熊果酸自微乳的制备及其生物利用度

Preparation and Bioavailability of Ursolic Acid Self-Microemulsion

目的:制备熊果酸自微乳给药体系,建立HPLC-MS方法研究熊果酸自微乳的生物利用度和药物动力学。方法:以OP乳化剂、吐温-20、异丙醇和油酸制备熊果酸自微乳给药系统,并考察其稳定性、粒径和Zeta电位。通过口服给药,研究其体内的生物利用度和药物动力学。结果:所制备的熊果酸自微乳在1个月内稳定,平均粒径32.74 nm,Zeta电位4.21 mV。自微乳的相对生物利用度326.5%;缓释片的相对生物利用度256.6%;相对与缓释片,自微乳的相对生物利用度为127.2%。结论:所制备的自微乳给药系统能提高熊果酸的生物利用度。

Objective：To prepare delivery system of ursolic acid self-microemulsion,and establish bioavailability and pharmacokinetics of ursolic acid self-microemulsion by HPLC-MS.Method：Ursolic acid self-microemulsion delivery system was prepared with OP emulsifier,Tween-20,isopropyl alcohol and oleic acid,and investigated its stability,particle size and Zeta potential.In vivo bioavailability and pharmacokinetics in rats were evaluated by oral administration.Result：Ursolic acid self-microemulsion was stable within a month,average particle size and Zeta potential were 32.74 nm and 4.21 mV,respectively.Relative bioavailability of ursolic acid self-microemulsion and sustained-release tablets were 326.5% and 256.6%,respectively;and then relative bioavailability of microemulsion delivery system was 127.2% to sustained-release tablets.Conclusion：This prepared self-microemulsion delivery system could enhance bioavailability of ursolic acid.