目的 使用热熔挤出工艺,采用泊洛沙姆407作为凝胶基质连续化生产洛索洛芬钠凝胶。方法 使用粉末x射线衍射、流变学表征、质构分析和体外渗透试验等方法,将热熔挤出法与冷溶法制得的凝胶进行比较。结果 2种方法制备的洛索洛芬钠凝胶在黏弹性、黏度、硬度、黏附性等方面,在统计学上无显著性差异,药物均以分子形式分散于凝胶基质中。体外渗透试验过程中,热熔挤出凝胶与冷溶法凝胶的最大稳态渗透速率分别为(14.12±0.55)和(13.17±2.26)μg·cm-2·h-1,两者在统计学上无显著性差异。结论 用热熔挤出工艺可以快速,连续化地生产凝胶制剂,展示了该工艺在半固体制剂连续制造中的新应用。
Abstract
OBJECTIVE To prepare loxoprofen sodium gels by hot melt extrusion process with poloxamer 407 as the gel matrix. METHODS The gels prepared by hot melt extrusion were compared with those by cold dissolution using powder x-ray diffraction, rheological characterization, textural analysis and in vitro permeation test. RESULTS There were non-significant differences in viscoelasticity, viscosity, hardness, and adhesion between the loxoprofen sodium gels prepared by the two methods, and the drugs were dispersed in the gel matrix in the form of molecules. During the in vitro permeation test, the maximum steady-state penetration rates of hot melt extrusion gel and cold dissolution gel were(14.12±0.55)and(13.17±2.26)μg·cm-2·h-1 respectively, and there was non-significant difference between them. CONCLUSION The hot melt extrusion method can be used to produce gel formulations in a rapid, continuous manufacturingprocess, demonstrating a new application in the continuous manufacturing of semisolid formulations.
关键词
热熔挤出 /
凝胶 /
洛索洛芬钠 /
泊洛沙姆
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Key words
hot melt extrusion /
gel /
loxoprofen sodium /
poloxamer
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中图分类号：
R944
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参考文献
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