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目的:研究一种青藤碱雷公藤甲素巴布剂裸鼠透皮吸收过程。方法:采用微透析联用HPLC的方法,以30%乙醇/生理盐水为灌流液,样品以Diamonsil-C18(4.6 mm×250 mm,5μm)为色谱柱,以甲醇-磷酸盐缓冲液(pH 9.0)(55∶45)为流动相,检测波长为225 nm的条件下进行分析,经过反透析法体内回收率校正后,所得的裸鼠皮下游离青藤碱雷公藤甲素浓度采用WINNONLIN 5.2程序以非房室模型方法计算药代动力学参数。结果:青藤碱达峰时间为14 h,达峰浓度为30.15μg.mL-1。雷公藤甲素达峰时间为10 h,达峰浓度为3.31μg.mL-1。结论:本方法能够在体、实时监测裸鼠皮下青藤碱雷公藤甲素的动态浓度,为局部药动学研究提供新的方法学参考。
Objective: To study the transdermal absorption of sinomenine to triptolide. METHODS: Microdialysis coupled with HPLC was used with 30% ethanol/physiological saline as the perfusion fluid. Diamonsil-C18 (4.6 mm×250 mm, 5 μm) was used as the chromatographic column with methanol-phosphate buffer (pH 9.0). ) (55:45) was the mobile phase and the detection wavelength was 225 nm. After the in vivo recovery of the reverse dialysis method was calibrated, the free subcutaneous free sinomenine concentration in nude mice was determined using the WINNONLIN 5.2 program. The non-compartment model method calculates pharmacokinetic parameters. Results: The peak time of sinomenine was 14 h and the peak concentration was 30.15 μg.mL-1. The peak time of triptolide was 10 h and the peak concentration was 3.31 μg.mL-1. Conclusion: This method can monitor the dynamic concentration of subcutaneous sinomenine triptolide in nude mice in vivo and provide a new methodological reference for local pharmacokinetic studies.