帕潘立酮长效注射混悬液的制备

摘要

Objective To prepare the paliperidone long-acting suspension for injection and study the quality of it.Methods The optimum formula was measured by using orthogonal design method regarding the content of paliperidone, Na-CMC,mannitol and the ground time as variable factors. Orthogonal design table L9 ( 34 ) was used in the experiment. The paliperidone long-acting suspension for injection was prepared by grinding the dispersion,and its quality was evaluated. Results The optimum prescription was as follows: using paliperidone 40 g, Na-CMC 15 g, mannitol 60 g, purified water 1 000 mL, appropriate amount of NaH2 PO4 and NaOH, and grinding for 1 h. Paliperidone long-acting suspension for injection was characterized by an average pH of 7. 0,and ratio of average sedimentation volume of 90. 3%. The suspension released smoothly within 1 h in vitro and achieved sustained release. The suspension was stable in a freeze-dried powder. Conclusion The preparation for paliperidone long-acting suspension for injection is simple and stable,which may be a novel drug delivery system.%目的：以帕潘立酮为主药,制备帕潘立酮长效注射混悬液,并对其质量控制进行研究。方法采用正交实验进行处方优化筛选,以药物含量、羧甲基纤维素钠含量、甘露醇含量及研磨时间为可变因素,选用L9(34)正交设计表进行实验,以研磨法制备帕潘立酮长效注射混悬液,对其进行质量评价。结果帕潘立酮长效注射混悬液的最佳处方为：帕潘立酮40 g,羧甲基纤维素钠15 g,甘露醇60 g,纯化水1000 mL及适量的磷酸二氢钠和氢氧化钠,最佳研磨时间为1 h。帕潘立酮长效注射混悬液的平均pH为7.0,平均沉降体积比为90.3%,体外1 h内可以平稳释放,达到缓释。将其制备成冻干粉后,其稳定性良好。结论帕潘立酮长效注射混悬液的制备方法简单,稳定性好,有望成为帕潘立酮的新型给药系统。