摘要
目的：评价国产和进口５－单硝酸异山梨醇酯缓释胶囊在人体生物等效性研究。方法： １８名健康受试者随机交叉给药，分别单次（４０ｍｇ）及多次口服进行人体生物等效性研究，用液相色谱／质谱联用测定血浆中５－单硝酸异山梨醇酯的浓度。结果：经数据处理，单次口服国产和进口５－单硝酸异山梨醇酯缓释胶囊的：ＡＵＣ０－３６分别为７４９０±１１４４μｇ·ｈ·Ｌ和７３５５±１００７μｇ·ｈ·Ｌ－１，ｔｐｅａｋ分别为４．９２±１．３１ｈ和４．６７±０．７９ｈ，Ｃｍａｘ分别为５１９．１５±６０．５３μｇ·Ｌ－１和５２３．６７±６８．９９μｇ·Ｌ－１；多次口服达稳态时：ＡＵＣ０－３６分别为８５１４±１３１８μｇ·ｈ·Ｌ－１和８５８６±８３６μｇ·ｂ·Ｌ－１，ｔｐｅａｋ分别为 ４．８３ ± ０．９４ｈ和 ４，７５ ±１．１４ｈ， Ｃｍａｘ分别为 ５７０．４４ ± ７８．８９μｇ·Ｌ－１和 ５８０．４３±６４．０４μｇ·Ｌ－１，波动系数ＦＩ分别为１３５．１０±１５．５３％和１３４．８２±９．７１％。国产５－单硝酸异山梨醇酯缓释胶囊单次给药及多次给药稳态时的相对生物利用度分别为 １０１．９±７．３％和 ９９．１±１１．９％。
OBJECTIVE:The bioequivalence of isosorbide-5-mononitrate sustained release capsule was studied in 18 healthy male volunteers. METHODS:A single oral dose and multiple oral doses of domestics or imported isosorbide-5-mononitrate sustained release capsule were given according to a randomized 2-way cross-over design. Multiple dose regimens used 40mg once day interval for 6 days. Plasma isosorbide-5-mononitrate conceniration was deteralned by HPLCIM S. RES UL TS: The pharmacokinetics parametrs obtained from the single-orel dose study were as follow: AUC0-36 were 7490 1144ug.h/L and 7355 1007ug.h/L, tpeak were 4.92 1 l.3lh and 4.67 f 0.79h, Cmax were 519.15 1 60.53ug/L and 523.67 f 68.99ug·L-1;The steady-state pharmacokinetics parameters were: AUCO-,,were 8514 1318ug·h·L-1; and 8586 1 836Pg·h·L-1, tpeak were 4.83 1 0.94h and 4.75 1 l.14h, Cmax were 570.44 1 78.89ug·L-1 and 80.43 1 64.04ug·L-1,FI were 135.10 1 15.53% and 134.82 1 9.71%, respectively. CONCLUSION: The result of stactical analysis showed that there were no significant difference the AUC0-36、 Cmax、 tpeak, between the two formations and the two preparartions were bioequivalent. A single oral dose and the steady-state relative bioavaiability of the domestics were 101.9 1 7.3% and 99.1 1 1l.9%.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2001年第3期215-218,共4页
The Chinese Journal of Clinical Pharmacology
