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中国临床药理学与治疗学 ›› 2006, Vol. 11 ›› Issue (1): 66-69.

• 研究原著 • 上一篇    下一篇

塞克硝唑阴道泡腾片人体药代动力学研究

王少华, 赵艳, 刘振胜, 李志平, 王霞1 , 赵美玲, 齐方梅   

  1. 青岛市市立医院药物临床试验机构, 1妇产科, 青岛 266011, 山东
  • 收稿日期:2005-11-23 修回日期:2005-12-07 出版日期:2006-01-06 发布日期:2020-10-23
  • 通讯作者: 王少华, 通讯作者, 女, 教授, 主要从事新药临床研究工作。 Tel:0532-82789191 E-mail:wsh pharm @yahoo.com .cn E-mail:wsh pharm @yahoo.com .cn
  • 作者简介:王少华, 通讯作者, 女, 教授, 主要从事新药临床研究工作。 Tel:0532-82789191 E-mail:wsh pharm @yahoo.com .cn 赵艳, 女, 药师, 主要从事新药临床研究工作。 Tel:0532-82789192 E-mail:shuang-1976@sohu.com

Study of pharmacokinetics of secnidazole vagina effervescent tablets in healthy volunteers

WANG Shao-hua, ZHAO Yan, LIU Zhen-sheng, LI Zhi-ping, WANG Xia1 , ZHAO Mei-ling, QI Fang-mei   

  1. Base for Drug Clinical Trial, 1Department of Gynaecology and Obstetrics, Qingdao Municipal Hospital, Qingdao 266011, Shandong, China
  • Received:2005-11-23 Revised:2005-12-07 Online:2006-01-06 Published:2020-10-23

摘要: 目的 :研究塞克硝唑阴道泡腾片人体内的药 代动力学特征 。方法 :单次给药分别应用 250 、500 、 750 mg, 多次给药应用 500 mg, 连用 7 d, 采用 HPLC 测定血浆中塞克硝唑的浓度。用 DAS 软件计算其 药代动力学参数。结果:健康已婚女性受试者单次 使用塞克硝唑阴道泡腾片 250 、500 、750 mg 后的 T1 /2β 分别为 18 .84 、15 .25 、21 .86 h, 与文献报道基本一 致;Tmax 分别为 12 .22 、14 .00 、18 .00 h, Cmax 分别为 3 .58 、 5 .42 、8 .00 mg·L -1 , AUC 分 别 为 103 .52 、 190 .99 、296 .92 mg·h -1·L-1 , 与口服制剂相比, 吸收 较慢, 峰浓度较低, 吸收量较少, 提示本药全身作用 较小, 不良反应也较少, 局部残留较多有利于发挥治 疗作用 。多次使用塞克硝唑 500 mg 后的 T1 2β = 22 .74 h 、Cmax =14 .30 mg·L -1 、Tmax =1 1 .60 h 、AUC = 520 .14 mg·h-1·L -1 , Cmax和 AUC 与单次给药相比明 显增大, 说明该药因半衰期较长, 长期用药有一定的 蓄积, 多次连续用药应引起注意。结论 :本试验提供 了塞克硝唑阴道泡腾片体内血药浓度的 HPLC 测定 方法及药动学参数, 为其临床应用和合理用药提供 了参考和依据。

关键词: 塞克硝唑;泡腾片;药代动力学 ;血药浓度 , 高效液相色谱法

Abstract: AIM:To study the pharmacokinetics of secnidazole vagina effervescent tablets in healthy volun- teers.METHODS :250, 500 and 750 mg secnidazole vagina effervescent tablets were used in single-dose groups;500 mg secnidazole vagina effervescent tablets were used for 7 days in multi-dose group .The concentra- tions of secnidazole in plasma were determined by HPLC . The parameters of pharmacokinetics were calculated by DAS software .RESULTS AND CONCLUSION:The pharmacokinetic parameters after administration of a single dose of secnidazole vagina effervescent tablets( 250, 500, 750 mg) in health married female volunteers were as fol- lows :T1/ 2β were 18 .84, 15 .25, and 21 .86 h, in accor- dance with the literatures ;Tmax were 12 .22, 14 .00, and 18 .00 h ;Cmax were 3 .58, 5 .42, and 8 .00 mg·L -1 ; AUC were 103 .52, 190 .99, and 296 .92 mg·h-1·L -1 , respectively.The absorption of secnidazole vagina effer- vescent tablets was slower and lower than oral tablets . The systemic actions and adverse reactions were fewer and rudimental concentrations were higher so as to show more local actions .The pharmacokinetic parameters after ad- ministration of multi doses of secnidazole vagina efferves- cent tablets ( 500 mg ) were as follows :T1/2β =22 .74 h, Cmax =14 .30 mg·L-1 , Tmax =11 .60 h, and AUC = 520 .14 mg·h-1·L -1 .Cmax and AUC were higher than the results of a single dose.These showed that the drug can cumulate after a long-time administration because of its long half-life and required more caution .

Key words: secnidazole , effervescent tablets , phar- macokinetics, plasma concentration , high performance liquid chromatography (HPLC)

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