Muraoka M, Kimura G, Zhaopeng H, Takada K
Department of Pharmaceutics and Pharmacokinetics, Kyoto Pharmaceutical University.
Nihon Rinsho. 1998 Mar;56(3):788-94.
Ulcerative colitis, Crohn's disease and hemorrhage colitis are typical example of colon specific diseases. The targeting of the drugs for these colon specific diseases was attempted by a new technology, where ethylcellulose (EC) was used as pharmaceutical material. Especially, pressure-controlled colon delivery capsule (PCDC) made of EC is a unique system. PCDC was prepared by coating the inner surface of gelatin capsule with water-insoluble polymer, EC. By adjusting the coating thickness of EC membrane to be approximately 40 microns, colon delivery of dug were obtained both in beagle dogs and human volunteers. PCDC containing 5-ASA was prepared and was administered orally to beagle dogs. After administration, 5-ASA appeared into the systemic circulation at 3-5 h which corresponds to the colon arrival time confirmed with sulfasalazine.
溃疡性结肠炎、克罗恩病和出血性结肠炎是典型的结肠特异性疾病。一种新技术尝试将药物靶向用于这些结肠特异性疾病,该技术使用乙基纤维素(EC)作为药物材料。特别是,由EC制成的压力控制结肠给药胶囊(PCDC)是一种独特的系统。PCDC是通过用水不溶性聚合物EC包被明胶胶囊的内表面制备而成。通过将EC膜的包衣厚度调整至约40微米,在比格犬和人类志愿者中均实现了药物的结肠给药。制备了含5-氨基水杨酸(5-ASA)的PCDC并口服给予比格犬。给药后,5-ASA在3-5小时进入体循环,这与用柳氮磺胺吡啶证实的结肠到达时间相对应。