scholarly journals Recent and Relevant Methodology in the Advancement of Solid Dispersion

2021 ◽  
Vol 11 (4-S) ◽  
pp. 247-257
Author(s):  
Shruti Talla ◽  
Kamlesh Wadher ◽  
Milind Umekar ◽  
R.T. Lohiya
Keyword(s):  
Solid Dispersion ◽  
Water Solubility ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Pharmaceutical Therapy ◽  
Supercritical Fluid Technology ◽  
Water Soluble Drugs ◽  
Recent Trends ◽  
Poorly Water Soluble ◽  
Preparation Techniques

Most of the promising drugs in development channels are poorly water-soluble drugs which limit formulation approaches, clinical application because of their low dissolution and bioavailability. And the major current challenges of the pharmaceutical industry are apropos strategies that improve the water solubility of drugs.  Solid dispersion has been considered one of the major evolutions in overcoming these issues with several successfully marketed products. Though solid dispersion has been outlined as an efficient drug delivery system, the design of specific dosage forms for pharmaceutical therapy is necessary to improve the solubility and bioavailability of poorly water-soluble drugs. Solid dispersion can be prepared by several methods such as solvent evaporation, melting, and supercritical fluid technology.  This review intends to provide an updated overview of the recent trends over the past few years in solid dispersion preparation techniques and polymer used. Along with the various pharmaceutical strategies and future visions for the solubilization of poorly water-soluble drugs Keywords: Solid dispersion, Bioavailability, Solubility, Dissolution parameters, Polymeric carrier

scholarly journals SOLUBILITY ENHANCEMENT OF POORLY WATER SOLUBLE DRUGS BY VARIOUS TECHNIQUES

2019 ◽  
Vol 8 (1) ◽  
Author(s):  
Sakshi Minocha ◽  
Dr. Shilpa Pahwa ◽  
Dr. Vandana Arora
Keyword(s):  
Solid Dispersion ◽  
Water Solubility ◽  
Water Soluble ◽  
Formulation Development ◽  
Particle Size Reduction ◽  
Bioavailability Enhancement ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Poor Water Solubility

Solubility is not the ability to dissolve or thaw a substance; it may happen not only due to dissolution but also because of a chemical reaction. Solubility is the phenomenon of dissolution of solid in liquid phase to provide a homogenous system. Solubility is one of the vital factors for accomplishing desired concentration of drug in systemic circulation for pharmacological response. Low aqueous solubility is the major problem seen with formulation development of new chemical entities as well as for the generic development. With all new discovered chemical entities about 40% drugs are lipophilic and doesn’t shown therapeutic range due to their poor water solubility. Drug with poor water solubility shows slow dissolution rates, incomplete absorption and low bioavailability when taken orally. Drug solubility and bioavailability enhancement are the important in the formulation of pharmaceuticals. The Biopharmaceutics Classification System shows that Class II and IV drugs have low water solubility, poor dissolution, and low bioavailability. This review mentions different approaches used for the enhancement of the solubility of poorly water-soluble drugs that includes particle size reduction, pH adjustment, and solid dispersion. This describes the techniques of solubilizaton for the attainment of effective absorption and improved bioavailability. Keywords: Solubility, BCS classification, Bioavailability, Solid-dispersion.

scholarly journals REVIEW ARTICLE: SOLUBILITY ENHANCEMENT BY SOLID DISPERSION

2017 ◽  
Vol 9 (3) ◽  
pp. 15
Author(s):  
A. N. Patil ◽  
D. M. Shinkar ◽  
R. B. Saudagar
Keyword(s):  
Solid Dispersion ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Full Potential ◽  
Drug Selection ◽  
Formulation Development ◽  
Poorly Water Soluble Drugs ◽  
New Chemical Entities ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

Enhancement of solubility, dissolution rate and bioavailability of the drug is a very challenging task in drug development, nearly 40% of the new chemical entities currently being discovered are poorly water soluble drugs. The solubility behaviour of the drugs remains one of the most challenging aspects in formulation development. This results in important products not reaching the market or not achieving their full potential. Solid dispersion is one of the techniques adopted for the formulation of such drugs and various methods are used for the preparation of solid dispersion. Solid dispersion is generally prepared with a drug which is having poor aqueous solubility and hydrophilic carrier. This article review various methods and concept of solid dispersion, criteria for drug selection, advantage and disadvantage, characterization, and application.

scholarly journals Insoluble Polymers in Solid Dispersions for Improving Bioavailability of Poorly Water-Soluble Drugs

Polymers ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 1679
Author(s):  
Thao T.D. Tran ◽  
Phuong H.L. Tran
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Dissolution Enhancement ◽  
Formulation Development ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Insoluble Polymers

