Gong Kenan, Rehman Ihtesham U, Darr Jawwad A
Clean Materials Technology Group, Department of Chemistry, University College London, Christopher Ingold Building, 20 Gordon Street, London WC1H 0AJ, UK.
J Pharm Biomed Anal. 2008 Dec 1;48(4):1112-9. doi: 10.1016/j.jpba.2008.08.031. Epub 2008 Sep 7.
Hydroxypropylmethyl cellulose (HPMC)-indomethacin (4:1, w/w) drug composites (DCs) were prepared via supercritical carbon dioxide (sc-CO(2)) assisted impregnation. The effect of processing temperature (at fixed pressures) on the physical and other properties of the resulting HPMC-indomethacin DCs was investigated using a range of analytical techniques, including differential scanning calorimetry (DSC), Fourier transform infrared (FTIR) spectroscopy, Raman spectroscopy, and powder X-ray diffraction (XRD) methods. The data suggest that for a 4:1 (w/w) HPMC-indomethacin ratio prepared at 130 degrees C (17.2 MPa), the indomethacin exists entirely in an amorphous dispersion within the polymer matrix. The primary interaction between HPMC and indomethacin appears to be hydrogen bonding between the carboxylic acid carbonyl group of indomethacin and hydroxyl group of HPMC. The initial (first 15 min) and overall drug release behavior within a 5h timeframe for the HPMC-indomethacin DCs, was analyzed. For the HPMC-indomethacin drug composite processed at 130 degrees C/17.2 MPa, drug release behavior obeyed a n-power law (n=0.54).
通过超临界二氧化碳（sc-CO₂）辅助浸渍法制备了羟丙基甲基纤维素（HPMC）-吲哚美辛（4:1，w/w）药物复合物（DCs）。使用一系列分析技术，包括差示扫描量热法（DSC）、傅里叶变换红外（FTIR）光谱法、拉曼光谱法和粉末X射线衍射（XRD）方法，研究了加工温度（在固定压力下）对所得HPMC-吲哚美辛DCs的物理性质和其他性质的影响。数据表明，对于在130℃（17.2MPa）下制备的4:1（w/w）HPMC-吲哚美辛比例，吲哚美辛完全以无定形分散体的形式存在于聚合物基质中。HPMC与吲哚美辛之间的主要相互作用似乎是吲哚美辛的羧酸羰基与HPMC的羟基之间的氢键。分析了HPMC-吲哚美辛DCs在5小时时间范围内的初始（前15分钟）和整体药物释放行为。对于在130℃/17.2MPa下加工的HPMC-吲哚美辛药物复合物，药物释放行为符合n次方定律（n = 0.54）。
