Download or read book Solubility enhancement of poorly water soluble drugs by solid dispersion written by Adela Kalivoda and published by Cuvillier Verlag. This book was released on 2012-06-25 with total page 198 pages. Available in PDF, EPUB and Kindle. Book excerpt: Summary Solid dispersions are a promising approach for controlled release drug delivery systems as both the bioavailability enhancement of poorly water-soluble drugs as well as the sustained release of water-soluble drugs are possible to optimize their in vivo performance. Different methods for the manufacture of solid dispersion systems have been introduced in literature. In the present work, two methods are compared: hot-melt extrusion and ultrasound-assisted compaction technique. Various carrier systems and drugs with different physicochemical properties are applied to investigate the feasibility of the technologies for pharmaceutical formulation. The formulations are compared to the corresponding untreated physical blends of the components regarding their solid state structure and dissolution behavior to assess the effect of the manufacturing technique. Ultrasound-assisted compaction technique improves the initial dissolution rate of fenofibrate, a poorly water-soluble model drug. The crystalline API is partially converted into its amorphous state. As equivalent results can be achieved if the polymers are added directly to the dissolution medium, the dissolution enhancement is attributed to an improved wettability of the drug. A statistical design of experiments is employed to investigate the effect of the process parameters on the results. Difficulties are encountered in the determination of process parameters which result in an optimal outcome. The process is very sensitive to the smallest changes of settings, for example of the position of the sonotrode. Additionally, the delivery of ultrasound energy is inhomogeneous. There is no or only insufficient user control of these parameters available. Furthermore, the duration of ultrasound energy delivery which is identified as a crucial parameter cannot be set by the user. The variable factors ultrasound energy, pressure of the lower piston and pressure of the upper piston affect the defined responses in the opposite direction. Hence, there are no settings which result in a satisfactory outcome. A strong influence of the material characteristics on the process is observed leading to a batch to batch variability. Due to an insufficient reproducibility of results, the application of the technology cannot be recommended in its current state in the pharmaceutical formulation development and/or production. Improvements in homogeneity of energy delivery, process monitoring, user control and amount of leakage are mandatory for an acceptable performance and a future application in the pharmaceutical sector. The polymers COP, HPMC and PVCL-PVAc-PEG are well suitable as carriers for hot-melt extruded formulations of fenofibrate. All three extrudates are amorphous one-phase systems with the drug molecularly dispersed in the polymer. The enhancement of the initial dissolution rate and the maximum concentration level achieved are dependent on the applied carrier system. Supersaturation levels of up to 12.1 times are reached which are not stable due to recrystallization processes. The application of blends of polymers as carriers reduces the decrease rate after cmax. Because of water absorption and polymer relaxation, the overall dissolution performance decreases with increasing storage times which can be avoided through an optimization of the packaging. If oxeglitazar is used as API, the initial dissolution rate of the extrudates is below that of the untreated drug, with the exception of the ternary blend of COP, HPMC and oxeglitazar which shows a substance-specific super-additive effect. In contrast to the other extrudates, the formulation of PVCL-PVAc-PEG and oxeglitazar does not form a molecularly dispersed solid solution of the drug in the carrier. Instead, an amorphous two-phase system is present. No changes are observed after storage, presumably due to higher glass transition temperatures of the hot-melt extruded systems which are considerably above those of the corresponding fenofibrate extrudates. With felodipine as API, the dissolution profile is enhanced with COP as single carrier. If HPMC or PVCL-PVAc-PEG is used as single or additional polymeric carriers, the dissolution is equivalent (HPMC) or lower (PVCL-PVAc-PEG) than that of the pure drug although molecularly disperse systems are present in all cases. Out of the two investigated methods only hot-melt extrusion is a suitable technology to manufacture solid dispersions with an improved dissolution behavior. The dissolution profile of the extrudates can be influenced by adding polymers with differing physicochemical characteristics. Predictions on the dissolution behavior of the extrudates with polymeric blends as carriers can be made if there is knowledge on the dissolution profiles of the corresponding single polymeric extrudates. Due to substance-specific effects, the results are not transferable from drug to drug. Even so, the data are promising as the release behavior of the manufactured extrudates can be easily modified and readily adapted to one's needs. Further