摘要
目的制备适合临床用药浓度和稳定性的双氯芬酸钠(DS)注射液。方法采用羟丙基-β-环糊精对DS进行包合,通过相溶解度图确定包合比例,并对抗氧剂种类以及灭菌条件进行筛选。结果当羟丙基-β-环糊精浓度>0.067 7 mol·L 1时,可以实现对DS的完全包合;以硫代甘油作为抗氧剂,注射液性质稳定;终端灭菌不宜采用热压灭菌法。结论羟丙基-β-环糊精可以增加DS在水中的溶解度,使其达到有效治疗浓度。制备得到的注射液性质稳定,满足临床用药要求。
OBJECTIVE To prepare diclofenac sodium injection with therapeutic concentration and high stability. METHODS Hydroxypropyl-β-cyclodextrin was used to form the inclusion complex with diclofenac sodium. The compounding rate was measured by phase solubility diagram. The optimal antioxidant and sterilization condition were selected. RESULTS The analysis showed the inclusion complex could be formed when the concentration of hydroxypropyl-β-cyclodextrin was more than 0.067 7 mol.L-1. Monothioglycerol was a suitable antioxidant to stabilize the injection. Filtration should be used for terminal sterilization. CONCLUSION Hydroxypropyl-β--cyclodextrin could increase the aqueous solubility of diclofenac sodium to reach the effective therapeutic concentration. The diclofenac sodium injection prepared was stable enough to satisfy the clinical requirement.
出处
《中国现代应用药学》
CAS
CSCD
2013年第10期1097-1101,共5页
Chinese Journal of Modern Applied Pharmacy
