秦至臻, 陈芊茜, 宋俊科, 吕扬, 杜冠华. 奥扎格雷两种晶型在大鼠体内的药代动力学研究J. 药学学报, 2015,50(2): 218-221.
引用本文: 秦至臻, 陈芊茜, 宋俊科, 吕扬, 杜冠华. 奥扎格雷两种晶型在大鼠体内的药代动力学研究J. 药学学报, 2015,50(2): 218-221.
QIN Zhi-zhen, CHEN Qian-xi, SONG Jun-ke, L� Yang, DU Guan-hua. Pharmacokinetic comparison of two ozagrel polymorph forms in SD ratsJ. Acta Pharmaceutica Sinica, 2015,50(2): 218-221.
Citation: QIN Zhi-zhen, CHEN Qian-xi, SONG Jun-ke, L� Yang, DU Guan-hua. Pharmacokinetic comparison of two ozagrel polymorph forms in SD ratsJ. Acta Pharmaceutica Sinica, 2015,50(2): 218-221.

奥扎格雷两种晶型在大鼠体内的药代动力学研究

Pharmacokinetic comparison of two ozagrel polymorph forms in SD rats

  • 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: To enhance the quality and efficiency of ozagrel by investigating the differences between the ozagrel polymorphs in bioavailability. Solid ozagrel in different polymorph forms were orally administered to SD rats. An HPLC method was established to determinate plasma level of ozagrel. The bioavailabilities of two polymorph forms were calculated and compared. The pharmacokinetic parameters of ozagrel, were as follows: Cmax was 32.72±17.04 and 34.01±19.13 mg·L-1, respectively; AUC0-t was 61.14±14.76 and 85.56±18.08 mg·L-1•h, respectively; t1/2 was 1.53±0.51 and 4.73±3.00 h, respectively. There was no significant difference in pharmacokinetic parameters between form Ⅰ and Ⅱ polymorphs of ozagrel while the t1/2 of form Ⅱ is longer, which indicates that the use of form Ⅱ polymorph as pharmaceutical product may prolong the effective action time in clinics. This would help the polymorph quality control in drug production.

     

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