羧甲司坦泡腾片的人体相对生物利用度研究  

Relative Bioavailability of Carbocisteine Effervescent Tablet in Healthy Volunteers

作　　者：戴敏[1] 钟秋[1] 孙华[1] 陈波[1] 曾照宏[1] 冒国光[1] 

机构地区：[1]皖南医学院弋矶山医院临床药理研究所,芜湖241001

出　　处：《中国临床药理学杂志》2001年第2期136-138,共3页The Chinese Journal of Clinical Pharmacology

摘　　要：目的：比较羧甲司坦泡腾片和普通片在健康人体内的药代动力学过程，并对两制剂的生物等效性做出评价。方法：１８名健康受试者随机交叉单剂量口服羧甲司坦泡腾片和羧甲司坦普通片剂１０００ｍｇ后，采用柱前衍生化高效液相色谱荧光检测法测定血浆中羧甲司坦浓度，进行药代动力学和生物利用度研究。结果：试验结果表明，羧甲司坦泡腾片和普通片剂的血药浓度时间曲线符合血管外给药一室模型，主要药代动力学参数ｔｍａｘ分别为１．５０±０．３４ ｈ和１．９７±０．３２ ｈ，Ｃ分别为１１．９１±２．６３ｍｇ·Ｌ－１和１１．３０±２．１９ｍｇ·Ｌ－１，ｔ１／２Ｋｅ分别为１．１８±０．３０ｈ和１．２０±０．２６ ｈ， ＡＵＣ０－８分别为 ３６．７２ ± ７．５８ ｍｇ· ｈ· Ｌ－１和 ３７．４３ ± ７．１９ ｍｇ· ｈ· Ｌ－１。相对生物利用度为９８．０５±８．５１％，结论：结果显示两种制剂生物等效。OBJECTIVE: A single oral dose 1000mg carbocisteine of reference (effervescent tablet) or test(tablet) drugs was given to healthy male volunteers according to an open randomized crossover study. METHODS: The concentrations in plasma were determined by HPLC method. The pharmacokinetic and bioavailability of test capsule were compared with reference capsule. RESULTS: The plasma concentration-time curves of the two products were all fitted to onecompartment model. The main pharmacokinetic parameters of carbocisteine were : tmax1.50 ± 0.34 h and 1 .97 ± 0.32 h,Cmax11.91 ± 2.63 mg.L-1 and 11.30 ± 2. 19 mg·L-1, t1/2Ke1.18 ± 0.30 h and 1 .20 ± 0.26 h, AUC0-836.72 ± 7.58(mg·h·L-1) and 37.43 ± 7. 19(mg·h·L-1) for effervescent tablet and tablet respectively. The relative bioavailability of effervescent tablet to tablet was 98.05 ± 8.51%. CONCLUSION: The results of statistical analysis showed that two formulations were bioequivalent.

关 键 词：羧甲司坦 相对生物利用度 药代动力学 泡腾片 粘液调节剂 

分 类 号：R974.1[医药卫生—药品] R969.1[医药卫生—药学]