[间硝苯地平在比格犬体内的药代动力学]
[Pharmacokinetics of m-nifedipine in Beagle dogs].
作者信息
Yang Zhi-fu, Zhou Si-yuan, Yang Tie-hong, Mei Qi-bing
机构信息
Department of Pharmacology, The Fourth Military Medical University, Xi'an 710032, China.
出版信息
Yao Xue Xue Bao. 2004 Aug;39(8):609-12.
AIM
To study the pharmacokinetics of m-nifedipine (m-Nif) in Beagle dogs.
METHODS
The Beagle dogs were divided into two groups. m-Nif was intravenously administered to the Beagle dogs in group 1 at the dose of 0. 288 mg x kg(-1), and it was orally administered to the Beagle dogs in group 2, 3 and 4 at the dose of 1.152, 3.456 and 10.370 mg x kg(-1), respectively. m-Nif in plasma was detected by reversed phase high performance liquid chromatography. The pharmacokinetic parameters were calculated by 3P97 software.
RESULTS
When m-Nif was intravenously administered, the plasma concentration-time curve was fit to a two-compartment model and T1/2beta was 117 min. When m-Nif was orally administered, the plasma concentration-time curve was fit to a one-compartment model. T1/2 (Ke) and Cmax were 147 min and 20 microg x L(-1); at the low dose of 1.152 mg x kg(-1). T1/2 (Ke) was 122 min and Cmax was 36 microg x L(-1) at the middle dose of 3.456 mg x kg(-1). T1/2 (Ke) was 144 min and Cmax was 69 microg x L(-1) at the high dose of 10.37 mg x kg(-1), respectively.
CONCLUSION
It was showed that the speed of elimination of m-Nif was high in Beagle dogs. The absolute bioavailability of m-Nif given orally was very low.
目的
研究间硝苯地平（m-Nif）在比格犬体内的药代动力学。
方法
将比格犬分为两组。第1组比格犬静脉注射m-Nif，剂量为0.288mg·kg⁻¹，第2、3、4组比格犬分别口服m-Nif，剂量为1.152、3.456和10.370mg·kg⁻¹。采用反相高效液相色谱法检测血浆中的m-Nif。用3P97软件计算药代动力学参数。
结果
静脉注射m-Nif时，血浆浓度-时间曲线符合二室模型，T1/2β为117分钟。口服m-Nif时，血浆浓度-时间曲线符合一室模型。低剂量1.152mg·kg⁻¹时，T1/2（Ke）为147分钟，Cmax为20μg·L⁻¹；中剂量3.456mg·kg⁻¹时，T1/2（Ke）为122分钟，Cmax为36μg·L⁻¹；高剂量10.37mg·kg⁻¹时，T1/2（Ke）为144分钟，Cmax为69μg·L⁻¹。
结论
结果表明，m-Nif在比格犬体内消除速度较快。m-Nif口服绝对生物利用度很低。
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