liquid forms and performance was assessed after formulation in a range of LBFs. The solubility of lumefantrine in LBF was enhanced 2- to 80-fold by isolation as the lumefantrine docusate IL when compared to lumefantrine free base. The increase in drug loading subsequently enhanced concentrations in the aqueous phase of model intestinal fluids during in vitro dispersion and digestion testing of the LBF. To assess in vivo performance, the systemic exposure of lumefantrine docusate after administration in Type II-MCF, IIIB-MCF, IIIB-LCF, and IV formulations was evaluated after oral administration to rats. In vivo exposure was compared to control lipid and aqueous suspension formulations of lumefantrine free base. Lumefantrine docusate in the Type IIIB-LCF showed significantly higher plasma exposure compared to all other formulations (up to 35-fold higher). The data suggest that isolation of a lipid-soluble IL, coupled with an appropriate formulation, is a viable means to increase drug dose in an oral formulation and to enhance exposure of lumefantrine in vivo.
Dissertations / Theses on the topic "Drugs – Solubility – Testing"
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Tandya, Andrian Chemical Sciences & Engineering Faculty of Engineering UNSW. "Dense gas particle processing for alternative drug delivery formulations." Awarded by:University of New South Wales. School of Chemical Sciences and Engineering, 2006. http://handle.unsw.edu.au/1959.4/25480.
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Pulmonary and oral drug administrations are usually the preferred methods of delivery of active pharmaceutical ingredients.Generally,pulmonary drug formulations are more attractive compared to oral formulations since they consist of micron-sized powders with high surface area thus having faster onset of action,as well as minimizing the drug dosage and side effects.Oral insulin formulations,if achievable,would provide an alternative to injectable insulin,as the common drawbacks of injectable insulin are the multiple daily injections and the possibility of skin infections at the injection site. In this study,the feasibility of using dense gas particle processing techniques known as the Aerosol Solvent Extraction System (ASES),Gas Anti-Solvent (GAS)and High-Pressure Media Milling (HPMM)for pharmaceutical processing was assessed.The ASEStechnique,utilizing dense ethane,was employed to prepare insulin-lactose formulations for pulmonary administration whilst the GAS and ASES techniques,utilizing dense CO2,were employed to prepare microencapsulated formulations containing insulin and Eudragit?? S100 for oral administration.Furthermore,the HPMM technique,utilizing dense hydrofluocarbon (HFC)134a/227ea,was employed to prepare suspension Metered Dose Inhaler (MDI)formulations containing budesonide and various surfactants. The Fine Particle Fraction (FPF)of processed insulin without the presence of lactose was found to be 44%.In other words,44% of processed insulin delivered to the impactor stages (excluding the throat and neck)has aerodynamic diameter of less than 5??m.With the addition of lactose as carrier,the FPFof the insulin-lactose (1:1w/w)formulation increased to 64%.The increase in FPFwas attributed to the lower density of lactose particles compared to that of insulin particles to produce an intimate mixture with enhanced powder flowability and aerodynamic performance. Proteins for oral delivery should ideally be formulated with acid-resistant polymer as a protective coating to protect against enzymatic degradation in the stomach.Eudragit?? S100,which is insoluble or almost impermeable at pH 1-4and soluble at pH 5-7,was used to prepare oral insulin formulations.The insulin release at pH 3was sustained by the Eudragit?? S100coating and the encapsulation efficiency of insulin??Eudragit?? S100formulations varied between 6% and 24% depending on the initial drug to polymer ratio. One of the major therapies utilizing metered dose inhaler formulations in the treatment of asthma has been studied using the HPMM process.The HPMM process has been demonstrated to be an efficient milling process for the enhancement of the physical stability and aerodynamic performance of budesonide in HFC-134a/227ea propellant formulations.No significant change in physical stability was observed in the formulations for 2 weeks.
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Bruce, Caroline Dietzsch 1976. "Recrystallization of guaifenesin from hot-melt extrudates containing Acryl-EZE® or Eudragit® L100-55." Thesis, 2008. http://hdl.handle.net/2152/3851.
