Department of Pharmaceutics, Shenyang Pharmaceutical University, PO Box 23, 103 Wenhua Road, Shenhe District, Shenyang, Liaoning Province 110016, PR China.
Eur J Pharm Sci. 2012 Apr 11;45(5):639-47. doi: 10.1016/j.ejps.2012.01.003. Epub 2012 Jan 11.
Fibrous ordered mesoporous carbon (FOMC) was developed as a new drug delivery system for loading an insoluble drug, designed to be orally administered, and then to enhance the drug loading capacity, improve the dissolution rate, enhance the oral bioavailability and reduce the gastric damage. Celecoxib (CEL) was chosen as a model drug. The nanostructures and effect of different pore sizes (4.4-7.0 nm) on drug loading and release properties were studied. The results showed that FOMC has a high drug loading capacity (0.599 g/g, drug weight/carrier weight) and the dissolution rate of CEL from FOMC was much faster than pure crystalline CEL using buffer (pH 6.8) as a dissolution medium. Moreover, the oral bioavailability of CEL loaded into FOMC was significantly improved compared with that of CEL capsules and the gastric damage caused by CEL which was loaded in FOMC was also reduced, demonstrating the protective effect of FOMC.
纤维有序介孔碳(FOMC)被开发为一种新的药物传递系统,用于负载难溶性药物,设计为口服给药,然后提高药物载药量、提高药物溶解速度、提高口服生物利用度并降低胃损伤。选择塞来昔布(CEL)作为模型药物。研究了不同孔径(4.4-7.0nm)的纳米结构及其对药物负载和释放性能的影响。结果表明,FOMC 具有高载药量(0.599g/g,药物重量/载体重量),且使用缓冲液(pH6.8)作为溶解介质时,FOMC 中 CEL 的溶解速度比纯结晶 CEL 快得多。此外,与 CEL 胶囊相比,负载到 FOMC 中的 CEL 的口服生物利用度显著提高,并且负载到 FOMC 中的 CEL 引起的胃损伤也降低了,表明 FOMC 具有保护作用。