Dry Grinding of Mefenamic Acid Particles for Enhancement of its Water Dissolution Rate
Dry Grinding of Mefenamic Acid Particles for Enhancement of its Water Dissolution Rate
复制标题
甲芬那酸颗粒干磨提高其水溶解度
DOI：
10.1002/ppsc.200601091
复制
发表时间：
2007
影响因子：
2.7
通讯作者：
S. Watano
中科院分区：
文献类型：
--
作者：
T. Iwasaki;Maiko Takahara;R. Sonoda;S. Watano
本文详细研究了干法研磨提高甲芬那酸(MA)的水溶出速率。通过比表面积、粉末X-射线衍射图、差示扫描量热法、红外光谱等测试手段分析了微粉的物化性质，研究了物化性质(特别是晶体结构)的变化对溶出度的影响。研磨过程中未发生晶型I(原始)向晶型II的多态转变和MA分子结构的变化。然而，随着磨削的进行，MA颗粒的比表面积增加，结晶度降低(即非晶化程度增加)。在研磨系统中达到研磨极限后，相对不对称的MA分子的羧基之间形成的氢键逐渐断裂，有效地提高了初始溶解速度。
This paper details an investigation into the enhancement of the water dissolution rate of mefenamic acid (MA) by means of a dry grinding treatment. The physico‐chemical properties of the ground MA particles were analyzed by measurements of specific surface area, powder X‐ray diffraction patterns, differential scanning calorimetry thermograms and infrared spectra, and the effects of the change in the physico‐chemical properties (especially, crystalline structure) on the dissolution rate were studied. The polymorphic transition from Form I (original) to II and the change of the molecular structure of MA did not occur in the grinding treatments. However, the specific surface area of the MA particles increased, and the crystallinity decreased (i.e., the amorphization level increased) as the grinding progressed. Hydrogen bonds formed between the carboxyl groups of the opposed asymmetric MA molecules were broken gradually after the grinding limit was attained in the grinding system, resulting in an effective improvement of the initial dissolution rate.