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目的建立间尼索地平血药浓度的高效液相色谱-质谱联用方法,研究Beagle犬单剂量口服间尼索地平控释微丸的药动学。方法用HPLC-MS法测定健康Beagle犬单剂量口服间尼索地平控释微丸和普通微丸的血药浓度,以DAS 2.0软件计算药动学参数。结果单剂量给药后,控释微丸和普通微丸的tmax分别为(11.154±0.5077)h和(2.213±0.3225)h,Cmax分别为(79.40±10.60)ng.mL1和(116.7±20.35)ng.mL1,AUC分别为(1227.8±296.0)ng.h.mL1和(867.8±146.7)ng.h.mL1,控释微丸的相对生物利用度为141.5%。结论本方法准确、灵敏,间尼索地平控释微丸血药浓度平稳,可较长时间保持血药浓度。
Objective To establish a HPLC-MS method for the determination of plasma concentration of nisoldipine in a single oral dose of nisoldipine controlled-release pellets. Methods Plasma concentrations of nisoldipine controlled-release pellets and normal pellets in a single dose oral dose of Beagle dogs were determined by HPLC-MS. The pharmacokinetic parameters were calculated by DAS 2.0 software. Results After single-dose administration, the tmax of controlled release pellets and ordinary pellets were (11.154 ± 0.5077) h and (2.213 ± 0.3225) h, respectively, with Cmax of (79.40 ± 10.60) ng.mL1 and (116.7 ± 20.35) ng .mL1 and AUC were (1227.8 ± 296.0) ng.h.mL1 and (867.8 ± 146.7) ng.h.mL1, respectively. The relative bioavailability of controlled release pellets was 141.5%. Conclusion The method is accurate and sensitive. The plasma concentration of nisoldipine controlled-release micro-pellets is stable and can maintain the plasma concentration for a long time.