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目的:考察穿心莲内酯直肠给药微乳处方的pH和吸收促进剂用量。方法:采用HPLC测定给药后不同时段家兔肠系膜血浆中穿心莲内酯的含量,绘制时间-血药浓度曲线,以曲线下面积AUC0-2为指标,通过正交试验确定直肠给药微乳处方的pH及吸收促进剂用量的最佳方案。结果:确定直肠微乳的最适处方为穿心莲内酯8 g,吐温-80 300 mL,无水乙醇600mL,肉豆蔻酸异丙酯30 mL,氮酮30 mL,水适量,调pH 7,共配成1 L。结论:按优选处方制得的穿心莲内酯直肠微乳稳定性良好。
OBJECTIVE: To investigate the pH and absorption enhancer of rectally administered andrographolide microemulsion. Methods: The contents of andrographolide in rabbit mesentery plasma were determined by HPLC at different time points. The time-concentration curves were plotted. The area under the curve AUC0-2 was used as an index to determine the rectal microemulsion prescription PH and absorption enhancer dosage of the best solution. Results: The optimal prescription of rectal microemulsion was 8 g of andrographolide, 300 mL of Tween-80, 600 mL of absolute ethanol, 30 mL of isopropyl myristate, 30 mL of Azone, A total of 1 L. Conclusion: The stability of andrographolide rectal microemulsion prepared by the preferred prescription is good.