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The physical stability of guaifenesin in melt-extruded acrylic matrix tablets was investigated. The initial study found that recrystallization was caused by guaifenesin supersaturation in Eudragit[Trademark] L100-55, and that the instability was confined to tablet surfaces. Drug release was not affected by crystal growth as guaifenesin is very water soluble. The addition of a polymer in which guaifenesin showed a higher solubility to the matrix blend decreased recrystallization on storage as supersaturation levels dropped. The second investigation identified heterogeneous nucleation as an additional factor in guaifenesin recrystallization. A quantitative assay showed that talc in matrix tablets accelerated the onset and extent of the recrystallization due to a nucleating effect on guaifenesin. Storage under elevated humidity conditions promoted recrystallization as well, but crystal growth was not correlated with water uptake, which implied a nucleating effect of moisture on guaifenesin. The third study investigated the effect of aqueous film-coating of the matrix tablets to stabilize amorphous guaifenesin using either hypromellose or ethylcellulose as coating polymers. The selection of the coating polymer influenced crystal morphology, and was a major factor in delaying the onset of crystallization, ranging from 1-3 weeks (ethylcellulose film-coatings) to 3-6 months (hypromellose film-coatings). Higher weight gains retarded recrystallization. Factors promoting drug and polymer diffusion, such as long curing times and elevated temperatures during both curing and storage, incomplete film coalescence and high core drug concentrations all resulted in an earlier onset of crystallization. The effects of single-screw extrusion (SSE) and twin-screw extrusion (TSE) of diltiazem hydrochloride and guaifenesin-containing blends in Eudragit[Trademark] L100-55 on drug morphology and dispersion were studied in the fourth project. Guaifenesin solubilized diltiazem hydrochloride, and plasticized Eudragit[Trademark] L100-55. Extrusion temperature influenced the drug morphology in single-screw extrudates, while TSE rendered all formulations amorphous due to higher dispersive mixing capabilities. Drug distribution improved with extrusion temperature and by TSE over SSE. Homogeneous matrices showed the slowest drug release at pH 1.0. Recrystallization was inversely correlated to drug distribution. In conclusion, the physical stability of guaifenesin in hot melt-extruded acrylic matrix tablets was shown to be affected by formulation, processing and post-processing factors.text
Books on the topic "Drugs – Solubility – Testing"
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Hanson, Royal. Handbook of dissolution testing. 3rd ed. Hockessin, Del: Dissolution Technologies, 2004.
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Pharmaceutical dissolution testing. New York: Marcel Dekker, 1992.
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Hanson, William A. Handbook of dissolution testing. 2nd ed. Eugene, Or: Aster Pub. Corp., 1991.
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Banakar, Umesh V. Drug dissolution and bioavailability: Critical considerations including simulations and predictions : 3-day seminar. [s.l.]: [Technomic Pub. Co], 1994.
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(Editor), Jennifer J. Dressman, and Johannes Kramer (Editor), eds. Pharmaceutical Dissolution Testing. Informa Healthcare, 2005.
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1952-, Young David, Devane John G, and Butler Jackie, eds. In vitro-in vivo correlations. New York: Plenum Press, 1997.
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Drug Dissolution & Bioavailability. (Seminar Notes - Oct. 1993). Technomic Pub Co, 1994.
Find full textBook chapters on the topic "Drugs – Solubility – Testing"
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Kwon, Keehwan, and Scott N. Peterson. "Expression and Solubility Testing in a High-Throughput Environment." In Structural Genomics and Drug Discovery, 75–88. New York, NY: Springer New York, 2014. http://dx.doi.org/10.1007/978-1-4939-0354-2_6.
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Jouyban, Abolghasem, and Mohammad A. A. Fakhree. "Experimental and Computational Methods Pertaining to Drug Solubility." In Toxicity and Drug Testing. InTech, 2012. http://dx.doi.org/10.5772/19206.
Full textConference papers on the topic "Drugs – Solubility – Testing"
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Shi, Gengbei, and Robin N. Coger. "Enhanced Oxygen Delivery to Liver Tissue Equivalent by Perfluorocarbon." In ASME 2010 Summer Bioengineering Conference. American Society of Mechanical Engineers, 2010. http://dx.doi.org/10.1115/sbc2010-19190.
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Bioartificial Liver Devices (BALs) have the potential to serve as a bridge strategy for patients awaiting liver transplants, and also show promise as drug testing platforms for the pharmaceutical industry [1]. Yet the limitations of O2 transport through the 3D tissue structures of current designs continue to present engineering challenges. In previous work our group successfully improved O2 availability for hepatocytes by introducing micropathways within the BAL’s cellular space [3–5]. The current study investigates the benefits of increasing O2 availability of the flow medium via perfluorocarbons (PFCs). PFCs were chosen since they have demonstrated effectiveness in increasing the overall oxygen solubility of their carrier liquids, e.g., artificial blood [2]. The study seeks to clarify the effects of PFCs on hepatocyte viability and functional performance under various culture conditions.