research will have to be conducted to verify the concept and the relevance of the results in vivo. Zusammenfassung Feste Dispersionen sind ein vielversprechender Ansatz zur Herstellung von Drug Delivery-Systemen mit kontrollierter Wirkstofffreisetzung, da sie sowohl die Bioverfügbarkeit schlecht wasserlöslicher Arzneistoffe verbessern als auch die Freisetzung gut wasserlöslicher Arzneistoffe verzögern können und so deren in vivo Verhalten optimieren. Verschiedene Herstellungsmethoden wurden in der Literatur vorgestellt. In der vorliegenden Arbeit werden zwei Technologien miteinander verglichen: Schmelzextrusion und Ultraschall gestützte Verpressung (USAC). Verschiedene Trägersysteme und Arzneistoffe mit unterschiedlichen physikochemischen Eigenschaften werden untersucht, um die Einsatzmöglichkeit im pharmazeutischen Bereich zu überprüfen. Die Struktur der hergestellten Systeme und deren Freisetzungsverhalten werden mit den physikalischen Mischungen der Komponenten verglichen, um den Einfluss der Formulierung zu bestimmen. Durch USAC wird die initiale Freisetzungsrate von Fenofibrat, einem schlecht wasserlöslichen Modellarzneistoff, verbessert. Eine teilweise Umwandlung vom kristallinen in den amorphen Zustand tritt auf. Vergleichbare Ergebnisse werden bei einer Polymerzugabe zum Freisetzungsmedium erreicht; daher wird davon ausgegangen, dass vor allem eine verbesserte Benetzbarkeit des Arzneistoffs eine Rolle spielt. Mittels statistischer Versuchsplanung wird der Einfluss der verschiedenen Prozessparameter untersucht. Die Einstellung der Prozessparameter, um ein optimales Ergebnis zu erhalten, gestaltet sich schwierig. Der Prozess reagiert auf kleinste Veränderungen, zum Beispiel der Position der Sonotrode, überaus sensitiv. Außerdem wird die Ultraschallenergie nicht homogen übertragen. Die Kontrolle dieser Parameter durch den Anwender ist nicht oder nur unzureichend möglich. Ebenso kann die Dauer der Ultraschallapplizierung, die essentiell für den Prozess ist, nicht eingestellt werden. Die Prozessparameter Ultraschallenergie, Unterstempeldruck und Sonotrodendruck beeinflussen die Zielgrößen in entgegengesetzter Richtung. Daher gibt es keine Einstellung, die für alle Zielgrößen optimale Ergebnisse liefert. Zusätzlich ist der Prozess stark abhängig von den Eigenschaften des verwendeten Materials: Die Verwendung unterschiedlicher Polymerchargen macht eine Anpassung der Prozessparameter notwendig, um vergleichbare Ergebnisse zu erhalten. Eine ausreichende Reproduzierbarkeit der Ergebnisse für einen Einsatz dieser Technologie in Formulierungsentwicklung oder Produktion ist nicht gegeben. Eine homogene Ultraschallenergiezufuhr sowie Verbesserungen der Prozessüberwachung, der Benutzerkontrolle und eine Verminderung der austretenden Materialmenge sind für eine akzeptable Leistung und eine zukünftige Anwendung im pharmazeutischen Bereich zwingend erforderlich. Die Polymere COP, HPMC, PVCL-PVAc-PEG sind für eine Freisetzungsverbesserung von Fenofibrat mittels Schmelzextrusion geeignet. Es liegen einphasige, molekulardisperse feste Lösungen vor. Abhängig von der Trägersubstanz wird die initiale Freisetzungsrate unterschiedlich stark erhöht, ebenso die maximale Konzentration des Arzneistoffes in Lösung. Eine bis zu 12.1-fache Übersättigung wird erreicht, die aufgrund von Rekristallisationsprozessen nicht stabil ist. Der Einsatz von polymeren Mischungen reduziert die Geschwindigkeit des Konzentrationsabfalls. Die Absorption von Wasser und Relaxationseffekte vermindern die Freisetzungserhöhung mit zunehmender Lagerdauer; dieser Entwicklung kann durch eine Optimierung des Packmittels entgegengewirkt werden. Wird der ebenfalls schwer wasserlösliche Arzneistoff Oxeglitazar verwendet, so ist die initiale Freisetzungsrate der Extrudate der des reinen Arzneistoffs unterlegen, mit Ausnahme der ternären Mischung von COP, HPMC und Oxeglitazar, die einen substanzspezifischen überadditiven Effekt aufweist. PVCL-PVAc-PEG-Oxeglitazar-Extrudate bilden im Gegensatz zu den übrigen Formulierungen keine molekulardisperse feste Lösung, sondern ein amorphes Zwei-Phasen-System. Eine Veränderung während der Lagerzeit wird nicht beobachtet, vermutlich aufgrund der höheren Glasübergangstemperaturen dieser Systeme. Lediglich das Freisetzungsprofil von COP-Felodipin-Extrudaten ist verbessert. Gegenüber dem reinen Arzneistoff ist die Freisetzung der übrigen Extrudate vergleichbar (HPMC) oder verringert (PVCL-PVAc-PEG), obwohl auch hier molekulardisperse Systeme vorliegen. Von den beiden untersuchten Technologien ist lediglich die Schmelzextrusion geeignet, um feste Dispersionen mit einem verbesserten Freisetzungsverhalten herzustellen. Das Freisetzungsprofil der Extrudate kann durch den Zusatz von Polymeren mit unterschiedlichen Eigenschaften optimiert und vorhergesagt werden, wenn das Freisetzungsprofil der Einzelpolymer-Extrudate bekannt ist. Die Ergebnisse sind aufgrund von substanzspezifischen Effekten nicht von Arzneistoff auf Arzneistoff übertragbar. Nichtsdestotrotz sind die Erkenntnisse dieser Arbeit vielversprechend, da gezeigt wird, dass das Freisetzungsprofil der Extrudate leicht beeinflusst und an spezifische Anforderungen angepasst werden kann. Weitere Untersuchungen sind notwendig, um das Konzept und die Relevanz der Ergebnisse in vivo zu überprüfen.

