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Evaluating on correlation between in vivo absorption kinetics and in vitro release kinetics of multiple components contained in gbe sustained-release pellets / 中草药
Chinese Traditional and Herbal Drugs ; (24): 2850-2856, 2017.
Article in Chinese | WPRIM | ID: wpr-852643
ABSTRACT
Objective The relationship between the in vivo absorption kinetics and the in vitro release kinetics of various components (including flavonoids and terpenoids) contained in Ginkgo biloba extract (GBE) sustained-release pellets were evaluated using multi-component integration kinetics which could provide a reference for more accurate assessment of in vitro and in vivo correlation. Methods The release rates in vitro of main ingredients (quercetin, isorhamnetin, bilobalide, ginkgolide A, ginkgolide B and ginkgolide C) were detected by HPLC-MS/MS. The integrated drug concentration was calculated, and the release rates in vitro of integrated components were then depicted according to the results. Plasma was collected at different time points after oral administration of GBE sustained-release pellets, multiple components contained in GBE sustained-release pellets were then determined. A novel approach of self-defined weighting coefficient (Wj) based on the area under the curve from zero to infinity AUC0—∞ had been created to obtain the holistic pharmacokinetic profiles of GBE sustained-release pellets. To evaluation the in vitro-in vivo correlation of GBE sustained-release pellets, the percent of integrated in vivo absorption calculated by the Wagner-Nelson methodwas plotted versus the percent of integrated in vitro drug release at the same time. Results The components contained in sustained- release pellets had a good release, the Wj of each component in GBE sustained-release pellets were as follows quercetin, 0.248 1; isorhamnetin, 0.009 2; bilobalide, 0.228 2; ginkgolide A, 0.296 4; ginkgolide B, 0.132 4; ginkgolide C, 0.090 3. The in vivo-in vitro correlation equation was Y = 0.930 8 X + 12.84, r = 0.962 9, indicated that the correlation between in vivo absorption kinetics and in vitro release kinetics is good. Conclusion The efficacy of the herbal medicines depends on a variety of components combined effect, using the integrated pharmacokinetic to analyze IVIVC could take the characteristic of each component into account, which is helpful for the study of the correlation between in vivo absorption kinetics and in vitro release kinetics.

Full text: Available Index: WPRIM (Western Pacific) Type of study: Prognostic study Language: Chinese Journal: Chinese Traditional and Herbal Drugs Year: 2017 Type: Article

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Full text: Available Index: WPRIM (Western Pacific) Type of study: Prognostic study Language: Chinese Journal: Chinese Traditional and Herbal Drugs Year: 2017 Type: Article