Study on local pharmacokinetics of baicalin gel after transdermal administration in rats by skin microdialysis in vivo
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摘要: 目的 建立大鼠在体皮肤微透析技术,研究黄芩苷凝胶经皮吸收局部药动学。 方法 采用HPLC-MS/MS联用技术测定大鼠皮肤微透析液中黄芩苷的浓度。SD大鼠在麻醉状态下做皮肤微透析预处理,然后将黄芩苷凝胶涂于探针所在皮肤表面,收集皮肤微透析液样品进行黄芩苷浓度测定,绘制黄芩苷浓度-时间曲线,计算经皮吸收局部药动学参数。 结果 用于定量分析的离子对为m/z 447.3→271.2,黄芩苷在检测浓度范围内线性关系良好,色谱的专属性、精密度等测定结果均符合生物样品测定要求。体内皮下探针对黄芩苷的回收率为(24.40±0.91)%,240 min内各取样点回收率保持稳定;黄芩苷经皮给药后8 h内微透析液中均可检测到黄芩苷的存在,且药物在皮肤组织内浓度持续升高,AUC0-t为(50.04±34.17) (mg·min)/L。 结论 在体皮肤微透析法可用于黄芩苷经皮吸收局部药动学研究。Abstract: Objective To develop a novel skin microdialysis technology in vivo,and to determine the pharmacokinetic of baicalin after transdermal administration in rats. Methods An HPLC-MS/MS method used for the determination of baicalin in skin microdialysis samples was established,SD rats were pretreated with skin microdialysis operation under anesthesia, and then the baicalin gel was applied to the skin surface of probe in vivo. The baicalin concentration of skin microdialysates was determined, the time curve of baicalin concentration was drawn and the topical pharmacokinetics parameters of percutaneous absorption was calculated. Results Baicalin was optimized at the transitions m/z 447.3→271.2. The linearity correlation was good and the assay exhibited good precision and accuracy. The subcutaneous probe recovery of baicalin in vivo was(24.40±0.91)% and was stable over the 240 min study period. Baicalin could be detected in the microdialysis samples after transdermal administration, and its concentration continued to rise in 8 h. AUC0-t in skin tissue was(50.04±34.17) mg·min·L-1. Conclusion The method of skin microdialysis in vivo could be used in the local pharmacokinetic research of baicalin.
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Key words:
- baicalin gel /
- microdialysis /
- dermatopharmacokinetics /
- rat
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