Mizuno N, Nishikata M, Morita E, Miyake K
J Pharmacobiodyn. 1986 Oct;9(10):787-92. doi: 10.1248/bpb1978.9.787.
The pharmacokinetics of sulfaguanidine in rats was studied after its intravenous or oral administration. In adult rats, its elimination from plasma, after intravenous administration of 2.5 or 25 mg/kg doses, could be described by a two-compartment open model, while its plasma concentration after oral administration of 25 mg/kg doses, agreed with the one- or two-compartment open model. Neonatal rats displayed a lower elimination of sulfaguanidine than adult rats. Comparison of the drug's gastrointestinal absorption showed that the maximum plasma concentration after oral administration was significantly higher for neonatal than for adult rats. However, there was no significant difference between the times required to reach maximum plasma concentrations. The area under the plasma concentration-time curve at 0-infinity h was significantly higher for neonatal than for adult rats. The absolute bioavailability (57.86%) in neonatal rats was approximately five times that (12.76%) in adult rats. Thus, sulfaguanidine was poorly absorbed by adult rats, but was efficiently absorbed by immature gastrointestines of neonatal rats.
研究了磺胺胍静脉注射或口服给药后在大鼠体内的药代动力学。在成年大鼠中,静脉注射2.5或25mg/kg剂量后,其从血浆中的消除可用二室开放模型描述,而口服25mg/kg剂量后的血浆浓度符合一室或二室开放模型。新生大鼠磺胺胍的消除比成年大鼠低。药物胃肠道吸收的比较表明,新生大鼠口服给药后的最大血浆浓度显著高于成年大鼠。然而,达到最大血浆浓度所需的时间之间没有显著差异。新生大鼠0至无穷大小时血浆浓度-时间曲线下面积显著高于成年大鼠。新生大鼠的绝对生物利用度(57.86%)约为成年大鼠(12.76%)的五倍。因此,磺胺胍在成年大鼠中吸收较差,但在新生大鼠未成熟的胃肠道中吸收良好。