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目的制备汉防己甲素注射乳剂,并对其进行评价。方法通过正交设计优选汉防己甲素乳剂的最佳处方,并对制备工艺进行优化。对样品进行质量、稳定性研究,并考察了汉防己甲素注射乳剂在大鼠体内的药动学和组织分布及对家兔耳缘静脉的刺激性。结果汉防己甲素注射乳的最佳处方及工艺为:中链甘油三酸酯-大豆油(100 mg.mL-1∶50 mg.mL-1),磷脂30 mg.mL-1,油酸5 mg.mL-1,pH值7～7.5,用105 kPa高压均质2～4次,121℃热压灭菌15 min。本品在低温条件保存较为稳定。与注射液相比,汉防己甲素注射乳显著减小了药物刺激性,两者在大鼠体内药动学参数未出现显著性差异。结论本研究制备获得的汉防己甲素注射乳工艺稳定,质量可控,并能减小汉防己甲素的刺激性。
Objective To prepare tetrandrine injection and evaluate its performance. Methods The optimal formulation of tetrandrine emulsion was optimized by orthogonal design and the preparation process was optimized. The quality and stability of the samples were studied. The pharmacokinetics and tissue distribution of tetrandrine injection in rats and the irritation of rabbit ear veins were also investigated. Results The best formulation and process of tetrandrine injection were: medium-chain triglyceride-soybean oil (100 mg.mL-1:50 mg.mL-1), phospholipid 30 mg.mL-1, oleic acid 5 mg.mL-1, pH 7 ~ 7.5, homogenized with high pressure 105 kPa 2 ~ 4 times, 121 ℃ autoclaved 15 min. This product is relatively stable at low temperature. Compared with the injection, injection of tetrandrine injection significantly reduced drug irritation, both in rats pharmacokinetic parameters were not significantly different. Conclusion The preparation of tetrandrine injection milk obtained in this study is stable, of controlled quality and can reduce the irritation of tetrandrine.