复方罗红霉素片在健康志愿者体内的药动学

任秀华 申玲玲 向道春 刘宇 陈倩 张冬林 方淑贤 刘东 杜光

中国药学杂志 ›› 2011, Vol. 46 ›› Issue (7) : 537-541.

PDF(946 KB)
PDF(946 KB)
中国药学杂志 ›› 2011, Vol. 46 ›› Issue (7) : 537-541.
论著

复方罗红霉素片在健康志愿者体内的药动学

  • 任秀华,申玲玲,向道春,刘宇,陈倩,张冬林,方淑贤,刘东,杜光*
作者信息 +

Pharmacokinetics of Complex Roxithromycin Tablets in Healthy Volunteers

  • REN Xiu-hua, SHEN Ling-ling, XIANG Dao-chun, LIU Yu, CHEN Qian, ZHANG Dong-lin, FANG Shu-xian, LIU Dong, DU Guang*
Author information +
文章历史 +

摘要

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/Fρmax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-tCLz/FVz/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。

Abstract

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-tCLz/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.

关键词

复方罗红霉素片 / 罗红霉素 / 氨溴索 / 高效液相色谱/质谱 / 药动学

Key words

complex roxithromycin tablets / roxithromycin / ambroxol / HPLC-MS/MS / pharmacokinetics

引用本文

导出引用
任秀华 申玲玲 向道春 刘宇 陈倩 张冬林 方淑贤 刘东 杜光. 复方罗红霉素片在健康志愿者体内的药动学[J]. 中国药学杂志, 2011, 46(7): 537-541
REN Xiu-hu;SHEN Ling-ling;XING Do-chun;LIU Yu;CHEN Qin;ZHNG Dong-lin;FNG Shu-xin;LIU Dong;DU Gung. Pharmacokinetics of Complex Roxithromycin Tablets in Healthy Volunteers[J]. Chinese Pharmaceutical Journal, 2011, 46(7): 537-541

参考文献


[1] QIN Y H, ZHAO H W, DING Z R, et al. Studies on pharmacokinetics and bioavailbilty of roxithromycin capsule in 18 healthy volunteers[J]. J Math Med(数理医药学杂志, 2003, 16 (2: 149-150.
[2] FENG W Y,XU D H, LIU T L. Bioequivalence of roxithromycin in human plasma determined by HPLC-MS[J]. J Chin Med Univ(中国医科大学学报, 2007, 36(4: 429-431.
[3] CHEN L, GAO S, LI J J, et al. HPLC-MS Determination of ambroxol hydrochloride and its pharmacokinetics and bioequivalence in human plasma[J]. Acta Acad Med Jiangxi(江西医学院学报, 2006, 46(6:43-46.
  [4] STETINOVA V, SMETANOVA L, KHOLOVA D, et al. Transepithelial transport of ambroxol hydrochloride across human intestinal Caco-2 cell monolayers[J]. Gener Physiol Biophys, 2009, 28(3:309-315.
[5] LI X Q, ZHONG D F, HUANG H H, et al. Detmethylation metabolism of roxithromycin in humanand rats[J]. Acta Pharmacol Sin(中国药理学报, 2001, 22(5:469-474.
[6] GUSTAVO H B M, MICHAEL B T, JUSTIN D B, et al. Identification and characterization of ambroxol as an enzyme enhancement agent for Gaucher Disease[J]. J Biol Chem, 2009, 284(35: 23502-23516.
[7] ISHIGURO N, SENDA C, KISHIMOTO W, et al. Identification of CYP3A4 as the predominant isoform responsible for the metabolism of ambroxol in human liver microsomes[J]. Xenobiotica, 2000, 30(1:71-80.
[8] YAMAZAKI H, SHIMADA T. Comparative studies of in vitro inhibition of cytochrome P450 3A4-dependent testosterone 6-hydroxylation by roxithromycin and its metabolites,troleandomycin, and erythromycin[J]. Drug Metab Dispos,1998, 26(11:1053-1057.
[9] HANG T J, ZHANG M, SONG M, et al. Simultaneous determination and pharmacokinetic study of roxithromycin and ambroxol hydrochloride in human plasma by LC-MS/MS[J]. Clin Chim Acta, 2007, 382(1-2: 20-24.
PDF(946 KB)

Accesses

Citation

Detail

段落导航
相关文章

/