【摘要】：研究奧扎格雷兩種晶型固體灌胃后,在SD大鼠胃腸道的吸收過程,評價(jià)其優(yōu)勢藥物晶型,探討該藥物晶型狀態(tài)對臨床用藥的影響。SD大鼠灌胃給予不同晶型奧扎格雷固體原料藥,采用高效液相色譜法測定血漿中奧扎格雷的濃度,計(jì)算其在大鼠體內(nèi)的藥代動力學(xué)參數(shù)并比對不同晶型之間的差異。大鼠經(jīng)口給予固體奧扎格雷晶型Ⅰ和晶型Ⅱ后,血液中奧扎格雷Cmax分別為32.72±17.04和34.01±19.13 mg·L-1,AUC0-t分別為61.14±14.76和85.56±18.08 mg·L-1·h,t1/2分別為1.53±0.51和4.73±3.00 h。大鼠口服不同晶型奧扎格雷后,晶II型血藥濃度-時間曲線下面積大于晶I型,半衰期較長,為優(yōu)勢晶型,提示在該藥物的生產(chǎn)中需要注意晶型的控制。
[Abstract]:The absorption process of ozagrel in gastrointestinal tract of SD rats was studied after oral administration of two crystal forms of ozagrel, and the dominant drug crystal patterns were evaluated. To investigate the effect of the crystalline state of the drug on clinical drug use, SD rats were given different crystal forms of ozagrel solid raw material, and the concentration of ozagrel in plasma was determined by high performance liquid chromatography (HPLC). The pharmacokinetic parameters in rats were calculated and the differences among different crystal types were compared. After oral administration of solid Ozagrel crystal type 鈪，

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