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 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 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 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 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 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 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."

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 Water Insoluble Drug Formulation written by Ron Liu and published by CRC Press. This book was released on 2018-03-12 with total page 781 pages. Available in PDF, EPUB and Kindle. Book excerpt: Properties and Formulation: From Theory to Real-World Application Scientists have attributed more than 40 percent of the failures in new drug development to poor biopharmaceutical properties, particularly water insolubility. Issues surrounding water insolubility can postpone or completely derail important new drug development. Even the much-needed reformulation of currently marketed products can be significantly affected by these challenges. More recently it was reported that the percentage increased to 90% for the candidates of new chemical entities in the discovery stage and 75% for compounds under development. In the most comprehensive resource on the topic, this third edition of Water-Insoluble Drug Formulation brings together a distinguished team of experts to provide the scientific background and step-by-step guidance needed to deal with solubility issues in drug development. Twenty-three chapters systematically describe the detailed discussion on solubility theories, solubility prediction models, the aspects of preformulation, biopharmaceutics, pharmacokinetics, regulatory, and discovery support of water-insoluble drugs to various techniques used in developing delivery systems for water-insoluble drugs. This book includes more than 15 water-insoluble drug delivery systems or technologies, illustrated with case studies and featuring oral and parenteral applications. Highlighting the most current information and data available, this seminal volume reflects the significant progress that has been made in nearly all aspects of this field. The aim of this book is to provide a handy reference for pharmaceutical scientists in the handling of formulation issues related to water-insoluble drugs. In addition, this book may be useful to pharmacy and chemistry undergraduate students and pharmaceutical and biopharmaceutical graduate students to enhance their knowledge in the techniques of drug solubilization and dissolution enhancement.

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 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 Enhancing Delivery of Poorly Water soluble Drugs by Innovative Amorphous Solid Dispersions written by Scott Victor Jermain and published by . This book was released on 2019 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: Poorly water-soluble drugs continue to dominate today’s drug development pipelines, and thus a multitude of technologies and solubility-enhancing methodologies have been commercialized to address this issue. One-such methodology to enhance the solubility of poorly water-soluble drugs is the development of amorphous solid dispersions. What was once considered a risky method of drug delivery (due to lack of drug kinetic stability in its amorphous state), formulating drugs as amorphous solid dispersions has grown significantly over the past two decades. Two amorphous solid dispersion-producing technologies have become well-understood for the development and successful delivery of poorly water-soluble drugs, and thus an overwhelming majority of commercialized amorphous solid dispersion products are processed by these two technologies; hot melt extrusion and spray drying. Each technology has distinct advantages and disadvantages, and thus many poorly water-soluble drugs are unable to process by either technology using conventional techniques. Thus, novel utilization of excipients and processing methods is necessary to continually expand the formulation design space. Furthermore, the development and commercialization of novel amorphous solid dispersion-producing technologies is necessary to further-expand the formulation design space. Therefore, the following research is an effort to expand the formulation design space of poorly water-soluble drugs while forming amorphous solid dispersions. The following research focuses on continued innovation in the field of amorphous solid dispersions to enhance the bioavailability of poorly water-soluble drugs. These research directions demonstrate innovative use of an ordinary excipient to enhance delivery of amorphous solid dispersions processed by hot melt extrusion. Additionally, these studies demonstrate the use (and further understanding) of a novel technology, KinetiSol, that allows for processing amorphous solid dispersions without the necessity of external thermal input or solvent(s). KinetiSol-processed materials are compared with spray dried materials to evaluate the kinetics behind drug release of a weakly basic drug processed with an ionic polymer, and findings from this study will be essential for future delivery of amorphous solid dispersions of weakly basic drugs in ionic polymers

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 Techniques of Solubilization of Drugs written by Samuel Hyman Yalkowsky and published by . This book was released on 1993 with total page 240 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Download or read book Solid Dispersions for Drug Delivery written by Vitaliy Khutoryanskiy and published by Mdpi AG. This book was released on 2022-01-11 with total page 244 pages. Available in PDF, EPUB and Kindle. Book excerpt: Since their first application in the improvement of solubility of orally delivered drugs, applications of solid dispersions have considerably expanded to include cancer, infections, and inflammatory conditions. This book presents recent advancements in the development and use of solid dispersions for different therapeutic applications. This book can be particularly useful for researchers as well as postgraduate students in formulation sciences and drug delivery. Undergraduate students will also find elements of this book very relevant to scientific fundamentals such as solubility and crystallization of amorphous materials as well as drug delivery challenges.

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 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.