| 双氯芬酸钠双释放肠溶胶囊的人体生物等效性 |
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| 引用本文： | 过林,裘福荣,王猛猛,贺敏,朱蕾蕾,元唯安,赵彤芳,叶宇婕,蒋健. 双氯芬酸钠双释放肠溶胶囊的人体生物等效性[J]. 中国医院药学杂志, 2015, 35(17): 1544-1547. DOI: 10.13286/j.cnki.chinhosppharmacyj.2015.17.04 |
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| 作者姓名： | 过林 裘福荣 王猛猛 贺敏 朱蕾蕾 元唯安 赵彤芳 叶宇婕 蒋健 |
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| 作者单位： | 上海中医药大学附属曙光医院临床药理科, 上海 201203 |
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| 基金项目： | 科技部"创新药物研究开发技术平台建设"(编号:2012ZX09303009-001);上海市中医临床重点实验室项目(编号:C10Dz2220200);高等学校博士学科点专项科研基金新教师类资助课题(编号:20123107120002) |
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| 摘 要： | 目的:研究双氯芬酸钠双释放肠溶胶囊在健康人体的药动学参数,评价其生物等效性。方法:采用随机交叉试验设计,40名健康男性受试者单剂量和多剂量口服双氯芬酸钠双释放肠溶胶囊受试与参比制剂,用高效液相色谱-串联质谱法(LC-MS/MS)测定血浆中双氯芬酸的血药浓度。结果:单剂量口服受试和参比制剂的主要药动学参数如下:Cmax分别为(708.9±306.8)、(704.7±383.3) ng·ml-1,t1/2分别为 (5.86±1.81),(6.20±1.73)h,tmax分别为(1.81±1.58),(1.81±1.58) h,AUC0-24分别为(2 500.0±577.3),(2 355.4±607.4) ng·h·ml-1;多剂量口服受试和参比制剂的主要药动学参数如下:Cssmax分别为 (594.4±228.4),(622.9±326.7) ng·ml-1,Cssmin分别为(30.1±14.9),(35.7±19.4) ng·ml-1,Cav分别为 (96.3±18.2),(92.8±19.9) ng·ml-1,t1/2分别为(6.32±1.40),(6.62±1.50) h,tmax分别为(1.67±1.24),(1.66±1.54)h,AUCss分别为(2 310.3±436.3)、(2 227.5±476.4) ng·h·ml-1,DF值分别为(623.7±325.4)%、(666.2±377.0)%。受试对参比制剂的单剂量和多剂量相对生物利用度F分别为为(108.4±21.3)%和(105.2±15.1)%。结论:LC-MS/MS法测定人血浆中双氯芬酸钠浓度快速、灵敏、专属性高,受试与参比制剂生物等效。
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| 关 键 词： | LC-MS/MS 双氯芬酸钠 药动学 生物等效性 |
| 收稿时间： | 2014-09-18 |
Bioequivalence of diclofenac sodium dual-release enteric-coated capsules in human |
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| GUO Lin,QIU Fu-rong,WANG Meng-meng,HE Min,ZHU Lei-lei,YUAN Wei-an,ZHAO Tong-fang,YE Yu-jie,JIANG Jian. Bioequivalence of diclofenac sodium dual-release enteric-coated capsules in human[J]. Chinese Journal of Hospital Pharmacy, 2015, 35(17): 1544-1547. DOI: 10.13286/j.cnki.chinhosppharmacyj.2015.17.04 |
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| Authors: | GUO Lin QIU Fu-rong WANG Meng-meng HE Min ZHU Lei-lei YUAN Wei-an ZHAO Tong-fang YE Yu-jie JIANG Jian |
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| Affiliation: | Department of Clinical Pharmacology, Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China |
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| Abstract: | OBJECTIVE To establish a method to investigate pharmacokinetics and bioequivalence of diclofenac sodium dual-release enteric-coated capsules.METHODS Forty healthy male volunteers were administrated with diclofenac sodium dual-release enteric-coated capsules by an open, randomized two period crossover approaches at single or multiple dosages. Plasma concentrations of didofenac were determined by LC-MS/MS method.RESULTS Main pharmacokinetic parameters of diclofenac after single dose of test drug and reference drug were as follows: Cmax(708.9±306.8), (704.7±383.3) ng·ml-1; t1/2 (5.86±1.81), (6.20±1.73) h; tmax (1.81±1.58), (1.81±1.58) h; AUC0-24(2 500.0±577.3), (2 355.4±607.4) ng·h·ml-1. Steady-state pharmacokinetic parameters were as follows: Cssmax (594.4±228.4), (622.9±326.7) ng·ml-1, Cssmin (30.1±14.9), (35.7±19.4) ng·ml-1, Cav (96.3±18.2), (92.8±19.9) ng·ml-1, t1/2 (6.32±1.40), (6.62±1.50) h, tmax (1.67±1.24), (1.66±1.54) h, AUCss (2 310.3±436.3), (2 227.5±476.4) ng·h·ml-1, DF (623.7±325.4)%, (666.2±377.0)%. Relative bioavailability in single and multiple dose tests were (108.4±21.3)% and (105.2±15.1)%, respectively.CONCLUSION LC-MS/MS method is rapid, specific and sensitive one for determination of diclofenac in human plasma. Statistical analysis indicates that two preparations are bioequivalent. |
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| Keywords: | LC-MS/MS diclofenac pharmacokinetics bioequivalence |
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