中国药物警戒 ›› 2022, Vol. 19 ›› Issue (11): 1170-1173.
DOI: 10.19803/j.1672-8629.20220390

• 生物模型方法在药品安全研究中的应用专栏 • 上一篇    下一篇

注射用帕瑞昔布钠肌肉刺激性考察

赵映淑1, 刘春1,*, 黎良程1, 王晨2#   

  1. 1海南省药品检验所安全性评价研究中心,海南 海口 570216;
    2中国食品药品检定研究院,北京 102629
  • 收稿日期:2022-07-08 发布日期:2022-11-17
  • 通讯作者: *刘春,女,硕士,副主任药师,药检药理与药物非临床安全性评价研究。E-mail: 61582604@qq.com; #为共同通信作者。
  • 作者简介:赵映淑,女,硕士,主管药师,药检药理与药物非临床安全性评价研究。
  • 基金资助:
    国家重点研发计划（SQ2022YFC3400054）; 海南省自然科学基金面上项目（819MS105）

Evaluation of muscular irritation of parecoxib sodium injection

ZHAO Yingshu1, LIU Chun1,*, LI Liangcheng1, WANG Chen2#   

  1. 1Center for Drug safety Evaluation of Hainan Institute for Drug Control, Haikou Hainan 570216, China;
    2National Institutes for Food and Drug Control, Beijing 102629, China
  • Received:2022-07-08 Published:2022-11-17

PDF (PC)

67

摘要： 目的 考察注射用帕瑞昔布钠经家兔肌内给药的刺激性,为临床安全用药提供参考。方法 采用家兔同体左右侧自身比对法,经股四头肌注射给药,浓度分别为20和5 mg·mL-1。通过一般状况、给药局部肉眼观察、解剖观察及组织病理学检查,综合判断其肌肉刺激性。结果 注射用帕瑞昔布钠显示出浓度-肌肉刺激性依赖关系,20 mg·mL-1引起中度刺激且不可逆,5 mg·mL-1引起轻度刺激且可逆。结论 注射用帕瑞昔布钠临床使用浓度具有肌肉刺激性风险,在本试验条件下,5 mg·mL-1为肌内注射安全浓度。

关键词: 帕瑞昔布钠, 注射剂, 家兔, 肌肉刺激性

Abstract: Objective To evaluate the muscular irritation of Parecoxib Sodium injection in rabbits, and to provide a guideline for clinical safety. Methods The sample was injected intramuscularly in quadriceps of the rabbits, and reactions in the intra-individual left and right self-comparison method were compared in the same rabbit. The high and low concentrations of sample were 20 and 5 mg·mL-1 (in a volume of 0.5 mL) respectively. The general status, local visual observation of drug administration, anatomical observation and histopathological examination were used to synthesize the muscular irritation of the subject (or Parecoxib Sodium) in rabbits. Results The results showed a significant concentration-dependent irritation relationship after i.m. injection in rabbit quadriceps, namely 20 mg·mL-1 induced a moderate and irreversible irritation while 5 mg·mL-1 induced a minor and reversible irritation. Conclusion The common clinical concentration of Parecoxib Sodium for injection (20 mg·mL-1) has a high risk of muscle irritation, and under this test condition, 5 mg·mL-1 is the safe concentration for intramuscular injection.

Key words: parecoxib sodium, injection, rabbit, muscular irritation

中图分类号: