摘要
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 a new intravenous tetrandrine emulsion and evaluate its properties. METHODS First, the formulation and preparation method of intravenous tetrandrine emulsion were optimized by orthogonal-design. Then the quality and sta- bility were investigated. Furthermore, the pharmacokinetics and tissue distribution as well as the irritation to auricular veins were stud- ied in rabbits. RESULTS The optimized formulation of intravenous tetrandrine emulsion was composed of 100 mg ~ mLi MCT, 50 mg mL LCT,30 mg mL-1 phospholipid, 5 mg mL i oleic acid and water phase. The pH value was adjusted to 7 -7.5. The e- mulsion was homogenized 2 -4 times at 105 kPa, then sterilized for 15 min at 121 C. This intravenous emulsion was stable at low tem- peratures. The pharmacokinetics and tissue distribution of intravenous tetrandrine emulsion were similar with those of tetrandrine injec- tion. However, the emulsion had slighter irritation. CONCLUSION The formulation and preparation method of intravenous tetran- drine emulsion optimized in the current study are reliable. The emulsion can decrease the irritation of tetrandrine.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2011年第22期1734-1739,共6页
Chinese Pharmaceutical Journal
关键词
汉防己甲素
注射乳
高压均质
tetrandrine
intravenous emulsion
high pressure homogenizer
