College of Pharmacy, Pusan National University, Busan 609-735, Korea.
Arch Pharm Res. 2010 Jan;33(1):115-23. doi: 10.1007/s12272-010-2233-7. Epub 2010 Feb 27.
Even though ion-exchange resins are good drug carriers to get sustained release properties, it may not be good enough only with themselves. For further sustained release effect, a diffusion barrier or coating on the resins' surface can be utilized. Initially, microencapsulation using a w/o/w double emulsion method was used to apply ethylcellulose (EC) onto the drug/resin complexes. Typical pharmaceutical waxes can be alternative materials to delay the drug release from the complex. After the coating, the coated resin particles were incorporated into fast-disintegrating tablets to get an idea regarding the effects of wet granulation and compression on the release. Among the different grades of ECs tested (Ethocel 20, 45, and 100), more viscous EC resulted in better morphologies and sustained release effects. Because the drug release rate was significantly dependent on the coating level, the release rate can be modified easily by changing different levels of the coating. The drug release rate was also strongly dependent on the granulation and compaction process as the coated particles were incorporated into the tablet dosage form. Among the tested waxes, stearic acid had an effect on the sustained release together with lubrication and wetting properties. Even though microencapsulation or wax coating may not be practical for real manufacturing, the results may give valuable information how to formulate sustained release dosage forms and their properties on the tablet preparation.
尽管离子交换树脂是一种很好的药物载体,可以获得持续释放的特性,但仅靠它们本身可能还不够。为了进一步达到持续释放的效果,可以在树脂表面利用扩散屏障或涂层。最初,采用 w/o/w 双重乳液法对药物/树脂复合物进行微囊化,用乙基纤维素(EC)对其进行包衣。典型的药用蜡可以作为替代材料,以延缓药物从复合物中的释放。包衣后,将包衣树脂颗粒掺入速崩片,以了解湿法制粒和压缩对释放的影响。在所测试的不同粘度等级的 EC(Ethocel 20、45 和 100)中,粘度更高的 EC 可形成更好的形态和持续释放效果。由于药物释放速率显著依赖于包衣水平,因此通过改变不同的包衣水平可以轻松调整释放速率。药物释放速率也强烈依赖于造粒和压缩过程,因为包衣颗粒被掺入片剂剂型中。在所测试的蜡中,硬脂酸对持续释放以及润滑和润湿性能有影响。尽管微囊化或蜡涂层在实际生产中可能不实用,但这些结果可能会提供有关如何在片剂制备中制定持续释放剂型及其特性的有价值信息。