摘要
目的建立测定血浆非洛地平浓度的高效液相色谱-质谱串联法,研究非洛地平缓释片的相对生物利用度及生物等效性。方法采用双周期交叉试验方法,20例男性健康志愿者分别单剂量口服非洛地平缓释片试验药或对照药。采用高效液相色谱-质谱串联法测定血浆非洛地平浓度,用DAS2.0软件对两药进行等效性评价。结果试验药与对照药的主要药动学参数:血药峰浓度(Cmax)分别为(2.15±0.63)和(2.29±0.63)ng.mL-1;达峰时间(tmax)分别为(6.33±1.57)和(6.68±1.32)h,半衰期(t1/2)分别为(18.22±2.75)和(19.04±2.27)h,药物浓度-时间曲线下面积(AUC0-48)分别为(58.11±5.15)和(61.13±6.31)ng.mL-1.h。受试制剂对参比制剂平均相对生物利用度F为(95.06±8.42)%。结论两种非洛地平缓释片生物等效。
Objective To set up a method for determination of felodipine in human plasma by HPLC-MS/MS and study the relative bioavailability and bioequivalenee of felodipine sustained-release tablets. Methods Twenty healthy male volun- teers were randomized to receive a single dose of tested felodipine sustained-release tablet or the reference tablet by a two-way crossover design. Plasma concentration of felodipine was determined by HPLC-MS/MS and the bioequivalenee between two for- mulations were evaluated by DAS2.0 program. Results The pharmaeokinetie parameters of the tested and the reference felo- dipine tablet were expressed as follows： C was （2. 15±0.63） ng · mL-1 and （2.29±0.63） ng · mL -1 ,t was （6.33±1.57） h and （6.68±1.32） h, t1/2 was （18.22±2.75） h and （19.04±2.27） h, AUC0.48 were （58.11±5.15） ng · mL-1 · h and （61.13±6.31 ） ng · mL -1 . h. The relative bioavailability F was （95.06 ±8.42 ） %. Condusion The two felodipine sustained-release tablets are bioequivalent.
出处
《医药导报》
CAS
北大核心
2013年第3期306-309,共4页
Herald of Medicine