Download or read book Formulating Poorly Water Soluble Drugs written by Robert O. Williams III and published by Springer Science & Business Media. This book was released on 2011-12-04 with total page 656 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume is intended to provide the reader with a breadth of understanding regarding the many challenges faced with the formulation of poorly water-soluble drugs as well as in-depth knowledge in the critical areas of development with these compounds. Further, this book is designed to provide practical guidance for overcoming formulation challenges toward the end goal of improving drug therapies with poorly water-soluble drugs. Enhancing solubility via formulation intervention is a unique opportunity in which formulation scientists can enable drug therapies by creating viable medicines from seemingly undeliverable molecules. With the ever increasing number of poorly water-soluble compounds entering development, the role of the formulation scientist is growing in importance. Also, knowledge of the advanced analytical, formulation, and process technologies as well as specific regulatory considerations related to the formulation of these compounds is increasing in value. Ideally, this book will serve as a useful tool in the education of current and future generations of scientists, and in this context contribute toward providing patients with new and better medicines.

Download or read book Solid Dispersion As A Solubility Enhancement Technique written by Kalpen Patel and published by LAP Lambert Academic Publishing. This book was released on 2013 with total page 92 pages. Available in PDF, EPUB and Kindle. Book excerpt: Solid dispersion was prepared by solvent evaporation technique and it is optimized by using different of polymer and lipid ratios. The prepared solid dispersions were evaluated for solubility study, assay and in vitro dissolution study. The solid state property was characterized by differential scanning Calorimetry(DSC). The solubility and dissolution rate were found significantly increased in these solid dispersion systems compared with pure drug alone. The highest improvement of solubility and dissolution rate was found with PEG 6000 and 45 mg phosphatidycholine. DSC studies of solid dispersions confirmed the there is no interaction between drug with excipients. This is attributed to improve bioavailability due to enhancement in rate and extent of drug release. The preparation of solid dispersion is a promising strategy to improve the solubility and dissolution of drug of low solubility and thereby bioavailability of the drug. The solvent evaporation method could be considered as a simple method for preparation of solid dispersion within a shorter period of times.

