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本文的目的在于对醋柳黄酮自微乳化给药系统进行评价,该给药系统用于提高难溶性药物醋柳黄酮的口服生物利用度。评价指标包括自微乳化时间、粒径及多分散指数、形态学特征、体外分散性、稳定性、在体小肠吸收及生物利用度。结果表明,该自微乳化给药系统在3 min内即形成微乳,平均粒径低于40 nm,多分散指数低于0.2,电镜下观察粒子形态为球形;20 min时体外累积释放百分率(以槲皮素计)接近90%,显著高于普通胶囊剂;加速试验条件下放置6个月,自微乳化给药系统的所有指标均未发生明显改变;该自微乳化给药系统的在体小肠吸收速率常数(以槲皮素计)显著高于醋柳黄酮乙醇溶液(P<0.05);以醋柳黄酮的混悬液为参比制剂,自微乳化给药系统的大鼠灌胃给药相对生物利用度(以槲皮素计)为518%。
The purpose of this article is to evaluate the self-microemulsifying delivery system of tilapia, which is used to increase the oral bioavailability of the slightly soluble drug, Evaluation criteria include self-microemulsification time, particle size and polydispersity index, morphological characteristics, in vitro dispersibility, stability, absorption in the small intestine and bioavailability. The results showed that the self-microemulsifying drug delivery system formed microemulsion within 3 min, the average particle size was less than 40 nm, the polydispersity index was less than 0.2, and the morphology of the particles was spherical under electron microscopy. The cumulative release percentage in vitro at 20 min To quercetin) was nearly 90%, significantly higher than ordinary capsules; accelerated test conditions for 6 months, all the indicators of self-microemulsifying drug delivery system did not change significantly; the self-microemulsifying drug delivery system in The intestinal absorption rate constant of the small intestine (calculated by quercetin) was significantly higher than that of the aloe vera flavonoids ethanol solution (P <0.05). The tilapia flavonoids suspension was used as the reference preparation, The relative bioavailability (calculated as quercetin) was 518%.