醋酸阿托西班注射液的处方工艺开发

Prescription technology development of atosiban acetate injection

目的改进醋酸阿托西班注射液处方并优化生产工艺,以增加醋酸阿托西班注射液的稳定性。方法以市售处方工艺为基础,在其中分别加入不同种类的抗氧剂,得到醋酸阿托西班注射液样品,将注射液样品分别置于以下条件下:温度(40±2)℃、相对湿度(75±5)%和温度(25±2)℃、相对湿度(60±5)%,进行加速试验,分别在0、1、2、3、6个月取样检验,通过测量外观色泽、pH值、溶液澄清度、有关物质、含量等指标和局部安全性考察,从而优选出稳定性较市售产品更好、使用安全的醋酸阿托西班注射液。结果经加速试验考察6个月,抗氧剂为0.1 g/100 ml亚硫酸氢钠时,制备的醋酸阿托西班注射液与已上市的醋酸阿托西班注射液比较,外观色泽、酸度、溶液澄清度指标相当,有关物质与含量明显优于已上市产品,可于室温下保存,稳定性明显增加。通过局部安全性试验表明此注射剂无刺激性、致敏性和溶解性。结论该注射剂处方合理,制备工艺可行,产品安全,稳定性高。

Objective To improve the prescription and to optimize the production process of acetate atosiban injection to increase the stability of acetate atosiban injection. Methods On the basis of the commercially available prescription process,in which the join different kinds of antioxidants,get the acetate atosiban injection samples,the injection samples respectively set under the following conditions：temperature （40±2）℃,relative humidity （75±5）%,temperature （25±2）℃and relative humidity （60±5）%,to carried out the acceleration test.Sampling to inspection at 0,1,2,3 and 6 months,opti-mized the stability of a commercially available products better,the use of safe acetate atosiban injection throuth mea-sured the color appearance,pH value,solution clarity,related substances and content index and local safety inspection. Results After 6 months of acceleration test,it was suggested that the injection sample with 0.1 g/100 ml sodium bisul-fate was comparable to the commercially available one in color,pH value and solution clarity and better than the com-mercially available one in related substances and content.By local safety test,it was demonstrated that the injection without excitant,sensitization and solubility. Conclusion The prescription of this injection is reasonable,the production process is feasible and the injection is safe for use and with high stability.