洛芬葡锌那敏分散片与复方锌布颗粒在健康人体的生物等效性

Bioequivalence of lofenpuxinnamin dispersible tablets and cmpound zinc gluconate and ibuprofen granules in healthy volunteers

目的建立液相色谱-质谱联用法,比较洛芬葡锌那敏分散片和复方锌布颗粒(抗组胺药)的生物等效性。方法用随机开放双周期自身交叉单剂量给药试验设计,清洗期为2周。20名健康受试者分别单次空腹口服洛芬葡锌那敏分散片(受试制剂)和复方锌布颗粒(参比制剂)(均相当于马来酸氯苯那敏4mg)。以引达帕胺为内标,用ESI正离子选择性反应监测(SRM)模式测定马来酸氯苯那敏血药浓度,计算药代动力学参数及评价生物等效性。结果以2种药物中的氯苯那敏为计,洛芬葡锌那敏分散片(受试制剂)和复方锌布颗粒(参比制剂)的Cmax分别为(12.27±3.04),(13.47±3.52)ng·mL-1;tmax分别为(2.43±1.49),(2.10±1.07)h;AUC0-t分别为(303.17±91.39),(315.58±76.78)ng·h·mL-1;AUC0-∞分别为(355.19±120.30),(365.71±100.48)ng·h·mL-1;t1/2分别为(24.86±5.83),(24.71±5.96)h。受试制剂相对参比制剂的生物利用度F为(99.80±41.20)%。结论洛芬葡锌那敏分散片(受试制剂)和复方锌布颗粒(参比制剂)中马来酸氯苯那敏生物等效。

Objective To establish a liquid chromatographymass spectrometry（ LC- MS/MS） method for evaluating the bioequivalenee of luofenpuxinnamin dispersible tabletsand compound zinc gluconate and ibuprofen granules in healthy volunteers. Methods According to a random opening, two - period crossover design （cleaning phase is two weeks）. Twenty healthy volunteers take a single same oral dose of luofenpuxinnamin dispersible tablets （test）and compound zinc gluconate and ibuprofen granules （reference） （ equal to 4 mg chlorpheniramine maleate）. Using indapamide as internal standard, the content of chlorpheniramine maleate was determined by SRM model. The pharmacokinetic parameters was calculate by soft were. Results The main pharmacokinetic parameters of luofenpuxinnamin dispersible tablets （test） and ibuprofen granules （reference） of were as follows： Cmax were （ 12. 27 ± 3.04） and （13.47 ±3.52）ng . mL-1; tmax were （2.43 ±1.49） and （2.10± 1.07） h; AUC0-t were （303.17 ±91.39） and （315.58 ± 76.78） ng . h . mL-1; AUC0-∞ were （355.19±120.30） and （365.71 ±100.48） ng. h . mL-1; t1/2 were （24.86 ±5.83） and （24.71 ± 5.96） h, resperitively. The relative bioavailability of test was （99. 80 ±41.20） %. Conclusion The chlorpheniramine maleate of test and reference was bioequivalence.