Download or read book Formulation and Processing Technologies for Dissolution Enhancement of Poorly Water soluble Drugs written by Justin Roy Hughey and published by . This book was released on 2012 with total page 458 pages. Available in PDF, EPUB and Kindle. Book excerpt: The number of newly developed chemical entities exhibiting poor water solubility has increased dramatically in recent years. In many cases this intrinsic property results in poor or erratic dissolution in biological fluids. Improving aqueous solubility of these compounds, even temporarily, can have a significant impact on in vivo performance. Single phase amorphous solid dispersions of a drug and polymer have emerged as a technique to not only increase the level of drug supersaturation but also maintain these levels for extended periods of time. Hot-melt extrusion (HME) has become the preferred processing technique to prepare systems such as these but has a number of limitations that prevent the successful formulation of many drug substances. Within this dissertation, the use of concentration enhancing polymers was investigated in parallel with a thorough evaluation of a novel fusion-based processing technique, KinetiSol® Dispersing (KSD), to prepare single phase amorphous solid dispersions that could not be successfully prepared by HME. Studies showed that the KSD technique is suitable for rendering thermally labile and high melting point drug substances amorphous through a combination of frictional and shearing energy. Compounds such as these were shown to degrade during HME processing due to relatively long residence times and low shear forces. Similarly, the KSD process was shown to successfully process solid dispersion compositions containing a high viscosity polymer with significantly lower levels of polymer degradation than obtained by HME processing. In the final study, KSD processing was used to prepare solid dispersions containing the hydrophilic polymer Soluplus[superscript TM] and methods were evaluated to formulate a tablet with rapid tablet disintegration characteristics, a requirement for sufficient dissolution enhancement. Combined, the studies demonstrated the effectiveness of combining proper polymer selection and formulation approaches with a suitable processing technique to form solid dispersion systems that provide rapid and extended durations of supersaturation.

Download or read book Drug Delivery Strategies for Poorly Water Soluble Drugs written by Dionysios Douroumis and published by John Wiley & Sons. This book was released on 2012-12-19 with total page 543 pages. Available in PDF, EPUB and Kindle. Book excerpt: Many newly proposed drugs suffer from poor water solubility, thus presenting major hurdles in the design of suitable formulations for administration to patients. Consequently, the development of techniques and materials to overcome these hurdles is a major area of research in pharmaceutical companies. Drug Delivery Strategies for Poorly Water-Soluble Drugs provides a comprehensive overview of currently used formulation strategies for hydrophobic drugs, including liposome formulation, cyclodextrin drug carriers, solid lipid nanoparticles, polymeric drug encapsulation delivery systems, self–microemulsifying drug delivery systems, nanocrystals, hydrosol colloidal dispersions, microemulsions, solid dispersions, cosolvent use, dendrimers, polymer- drug conjugates, polymeric micelles, and mesoporous silica nanoparticles. For each approach the book discusses the main instrumentation, operation principles and theoretical background, with a focus on critical formulation features and clinical studies. Finally, the book includes some recent and novel applications, scale-up considerations and regulatory issues. Drug Delivery Strategies for Poorly Water-Soluble Drugs is an essential multidisciplinary guide to this important area of drug formulation for researchers in industry and academia working in drug delivery, polymers and biomaterials.

