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以半合成脂肪酸酯和大豆磷酯为基质,研制了双氯灭痛中空栓剂。与实心栓剂相比较结果表明,中空栓剂溶出适度大于实心栓剂;含大豆磷酯的栓剂对直肠粘膜刺激性小;各种栓剂药物动力学参数表明血药浓度—时间曲线下面积均相似;含大豆磷酯栓剂的半衰期(T_(1/2))小于不含大豆磷酯的栓剂;中空栓剂的峰时小于实心栓剂,而峰浓度却大于实心栓剂。本药物在家兔体内显示为二室模型。
With semi-synthetic fatty acid ester and soybean phospholipid as the matrix, developed a hollow clopidogrel suppository. Compared with the solid suppository, the results showed that the hollow suppository dissolves moderately more than the solid suppository; the suppository containing soybean phospholipid is less irritating to the rectal mucosa; the pharmacokinetic parameters of various suppositories indicate that the areas under the blood concentration-time curve are similar; The half-life (T 1/2) of phospholipid suppository was smaller than that without soybean phospholipid. The time of hollow suppository was smaller than that of solid suppository, but the peak concentration was larger than that of solid suppository. The drug appears in rabbits as a two-compartment model.