左旋氨氯地平片在健康人体的药物动力学及生物等效性

Pharmacokinetics and bioequivalence of Levamlodipine Besylate tablets in healthy volunteers

目的评价苯磺酸左旋氨氯地平片(分散片)在健康人体内的药物动力学与生物等效性。方法18名健康志愿者随机交叉单剂量口服左旋氨氯地平后,取血,采用LC-MS-MS法测定血浆中药物浓度。结果单次口服左旋氨氯地平片(参比、受试)和左旋氨氯地平分散片(受试)5 mg后的Cmax分别为(2.106±0.433)、(2.062±0.447)和(2.148±0.419)ng.mL-1;tmax分别为(5.2±1.1)、(5.1±0.7)和(4.9±0.8)h;AUC0→120分别为(72.962±18.884)、(70.986±16.237)和(68.955±19.200)ng.h.mL-1。受试制剂相对于参比制剂的生物利用度F分别为(98.7%±11.7%)和(95.2%±12.3%)。结论受试制剂苯磺酸左旋氨氯地平片(片及分散片)与参比制剂苯磺酸左旋氨氯地平片(施慧达)具有生物等效性。

Objective To evaluate the bioequivalence of Levamlodipine Besylate tablets. Methods According to the cross over design , each volunteer was given a single oral dose of levamlodipine besylate tablets and then the plasma was obtained and determined by LC-MS-MS method. Results The main pharmacokinetic parameters of single dose of the three products were as follows ： Cmax was （2.106±0.433）, （2.062±0.447） and （2.148±0.419） ng·mL^-1, tmax was （5.2±1.1）, （5.1±0.7） and （4. 9±0.8） h, AUC0→120 was （72. 962±18. 884）, （70. 986±16. 237） and （68. 955±19. 200） ng h · mL^-1 for reference and test respectively. The relative bioavailability was （98. 7%±11.7%） and （95.2 %± 12.3 %）, respectively. Conclusion The levamlodipine besylate tablets were bioequivalent.