Anzenbacherová Eva, Anzenbacher Pavel, Svoboda Zbynek, Ulrichová Jitka, Kvetina Jaroslav, Zoulová Jana, Perlík Frantisek, Martínková Jirina
Institute of Medical Chemistry and Biochemistry, Faculty of Medicine, Palacky University, Olomouc, Czech Republic.
Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2003 Dec;147(2):155-9.
To prove the suitability of minipigs as experimental animal in modeling of the drug metabolism and pharmacokine-tics in man, propafenone metabolism in vitro at the microsomal level as well as propafenone pharmacokinetics in the minipig was studied. The results were compared with those obtained for humans. It can be concluded that whereas the microsomal in vitro system of minipig may be a good model for drug metabolism in the man, the pharmacokinetics in the whole organism is more complex reflecting differences in substrate specificities of many enzymatic and transport systems. In this particular case, it has been documented that the glucuronidation of propafenone principal metabolite (5-hydroxypropafenone) is more efficient in the minipig.
为证明小型猪作为人类药物代谢和药代动力学建模实验动物的适用性，研究了小型猪微粒体水平上普罗帕酮的体外代谢以及其药代动力学，并将结果与人类的结果进行比较。可以得出结论，虽然小型猪的微粒体体外系统可能是人类药物代谢的良好模型，但整个生物体中的药代动力学更为复杂，反映出许多酶和转运系统底物特异性的差异。在这种特殊情况下，已证明普罗帕酮主要代谢物（5-羟基普罗帕酮）在小型猪中的葡萄糖醛酸化更为有效。
