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目的测定盐酸青藤碱控释微丸在Beagle犬体内药物动力学参数,计算相对生物利用度。方法采用反相高效液相色谱法,流动相为甲醇-乙腈-0.05mol.L-1磷酸二氢铵溶液(50:12:190),柱温为30℃,流速为0.7mL.min-1;检测波长为264nm;结果盐酸青藤碱在50～4000ng.mL-1内,主药与内标峰面积比(R)与浓度(C)间线性关系良好,线性方程为R=3.6×10-4C+0.02,r=0.9964,方法的精密度和回收率均符合中国药典2005版二部的规定。受试制剂和参比制剂的主要药物动力学参数分别为:t1/2:(19.9±4.3)h,(17.8±2.1)h;Cmax:(638±128)ng.mL-1,(1738±396)ng.mL-1;Tmax:(6.2±1.1)h,(7.0±1.0)h;AUC0～t:(20.2±3.3)h.μg.mL-1,(22.8±5.0)h.μg.mL-1,相对生物利用度为(90.1±10.4)%。结论盐酸青藤碱控释微丸在Beagle犬体内血药浓度曲线平稳,维持时间长,控释效果较好,达到了预期的目标。
Objective To determine the pharmacokinetic parameters of sinomenine hydrochloride controlled-release pellets in Beagle dogs and calculate the relative bioavailability. Methods The mobile phase was methanol-acetonitrile-0.05mol.L-1 ammonium dihydrogen phosphate solution (50: 12: 190) using reversed-phase high performance liquid chromatography with a column temperature of 30 ℃ and a flow rate of 0.7mL.min-1 ; Detection wavelength of 264nm; Results sinomenine hydrochloride in 50 ~ 4000ng.mL-1, the main drug and the internal standard peak area ratio (R) and concentration (C) good linear relationship between the linear equation R = 3.6 × 10 -4C + 0.02, r = 0.9964, the precision and recovery of the method are in line with the provisions of the Chinese Pharmacopoeia 2005 edition two. The main pharmacokinetic parameters of the test preparation and the reference preparation were as follows: t1 / 2: (19.9 ± 4.3) h, (17.8 ± 2.1) h; Cmax: (638 ± 128) ng.mL- 396) ng.mL-1; Tmax: (6.2 ± 1.1) h, (7.0 ± 1.0) h; AUC0 ~ t: (20.2 ± 3.3) h.μg.mL-1, (22.8 ± 5.0) mL-1, the relative bioavailability was (90.1 ± 10.4)%. Conclusion The sinomenine hydrochloride controlled-release pellets in Beagle dog’s blood concentration curve is stable, maintaining a long time, the controlled release effect is good, reaching the desired goal.