比较研究黄连粉末及煎煮液中小檗碱、药根碱在2型糖尿病大鼠药动学特征

Pharmacokinetics of berberine and jateorrhizine from Rhizoma coptidis powder and decoction in diabetic rats

目的:比较研究黄连粉末及煎煮液中的盐酸小檗碱(BER)和盐酸药根碱(JAT)在2型糖尿病大鼠药动学变化,揭示古方应用黄连治疗消渴症选择丸剂的科学内涵。方法:将黄连粉末及其煎煮液灌胃于2型糖尿病大鼠,应用RP-HPLC测定血浆中小檗碱、JAT的血药浓度,DAS2.0药动学软件计算药动学参数。结果:BER、JAT的药动学过程均为二室开放模型;与煎煮液组比较,黄连粉末口服给药组BER、JAT AUC均显著增加,V1/F显著减小,CL/F显著降低,Tmax提前,t1/2Ka及t1/2α缩短,t1/2β延长。结论:与煎煮液比较,黄连粉末效应物质生物利用度更高,吸收更快,消除更慢,提示黄连用于治疗2型糖尿病选择粉末形态如丸剂入药优于煎剂入药。

OBJECTIVE To investigate the pharmacokinetics of berberine （BER） and jateorrhizine （JAT） from Rhizoma coptidis powder and decoction in diabetic rats, and reveal the scientific reasons for why ancient prescriptions chose pills to treat diabetes. METHOI）S Concentrations of BER and JAT in rat plasma were detected by RP-HPLC after rats were orally admin- istered with Rhizoma coptidis powder and decoction. Pharmacokinetie parameters were calculated by DAS 2. 0 pharmaeokinetic software. RESULTS In vivo pharmacokinetic models of BER and JAT were two - compartment open models. Compared to decoction group, BER and JAT in powder group showed a significantly higher AUC, lower V1/F and CL/F, slight shorter T t1/2Ka, t1/2. and a longer t1/2β. CONCLUSION Compared with Rhizoma coptidis decoction, the effective substance in pow- der show a higher bioavailability, faster absorption and slower elimination. It is suggested that we should choose a powder form like pills rather than decoction when Rhizoma coptidis is used to treat type 2 diabetes.