Download or read book Recent trends in solubility and bioavailability enhancement for poorly water soluble drugs written by 최한곤 and published by 한양대학교 출판부. This book was released on 2019-12-17 with total page 696 pages. Available in PDF, EPUB and Kindle. Book excerpt: 난용상 약물의 용해도 및 생체[이용율 증진에 대한 최근 연구동향을 모아 발간하고자 함 1. Silymarin-loaded solid nanoparticles with excellent hepatic protection: physicochemical characterization and in vivo evaluation. 2. The Influence of Bile Salt on the Chemotherapeutic Response of Docetaxel-loaded Thermosensitive Nanomicelles. 3. Enhanced oral bioavailability of fenofibrate using polymeric nanoparticulated systems: Physicochemical characterization and in vivo investigation. 4. Tumor-targeting. pH-sensitive nanoparticles for docetaxel delivery to drug-resistant cancer cells. 5. Comparative study on solid self-nanoemulsifying drug delivery and solid dispersion system for enhanced solubility and bioavailability of ezetimibe. 6. Novel electrosprayed nanospherules for enhanced aqueous solubility and oral bioavailability of poorly water-soluble fenofibrate. 7. Receptor-targeted. drug-loaded. functionalized graphene oxides for chemotherapy and photothermal therapy. 8. Progressive slowdown/prevention of cellular senescence by CD9-targeted delivery of rapamycin using lactose-wrapped calcium carbonate nanoparticles. 9. Optimization and physicochemical characterization of a cationic lipid-phosphatidylcholine mixed emulsion formulated as a highly efficient vehicle that facilitates adenoviral gene transfer. 10. Combination of NIR therapy and regulatory T cell modulation using layer-by-layer hybrid nanoparticles for effective cancer photoimmunotherapy. 11. Cyclic RGD-conjugated Pluronic® blending system for active. targeted drug delivery. 12. Transferrin-Conjugated Polymeric Nanoparticle for Receptor-Mediated Delivery of Doxorubicin in Doxorubicin-Resistant Breast Cancer Cells. 13. Self-microemulsifying drug delivery system (SMEDDS) for improved oral delivery and photostability of methotrexate. 14. Comparison of 1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol-loaded self-emulsifying granule and solid self-nanoemulsifying drug delivery system: powder property. dissolution and oral bioavailability. 15. Liposomal Formulations for Nose-to-Brain Delivery: Recent Advances and Future Perspectives. 16. Development of folate-functionalized zein nanoparticles for ligand-directed delivery of paclitaxel.

Download or read book Ternary Solid Dispersion Strategy for Solubility Enhancement of Poorly Soluble Drugs by Co Milling Technique written by Marouene Bejaoui and published by . This book was released on 2022 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: Amorphous ternary solid dispersion has become one of the strategies commonly used for improving the solubility and bioavailability of poorly water soluble drugs. Such multicomponent solid dispersion can be obtained by different techniques, this chapter provides an overview of ternary solid dispersion by co-milling method from the perspectives of physico-chemical characteristics in vitro and in vivo performance. A considerable improvement of solubility was obtained for many active pharmaceutical ingredients (e.g., Ibuprofen, Probucol, Gliclazid, Fenofibrate, Ibrutinib and Naproxen) and this was correlated to the synergy of multiple factors (hydrophilicity enhancement, particle size reduction, drug-carrier interactions, anti-plasticizing effect and complexation efficiency). This enhanced pharmacokinetic properties and bioavailability of these drug molecules (1.49 to 15-folds increase in plasma drug concentration). A particular focus was accorded to compare the ternary and binary system including Ibuprofen and highlighting the contribution of thermal and spectral characterization techniques. The addition of polyvinylpyrrolidone (PVP K30), a low molecular weight molecule, into the binary solid dispersion (Ibuprofen/Œ≤-cyclodextrin), leads to a 1.5,Äì2 folds increase in the drug intrinsic dissolution rate only after 10¬†min. This resulted from physical stabilization of amorphous Ibuprofen by reducing its molecular mobility and inhibiting its recristallization even under stress conditions (75% RH and T¬†=¬†40¬∞C for six months).

