Pandey Suneel, Patil Arun T
Department of Pharmaceutical Sciences, Rashtrasant Tukadoji Maharaj Nagpur University, Nagpur-440 033, Maharashtra, India.
Curr Drug Deliv. 2014;11(2):179-90. doi: 10.2174/15672018113109990046.
In direct compression (DC), the significance of usual flow properties of powder from the hopper to the dies of the tablet machine cannot be overstressed. Ensuring the free flow of powder presents a number of challenges to the pharmaceutical formulator in case of high speed tabletting. This research work was conceived to obtain directly compressible agglomerates by spherical crystallization technique and were comparatively evaluated for physicochemical properties as well as tableting properties of agglomerates and unprocessed aceclofenac. Agglomerates of aceclofenac were developed via spherical crystallization method by a solvent arrangement containing dichloromethane (DCM) as a good solvent, water as a bad solvent and acetone as a bridging liquid. Hydroxypropyl cellulose (HPC) in variable quantity was implemented as hydrophilic polymer. The agglomerates were evaluated for yield, solubility, drug content, FTIR spectroscopy, porosity, particle size, micromeritic properties, differential scanning calorimetry (DSC), X-ray diffraction studies (XRD), scanning electron microscopy (SEM), and dissolution studies. The agglomerates expressed improved micromeritic and dissolution properties, in equivalence to pure drug. Formulation F3 (optimized agglomerates) exposed estimable rotundity, better drug release, and easily compression into tablets by high speed DC Technique. The tablets showed acceptable physicochemical properties and complied with the pharmacopoeial specifications. The dissolution rate of prepared tablets from agglomerates was better than the tablets of pure drug. The F3 agglomerates show splendid physicochemical and micromeritic properties. Agglomerated compression mix also showed good tableting properties as needed for high speed compression and enough stability under accelerated conditions at least for 1 month.
在直接压片（DC）中，从料斗到压片机模具的粉末通常流动特性的重要性再怎么强调也不为过。在高速压片的情况下，确保粉末的自由流动给药物配方设计师带来了许多挑战。本研究旨在通过球形结晶技术获得直接可压性团聚体，并对团聚体和未加工的醋氯芬酸的物理化学性质以及压片性质进行比较评估。醋氯芬酸团聚体通过球形结晶法，采用以二氯甲烷（DCM）作为良溶剂、水作为不良溶剂以及丙酮作为桥连液的溶剂体系来制备。使用不同量的羟丙基纤维素（HPC）作为亲水性聚合物。对团聚体的收率、溶解度、药物含量、傅里叶变换红外光谱（FTIR）、孔隙率、粒径、粉体学性质、差示扫描量热法（DSC）、X射线衍射研究（XRD）、扫描电子显微镜（SEM）以及溶出度研究进行了评估。团聚体表现出与纯药物相当的改善的粉体学和溶出性质。配方F3（优化的团聚体）表现出良好的圆整度、更好的药物释放，并且可以通过高速直接压片技术轻松压制成片。该片剂显示出可接受的物理化学性质，并符合药典规格。由团聚体制备的片剂的溶出速率优于纯药物片剂。F3团聚体表现出优异的物理化学和粉体学性质。团聚体压缩混合物在高速压缩所需的压片性质方面也表现良好，并且在加速条件下至少1个月具有足够的稳定性。
