Akhgari A, Farahmand F, Afrasiabi Garekani H, Sadeghi F, Vandamme T F
School of Pharmacy and Pharmaceutical Research Centre, Vakilabad blvd., PO Box 91775-1365, Mashhad University of Medical Science, Mashhad, Iran.
Eur J Pharm Sci. 2006 Jul;28(4):307-14. doi: 10.1016/j.ejps.2006.03.005. Epub 2006 Mar 28.
The aim of this study was to assess some permeability and swelling characteristics of free films prepared by combination of inulin as a bacterially degradable system and time- or pH-dependent polymers as a coating formulation for colonic drug delivery. Different free films were prepared by casting and solvent evaporation method. Formulations containing inulin with Eudragit RS, Eudragit RL, Eudragit RS-Eudragit RL, Eudragit FS and Eudragit RS-Eudragit S with different ratios of inulin were prepared. After preparation, free films were evaluated by water vapor transmission test, swelling experiment and permeability to indomethacin and theophylline in different media. Formulations containing Eudragit FS had high resistance to water vapor permeation; but were unable to protect premature swelling and drug release in simulated small intestine media. Also, combination of Eudragit RS and Eudragit S had no suitable characteristics for colon delivery. However, Eudragit RS and Eudragit RL in combination with inulin made free films which had more swelling and permeation of drug in the colonic medium rather than the other media. It was shown that formulations containing sustained release polymethacrylates in combination with inulin have more potential as a coating system for specific colon delivery compared with pH-dependent polymers.
本研究的目的是评估由菊粉（一种可被细菌降解的体系）与时间或pH依赖性聚合物组合制备的游离膜的一些渗透性和溶胀特性，该组合作为结肠给药的包衣制剂。通过流延和溶剂蒸发法制备了不同的游离膜。制备了含有菊粉与不同比例菊粉的丙烯酸树脂RS、丙烯酸树脂RL、丙烯酸树脂RS - 丙烯酸树脂RL、丙烯酸树脂FS以及丙烯酸树脂RS - 丙烯酸树脂S的制剂。制备后，通过水蒸气透过测试、溶胀实验以及在不同介质中对吲哚美辛和茶碱的渗透性对游离膜进行了评估。含有丙烯酸树脂FS的制剂对水蒸气渗透具有高抗性；但在模拟小肠介质中无法防止过早溶胀和药物释放。此外，丙烯酸树脂RS和丙烯酸树脂S的组合不具备适合结肠给药的特性。然而，丙烯酸树脂RS和丙烯酸树脂RL与菊粉组合制成的游离膜在结肠介质中比在其他介质中具有更多的药物溶胀和渗透。结果表明，与pH依赖性聚合物相比，含有缓释聚甲基丙烯酸酯与菊粉组合的制剂作为特定结肠给药的包衣系统具有更大的潜力。
