正交试验优化注射用重组人白细胞介素12处方

目的:优化注射用重组人白细胞介素12的处方。方法:采用正交试验设计,以甘露醇含量(A)、人血白蛋白含量(B)和pH值(C)为因素,活性、水分和外观的综合评分为指标优化处方,制备3批优化处方制剂并测定其活性、水分、pH值等。结果:优化处方为A4%、B0.5%、C7.4;3批制剂冻干后活性约为8400、8111、8511u.μg-1,水分<3%,pH值约为7.35～7.42,均符合质量标准要求(批间比较P>0.05)。结论:以优化处方制备的注射用重组人白细胞介素12活性较高,工艺重现性好。

Optimization of the Formulation of Recombinant Human Interleukin-12 for Injection by Orthogonal Test

OBJECTIVE： To optimize the formulation of recombinant human interleukin-12 for injection. METHODS： The for- mulation was optimized by orthogonal design with the content of manicol （A） and human serum albumin （B）, pH value （C） as factors and activity, moisture and appearance as index. The activity, moisture, pH value and other index of 3 batches of samples were measured as well. RESULTS： The optimal formulation was as follows： A of 4%, B of 0.5% and C of 7.4. The activities of 3 batches of samples after freeze drying were 8 400 u·μg^-1, 8111 u·μg^-1 and 8 511 u·μg^-1 respectively. The moisture was lower than 3%, and pH value was 7.35-7.42. The indexes were all up to the quality standard （comparison among batches, P〉0.05）. CONCLUSIONS： The recombinant human interleukin-12 for injection prepared by optimized formulation possessed high activity and is reproducible in preoaration technolozv.