Improvement of Bioavailability for Lovastatin using Self-microemulsifying Drug Delivery System

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DOI: 10.4333/KPS.2002.32.4.267

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摘要: A self-microemulsifying drug delivery system (SMEDDS) was developed to increase the dissolution rate, solubility, and ultimately bioavailability of a poorly water soluble drug, lovastatin. SMEDDS mixtures oils, surfactants, cosurfactants, which emulsify under conditions gentle agitation, similar those would be encountered in gastro-intestinal (GI) tract. Various types self-emulsifying formulations were prepared using four oil (Capryol 90, Lauroglycol Labrafil M 1944 CS 2125), two surfactants (Cremophor EL Tween 80), three cosurfactants (Carbitol, PEG 400 propylene glycol). The efficiency emulsification studied laser diffraction size analyzer determine particle distributions resultant emulsions. Optimized selected for assessment Carpryol 90 (40%), Cremophor (30%) Carbitol (30%). containing lovastatin (20 mg 5 mg) compared conventional tablet by oral administration as prefilled hard gelatin capsules fasted beagle dogs vivo study. area serum concentration-time curve from time zero last measured serum, , significantly greater SMEDDS, suggesting that 130% 192% respectively. afforded improvement absolute relative previous data formulation. These indicate utility dispersed potentially other absorbed drugs.

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