间硝苯地平类似物MN9201在Beagle犬体内的药动学

Determination of MN9201,a m-nifedipine analogue,in beagle dog by RP-HPLC

目的:研究间硝苯地平类似物MN9201在Beagle犬体内的药动学。方法:10只Beagle犬随机均分成两组,分别静注二氢吡啶类药物间硝苯地平(0．288 mg·kg^(-1))和MN9201(0．312 mg·kg^(-1)),然后用反相高效液相色谱法测定血浆中原型药物浓度,血浆药物浓度-时间数据用3P97药动学软件分析。结果:Beagle犬静注间硝苯地平和MN9201后,其体内过程均符合二室模型,t_(1/2)β分别为(107±26)和(149±31)min,AUC分别为(16998±2752)和(22328±3361)μg·min·L^(-1)。结论:MN9201在Beagle犬体内代谢速度相对于间硝苯地平缓慢,可能具有相对较好的应用前景。

Objective ：To feature the pharmacokinetics of MN9201, a m-nifedipine analogue, in Beagle dogs. Methods：The Beagle dogs were randomly i.v. injected with either m-nifedipine 0. 288 mg·kg^-1 or MN9201 0. 312 mg·kg^-1. The plasma samples for the dogs were collected to measure the concentration of the tested parent drugs by reversed phase high performance liquid chromatography. The pharmacokinetic parameters were calculated with 3P97 software. Results：The pharmacokinetic profiles of m-nifedipine and MN9201 all obeyed a two-compartment model, giving t1/2β of （107 ± 26） vs. （149 ± 31） min and AUC of （16998 ±2752） vs. （22 328 ±3 361）μg·min^-L-1 Conclusion：The elimination rate of MN9202 was slower than m-nifedipine in Beagle dogs.