School of Pharmacy, Yantai University, Yantai 264005, China; State Key Laboratory of Long-acting and Targeting Drug Delivery System, Yantai, China.
J Pharm Biomed Anal. 2011 Dec 5;56(4):825-9. doi: 10.1016/j.jpba.2011.07.017. Epub 2011 Jul 23.
To study pharmacokinetic properties of puerarin poly(amido amine) (PAMAM) dendrimer complex, a sensitive liquid chromatography tandem mass spectrometry method (LC-MS/MS) was developed and validated to determine puerarin in rabbit aqueous humor using microdialysis sampling. Astilbin was used as the internal standard. The linear range for puerarin was from 2 to 1000ng/mL (r=0.9986) based on 20μL of aqueous humor. The coefficients of variations for intra-day and inter-day precisions were less than 10.0%, and the relative error of accuracy was within ±6.3%. The mean extraction recovery of puerarin varied from 80.4% to 85.5%. Microdialysis provides a complete concentration versus time profile. A significant difference was observed in main pharmacokinetic parameters of C(max), AUC and t(1/2) between puerarin solution and puerarin PAMAM dendrimer complex. Complex formation resulted in an obvious increase in bioavailability of puerarin after topical administration to rabbit according to the above LC-MS/MS assay method.
为了研究葛根素聚酰胺-胺（PAMAM）树枝状大分子复合物的药代动力学性质，建立并验证了一种灵敏的液相色谱-串联质谱法（LC-MS/MS），采用微透析采样法测定兔房水中的葛根素。以梓醇为内标。基于 20μL 房水，葛根素在 2 至 1000ng/mL 范围内呈线性（r=0.9986）。日内和日间精密度的变异系数均小于 10.0%，准确度的相对误差在±6.3%范围内。葛根素的平均提取回收率在 80.4%至 85.5%之间。微透析提供了完整的浓度-时间曲线。根据上述 LC-MS/MS 检测方法，葛根素溶液和葛根素 PAMAM 树枝状大分子复合物的 C(max)、AUC 和 t(1/2)等主要药代动力学参数存在显著差异。复合物形成导致局部给予兔后葛根素的生物利用度明显增加。
