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Abstract
Ginkgolide B (GB), an important active constituent of Ginkgo biloba extract, has been used in clinical applications for the treatment of dementia, cerebral insufficiency or related cognitive decline. To investigate the main pharmacokinetic characteristics of three different GB formulations in beagle dogs, a simple, specific and sensitive LC-MS/MS method was established and validated. The separation of the analytes was achieved on an Agilent Eclipse Plus C18 column (1.8 μm, 2.1 × 50 mm) with a mobile phase consisting of water and acetonitrile. The flow rate was set at 0.4 mL/min. Quantitation was performed using multiple reaction monitoring (MRM) in negative ion mode, with the transitions at m/z (Q1/Q3) 423.1/367.1 for GB and m/z 269.3/170.0 for IS. The linear calibration curve of GB was obtained over the concentration range of 2–200 ng/mL. The intra- and inter-day precisions were <15% and the accuracies were within ±12.7%. The validated method was applied to compare the pharmacokinetic characteristics of GB in healthy beagle dogs after oral administration of three formulations (HME08, GB capsule prepared by hot-melt extrusion technology; LL06, GB pellet prepared by liquid layer technology; conventional GB tablet). The Cmax values of GB from different formulations in beagle dog plasma were 309.2, 192.4 and 66.6 µg/L, and the AUC values were 606.7, 419.1 and 236.2 µg/L·h, respectively. The data suggested that the exposure level of GB from HME08 and LL06 in beagle dog plasma was greatly improved compared with conventional tablets. This study should be helpful for the design and development of oral GB preparations.
Highlights
Ginkgo biloba extract (GBE), an extract of Ginkgo biloba tree leaves, has been used in clinic for the treatment of vascular and age‐related deterioration of cognitive functions, including dementia and peripheral arterial occlusive diseases [1,2]
Accumulating evidence suggests that ginkgolide B (GB, chemical structure shown in Figure 1) exhibited the strongest pharmacological activity among the ginkgolides
The subsequent in vitro experiments revealed that HME08 and LL06 had good dissolution compared with conventional tablet
Summary
Ginkgo biloba extract (GBE), an extract of Ginkgo biloba tree leaves, has been used in clinic for the treatment of vascular and age‐related deterioration of cognitive functions, including dementia and peripheral arterial occlusive diseases [1,2]. Accumulating evidence suggests that ginkgolide B (GB, chemical structure shown in Figure 1) exhibited the strongest pharmacological activity among the ginkgolides. It could reduce the platelet aggregation and the formation of thrombosis by Molecules 2015, 20, page–page; doi:10.3390/molecules201119678 www.mdpi.com/journal/molecules. The wide use of GB has been limited due to its poor water solubility and the low oral bioavailability and limited the desired effect of marketed products, so it is necessary to develop a new formulation of GB to increase the oral absorption and bioavailability. To combat the unsatisfactory bioavailability of GB, two new GB formulations prepared by hot‐melt extrusion (HME) and liquid layer technology are evaluated. Determination of the preclinical pharmacokinetic profile of the three GB formulations is necessary and important
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