Mantas Athanasios, Petit Marie-Amélie, Mihranyan Albert
Nanotechnology and Functional Materials, Department of Materials Science and Engineering, Box 534 Uppsala University, 75121 Uppsala, Sweden.
Pharmaceutics. 2020 Jan 17;12(1):71. doi: 10.3390/pharmaceutics12010071.
We have previously reported that heated powder mixtures of ibuprofen (IBU) and high surface area nanocellulose exhibit an enhanced dissolution and solubility of the drug due to IBU amorphization. The goal of the present work was to further elaborate the concept and conduct side-by-side in vitro drug release comparisons with commercial formulations, including film-coated tablets, soft gel liquid capsules, and IBU-lysine conjugate tablets, in biorelevant media. Directly compressed tablets were produced from heated mixtures of 20% / IBU and high surface area Cladophora cellulose (CLAD), with 5% / sodium croscarmelose (AcDiSol) as superdisintegrant. The side-by side studies in simulated gastric fluid, fasted-state simulated intestinal fluid, and fed-state simulated intestinal fluid corroborate that the IBU-CLAD tablets show more rapid and less variable release in various media compared to three commercial IBU formulations. On the sidelines of the main work, a possibility of the presence of a new meta-crystalline form of IBU in mixture with nanocellulose is discussed.
我们之前曾报道，布洛芬（IBU）与高比表面积纳米纤维素的加热粉末混合物由于IBU非晶化而使药物的溶出度和溶解度增强。本工作的目标是进一步阐述这一概念，并在生物相关介质中与包括薄膜包衣片、软胶囊液剂胶囊和IBU-赖氨酸共轭片在内的市售制剂进行体外药物释放的平行比较。由20%/IBU与高比表面积枝管藻纤维素（CLAD）的加热混合物制备直接压片，其中5%/交联羧甲基纤维素钠（AcDiSol）作为超级崩解剂。在模拟胃液、禁食状态模拟肠液和进食状态模拟肠液中的平行研究证实，与三种市售IBU制剂相比，IBU-CLAD片在各种介质中显示出更快且更稳定的释放。在主要工作之余，还讨论了与纳米纤维素混合的IBU存在一种新的亚晶型的可能性。
