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将丙烯酸酯基质进行热处理作为控制药物释放的一种手段。

Thermal treating of acrylic matrices as a tool for controlling drug release.

作者信息

Hasanzadeh Davood, Ghaffari Solmaz, Monajjemzadeh Farnaz, Al-Hallak M H D-Kamal, Soltani Ghazal, Azarmi Shirzad

机构信息

Department of Pharmaceutics, Tabriz University of Medical Sciences, Iran.

出版信息

Chem Pharm Bull (Tokyo). 2009 Dec;57(12):1356-62. doi: 10.1248/cpb.57.1356.

Abstract

The purpose of the present study was to investigate the effect of thermal-treating on the release of ibuprofen from the granules prepared using aqueous dispersions of Eudragit. To accomplish this goal, different formulations were prepared using wet granulation method containing two different types of Eudragit aqueous dispersions, RS30D, RL30D and Avicel as filler. Tablets were prepared using direct compression method. The prepared tablets were thermally treated at 50 and 70 degrees C for 24 h. The drug release from tablets was assessed before and after thermal-treating. The results of release study showed that, thermally-treating the tablets at the temperatures higher than glass transition temperature (Tg) of the polymer can decrease the drug release from matrices. For mechanistic evaluation of the effect of thermal-treating, powder X-ray diffraction (XPD), scanning electron microscopy (SEM), differential scanning calorimeter (DSC), Fourier transform infrared (FT-IR) and helium pycnometer have been employed. The SEM graphs showed that the tablets have smoother surface with less porosity after thermal-treating. FT-IR spectra showed no change in the spectrum of thermally-treated tablet compared to control. In DSC graphs, no crystalline change was seen in the heat-treated samples of ibuprofen tablets, but decreased and widened peak size were related to the probable formation of solid solution of ibuprofen in Eudragit matrix. The results of helium pycnometer showed a significant decrease in the total porosity of some heat-treated samples. This study revealed the importance of thermal treating on the drug release from sustained release tablets containing Eudragit polymer.

摘要

本研究的目的是考察热处理对使用尤特奇水分散体制备的颗粒剂中布洛芬释放的影响。为实现这一目标,采用湿法制粒法制备了不同的制剂,其中包含两种不同类型的尤特奇水分散体RS30D、RL30D以及作为填充剂的微晶纤维素。采用直接压片法制备片剂。将制得的片剂在50℃和70℃下热处理24小时。在热处理前后对片剂的药物释放进行评估。释放研究结果表明,在高于聚合物玻璃化转变温度(Tg)的温度下对片剂进行热处理可降低药物从基质中的释放。为对热处理效果进行机理评估,采用了粉末X射线衍射(XPD)、扫描电子显微镜(SEM)、差示扫描量热仪(DSC)、傅里叶变换红外光谱(FT-IR)以及气体比重计。SEM图显示,热处理后片剂表面更光滑,孔隙率更低。FT-IR光谱显示,与对照相比,热处理片剂的光谱没有变化。在DSC图中,布洛芬片剂的热处理样品未观察到结晶变化,但峰尺寸减小和变宽与布洛芬在尤特奇基质中可能形成固溶体有关。气体比重计的结果显示,一些热处理样品的总孔隙率显著降低。本研究揭示了热处理对含尤特奇聚合物的缓释片剂药物释放的重要性。

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