ABSTRACT
OBJECTIVE:To study the pharmacokinetics effects of naloxone combination on Shenmai injection in rats in vivo. METHODS:12 rats were randomly divided into monotherapy group (Shenmai injection 9.00 ml/kg,iv) and combination group (Shenmai injection 9.00 ml/kg+naloxone 1.80 ml/kg,iv). The blood samples were collected before administration and 0.083,0.25, 0.5,0.75,1,1.5,2,3,6,12,24,48,96 and 144 h after administration. HPLC was adopted to determine the plasma concentra-tions of ginsenosides Rg1,Re and Rb1,and DAS 2.0 software was used to calculate the pharmacokinetic parameters. RESULTS:Compared with monotherapy group,the plasma concentration of ginsenosides Rg1 in combination group was increased,CL was de-creased,t1/2 and MRT were prolonged,and AUC0-144 h was increased;the plasma concentration of ginsenosides Re was increased,Ke was decreased,t1/2 was prolonged,MRT was shortened,and AUC0-144 h was increased;the plasma concentration of ginsenosides Rb1 was decreased,Ke was increased,t1/2 and MRT were shortened,and AUC0-144 h was decreased,with significant differences(P<0.01 or P<0.05). CONCLUSIONS:Shenmai injection combined with naloxone can slow down the removing of ginsenosides Rg1 and Re in vivo,and obviously the plasma concentration of Shenmai injection is higher than monotherapy group;speed up the removing of ginsenosides Rb1,and the plasma concentration of Shenmai injection is lower than monotherapy group obviously.
ABSTRACT
Scutellarin is the main effective constituent of breviscapine, a flavonoid mixture isolated from the dried whole plant of Erigeron breviscapus (Vant.) Hand-Mazz, and valsartan is used as an antihypertensive drug. These two drugs have already been clinically used together to treat diabetic nephropathy (DN) in China, and the combined medications showed some enhanced protection against DN. The aim of this study is to investigate the potential pharmacokinetic interaction between scutellarin and valsartan in rats. Breviscapine injection (20 mg x kg(-1), i.v.) and valsartan (15 mg x kg-, i.g.), either alone or together were given to 18 male Sprague-Dawley rats. Concentrations of scutellarin and valsartan were quantified by HPLC, and pharmacokinetic parameters were calculated by non-compartmental methods. We found that the pharmacokinetic parameters of scutellarin altered significantly after co-administration of oral valsartan. The plasma clearance (CL(p)) and the bile clearance (CL(b)) of scutellarin were reduced significantly in the presence of valsartan. After oral administration of valsartan with or without intravenous scutellarin, however, the pharmacokinetic parameters of valsartan were comparable. In conclusion, our data suggests that the concurrent use of valsartan reduces the biliary excretion of scutellarin, and this may be due to the inhibitory effect of valsartan on the biliary excretion of scutellarin mediated by Mrp2 (Multidrug resistance-associated protein 2).
ABSTRACT
OBJECTIVE:To promote rational use of traditional Chinese medicines. METHODS:The practical importance of applying basic pharmacoeconomic theory to the rational use of traditional Chinese medicines was analyzed and the measures regarding how to apply the pharmacoeconomic theory to guide rational use of traditional Chinese medicines were put forward. RESULT & CONCLUSION: It is quite necessary and practical to apply the basic pharmacoeconomic theory to the rational use of traditional Chinese medicine, which plays a positive role in promoting rational use of traditional Chinese medicines.