蒿甲醚、蒿琥酯及其代谢产物双氢青蒿素在血浆中的薄层扫描定量法

THIN-LAYER CHROMATOGRAPHIC DENSITOMETRIC METHOD FOR SIMULTANEOUS DETERMINATION OF ARTEMETHER OR ARTESUNATE AND THEIR METABOLITE IN RAT PLASMA

报道了用薄层密度扫描定量法同时测定血浆中蒿甲醚(MDA)和双氢青蒿素(DHA)(A);蒿琥酯(AS)和DHA(B)以及单独测定DHA (C)的分析方法。线性范围除B法中AS为0.1至3.5μg外,余均为0.1至4.0μg(r均大于0.99,p<0.005)。检测限A法均为0.03μg;B、C法均为0.01μg。MDA和DHA平均回收率分别为82.8和92.2％;AS和DHA分别为95.5和89.2％;DHA为96％(c.v.均在6％以内)。并进行了大鼠DHA,MDA和DHA及AS和DHA的药物动力学研究,提供了各自的参数。

The metabolite pharmacokinetics of both artemether (MDA) andartesunate (AS) as well as their effective metabolite dihydroartemisinine (DHA)has been studied by TLC methods. MDA together with DHA(A),AS together withDHA (B) and DHA (C) were extracted with petroleum ether-dichloromethane(2:1) from rat plasma (0.5 ml), and their concentrations were determined incomparison with external standard. The relationship between the drug quantitiesand the absorption values in the range of 0.1 to 3.5 or 4.0 /μg was linear. Thecorrelation coefficients were all about 0.99(p<0.0005). The detection limits wereabout 0.03μg. The mean recoveries were 82.8% (cv=5.4)and 92.2 / (cv=5.3%)for MDA and DHA respectively; and 95.5% (cv=4.0%)and 89.2% (cv=1.7%)for AS and DHA respectively; and 96% (ev=1.9%)for DHA. The methodspresented successfully the corresponding pharmacokinetic parameters.