盐酸青藤碱控释微丸在Beagle犬体内药物动力学研究  

Pharmacokinetics of Sinomenine Hydrochloride Controlled-release Pellets in Beagle Dogs

作　　者：张丽锋[1] 张淑秋[1] 王锐利[1] 白克华[1] 

机构地区：[1]山西医科大学药学院临床药学教研室,太原030001

出　　处：《中国现代应用药学》2009年第2期109-111,共3页Chinese Journal of Modern Applied Pharmacy

摘　　要：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 pharmacokinetic parameters of sinomenine hydrochloride controlled-release pellets in Beagle dogs and calculate the relative bioavailability. METHODS To use a high performance liquid chromatography （HPLC） method with the mobile phase consisted of methanol-aeetonitrile -0.05 mol·L^-1 ammonium dihydrogen phosphate solution （50： 12： 190） , colunm temperature was 30 ℃ , flow rate of mobile phase was 0. 7 mL·min^-1 and wavelength of detector was set at 264 nm. RESULTS In the range of 50-4 000 ng · mL^-1, the linear between peak-area ratios of sinomenine hydroehloride to IS and drug concentration was good,R = 3.6 × 10^-4 C ＋ 0.02, r = 0. 996 4. The precision and recovery were fit for Ch. P （2005） Vol Ⅱ. The pharmacokinetic parameters were t1/2 （ 19.9 ±4.3） and（ 17.8 ±2.1 ） h,Cmax （638 ± 128） and（ 1 738 ±396） ng · mL^-1 , Tmax （6.2 ± 1.1 ） and（7.0 ± 1.0） h, AUC0-1 （20.2 ± 3.3 ） and （22.8 ± 5.0） h·ug·mL^-1 for test and reference preparations, respectively. The relative bioavailability was（90.1 ± 10.4 ）%. CONCLUSION The concentration-time curve of sinomenine hydroehloride controlledrelease pellets in Beagle dogs was flatter and the duration was longer. The present studies achieved our prospective aims.

关 键 词：盐酸青藤碱 微丸 高效液相色谱法 药物动力学 

分 类 号：R965.1[医药卫生—药理学]