08. August 2018
Combinatorial chemistry, computational molecular modeling and high throughput screening in drug discovery have significantly increased the number of poorly soluble drugs. About 40% of drugs developed in the past and about 90% of the drugs in development are poorly soluble drugs. When administered orally, a drug has to first dissolve in gastrointestinal fluids before it can be absorbed in to the blood and reach its site of action. The objective of this review article is to outline the key...
27. November 2017
Drug solubility can pose a great challenge for the development of novel formulations and impacts a wide spectrum of drugs with poor solubilities. Drug efficacy is known to be proportionally related to the solubility of a drug. Poor solubility of a drug leads to low dissolution rate and in turn to low absorption in the gastrointestinal tract following oral administration. Pharmaceutical particle technology is often used to improve poor aqueous solubility of drug compounds that limits in vivo bioa
20. March 2017
Abstract Rifampicin-loaded submicron-sized particles were prepared through supercritical anti-solvent process using ethyl cellulose as polymeric encapsulating excipient. Ethyl acetate and a mixture of ethyl acetate/dimethyl sulfoxide (70/30 and 85/15) were used as solvents for both drug and polymeric excipient. When ethyl acetate was used, rifampicin was crystallized separately without being embedded within the ethyl cellulose matrix while by using the ethyl acetate/dimethyl sulfoxide mixture,...
03. January 2017
Abstract AIDS constitutes one of the most serious infectious diseases, representing a major public health priority. Efavirenz (EFV), one of the most widely used drugs for this pathology, belongs to the Class II of the Biopharmaceutics Classification System for drugs with very poor water solubility. To improve EFV’s dissolution profile, changes can be made to the physical properties of the drug that do not lead to any accompanying molecular modifications. Therefore, the study objective was to...