Rivera Cid P, Gonzalez Fernandez E, Martin F R, Braña M F
Eur J Drug Metab Pharmacokinet. 1986 Oct-Dec;11(4):255-67. doi: 10.1007/BF03189110.
The pharmacokinetics, biotransformation, protein binding and tissue distribution of mitonafide and pinafide were studied after single i.v. and oral administration of each drug (20 mg/Kg) in female rats. In pregnant rats a study of cross placental-barrier after i.v. administration of the two drugs was also performed. The drugs were absorbed fairly rapidly with a mean peak plasma level of 7.63 +/- 0.70 micrograms eq/ml for the 3H-mitonafide and with 6.16 +/- 0.77 micrograms eq/ml for the 3H-pinafide between 30 minutes and 1 hour after oral dosing. For both drugs, the pharmacokinetics can be described by a two-compartment open model. The mean elimination half-lives were 17.8 h and 47.5 h for 3H-mitonafide and 3H-pinafide, respectively. Two metabolites for each compound as well as unchanged drugs were identified in urine by TLC and GC/MS by comparison of their chromatographic properties with a number of reference compounds. Approximately 30% of the radioactive drug was excreted over a 48 h period for 3H-mitonafide and 24% for 3H-pinafide in urine, after i.v. administration. The cross placental-barrier studies showed that both 3H-mitonafide and 3H-pinafide were present in the 14-day fetuses.
在雌性大鼠中，单次静脉注射和口服给予每种药物（20mg/Kg）后，研究了米托萘胺和匹萘胺的药代动力学、生物转化、蛋白结合和组织分布。在怀孕大鼠中，还进行了静脉注射这两种药物后跨胎盘屏障的研究。口服给药后30分钟至1小时之间，3H-米托萘胺的平均血浆峰值水平为7.63±0.70微克当量/毫升，3H-匹萘胺为6.16±0.77微克当量/毫升，两种药物吸收相当迅速。对于两种药物，药代动力学均可用二室开放模型描述。3H-米托萘胺和3H-匹萘胺的平均消除半衰期分别为17.8小时和47.5小时。通过TLC和GC/MS，通过将每种化合物的色谱性质与多种参考化合物进行比较，在尿液中鉴定出每种化合物的两种代谢物以及未变化的药物。静脉注射给药后，在48小时内，3H-米托萘胺约30%的放射性药物经尿液排泄，3H-匹萘胺为24%。跨胎盘屏障研究表明，14天龄胎儿体内均存在3H-米托萘胺和3H-匹萘胺。
