الفهرس | Only 14 pages are availabe for public view |
Abstract The dissolution rate of the drug is the rate limiting step in absorption of most drugs after oral administration. Also, the dissolution rate is a determining factor for the drug bioavailability. In recent years, almost 35- 40% of the newly developed active pharmaceutical ingredients (APIs) created via drug discovery screens display limited aqueous solubility and erratic dissolution behavior, hence have limited absorption and bioavailability. These APIs are unable to continue the production cycle because of difficulty of manufacturing into suitable dosage form. Accordingly, many approaches were probed by scientists to enhance drug solubility and dissolution rate, and thus oral bioavailability of poorly soluble drugs. These include chemical modification approaches (e.g. salt and pro-drug formation), physical modification approaches (e.g. Particle size reduction, complexation and crystalline structure modification) and miscellaneous approaches as hydrotropic solubilization. |