The effect of stroke and other components in Xing-Nao-Jing on the pharmacokinetics of geniposide

Geniposide is a bioactive substance derived from gardenia, which has been used in traditional Chinese preparation, such as “Xing-Nao-Jing” (XNJ) for stroke treatment. Stroke and the ingredients of herbal preparation affect the pharmacokinetics of geniposide. A comparative pharmacokinetic study of geniposide in stroke and sham-operated rats after administration of XNJ and geniposide was proceeded to evaluate the effect of stroke on pharmacokinetics of geniposide, while the influence of other components in XNJ was determined by using gardenia extract and geniposide–borneol compounds in rats with stroke to compare. Stroke was induced by middle cerebral artery occlusion followed by reperfusion 2h later. Plasma concentration of geniposide was determined by HPLC. Various pharmacokinetic parameters were estimated from the plasma concentration versus time data using non-compartmental methods. The maximum plasma concentration (Cmax) and area under the curve (AUC0−t) in stroke after administration of XNJ were 5.97±3.82μg/mL, and 570.06±274.32μg·min/mL, respectively, which were 5 times compared with sham-operated rats or the stroke-afflicted rats given geniposide. In stroke, the Cmax and AUC0−t of geniposide–borneol group and gardenia extraction group were close to XNJ group and geniposide group, respectively. The geniposide–borneol group had a higher value. Stroke improved the absorption of geniposide in XNJ. Borneol may be the key ingredient in XNJ improving the absorption of geniposide. [Display omitted]