In recent decades, solid dispersions have been demonstrated as an effective approach for improving the bioavailability of poorly water-soluble drugs, as have solid dispersion techniques that include the application of nanotechnology. Many studies have reported on the ability to change drug crystallinity and molecular interactions to enhance the dissolution rate of solid dispersions using hydrophilic carriers. However, numerous studies have indicated that insoluble carriers are also promising excipients in solid dispersions. In this report, an overview of solid dispersion strategies involving insoluble carriers has been provided. In addition to the role of solubility and dissolution enhancement, the perspectives of the use of these polymers in controlled release solid dispersions have been classified and discussed. Moreover, the compatibility between methods and carriers and between drug and carrier is mentioned. In general, this report on solid dispersions using insoluble carriers could provide a specific approach and/or a selection of these polymers for further formulation development and clinical applications.

scholarly journals Overview of the Manufacturing Methods of Solid Dispersion Technology for Improving the Solubility of Poorly Water-Soluble Drugs and Application to Anticancer Drugs

Pharmaceutics ◽  
2019 ◽  
Vol 11 (3) ◽  
pp. 132 ◽  
Author(s):  
Phuong Tran ◽  
Yong-Chul Pyo ◽  
Dong-Hyun Kim ◽  
Sang-Eun Lee ◽  
Jin-Ki Kim ◽  
...  
Keyword(s):  
Anticancer Drugs ◽  
Small Molecule ◽  
Solid Dispersion ◽  
Route Of Administration ◽  
Water Soluble ◽  
Biologic Drugs ◽  
Poorly Water Soluble Drugs ◽  
Small Molecule Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

Approximately 40% of new chemical entities (NCEs), including anticancer drugs, have been reported as poorly water-soluble compounds. Anticancer drugs are classified into biologic drugs (monoclonal antibodies) and small molecule drugs (nonbiologic anticancer drugs) based on effectiveness and safety profile. Biologic drugs are administered by intravenous (IV) injection due to their large molecular weight, while small molecule drugs are preferentially administered by gastrointestinal route. Even though IV injection is the fastest route of administration and ensures complete bioavailability, this route of administration causes patient inconvenience to visit a hospital for anticancer treatments. In addition, IV administration can cause several side effects such as severe hypersensitivity, myelosuppression, neutropenia, and neurotoxicity. Oral administration is the preferred route for drug delivery due to several advantages such as low cost, pain avoidance, and safety. The main problem of NCEs is a limited aqueous solubility, resulting in poor absorption and low bioavailability. Therefore, improving oral bioavailability of poorly water-soluble drugs is a great challenge in the development of pharmaceutical dosage forms. Several methods such as solid dispersion, complexation, lipid-based systems, micronization, nanonization, and co-crystals were developed to improve the solubility of hydrophobic drugs. Recently, solid dispersion is one of the most widely used and successful techniques in formulation development. This review mainly discusses classification, methods for preparation of solid dispersions, and use of solid dispersion for improving solubility of poorly soluble anticancer drugs.

scholarly journals Lipid-based systems as a promising approach for enhancing the bioavailability of poorly water-soluble drugs

2013 ◽  
Vol 63 (4) ◽  
pp. 427-445 ◽  
Author(s):  
Katja Čerpnjak ◽  
Alenka Zvonar ◽  
Mirjana Gašperlin ◽  
Franc Vrečer
Keyword(s):  
Drug Delivery ◽  
Oral Bioavailability ◽  
Drug Delivery Systems ◽  
Water Solubility ◽  
Pharmaceutical Products ◽  
Delivery Systems ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

Abstract Low oral bioavailability as a consequence of low water solubility of drugs is a growing challenge to the development of new pharmaceutical products. One of the most popular approaches of oral bioavailability and solubility enhancement is the utilization of lipid-based drug delivery systems. Their use in product development is growing due to the versatility of pharmaceutical lipid excipients and drug formulations, and their compatibility with liquid, semi-solid, and solid dosage forms. Lipid formulations, such as self-emulsifying (SEDDS), self-microemulsifying SMEDDS) and self- -nanoemulsifying drug delivery systems (SNEDDS) were explored in many studies as an efficient approach for improving the bioavailability and dissolution rate of poorly water-soluble drugs. One of the greatest advantages of incorporating poorly soluble drugs into such formulations is their spontaneous emulsification and formation of an emulsion, microemulsion or nanoemulsion in aqueous media. This review article focuses on the following topics. First, it presents a classification overview of lipid-based drug delivery systems and mechanisms involved in improving the solubility and bioavailability of poorly water-soluble drugs. Second, the article reviews components of lipid-based drug delivery systems for oral use with their characteristics. Third, it brings a detailed description of SEDDS, SMEDDS and SNEDDS, which are very often misused in literature, with special emphasis on the comparison between microemulsions and nanoemulsions.

Sign in / Sign up

Export Citation Format

Share Document