Download or read book Enhancement of the Dissolution of a Poorly Water Soluble Drug written by Sachin Kumar and published by LAP Lambert Academic Publishing. This book was released on 2013 with total page 112 pages. Available in PDF, EPUB and Kindle. Book excerpt: Up to 40% of new chemical entities discovered by the pharmaceutical industry today are poorly soluble or lipophilic compounds. The solubility issues complicating the delivery of these new drugs also affect the delivery of many existing drugs. Poorly water-soluble drugs show unpredictable absorption, since their bioavailability depends upon the dissolution in the gastrointestinal tract. The dissolution characteristics of poorly soluble drugs can be enhanced by several methods. Among these methods, solid dispersions (SDs) and cyclodextrins (CDs) have been extensively studied to improve solubility, dissolution, and bioavailability of various drugs. The present manuscript reveals the significance and methodology of enhancing solubility of a poorly water soluble drug which can be useful to apply for other poorly water soluble drugs.

Download or read book Amorphous Solid Dispersions written by Navnit Shah and published by Springer. This book was released on 2014-11-21 with total page 702 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume offers a comprehensive guide on the theory and practice of amorphous solid dispersions (ASD) for handling challenges associated with poorly soluble drugs. In twenty-three inclusive chapters, the book examines thermodynamics and kinetics of the amorphous state and amorphous solid dispersions, ASD technologies, excipients for stabilizing amorphous solid dispersions such as polymers, and ASD manufacturing technologies, including spray drying, hot melt extrusion, fluid bed layering and solvent-controlled micro-precipitation technology (MBP). Each technology is illustrated by specific case studies. In addition, dedicated sections cover analytical tools and technologies for characterization of amorphous solid dispersions, the prediction of long-term stability, and the development of suitable dissolution methods and regulatory aspects. The book also highlights future technologies on the horizon, such as supercritical fluid processing, mesoporous silica, KinetiSol®, and the use of non-salt-forming organic acids and amino acids for the stabilization of amorphous systems. Amorphous Solid Dispersions: Theory and Practice is a valuable reference to pharmaceutical scientists interested in developing bioavailable and therapeutically effective formulations of poorly soluble molecules in order to advance these technologies and develop better medicines for the future.

Download or read book Investigation of Amorphous Solid Dispersions for Solubility Enhancement of Poorly Water soluble Drugs written by Andrew Olutoye Ojo and published by . This book was released on 2021 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: The preparation of amorphous solid dispersions (ASDs) has enabled the development of oral dosage forms for many poorly water-soluble compounds. The aim of the work presented in this dissertation is to advance our understanding of ASDs, specifically their long-term stability with respect to crystallization and the implications of instability on product performance. Advancing knowledge in these areas is pivotal for the pharmaceutical industry and its efforts in drug discovery. Much of our understanding of ASD stability results from empirical or extrapolative models that have been applied to describe stability. Their application has been limited and they do not provide fundamental insights into the recrystallization process to aid in the rationale development in ASDs. Notably, they fail to consider supersaturation as the driving force for crystallization, diffusivity in viscous systems, and interfacial effects. The works presented in this dissertation model the mechanisms of crystal nucleation and growth in ASDs by incorporating these concepts, develop and apply characterization tools to determine critical model parameters, and study the effects of crystallization on product performance.

