Institute of Pharmaceutical Sciences, Department of Pharmacognosy, Karl-Franzens-University Graz, 8010 Graz, Austria.
Phytother Res. 2010 Mar;24(3):445-50. doi: 10.1002/ptr.3074.
A sensitive LC-ESI-MS method with a solid-phase extraction was established for the determination of bilobalide, ginkgolide A and ginkgolide B in human plasma; bioavailability and pharmacokinetics of three different Ginkgo biloba L. preparations have been investigated. The preparations used in the present single-dose pharmacokinetic study were different formulations of Ginkgo biloba L. extracts (Geriaforce tincture, new Ginkgo fresh plant extract tablets and EGb 761) with various excipients. The analysis of Ginkgo terpene lactones was performed by LC-MS on a Zorbax SB-C18 column. The mobile phase consisted of water + 0.1% acetic acid and methanol 68/32 (v/v) to 49/51 (v/v) at a flow rate of 200 microL/min. Bilobalide, ginkgolide A and ginkgolide B were monitored using the selected-ion monitoring (SIM) mode at m/z of 325, 453 and 423, respectively.The amounts of the active compounds (terpene lactones) in the administered products were in the low-mg range per dose. The assay method was successfully applied to the study of the pharmacokinetics and bioavailability of bilobalide, ginkgolide A and ginkgolide B in humans. The resulting maximum concentrations (median) of bilobalide, ginkgolide A and ginkgolide B in plasma after administration of the maximum daily dose of the different Ginkgo products were 3.53, 3.62, and 1.38 ng/mL respectively after administration of Geriaforce tincture; 11.68, 7.36, and 4.18 ng/mL, respectively after taking Ginkgo fresh plant extract tablets; and 26.85, 16.44, 9.99 ng/mL, respectively after administration of EGb 761 tablets. These data are relevant to demonstrate relative bioavailabilities of different Ginkgo biloba L. preparations (Geriaforce tincture, new Ginkgo fresh plant extract tablets and EGb 761).
建立了一种灵敏的 LC-ESI-MS 方法，结合固相萃取，用于测定人血浆中的白果内酯、银杏内酯 A 和银杏内酯 B；研究了三种不同银杏叶 L. 制剂的生物利用度和药代动力学。本单剂量药代动力学研究中使用的制剂是不同配方的银杏叶提取物（Geriaforce 酊剂、新型银杏新鲜植物提取物片剂和 EGb 761），含有不同的赋形剂。银杏萜内酯的分析采用 LC-MS 在 Zorbax SB-C18 柱上进行。流动相由水+0.1%乙酸和甲醇 68/32（v/v）至 49/51（v/v）组成，流速为 200 μL/min。白果内酯、银杏内酯 A 和银杏内酯 B 分别采用选择离子监测（SIM）模式，监测 m/z 为 325、453 和 423。给予产品中活性化合物（萜内酯）的量为低毫克剂量。该测定方法成功应用于测定人体中白果内酯、银杏内酯 A 和银杏内酯 B 的药代动力学和生物利用度。在给予不同银杏产品的最大日剂量后，Geriaforce 酊剂、银杏新鲜植物提取物片剂和 EGb 761 片剂分别测定的血浆中白果内酯、银杏内酯 A 和银杏内酯 B 的最大浓度（中位数）分别为 3.53、3.62 和 1.38ng/mL；分别为 11.68、7.36 和 4.18ng/mL；分别为 26.85、16.44 和 9.99ng/mL。这些数据与证明不同银杏叶 L. 制剂（Geriaforce 酊剂、新型银杏新鲜植物提取物片剂和 EGb 761）的相对生物利用度有关。
