Effect of formula compatibility on berberine pharmacokinetics in brain tissue of rats / 中草药

ABSTRACT

Objective: To investigate the variation in pharmacokinetics of berberine in the brain tissue of rats under the conditions of compound compatibility with geniposide and baicalin or the primary formula HuanglianJiedu Decoction (HJD). Methods: The rats were divided into three groups including berberine group (247.39 mg/kg), compound combination group (berberine, geniposide, and baicalin of 247.39, 130.11, and 113.01 mg/kg) and HJD group (HJD 3.92 g/kg and berberine 247.39 mg/kg). After ig administration of those compounds or formula, the brain tissues of rats were collected immediately at 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, 12, and 24 h respectively. The brain tissue was taken from the six rats in each group. A sensitive UPLC-MS method was developed for determining the concentration of berberine in the brain tissue of rats. The concentration-time curve was plotted and the pharmacokinetic parameters of rats in each group were calculated by DAS 2.0 software. Results: These results showed that the Cmax (368.59 ng/g) of berberine in rats with compound combination was increased compared with those with berberine alone (Cmax 108.01 ng/g), which is pronouncedly larger than the Cmax (31.97 ng/g) of berberine in the HJD group. Meanwhile, the AUC0-∞ of berberine in the compound combination group was 3 236.60 min∙ng/g which was much greater than the AUC0-∞ in rat brain with berberine (2 701.37 min∙ng/g) or HJD (420.34 min∙ng/g). Conclusion: The combination of geniposide and baicalin could promote the concentration of berberine, while the primary formula HJD could decrease the distribution of berberine in the brain tissue of rats.