Colombo P, Bettini R, Massimo G, Catellani P L, Santi P, Peppas N A
Pharmaceutical Department, University of Parma, Italy.
J Pharm Sci. 1995 Aug;84(8):991-7. doi: 10.1002/jps.2600840816.
Swellable controlled release devices of buflomedil pyridoxalphosphate in hydroxypropyl methylcellulose were prepared, and their swelling and release behavior was investigated. The drug release as a function of time was investigated for various system parameters. Three distinct fronts were observed during the swelling and release processes, i.e., a swelling, a drug diffusion, and an erosion front. The drug diffusion front could be readily determined due to the drug's yellow color. The relative positions of the fronts and the drug release rate were studied as functions of the initial porosity and the molecular weight of the polymer carrier. It was shown that the drug diffusion front best describes the overall release behavior of the system. The fractional drug release was a strong function of the dissolved drug gel layer thickness, which separates the diffusion front from the erosion front. The effect of drug solubility was also investigated by altering the pH and the ionic strength of the dissolution medium. It was shown that as drug solubility increased, the undissolved drug gel layer thickness decreased, again showing the importance of the movement of the diffusion front in controlling the overall release.
制备了丁咯地尔磷酸吡哆醛在羟丙基甲基纤维素中的可膨胀控释制剂,并研究了其膨胀和释放行为。针对各种系统参数,研究了药物释放随时间的变化情况。在膨胀和释放过程中观察到三个不同的前沿,即膨胀前沿、药物扩散前沿和侵蚀前沿。由于药物的黄色,药物扩散前沿很容易确定。研究了前沿的相对位置和药物释放速率与初始孔隙率和聚合物载体分子量的关系。结果表明,药物扩散前沿最能描述该系统的整体释放行为。药物释放分数强烈依赖于溶解药物凝胶层的厚度,该凝胶层将扩散前沿与侵蚀前沿分隔开。还通过改变溶出介质的pH值和离子强度研究了药物溶解度的影响。结果表明,随着药物溶解度的增加,未溶解药物凝胶层的厚度减小,这再次表明扩散前沿的移动在控制整体释放中的重要性。