| 利巴韦林含片的人体药动学及生物等效性研究 |
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| 引用本文： | 罗晨辉,陈笑艳,孙玉明,于华玲,蒋云,仇宇,钟大放,周晓,刘亚利. 利巴韦林含片的人体药动学及生物等效性研究[J]. 金属学报, 2008, 13(2): 169-173 |
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| 作者姓名： | 罗晨辉 陈笑艳 孙玉明 于华玲 蒋云 仇宇 钟大放 周晓 刘亚利 |
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| 作者单位： | 1.湖南省肿瘤医院临床药理基地, 长沙 410013, 湖南;2.沈阳药科大学药物代谢与药物动力学实验室, 沈阳 110016, 辽宁 |
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| 摘 要： | 目的:建立人血浆中利巴韦林的HPLC-MS分析方法, 用以测定18 名健康男性受试者舌下含服不同厂家的利巴韦林含片后的血药浓度, 估算受试制剂和参比制剂的药动学参数, 评价两种制剂是否生物等效。方法:采用双周期随机交叉试验设计。分别给予18 名男性健康受试者试验制剂或参比制剂80 mg, 采集静脉血样, 血浆样品去蛋白后用HPLC/MS/MS 法检测药物浓度。计算药动学参数, 判定两制剂是否生物等效。结果:测定利巴韦林的线性范围为2 ~ 500 ng/mL (r2 为0.9944), 平均回收率>90 %, 日内RSD 和日间RSD 均<10 %。测得血浆中两种制剂的利巴韦林的主要药代动力学参数tmax 、Cmax 、t 1/2 、AUC0 -72 和AUC0→∞分别为:(1.1 ±0.5) 、(1.1 ±0.4) h, (249±89) 、(232 ±65) ng/mL, (34 ±11) 、(34 ±11) h,(2828 ±1215) 、(2685 ±1096) ng。h。mL-1, (3600 ±1568) 、(3416 ±1379) ng。h。mL-1 。以AUC0 -72 计算, 利巴韦林含片的相对生物利用度平均为(106±16) %。结论:本方法更简便、准确, 灵敏度得到很大提高。两种制剂的利巴韦林药代动力学参数无统计学差异, 具有生物等效性。
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| 关 键 词： | 利巴韦林 药动学 生物等效性 高效液相串联-色谱质谱联用色谱法 |
| 收稿时间： | 2007-11-17 |
| 修稿时间： | 2008-01-15 |
Bioequivalence and pharmacokinetics of ribavirin buccal tablets in healthy volunteers |
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| LUO Chen-hui,CHEN Xiao-yan,SUN Yu-ming,YU Hua-ling,JIANG Yun,QIU Yu,ZHONG Da-fang,ZHOU Xiao,LIU Ya-li. Bioequivalence and pharmacokinetics of ribavirin buccal tablets in healthy volunteers[J]. Acta Metallurgica Sinica, 2008, 13(2): 169-173 |
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| Authors: | LUO Chen-hui CHEN Xiao-yan SUN Yu-ming YU Hua-ling JIANG Yun QIU Yu ZHONG Da-fang ZHOU Xiao LIU Ya-li |
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| Affiliation: | 1.Department of Clinical Pharmacology, Tumor Hospital of Hunan Province, Changsha 410013, Hunan, China;2.Laboratory of Drug Metabolism and Pharmacokinetics, Shenyang Pharmaceutical University, Shenyang 110015, Liaoning,China |
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| Abstract: | AIM:To determine ribavirin in human plasma by an LC/MS/MS method and to study the bioequivalence and pharmacokinetics of reference and test ribavirin formulations.METHODS:A double-phased stochastical crossover study design was conducted.18 healthy volunteers were given a single dose of 80 mg ribavirin of reference and test formulations.The drug was extracted from collected plasma and analyzed by LC/MS/MS.The pharmacokinetic parameters as well as relative bioavailability were measured.RESULTS:The calibration curve was linearwithin the range of 2 - 500 ng/mL (r2 =0.9944).The average recovery was more than 90 %.The average RSD within 3 days and between 3 days were all less than 10 %.The major pharmacokinetic parameters tmax 、Cmax 、t 1/2 、AUC0 -72 and AUC0~∞ of reference and test ribavirin formulations were (1.1 ±0.5) and (1.1 ±0.4) h, (249 ±89) and (232 ±65) ng/mL, (34 ±11) and (34 ±11) h, (2828 ±1215) and (2685 ±1096) ng。h。mL -1, (3600 ±1568) and (3416 ±1379) ng。h。mL -1.The relative bioavailability of test buccal tablet was(106 ±16) %. CONCLUSION:The method is more simple, more accurate and much more sensitive.There is no significant difference between the main pharmacokinetic parmeters of two formulations of ribavirin (P >0.05), they are bioequivalent. |
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| Keywords: | ribavirin pharmacokinetics bioequiavailability LC-MS/MS |
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