盐酸氨溴索口腔崩解片在健康志愿者及生物等效性.docVIP

盐酸氨溴索口腔崩解片在健康志愿者的生物等效性 许艳华1，薛洪源1，杨汉煜2，贺文涛1，王宇奇1，贾丽霞1 （1.白求恩国际和平医院 临床药理室，河北 石家庄 050082；2. 石药集团中奇制药技术有限公司，河北 石家庄 050011） [摘要] 目的: 研究盐酸氨溴索口腔崩解片的人体生物利用度和生物等效性。方法:采用随机交叉试验设计，20名健康男性志愿者单剂量口服试验制剂盐酸氨溴索口腔崩解片与参比制剂盐酸氨溴索片60 mg，用液相色谱-串联质谱法测定血浆中氨溴索的浓度，计算两药的药动学参数。结果:单剂量口服试验与参比制剂后氨溴索的Cmax分别为（84.7±29.3）和（81.2±28.2）ng·mL-1，tmax分别为（1.7±0.5）h和（1.8±0.4）h，t1/2分别为（7.9±0.9）h和（8.3±1.0）h，AUC0-24h分别为（638.7±180.8）ng·h·mL-1和（591.4±148.3）ng·h·mL-1，试验制剂的相对生物利用度为（108.2±16.5）% [关键词] 盐酸氨溴索；口腔崩解片；相对生物利用度；生物等效性；药动学；液相色谱-串联质谱法 [中图分类号] [文献标识码] A [文章编号] 1001－5217 Bioequivalence of ambroxol hydrochloride orally disintegrating tablets in healthy volunteers XUE Hong-yuan1, YANG Han-yu2, HOU Yan-ning1, HE Wen-tao1, WANG Yu-qi1, JIA Li-xia1 (1. Dep. of Pharmacology, Bethune International Peace Hospital, Shijiazhuang 050082, China; 2. Shijiazhuang Pharmaceutical Group Co. Ltd. Zhongqi Corporation, Shijiazhuang 050011, China) Abstract: OBJECTIVE To study the bioequivalence and relative bioavailability of ambroxol hydrochloride orally disintegrating tablets. METHODS A single oral adminstration of 60 mg test and reference tablets were given to 20 healthy male volunteers according to a randomized crossover design. The concentrations of ambroxol in plasma were determined by a HPLC/MS/MS method. The pharmacokinetic parameters and bioavailability of test tablets were compared with those of reference tablets. RESULTS After a single oral adminstration of 60 mg test and reference tablets, the pharmacokinetic parameters were as follows: Cmax were (84.7?9.3) 8and (81.2?8.2) n g·mL-1, tmax were (1.7?.5) (and (1.8?(.4) h, t1/2 were (7.9?.9) e and (8.3?.0) ?h, AUC0-24h were (638.7?80.8) and (591.4?48.3) nphg·h·mL-1, The relative bioavailability of tested tablets was (108.2?6.5) v%. CONCLUSION The two preparations were bioequivalent. KEY WORDS: ambroxol hydrochloride; orally disintegrating tablet; relative bioavailability; bioequivalence; pharmacokinetics; HPLC/MS/MS 盐酸氨溴索（ambroxol hydrochloride）为溴己新的活性代谢产物