Preparation and Evaluation of Oral Bioavailability of o/w and w/o Puerarin-loaded Microemulsions
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.
T. T. Tang CH. F. Deng D. W. Xiang J. F. Peng X. B. Hu X. L. LU D. X. Xiang Da Xiong Xiang
Key Laboratory of Traditional Chinese medicine preparation, Hunan province,Second Xiangya Hospital of Central South University, Changsha 410011 School of Pharmaceutical Sciences, Central South University, Changsha 410013
国内会议
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
昆明
英文
169-177
2011-11-05（万方平台首次上网日期，不代表论文的发表时间）