甲壳胺对硝苯地平片剂药代动力学和生物利用度的影响  

The effects of chitin on the pharmacokinetics and the bioavailability of nifedipine tablet

作　　者：徐亚杰[1] 卜跃华[1] 王东凯[2] 

机构地区：[1]中国医科大学第一临床学院药剂科,沈阳110001 [2]沈阳药科大学药学系,1110015

出　　处：《中国药学杂志》1999年第12期827-829,共3页Chinese Pharmaceutical Journal

摘　　要：目的：测定甲壳胺对硝苯地平片剂药代动力学和生物利用度的影响。方法：采用气相色谱法研究了１０ 名男性健康志愿者随机单剂量口服市售片和以甲壳胺为辅料的硝苯地平片剂后，药物在体内的经时过程并计算药代动力学参数。结果：以甲壳胺为辅料的片剂和市售片的ｔ１／２ｋａ分别为０－４１ ｈ 和０－７７ ｈ，ｔ１／２ｋｅ分别为２－６４ ｈ 和２－６３ ｈ ，ｔｍａｘ 分别为１－５９ ｈ 和２－０３ ｈ ，ｃｍａｘ分别为１０４－６１ μｇ·Ｌ－ １ 和５７－３６ μｇ·Ｌ－ １ ，ＡＵＣ分别为５８６－１８ μｇ·ｈ·Ｌ－１ 和３４２－２７ μｇ·ｈ·Ｌ－１ ，其相对生物利用度为１５１－８ ％ 。结论：甲壳胺可显著提高硝苯地平的生物利用度，明显改善药物的吸收。OBJECTIVE: To determine the effects of chitin on the pharmacokinetics and the bioavailability of nifedipine tablet METHOD: By a random cross over arrangement, ten healthy volunteers received a single dose of either nifedipine tablet with chitin in it or nifedipine tablet bought from a drug store after an overnight fast The nifedipine in human plasma was detected by gas chromatography and the pharmacokinetic parameters were calculated RESULTS: t 1/2ka were 0 41 h and 0 77 h, respectively t 1/2ke were 2 64 h and 2 63 h, respectively The peak plasma levels with t max were 104 61 μg·L -1 at 1 59 h and 57 36 μg·L -1 at 2 03 h,respectively The area under the plasma concentration time curves were 586 18 μg·h·L -1 and 342 27 μg·h·L -1 , respectively The relative bioavailability was 151 8% CONCLUSION: The results showed that chitin could significantly raise the nifedipine bioavailability and improve the absorption of nifedipine in gastrointestinal tract

关 键 词：甲壳胺 硝苯地平 生物利用度 药代致力学 

分 类 号：R972[医药卫生—药品]