Method of enhancement of solubility review
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Solubility is the phenomenon of dissolution of solid in liquid phase to give a homogenous system. Solubility is one of the important parameter to achieve desired concentration of drug in systemic circulation for pharmacological response that is called bioavailability. Therapeutic effectiveness of a drug basically depends upon bioavailability and the solubility of drug moiety. Most of the chemical entities that are being discovered are lipophilic and have poor aqueous solubility. A more than 40% drug suffers from poor water solubility hence new chemical entities developed in pharmaceutical industry are lipophillic and fail to reach the market due to their poor water solubility. Currently number of techniques addressed the enhancement of solubility and dissolution rate of poorly soluble drugs. Water is the solvent of choice for liquid pharmaceutical formulations. Most of drugs weakly acidic and weakly basic with poor aqueous solubility. Hence various techniques are used for the improvement of the solubility of poorly water-soluble drugs include micronization, chemical modification, pH adjustment, solid dispersion, complexation, co‐solvency, micellar solubilization, hydrotropy etc. In this review we concentrated on improvement of the solubility and bioavailability of poorly water soluble drugs by applying various new methods. Show Keywords: Solubility, Hydrotropy, Mixed Hydrotropy, Micronization, Co‐Solvency, Micellar Solubilization Suggested Citation: Devhare, Lalchand and Kore, P. K., A Recent Review on Bioavailability and Solubility Enhancement of Poorly Soluble Drugs by Physical and Chemical Modifications (September 30, 2016). Research Chronicle in Health Sciences 2016,2(5),299-308 , Available at SSRN: https://ssrn.com/abstract=4455504 B.A. Bhairav, J.K. Bachhav, R.B. Saudagar. Review on Solubility Enhancement Techniques. Asian J. Pharm. Res. 2016; 6(3): 147-152. doi: 10.5958/2231-5691.2016.00025.3 Recomonded Articles:Asian Journal of Pharmaceutical Research (AJPRes.) is an international, peer-reviewed journal, devoted to pharmaceutical sciences. AJPRes. publishes Original Research Articles, Short Communications..... Read more >>> Solubility, the phenomenon of dissolution of solute in solvent to give a homogenous system, is one of the important parameters to achieve desired concentration of drug in systemic circulation for desired (anticipated) pharmacological response. Low aqueous solubility is the major problem encountered with formulation development of new chemical entities as well as for the generic development. More than 40% NCEs (new chemical entities) developed in pharmaceutical industry are practically insoluble in water. Solubility is a major challenge for formulation scientist. Any drug to be absorbed must be present in the form of solution at the site of absorption. Various techniques are used for the enhancement of the solubility of poorly soluble drugs which include physical and chemical modifications of drug and other methods like particle size reduction, crystal engineering, salt formation, solid dispersion, use of surfactant, complexation, and so forth. Selection of solubility improving method depends on drug property, site of absorption, and required dosage form characteristics. PubMed Disclaimer FiguresRepresentations of hydrophobic cavity and hydrophilic outer surface of cyclodextrin [44]. 1 : 1 and 1 : 2 drug cyclodextrin complexes [47]. Similar articles
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Enhancement of apixaban's solubility and dissolution rate by inclusion complex (β-cyclodextrin and hydroxypropyl β-cyclodextrin) and computational calculation of their inclusion complexes. What are the methods for solubility enhancement?Various techniques are used for the enhancement of the solubility of poorly soluble drugs which include physical and chemical modifications of drug and other methods like particle size reduction, crystal engineering, salt formation, solid dispersion, use of surfactant, complexation, and so forth. What are the methods to determine solubility?Traditionally, the equilibrium solubility at a given pH and temperature is determined by the shake flask method. According to this method the compound is added in surplus to a certain medium and shaken at a predetermined time, usually 24h or longer. What is the solubility method of analysis?Phase solubility analysis is a technique for quantitatively determining the purity of a substance through the application of precise solubility measurements. At a given temperature, a definite amount of a pure substance is soluble in a definite quantity of solvent. What are the approaches to enhance solubility of drug molecule?Techniques for Solubility Enhancement Particle size reduction like micronization and nanosuspension, modification of the crystal habit like polymorphs, amorphous form and cocrystallization, drug dispersion in carriers like eutectic mixtures, solid dispersions, solid solutions and cryogenic techniques. |
