Preparation and Evaluation of Oral Bioavailability of o/w and w/o Puerarin-loaded Microemulsions

来源 :中华中医药学会制剂分会、世界中联中药药剂专业委员会2011学术年会暨“龙津杯”中药制剂创新与发展论坛 | 被引量 : 0次 | 上传用户:yaojunsyt
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The purpose of this study was to develop oil-in-water (o/w) and water-in-oil (w/o) microemulsion formulations for improving the oral absorption of poorly water-soluble drug, puerarin. During screening and preparation, the influence of the oils, surfactants and co-surfactants on the solubility of puerarin was investigated in details. The pseudo-ternary phase diagrams were developed for various o/w and w/o microemulsion formulations to indentify the most efficient microemulsion region, respectively. After the step-by-step experiments mentioned above, the ultimate optimized o/w and w/o microemulsion formulations were formed with 3.1% ethyl oleate, 18.5% Cremophor RH 40, 9.2% 1,2-propanediol, 69.2% water and 45.0% ethyl oleate, 22.5% soybean lecithin, 22.5% ethanol, 10.0% water (w/w), respectively.The o/w and w/o microemulsion formulations were characterized by droplet size, viscosity, electro-conductivity and stability study. During the bioavailability study of those microemulsions, the plasma concentrations of puerarin were determined using an HPLC method following gavage administration in rats. There was a significant improvement in the oral bioavailability of puerarin compared with suspension formulation (P<0.05). The relative bioavailabilities of o/w and w/o puerarin-loaded microemulsions were 4.42-fold and 8.31-fold compared with puerarin suspension, respectively. These results indicated that o/w and w/o microemulsions are promising drug delivery systems for puerarin by the oral route.
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