盐酸氨溴索口腔崩解片人体生物等效性研究

目的:研究盐酸氨溴索口腔崩解片在健康人体内的生物等效性。方法:18名健康受试者单剂量随机交叉口服盐酸氨溴索口腔崩解片或普通片60mg,采用高效液相色谱法测定血药浓度,以3p97程序计算药动学参数与相对生物利用度。结果:口腔崩解片与普通片在体内血药浓度均呈一室模型,tmax分别为(2·39±0·61)、(2·19±0·92)h,Cmax分别为(91·26±49·81)、(90·17±42·96)ng·mL-1,AUC0～25分别为(515·14±289·84)、(566·20±293·98)ng·h·mL-1,AUC0～∞分别为(591·57±285·22)、(673·58±301·18)ng·h·mL-1。经方差分析和双单侧t检验,口腔崩解片与普通片药动学参数无显著性差异(P>0·05),盐酸氨溴索口腔崩解片的相对生物利用度为(90·98±10·88)%。结论:盐酸氨溴索口腔崩解片与普通片具有生物等效性。

Bioequiavailability of Ambroxol Hydrochloride Orally Disintegrating Tablets in Healthy Subjects

OBJECTIVE:To study the bioequiavailability of ambroxol hydrochloride orally disintegrating tablets in healthy volunteers.METHODS:A total of 20 volunteers were assigned to receive oral single does of 60mg of orally disintegrating tablets or common tablets of ambroxol hydrochloride by randomized crossover way and the plasma concentrations of ambroxol were determined by HPLC.The pharmacokinetic parameters were calculated with 3p97 pharmacokinetic program and the bioequiavailability was evaluated.RESULTS:The concentration curves of both the orally disintegrating tablets and the common tablets of ambroxol could be described as one-compartment model.The main pharmacokinetic parameters of orally disintegrating tablets and the common tablets of ambroxol hydrochloride were the following:tmax:(2.39± 0.61) h vs.(2.19± 0.92) h;Cmax:(91.26± 49.81) ng· mL-1 vs.(90.17± 42.96) ng· mL-1;AUC0～ 25:(515.14± 289.84) ng· h· mL-1 vs.(566.20± 293.98) ng· h· mL-1;AUC0～ ∞:(591.57± 285.22) ng· h· mL-1 vs.(673.58± 301.18) ng· h· mL-1,showing no significant difference between the two preparations in variance analysis and t-test(P>0.05).The relative bioavailability of the orally disintegrating tablet was(90.98± 10.88) %.CONCLUSION:The orally disintegrating tablets and the common tablets of ambroxol hydrochloride are bioequivalent.