头孢氨苄缓释片和普通胶囊的多剂量生物利用度和药物动力学比较  

Comparisons of multiple-dosage bioavailability and pharmacokinetics of cefalexin between sustain-released tablet and conventional capsule

作　　者：李珍[1] 戴兴凌[1] 沈意翔[1] 李萍[1] 刘皋林[1] 胡晋红[1] 

机构地区：[1]上海长海医院临床药理研究室

出　　处：《新药与临床》1997年第4期194-196,共3页

摘　　要：目的：比较头孢氨苄（ＣＥＸ）缓释片和普通胶囊的多剂量生物利用度和药物动力学。方法：１０例健康志愿者随机交叉口服ＣＥＸ缓释片５００ｍｇ，ｑ１２ｈ，ＣＥＸ普通胶囊２５０ｍｇ，ｑ６ｈ，服药３ｄ达稳态后进行波动试验和稳态药物动力学研究，ＨＰＬＣ法测定血药浓度。结果：ＣＥＸ缓释片Ｃｓｍａｘ，Ｃｓｍｉｎ和波动系数（ＦＩ）分别为１０．７±１．９μｇ／ｍＬ，０．６９±０．１４μｇ／ｍＬ和１．７５±０．０６；Ｔｍａｘ，Ｃｍａｘ，ＡＵＣ分别为３．１±０．７ｈ，９．９±１．２μｇ／ｍＬ，５０±１１ｈ·μｇ／ｍＬ。缓释片Ｔｍａｘ较普通胶囊明显延长（Ｐ＜０．０１），Ｃｍａｘ和ＡＵＣ与普通胶囊相比无显著性差异（Ｐ＞０．０５）。结论：ＣＥＸ缓释片达峰时间延长，维持有效血药浓度的时间较长。AIM: To compare the multiple dosage bioavailability and pharmacokinetics of cefalexin (CEX) between sustain-released tablet and conventional capsule. METHODS: Ten healthy volunteers were administered with CEX sustain-released tablet 500 mg bid and conventional capsule 250 mg qid in a random cross-over study. Plasma concentration was detected by HPLC method. RESULTS: C ss max , C ss main and FI were 10.7±1.9 μg/mL, 0.69±0.14 μg/mL and 1.75±0.06; T max , C max and AUC were 3.1±0.7 h, 9.9±1.2 μg/mL and 50±11 h·μg/mL respectively for sustain-released tablet. There was a difference in T max (P<0.01), but no significant differences (P>0.05) in C ss max , C ss min , FI, C max and AUC between the two preparations during steady state. CONCLUSION: CEX sustain-released tablet has longer T max , higher maintained plasma levels and longer effective concentration duration than those of conventional capsule.

关 键 词：头孢氨苄 迟效制剂 生物学效用 药物动力学 

分 类 号：R978.1[医药卫生—药品]