Mauludin Rachmat, Müller Rainer H, Keck Cornelia M
Department of Pharmaceutics, Biopharmaceutics & NutriCosmetics, Free University of Berlin, Kelchstr. 31, 12169 Berlin, Germany.
Int J Pharm. 2009 Mar 31;370(1-2):202-9. doi: 10.1016/j.ijpharm.2008.11.029. Epub 2008 Dec 7.
Dried rutin nanocrystals have been prepared by lyophilization and investigated regarding their physicochemical properties with respect to re-dispersability, particle size, morphology and dissolution behavior. Photon correlation spectroscopy (PCS) and laser diffractometry (LD) were employed to determine the particle size. Morphology of the particles was analyzed by light microscopy. Lyophilized rutin nanocrystals were incorporated into tablets and the dissolution behavior of the tablets was evaluated. Very fine particles of lyophilized rutin could be completely re-dispersed in the water. The PCS size average and polydispersity index (PI) of lyophilized rutin were of 721nm and of 0.288 after re-dispersion. The rutin nanocrystal-loaded tablets were produced using direct compression. The dissolution velocity of the rutin nanocrystal-loaded tablet was superior compared to rutin microcrystal-loaded and a marketed tablet. After 30min rutin was released and dissolved completely from the nanocrystal tablets in water. In contrast, only 71% and 55% of the total amount of rutin were dissolved from the microcrystal tablets and the marketed tablet, respectively. The improving dissolution behavior of the rutin nanocrystal-loaded tablet should lead to a better bioavailability of the poorly soluble rutin in the body.
通过冻干法制备了干燥的芦丁纳米晶体,并对其再分散性、粒径、形态和溶解行为等物理化学性质进行了研究。采用光子相关光谱法(PCS)和激光衍射法(LD)测定粒径。通过光学显微镜分析颗粒的形态。将冻干的芦丁纳米晶体压制成片剂,并对片剂的溶解行为进行了评价。冻干芦丁的极细颗粒可在水中完全再分散。再分散后,冻干芦丁的PCS尺寸平均值和多分散指数(PI)分别为721nm和0.288。采用直接压片法制备了芦丁纳米晶载药片剂。芦丁纳米晶载药片剂的溶解速度优于芦丁微晶载药片剂和市售片剂。30分钟后,芦丁从纳米晶片剂中完全释放并溶解于水中。相比之下,芦丁微晶片剂和市售片剂中芦丁的总溶出量分别仅为71%和55%。芦丁纳米晶载药片剂溶解行为的改善应会使难溶性芦丁在体内具有更好的生物利用度。