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目的通过测定兔血小板聚集和血栓素B2(TXB2)、6-酮-前列腺素F_(Ⅰα)(6-keto-PGF_(Ⅰα))的含量,比较观察阿魏酸(F)、吲哚美辛(I)、阿魏酸-吲哚美辛结合物(FI)和阿魏酸-吲哚美辛-淀粉高分子载体衍生物(FIS)在抗血栓方面的药理作用特点。方法用比浊法和放免法测定F、I、FI和FIS在体外对兔血小板聚集和对TXB2,6-keto-PGF_(1α)生成的影响。结果F、I、FI和FIS显著地抑制ADP和AA诱导的兔血小板聚集和TXB_2,6-keto-PGF_(Ⅰα)的产生。在 12.5-240μmol/L的剂量范围内,对血小板聚集的抑制率, F为 11.3%-31.8%(ADP诱导)和 3.3%-18.5%(AA诱导)、I为3%-34.3%(ADP诱导)和2%-20.2%(AA诱导)、FI为5.0%-59.3%(ADP诱导)和0.3%-63.1%(AA诱导)、FIS为3.1%-39.1%(ADP诱导)和1.5%-39.6%(AA诱导)。剂量为 240.0μmol/L时对TXB_2和6-keto-PGF_(Ⅰα)产生的抑制率, F为 14.8%和 1.2%、Ⅰ为 24.9%和 26.2%、 FI为 40.6%和29.3%?
OBJECTIVE: To investigate the effect of ferulic acid (F), indomethacin (TXB2) and 6-keto-PGF_ (Iα) (I), pharmacological effects of ferulic acid-indomethacin conjugates (FI) and ferulic acid-indomethacin-starch polymer carrier derivatives (FIS) Methods The turbidimetric and radioimmunoassay methods were used to determine the effect of F, I, FI and FIS on platelet aggregation and TXB2, 6-keto-PGF_ (1α) production in vitro. Results F, I, FI and FIS significantly inhibited ADP and AA-induced rabbit platelet aggregation and the production of TXB_2, 6-keto-PGF_ (Ⅰα). The inhibition of platelet aggregation was 11.3% -31.8% (ADP induction) and 3.3% -18.5% (AA induction) in the dose range of 12.5-240 μmol / L, I was 3% -34.3% (ADP induction) and 2% -20.2% (AA induction), FI was 5.0% -59.3% (ADP induction) and 0.3% -63.1 % (AA induction), FIS 3.1% -39.1% (ADP induction) and 1.5% -39.6% (AA induction). The inhibitory rates of TXB_2 and 6-keto-PGF_ (Ⅰα) at doses of 240.0μmol / L were 14.8% and 1.2% for F, 24.9% and 26.2% for I, and FI was 40.6% and 29.3%?