第 51 卷第 4 期 Vol. 51 No. 4 2021 年 8 月 Aug 2021

所属栏目：医药及中间体 注射用尼可地尔的冻干工艺研究

刘 玺，邢建峰* （西安交通大学 药学院，陕西 西安 710061）

摘　要：研究了注射用尼可地尔的处方及冻干生产工艺。采用单因素实验方法，以冻干粉针剂的性状、pH、含量及有关物质等为考察指标，对处方中赋形剂的类型、用量、pH范围及冻干工艺参数进行筛选及优化。获得了优化处方及冻干工艺：制备规格为12 mg的注射用尼可地尔，甘露醇作为赋形剂，加入量为18 mg，pH范围为6.5~7.5，选择2次退火，退火温度为-15 ℃，退火保持时间为2 h，制备的冻干粉针剂成型性好、易复溶。该制剂处方工艺设计合理，工艺路线可行，为注射用尼可地尔的处方及工艺筛选提供借鉴。

关键词：注射用尼可地尔；处方；工艺研究；冻干；稳定性

中图分类号：O657　　文献标识码：A　　文章编号：1009-9212（2021）04-0013-04

Freeze-drying Technology for the Preparation of Injection-nicorandil

LIU Xi, XING Jian-feng* (School of Pharmacy, Xi'an Jiaotong University, Xi'an 710061, China)

Abstract：The formulation and freeze-drying process of nicorandil used for injection were studied. Single factor experiment was used to optimize the excipient type, dosage, pH range and parameters for freeze-drying process. The optimal formulation and freeze-drying process were as followings: in 12 mg of nicorandil for injection, 18 mg of mannitol was used with a pH range between 6.5 and 7.5; a second annealing method was selected with a temperature of -15 ℃ and an annealing holding time of 2 h. The freeze-dried powder for injection has good formability and is easy to redissolve. The formulation process of the preparation is reasonable and feasible. This study provides a basis for the prescription and process screening of nicorandil for injection．

Key words：nicorandil for injection; prescription; formulation and preparation technique; freeze-drying; stability

基金项目：国家自然科学基金项目（81973253，81773663）。

作者简介：刘 玺（1984—），女，陕西西安人，工程师，主要从事制剂研发及药物分析工作（E-mail：404465438@qq.com）。

联 系 人：邢建峰，博士，教授，研究方向：新型药物递送系统研究研究与应用。

收稿日期：2021-07-13