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药学学报  2015 

奥扎格雷两种晶型在大鼠体内的药代动力学研究

, PP. 218-221

Keywords: 奥扎格雷,晶型,药代动力学,hplc

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Abstract:

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±19.13mg·l-1,auc0-t分别为61.14±14.76和85.56±18.08mg·l-1?h,t1/2分别为1.53±0.51和4.73±3.00h。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。

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