丹参总酚酸与三七总皂苷合用4种丹酚酸成分在大鼠体内的药动学

 目的 建立丹参总酚酸与三七总皂苷合用(5∶1)灌胃给药后大鼠血浆中原儿茶醛、迷迭香酸、紫草酸、丹酚酸B含量的测定方法，并对其进行药动学研究。方法 采用HPLC-UV方法测定，色谱柱：Zorbax SB-C₁₈ column (4.6 mm×250 mm, 5 μm)，流速：1 mL·min^-1，柱温：30 ℃，检测波长：280 nm，以乙腈和体积分数为0.026%的磷酸水溶液梯度洗脱，血浆样品以体积分数为10%的盐酸酸化，而后用乙酸乙酯萃取2次，并根据测定结果求算药动学参数。结果 4种成分的日内与日间RSD均小于15%，提取回收率均大于70%，线性关系良好。原儿茶醛在10.0 min 达峰，ρ_max为6.466 mg·L^-1，AUC_0-∞值为82.1 mg·min·L^-1，迷迭香酸在11.7 min达峰，ρ_max为10.50 mg·L^-1，AUC_0-∞值为564.8 mg·min·L^-1，紫草酸在20.8 min达峰，ρ_max为5.950 mg·L^-1，AUC_0-∞值为1 123 mg·min·L^-1，丹酚酸B在8.3 min达峰，ρ_max为48.12 mg·L^-1，AUC_0-∞值为4 026 mg·min·L^-1。结论 该法适用于原儿茶醛、迷迭香酸、紫草酸和丹酚酸B的血药浓度测定与药动学研究。

Pharmacokinetics of the Combination of Salvianolic Acids and Panax Notoginseng Saponins in Rat Plasma

OBJECTIVE To optimize the technology parameters of chitosan microspheres loaded with ferulic acid and to study drug releasing mechanism. METHODS The Doehlert design and response surface method were used to optimize technology. The entrapment efficiency was influenced by drug amount and pH of TPP solution.RESULTS Under the optimized conditions， the mean entrapment efficiency and drug loading were 73.77％ and 8.08％ respectively.The release of ferulic acid from chitosan microspheres was in accordance with Higuchi equation and Weibull equation. The microscope observation indicated that ferulic acid were distributed in chitosan microspheres in crystal form. CONCLUSION There was no relation between ferulic acid and chitosan. The sustained-releasing mechanism of ferulic acid from chitosan microspheres was related with the mesh structure of microspheres.