黄连粉末中小檗碱、药根碱及单体化合物在2型糖尿病大鼠体内的药动学和药效学特征分析

Pharmacokinetic and pharmacodynamic characteristics of berberine and jateorhizine in Coptidis Rhizoma powder and their monomeric compounds in type 2 diabetic rats

该文比较分析了黄连粉末(HL-P)中的小檗碱(BER)、药根碱(JAT)与单体化合物及二者混合物(BJ)在2型糖尿病(T2D)大鼠体内的药动学和药效学特征,以揭示黄连以粉末状态治疗T2D的优越性机制。将T2D大鼠灌胃给药治疗63 d,观察各组药代动力学参数、动态血糖水平及血脂值,结果表明:HL-P组与其他对应组相比,BER及JAT的tmax,T1/2ka降低,Cmax,AUCinf,AUClast,VL/F均显著增大;与模型组比较,HL-P组治疗从第18 d起,BER组及BJ组从第36 d起血糖值下降显著,而JAT组血糖值下降不明显;与模型组比较,各治疗组FFA值均下降明显,HL-P组TG,HDL,LDL值有显著改善,BER组LDL值及BJ组HDL值有显著改善。上述结果显示黄连粉末具有优越的药代动力学特征及优良的降低血糖及血脂作用活性。提示黄连用于治疗T2D宜选择粉末形态口服应用具有一定科学依据。

This article focused on a comparative analysis on the pharmacokinetic and pharmacodynamic characteristics of berberine（ BER） and jateorhizine（ JAT） in Coptidis Rhizoma powder（ HL-P） and their monomeric compounds（ BER ＋ JAT,BJ） in type 2 diabetic（ T2D） rats to explore the beneficial effect of HL-P in the treatment of T2 D. The T2 D rats were treated with HL-P,BER,JAT and BJ,respectively for 63 d. The pharmacokinetic parameters,dynamic changes in blood glucose level and blood lipid values were measured. The results showed that,compared with other corresponding group,tmax,T1 /2kaof BER and JAT in HL-P group were reduced,while Cmax,AUCinf,AUClast,VL/ F were significantly increased; compared with model group,blood glucose levels were decreased significantly in HL-P group since the 18 th day,while those in BER or BJ group were reduced since the 36 th day,however,blood glucose levels showed no obvious changes in JAT group; compared with model group,FFA values in all treatment group were decreased significantly. Moreover,TG,HDL and LDL value in HL-P group,LDL value in BER group and HDL value in BJ group were improved significantly. The above results showed that Coptidis Rhizoma powder showed excellent pharmacokinetic characteristics and excellent activity of lowering blood glucose and lipid. It provided a scientific basis for oral application of Coptidis Rhizoma powder in the treatment of T2 D.