| 摘要: |
| 目的:制备青蒿素自乳化系统,并对家兔体内药动学过程进行考察。方法:通过绘制相图并结合溶出度试验,以形成乳剂的乳化程度和乳化时间为指标,应用正交试验设计筛选最佳处方。用高效液相色谱法测定青蒿素的血药浓度,以青蒿素原料药作对照,比较家兔体内的药动学参数。结果:青蒿素自乳化系统主要由青蒿素、吐温-85 、油酸乙酯、乙醇组成。青蒿素自乳化制剂与青蒿素原料药在家兔体内平均滞留时间分别为4.750 h和4.628 h,家兔药动学研究结果表明,青蒿素自乳化系统口服后能很大程度上提高生物利用度。结论:自乳化制剂可以显著提高青蒿素的体外溶出及体内吸收。 |
| 关键词: 青蒿素 自乳化剂 生物利用度；药代动力学 |
| DOI：10.3724/SP.J.1008.2008.00822 |
| 投稿时间：2007-07-13修订日期：2008-06-10 |
| 基金项目: |
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| Preparation of self-emulsified artemisinin and its pharmacokinetics in rabbits |
| YIN Yu-juan,L Xiao-man,LI Guo-dong* |
| (Department of Pharmaceutics,School of Pharmacy,Second Military Medical University,Shanghai 200433,China) |
| Abstract: |
| Objective:To prepare self-emulsified artemisinin and to investigate its pharmacokinetics in rabbits.Methods: The optimized formula was screened using an orthogonal experimental design,tertiary-phase diagram and solubility test; the extents of emulsification and emulsifying time were taken as the indices.The plasma concentrations of indirubin were determined by HPLC method.The crude artemisinin was taken as control and the pharmacokinetic parameters were compared between the 2 groups.Results: The artemisinin self-emulsifying drug delivery system(SEDDS) was composed of artemisinin,Tween-85,ethyl-oleate,and ethanol.The mean retention times(MRT) was 4.628 h for crude artemisinin and 4.750 h for self-emulsion.Pharmacokinetic study in rabbits demonstrated that the SEDDS of artemisinin greatly enhanced the bioavailability of artemisinin via oral administration.Conclusion: SEDDS can greatly increase the in vitro dissolution and in vivo absorption of artemisinin. |
| Key words: artemisinin self-emulsifying agents biological availability pharmacokinetics |
