Philip Anil K, Pathak Kamla
Department of Pharmaceutics, Rajiv Academy for Pharmacy, Mathura, 286001, Uttar Pradesh, India.
AAPS PharmSciTech. 2006 Jul 7;7(3):56. doi: 10.1208/pt070356.
A nondisintegrating, controlled release, asymmetric membrane capsular system of flurbiprofen was developed and evaluated for controlled release of the drug to overcome some of its side effects. Asymmetric membrane capsules were prepared using fabricated glass mold pins by phase inversion process. The effect of different formulation variables was studied based on 2(3) factorial design; namely, level of osmogen, membrane thickness, and level of pore former. Effects of polymer diffusibility and varying osmotic pressure on drug release were also studied. Membrane characterization by scanning electron microscopy showed an outer dense region with less pores and an inner porous region for the prepared asymmetric membrane. Differential scanning calorimetry studies showed no incompatibility between the drug and the excipients used in the study. In vitro release studies for all the prepared formulations were done (n = 6). Statistical test (Dunnett multiple comparison test) was applied for in vitro drug release at P > .05. The best formulation closely corresponded to the extra design checkpoint formulation by a similarity (f2) value of 92.94. The drug release was independent of pH but dependent on the osmotic pressure of the dissolution medium. The release kinetics followed the Higuchi model and the mechanism of release was Fickian diffusion.
开发并评估了一种用于氟比洛芬控释的非崩解型、控释、不对称膜胶囊系统,以克服其一些副作用。采用预制玻璃模具销通过相转化法制备不对称膜胶囊。基于2(3)析因设计研究了不同处方变量的影响,即渗透剂水平、膜厚度和成孔剂水平。还研究了聚合物扩散性和不同渗透压对药物释放的影响。扫描电子显微镜对膜的表征显示,制备的不对称膜有一个孔较少的外部致密区域和一个内部多孔区域。差示扫描量热法研究表明,药物与研究中使用的辅料之间不存在不相容性。对所有制备的制剂进行了体外释放研究(n = 6)。对体外药物释放应用统计学检验(Dunnett多重比较检验),P > 0.05。最佳制剂与额外设计检查点制剂的相似性(f2)值为92.94,非常接近。药物释放与pH无关,但取决于溶出介质的渗透压。释放动力学遵循Higuchi模型,释放机制为菲克扩散。