Maghsoodi M, Hassan-Zadeh D, Barzegar-Jalali M, Nokhodchi A, Martin Gary
Drug Applied Research Center and School of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
Drug Dev Ind Pharm. 2007 Nov;33(11):1216-24. doi: 10.1080/03639040701377730.
Naproxen was crystallized from acetone-water in the presence of different concentrations of hydroxypropylcellulose (HPC). Naproxen particles recrystallized in the presence of HPC exhibited an obvious improvement in their packing, flow, and mechanical properties compared to naproxen recrystallized in the absence of the polymer (control particles). The results showed that the particle size distributions of the treated samples were broader than those obtained when HPC was absent. The agglomerates produced in the presence of 0.25% HPC displayed superior flow characteristics (displaying both a low angle of repose and Carr index) in comparison to samples produced in the presence of other concentrations of HPC. This was attributed to the spherical shape and smooth surface, since the area of contact in the powder bed for spherical agglomerates was smaller than that for other crystal shapes. However it was found that the tensile strength of tablets with the particles isolated in the presence of 1% HPC was increased to a greater extent than tablets produced using the spherical particles. Generally, the tensile strengths of the tablets increased with increasing concentrations of HPC present in the crystallization medium. Differential scanning calorimetry (DSC) and X-ray powder diffraction studies showed that naproxen particles, crystallized in the presence of HPC did not undergo structural modifications.
萘普生在不同浓度羟丙基纤维素(HPC)存在下从丙酮 - 水体系中结晶。与在无聚合物情况下重结晶的萘普生(对照颗粒)相比,在HPC存在下重结晶的萘普生颗粒在堆积、流动性和机械性能方面有明显改善。结果表明,处理后样品的粒度分布比无HPC时更宽。与在其他浓度HPC存在下制备的样品相比,在0.25% HPC存在下产生的团聚体表现出优异的流动特性(具有低休止角和卡尔指数)。这归因于其球形形状和光滑表面,因为球形团聚体在粉末床中的接触面积小于其他晶体形状。然而,发现用在1% HPC存在下分离出的颗粒压制的片剂的抗张强度比使用球形颗粒制备的片剂有更大程度的提高。一般来说,片剂的抗张强度随着结晶介质中HPC浓度的增加而增加。差示扫描量热法(DSC)和X射线粉末衍射研究表明,在HPC存在下结晶的萘普生颗粒未发生结构改性。