论文部分内容阅读
应用高效液相色谱法及气相色谱法，研究了９名健康志愿者口服单剂量普罗帕酮的药代动力学及与异喹胍，Ｓ－美芬妥英羟化代谢多态性的相关性。结果表明，６名志愿者中普罗帕酮按一房室模型消除，其余３名符合二房室模型。普罗帕酮消除半衰期为３．４±ｓ１．１ｈ，药时曲线下面积为２．５±ｓ１．１μｇ·＝ｍＬ１，血浆清除率为１４５±ｓ６４Ｌ·ｈ１．普罗帕酮药代动力学参数在异喹胍强与弱代谢者中有较大的差异，而与Ｓ－美芬妥英不同羟化代谢表型则无明显相关性．同时服用普罗帕酮和异喹胍时，两药氧化代谢可产生互相抑制性影响．而普罗帕酮与Ｓ－美芬妥英公用则无明显改变，提示普鲁帕酮和异喹胍可能由同一肝微粒体细胞色素Ｐ４５０同工酶所催化代谢
Pharmacokinetics of a single oral dose of propafenone in nine healthy volunteers and its relationship with the isoquercitrin and S-mephenytoin hydroxylated metabolic polymorphisms were studied by high performance liquid chromatography and gas chromatography . The results showed that propafenone was eliminated in one of the six volunteers and the remaining three matched the two-compartment model. Propafenone half-life of 3.4 ± s1.1h elimination, the area under the curve when the drug was 2.5 ± s1.1μg · = mL1, the plasma clearance rate of 145 ± s64L · h1. The pharmacokinetic parameters of propafenone were significantly different between strong and poor metabolites of isoquinquidine, but no significant correlation with the different metabolic phenotypes of S-mephenytoin. When taking propafenone and isoquinidine, the two drugs can produce mutual inhibitory effects on oxidative metabolism. Propafenone and S-mephenytoin common no significant change, suggesting that the palpase and isoquinidine may be metabolized by the same liver microsomal cytochrome P450 isoenzyme