Modi Aftab, Tayade Pralhad
Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz (E), Mumbai-400 098, India.
AAPS PharmSciTech. 2006 Aug 18;7(3):68. doi: 10.1208/pt070368.
This article investigates enhancement of the dissolution profile of valdecoxib using solid dispersion with PVP. The article also describes the preparation of fast-dissolving tablets of valdecoxib by using a high amount of superdisintegrants. A phase solubility method was used to evaluate the effect of various water-soluble polymers on aqueous solubility of valdecoxib. Polyvinyl pyrrolidone (PVP K-30) was selected and solid dispersions were prepared by the method of kneading. Dissolution studies using the USP paddle method were performed for solid dispersions of valdecoxib. Infrared (IR) spectroscopy, differential scanning calorimetry (DSC), and x-ray diffractometry (XRD) were performed to identify the physicochemical interaction between drug and carrier, hence its effect on dissolution. Tablets were formulated containing solid dispersion products and compared with commercial products. IR spectroscopy, XRD, and DSC showed no change in the crystal structure of valdecoxib. Dissolution of valdecoxib improved significantly in solid dispersion products (< 85% in 5 minutes). Tablets containing solid dispersion exhibited better dissolution profile than commercial tablets. Thus, the solid dispersion technique can be successfully used for improvement of dissolution of valdecoxib.
本文研究了使用聚乙烯吡咯烷酮(PVP)固体分散体提高伐地考昔的溶出曲线。本文还描述了通过使用大量超级崩解剂制备伐地考昔速溶片的方法。采用相溶解度法评估各种水溶性聚合物对伐地考昔水溶性的影响。选择聚乙烯吡咯烷酮(PVP K-30),并通过捏合法制备固体分散体。采用美国药典桨法对伐地考昔固体分散体进行溶出度研究。进行红外(IR)光谱、差示扫描量热法(DSC)和X射线衍射法(XRD)以确定药物与载体之间的物理化学相互作用,从而确定其对溶出的影响。制备含有固体分散体产品的片剂,并与市售产品进行比较。IR光谱、XRD和DSC显示伐地考昔的晶体结构没有变化。伐地考昔在固体分散体产品中的溶出度显著提高(5分钟内<85%)。含有固体分散体的片剂比市售片剂表现出更好的溶出曲线。因此,固体分散技术可成功用于改善伐地考昔的溶出度。