奥扎格雷两种晶型在大鼠体内的药代动力学研究

发布时间：2019-02-16 21:13

【摘要】：研究奥扎格雷两种晶型固体灌胃后,在SD大鼠胃肠道的吸收过程,评价其优势药物晶型,探讨该药物晶型状态对临床用药的影响。SD大鼠灌胃给予不同晶型奥扎格雷固体原料药,采用高效液相色谱法测定血浆中奥扎格雷的浓度,计算其在大鼠体内的药代动力学参数并比对不同晶型之间的差异。大鼠经口给予固体奥扎格雷晶型Ⅰ和晶型Ⅱ后,血液中奥扎格雷Cmax分别为32.72±17.04和34.01±19.13 mg·L-1,AUC0-t分别为61.14±14.76和85.56±18.08 mg·L-1·h,t1/2分别为1.53±0.51和4.73±3.00 h。大鼠口服不同晶型奥扎格雷后,晶II型血药浓度-时间曲线下面积大于晶I型,半衰期较长,为优势晶型,提示在该药物的生产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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