CAJ | 학술논문

本文考察了双嘧达莫凝胶骨架缓释片(MT)和漂浮渗透泵(FOP)两种制剂比格人体内药物动力学,并作了体内外相关性分析.以双嘧达莫市售普通片为参比制剂设计了三交叉动物体内实验,以高效液相色谱法检测血药浓度.以体内吸收分数与体外累计释放量作比较米评价体内外相关性.结果表明两种缓控释制剂均表现出体内缓释效果,其中FOP缓释效果更好;FOP生物利用度高于MT;体内外相关系FOP优丁MT.分析认为双嘧达莫在消化道上端吸收,由此可以认为双嘧达莫制成漂浮制剂有利于口服药物传递对于FOP来说现用体外释放方法已可反应体内情况,而对于MT体外溶出方法需进一步改进.
본문고찰료쌍밀체막응효골가완석편(MT)화표부삼투빙(FOP)량충제제비격인체내약물동역학,병작료체내외상관성분석.이쌍밀체막시수보통편위삼비제제설계료삼교차동물체내실험,이고효액상색보법검측혈약농도.이체내흡수분수여체외루계석방량작비교미평개체내외상관성.결과표명량충완공석제제균표현출체내완석효과,기중FOP완석효과경호;FOP생물이용도고우MT;체내외상관계FOP우정MT.분석인위쌍밀체막재소화도상단흡수,유차가이인위쌍밀체막제성표부제제유리우구복약물전체대우FOP래설현용체외석방방법이가반응체내정황,이대우MT체외용출방법수진일보개진.
A novel floating osmotic pump controlled release system (FOP) and traditional matrix sustained release tablets (MT) of dipyridamole (DIP) were characterized in terms of pharmacokinetics,drug release,and in vitro-in vivo correlation.In vivo study was performed by a three-crossover study in six beagle dogs relative to the conventional tablet (CT).A HPLC method for the determination of DIP in the plasma was developed.Cumulative percent of absorption fraction was compared to that of in vitro cumulative release.Both FOP and MT displayed obvious extended release characteristic in vivo while FOP showed a better extended release behavior.The bioavailability of FOP was higher than that of MT and a zero-order release linear correlation of DIP between fraction absorbed in vivo and fraction dissolved in vitro was established for FOP while not for MT.The results indicated the existence of an absorption window in upper part of the GI track of DIP,which meant that floating system could be excellent for the drug delivery.In addition,the in vitro model was a good choice for depicting in vivo absorption and for optimization of the formulation of FOP if it is needed to be bio-equivalent to MT.