Download or read book Solubility Enhancement written by Vinod Wagh and published by LAP Lambert Academic Publishing. This book was released on 2013-01 with total page 108 pages. Available in PDF, EPUB and Kindle. Book excerpt: Currently only 8% of new drug candidates have both high solubility and permeability. More than 40% of potential drug products suffer from poor water solubility. This frequently results in potentially important products not reaching the market or not achieving their full potential. Experience with solid dispersions over the last 20-30 years indicates that this is a very fruitful approach to improving the release rate and oral bioavailability of poorly water soluble drugs. So this article highlights technology various approaches for the preparation of solid dispersion, technology involved, detail description of poorly water soluble drugs & carriers.

Download or read book Factors Influencing the Release of Poorly Water soluble Drugs from Solid dispersion Granules During Storage written by Manish K. Gupta and published by . This book was released on 2002 with total page 314 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Download or read book Pharmaceutical Dosage Forms written by Larry L. Augsburger and published by CRC Press. This book was released on 1990-03-30 with total page 640 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Download or read book Pharmaceutical Amorphous Solid Dispersions written by Ann Newman and published by John Wiley & Sons. This book was released on 2015-02-27 with total page 505 pages. Available in PDF, EPUB and Kindle. Book excerpt: Providing a roadmap from early to late stages of drug development, this book overviews amorphous solid dispersion technology – a leading platform to deliver poorly water soluble drugs, a major hurdle in today’s pharmaceutical industry. • Helps readers understand amorphous solid dispersions and apply techniques to particular pharmaceutical systems • Covers physical and chemical properties, screening, scale-up, formulation, drug product manufacture, intellectual property, and regulatory considerations • Has an appendix with structure and property information for polymers commonly used in drug development and with marketed drugs developed using the amorphous sold dispersion approach • Addresses global regulatory issues including USA regulations, ICH guidelines, and patent concerns around the world

Download or read book Improving the Dissolution Rate of Poorly Water Soluble Drugs by Solid Dispersion and Solid Solution written by Rina J. Chokshi and published by . This book was released on 2001 with total page 296 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Download or read book Solubility Enhancement of Certain Drugs by Solid Dispersion Technique written by Vidyadhara Suryadevara and published by LAP Lambert Academic Publishing. This book was released on 2014-12-26 with total page 228 pages. Available in PDF, EPUB and Kindle. Book excerpt: Recent advances in novel drug delivery systems (NDDS) aim to enhance safety and efficacy of drug molecules by formulating a convenient dosage form for administration and to achieve better patient compliance. One such approach was fast dissolving tablets which have gained acceptance and popularity in the recent time. Several pharmaceutical industries prepared fast dissolving tablets by direct compression technique by selecting suitable super disintegrants. Direct compression technique offers important advantages such as increased output, reduced cost, less machinery and improved drug stability compared to wet granulation method.The aim of the work is to enhance the solubility, dissolution rate and oral bioavailability of poorly soluble drugs lovastatin and simvastatin by formulating them as solid dispersions using various techniques with PEG-6000 as a carrier and subsequent preparation of fast dissolving tablets with the prepared solid dispersions using different concentrations of super disintegrants and comparing them with that of the marketed product.

Download or read book Solubility Enhancement by Solid Dispersion Technique written by Kantilal Narkhede and published by LAP Lambert Academic Publishing. This book was released on 2012-07 with total page 112 pages. Available in PDF, EPUB and Kindle. Book excerpt: Bicalutamide is poorly soluble drug which is non-steroidal androgen having pKa 12. Aqueous in vitro solubility of bicalutamide is low at 50 g/mL at pH 7 and 37 C. The drug exhibits low bioavailability related to its poor water solubility. Therefore, bicalutamide bioavailability can be improved by increasing its solubility. Solid dispersion technique is most effective technique to improve solubility of drug. Solid dispersions of bicalutamide were prepared by using solvent evaporation technique using HPMC and surfactant like SLS. Solubilities were calculated by using In-vitro dissolution technique. 1:4 drug: HPMC ratio was found efficient with 2% SLS concentration. Using this solid dispersion tablet was formulated and evaluated. In evaluation it was found that Bicalutamide showing 97.251% release at 120 min which is higher than standard drug."