alexa Abstract | Polymeric precipitation Inhibitors to improve the dissolution and absorption of poorly water-soluble drugs

Journal of Chemical and Pharmaceutical Research
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Original Articles Open Access

Abstract

BCS class II drugs offer challenging problems in their pharmaceutical product development process because of their low solubility and dissolution rates. The basic drug will precipitate upon a shift from gastric pH (pH 1.5) to intestinal pH (pH 6.5-7.0). With the increasing number of poorly water-soluble compounds in present day drug discovery pipelines, the concept of supersaturation as an effective formulation approach for enhancing bioavailability is gaining steam. This is intended to design the formulation which yields significantly high intraluminal concentrations of the drug than the thermodynamic equilibrium solubility through achieving supersaturation and therefore to enhance the intestinal absorption. The major challenges faced by scientists in developing supersaturatable formulations include controlling the rate and degree of supersaturation with the application of polymeric precipitation inhibitor and maintenance of post-administration supersaturation. The extent of precipitation can be measured using various techniques. The precipitation of a poorly water-soluble weakly basic drugs were investigated under different concentration. It has been shown that the drug precipitates rapidly under supersaturation. Solid dispersion techniques and self-micro-emulsifying drug delivery systems (SMEDDS) with the inclusion of certain polymers can prevent recrystallization, stabilize amorphous APIs, enhance solubility and process ability and facilitate dissolution. Different polymers have been evaluated as precipitation inhibitors. HPMC was shown to be the most potent polymeric precipitation inhibitor.

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Author(s): Yashashwini M P K Kulkarni and Sharon Fredric

Keywords

supersaturation, polymeric precipitation inhibitors, intraluminal concentrations, solid dispersion, SMEDDS, Inhibitors

 
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