中国组织工程研究 ›› 2011, Vol. 15 ›› Issue (16): 3005-3008.doi: 10.3969/j.issn.1673-8225.2011.16.037

• 生物材料学术探讨 biomaterial academic discussion • 上一篇    下一篇

局部麻醉缓释药物的制备及镇痛作用

房立峰   

  1. 唐山市中医医院麻醉科,河北省唐山市  063000
  • 收稿日期:2011-01-31 修回日期:2011-02-21 出版日期:2011-04-16 发布日期:2011-04-16
  • 作者简介:房立峰,男,1975年生,河北省唐山市人,汉族,1999年天津医科大学毕业,主要从事分娩镇痛方法与药物的选择等研究。 mo840928@163.com

Preparation and analgesic effect of sustained-release local anesthetic drugs

Fang Li-feng   

  1. Department of Anesthesiology, Tangshan Hospital of Traditional Chinese Medicine, Tangshan  063000, Hebei Province, China
  • Received:2011-01-31 Revised:2011-02-21 Online:2011-04-16 Published:2011-04-16
  • About author:Fang Li-feng, Department of Anesthesiology, Tangshan Hospital of Traditional Chinese Medicine, Tangshan 063000, Hebei Province, China

摘要:

背景:临床常用的局部麻醉药物体内生物半衰期短,且局部组织的高浓度极易造成药物经血管吸收入血产生中枢神经和心血管毒性。因此,国内外学者开始进行局部麻醉缓释给药系统研究。
目的:总结近年局部麻醉缓释药物的制备及镇痛效果的研究现状。
方法:由作者应用计算机检索维普数据库中与局部麻醉缓释药物的制备及镇痛作用有关的文章,检索时限1998-01/ 2009-10。检索关键词:局麻药,微球,乳酸羟基乙酸共聚物,药物体外释放,镇痛。选择33篇文献进行分析。
结果与结论:采用W1/O/W2双重乳化-溶剂挥发法、乳化溶剂挥发法、乳化-交联法、高压电场法制备的局麻药载体的微球,形态均圆整,流动性好,80%以上的微球粒径在50~100 μm之间,可提高载药量和包封率。在对微球的体外释放性能进行考察时均得到了可延长药物的体外释放时间、相对较平稳的血药浓度、明显的缓释作用和良好安全性的结果。

关键词: 局麻药, 微球, 乳酸羟基乙酸共聚物, 药物体外释放, 镇痛

Abstract:

BACKGROUND: In vivo half-life period of local anesthetic drugs used in clinic is short, and a high dose in local tissue can easily lead to central nervous system and cardiovascular toxicity. Therefore, scholars have begun to study sustained-release local anesthetic delivery system.
OBJECTIVE: To conclude the progress in preparation and analgesic effect of sustained-release local anesthetic drugs.
METHODS: A computer-based search of VIP databases was performed for articles published from January 1998 to October 2009, addressing the preparation and analgesic effect of sustained-release local anesthetic drugs, by using “local anesthetic drugs, microsphere, lactic acid glycolic acid, in vitro drug release, analgesic”. Totally 33 articles were selected.
RESULTS AND CONCLUSION: The microspheres, which were prepared by using W1/O/W2 double emulsion-solvent evaporation method, emulsion-solvent evaporation method, emulsion-crosslinking method, and high voltage electric field method. The microspheres were spherical shape with good mobility, and 80% of them are 50-100 μm in diameter, which can increase the drug loading and encapsulation efficiency. It was observed that the in vitro release time was prolonged, and a relatively stable plasma concentration was obtained. A better sustained action and safety was found.

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