含天然乳化剂的新型葛根素自微乳与传统自微乳体内外性能的对比研究

Comparative Study on Properties of Natural Emulsifier Self-Microemulsion and Nonionic Surfactants SelfMicroemulsion of Puerarin in Vitro and in Vivo

目的制备新型葛根素自微乳,旨在降低传统自微乳的毒性,同时能保持自微乳原有性能。方法以阿拉伯胶代替50%处方量聚山梨酯80制备葛根素自微乳;评价2种自微乳的自乳化速率、微乳形态、粒径分布;采用大鼠在体单向肠灌流模型对2种自微乳的肠道吸收进行评价。结果含天然乳化剂自微乳(NE-SMEDDS)较含合成非离子型乳化剂自微乳(NSSMEDDS)的自乳化速率基本保持一致,所形成的微乳粒径及粒径分布范围有所变大,但仍小于100 nm;含天然乳化剂自微乳对葛根素的促吸收效果略优于含合成非离子型乳化剂自微乳。结论利用天然乳化剂代替50%的合成乳化剂制备自微乳,能基本保持自微乳原有的体内外行为。

OBJECTIVE To prepare a new puerarin self-microemulsion to reduce the toxicity of traditional self-microemulsion and maintain the characteristics in vitro and in vivo. METHODS Nonionic surfaetant self-mieroemulsion （NS-SMEDDS） and natural emul- sifier self-mieroemulsion（NE-SMEDDS） were prepared. The micro-emulsifying rate and the shape and distribution of particle size of the micro-emulsion were evaluated. Meanwhile the intestinal absorption of NS-SMEDDS was compared with NE-SMEDDS by in situ single pass peffusion model. RESULTS The micro-emulsifying rate of NE-SMEDDS was almost the same as NS-SMEDDS. The particle size distribution of NE-SMEDDS was wider than NS-SMEDDS, but both of them were less than 100 nm. The absorption enhancement effect of NE-SMEDDS for puerarin was slightly better than NS-SMEDDS. CONCLUSION The in vitro and in vivo characteristics of self-mi- croemulsion can be maintained by replacing the 50% nonionic surfactants with natural emulsifier.