ABSTRACT
Vinpocetine (VP) has been widely used to treat cerebrovascular disorders and nerve injury. Borneol (BN), as an important traditional Chinese medicine, is commonly used to promote the absorption and distribution of central nervous system drugs. In this work, a LC-MS/MS method was developed to determine the level of VP in rat plasma and tissues, and to evaluate the effect of co-administration of BN with VP by oral gavage on the absorption and tissue distribution of VP in rats. Rats were divided into VP (10 mg·kg-1), VP (10 mg·kg-1) + BN (75 mg·kg-1) and VP (10 mg·kg-1) + BN (150 mg·kg-1) groups for pharmacokinetic study, and divided into VP (10 mg·kg-1) and VP (10 mg·kg-1) + BN (150 mg·kg-1) groups for tissue distribution study. The animal experiment was approved by Ethics Committee of Hubei University, and complied with the guideline for caring and using of laboratory animals. Compared to VP group, the AUC0-∞, MRT0-∞ and t1/2z of VP + BN (150 mg·kg-1) group increased significantly, by 1.98-, 1.22- and 1.42-fold respectively, and the exposure in plasma, liver, kidney and brain increased by 2-, 1.5-, 1.5- and 1.3-fold respectively. The pharmacokinetic results suggested that co-administration of BN with VP is beneficial for overcoming the undesirable pharmacokinetic characteristics of VP, such as short residence time, low oral bioavailability and brain exposure in clinical usage.
ABSTRACT
Objective: To study the effects of Jinqi Jiangtang Tablet (JQJT) in compatibility on the pharmacokinetics of berberine hydrochloride (BH) in rats. Methods: Male SD rats were ig administered with JQJT (0.42 g/kg, equivalently 5 mg/kg BH), BH (5 mg/kg) + chlorogenic acid (CA, 3 mg/kg), and BH (5 mg/kg), respectively. The plasma concentration at indicated time points were determined by LC-MS/MS method after the drug administrations. The pharmacokinetic parameters of BH were calculated with DAS 3.0 software using non-compartmental model. Results: After the drug administration, no significant change was found for the MRT0~∞, tmax, and t1/2 values of BH, whereas the AUC0~∞ and Cmax values of BH were in the order of BH group >JQJT group > BH + CA group, and the CLz and Vz values of BH were in the order of BH + CA group > JQJT group ≈ BH group. Conclusion: The pharmacokinetic results indicate that the co-administration of BH + CA decreases the absorpation, while increases the plasma clearance and distribution of BH in rats. Additionally, the results also suggest that the compatibility of astragalus root or honeysuckle with Coptidis Rhizoma is likely to produce the opposite effect on the plasma elimination and distribution of BH in vivo in rats.