Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
Drug Dev Ind Pharm. 2011 Dec;37(12):1463-72. doi: 10.3109/03639045.2011.587428. Epub 2011 Jun 27.
The present research investigates the enhancement of the dissolution rate of celecoxib by using spray-drying to prepare a solid dispersion with various polymers, namely Kollicoat IR® (Kollicoat), polyvinyl alcohol (PVA) 22000, or polyethylene glycol 6000 (PEG). The investigated drug-to-polymer mass ratios were 1:1, 1:2, and 1:4 by weight. Hydroalcoholic or methylene chloride solvent systems were used. The obtained yields ranged from 65% to 78%, whereas the entrapment efficiencies were between 68% and 82%. The results revealed an increase in the dissolution rate of the prepared particles up to 200% within 20 min. The prepared particles were investigated using differential scanning calorimetry, scanning electron microscopy, X-ray diffraction, and Fourier transform infrared spectroscopy. The increased dissolution rate was attributed to hydrogen bond formation between celecoxib and each polymer together with the reduced size of the formed particles offering a greater overall surface area. It was concluded that spray-drying may be considered a successful one-step technique to improve the dissolution rate of celecoxib when using Kollicoat, PVA, or PEG as the carrier polymer.
本研究通过喷雾干燥法制备了 Celecoxib 的固体分散体，使用了不同的聚合物，即 Kollicoat IR®（Kollicoat）、聚乙烯醇（PVA）22000 或聚乙二醇 6000（PEG），以提高其溶解速率。研究了药物与聚合物的质量比分别为 1:1、1:2 和 1:4。使用了水醇或二氯甲烷溶剂体系。获得的产率在 65%至 78%之间，而包封效率在 68%至 82%之间。结果表明，在 20 分钟内，制备的颗粒的溶解速率提高了 200%。使用差示扫描量热法、扫描电子显微镜、X 射线衍射和傅里叶变换红外光谱对制备的颗粒进行了研究。溶解速率的提高归因于 Celecoxib 与每种聚合物之间形成氢键以及形成的颗粒尺寸减小，从而提供了更大的总表面积。结论是，当使用 Kollicoat、PVA 或 PEG 作为载体聚合物时，喷雾干燥可以被认为是一种提高 Celecoxib 溶解速率的成功的一步法技术。
