复方罗红霉素片在健康志愿者体内的药动学

Pharmacokinetics of Complex Roxithromycin Tablets in Healthy Volunteers

目的研究复方罗红霉素片在健康志愿者体内的药动学。方法 48名健康成年志愿者,男女各半,采用随机分组三制剂平行设计,分别单剂量口服复方罗红霉素片、300 mg罗红霉素片、60 mg盐酸氨溴索片、300 mg罗红霉素片合用60 mg盐酸氨溴索片后,用串联质谱法(LC-MS/MS)分别测定血浆中罗红霉素或氨溴索的浓度,采用DAS2.1程序分别计算各受试者的有关药动学参数,并用SPSS11.5对其单因素方差分析。结果复方罗红霉素片组与两单药合用组相比,罗红霉素和氨溴索的人体药动学参数无明显差异(P>0.05)。复方罗红霉素片与对照药罗红霉素片组相比,罗红霉素的人体药动学参数AUC、CLz/F、Vz/F、mρax经统计有显著差异(P<0.05),而其他参数无明显差异;复方罗红霉素片组与盐酸氨溴索片组相比,氨溴索的人体药动学参数AUC、MRT0-t、CLz/F、Vz/F经统计有显著差异(P<0.05),而其他参数无明显差异。结论复方罗红霉素片与两药合用的对照药相比,罗红霉素及氨溴索药动学参数均无明显差异,而与单药相比,罗红霉素及氨溴索的药动学参数有明显差异。

OBJECTIVE To study the pharmacokinetics of complex roxithromycin tablets in healthy volunteers.METHODS 48 Healthy volunteers were administrated randomly and parallelly with complex roxithromycin tablets（I）,300 mg roxithromycin tablets（Ⅱ）,60 mg ambroxol hydrochloride tablets（III） and combined roxithromycin tablets and ambroxol hydrochloride tablets（Ⅳ）,respectively.The concentrations of roxithromycin or ambroxol in plasma were determined by LC-MS/MS.The pharmacokinetic parameters were calculated with DAS2.1 and evaluated by one-factor analysis of variance.RESULTS Compared with group Ⅳ,the pharmacokinetic parameters of roxithromycin and ambroxol in group Ⅰ showed no significant difference.However,compared with group Ⅱ,the pharmacokinetic parameters of roxithromycin of group Ⅰ including AUC,CLz/F,Vz/F and ρmax,displayed significant difference.Compared with group Ⅲ,the pharmacokinetic parameters of ambroxol of group Ⅰ including AUC,MRT0-t,CLz/F and Vz/F revealed significant difference.CONCLUSION The pharmacokinetic parameters of roxithromycin and ambroxol had no significant difference between groupⅠ and group Ⅳ,while their pharmacokinetic parameters had significant difference between group Ⅰ and group Ⅱ/ group Ⅲ.