Hirayama F, Hirashima N, Abe K, Uekama K, Ijitsu T, Ueno M
Faculty of Pharmaceutical Sciences, Kumamoto University, Japan.
J Pharm Sci. 1988 Mar;77(3):233-6. doi: 10.1002/jps.2600770310.
Heptakis(2,6-di-O-ethyl)-beta-cyclodextrin (2) was prepared and its physicochemical properties, such as aqueous solubility and surface activity, were compared with those of beta-cyclodextrin (1) and heptakis(2,6-di-O-methyl)-beta-cyclodextrin (3). A possible utility of 2 as a sustained-release drug carrier was examined using a water-soluble drug, isosorbide dinitrate. The dissolution and release rates of isosorbide dinitrate from capsule and tablet forms were significantly retarded by the complexation with 2. The sustained-release pattern of isosorbide dinitrate was produced for a long period after the oral administration of a single dose of capsule or tablet containing the 2 complex to rats. The results indicated that 2 may serve as a hydrophobic drug carrier for sustained-release of isosorbide dinitrate.
制备了七（2,6-二-O-乙基）-β-环糊精（2），并将其物理化学性质，如在水中的溶解度和表面活性，与β-环糊精（1）和七（2,6-二-O-甲基）-β-环糊精（3）进行了比较。使用水溶性药物硝酸异山梨酯研究了2作为缓释药物载体的可能用途。硝酸异山梨酯与2络合后，其从胶囊和片剂形式中的溶解和释放速率显著减慢。给大鼠口服单剂量含有2络合物的胶囊或片剂后，硝酸异山梨酯在很长一段时间内呈现出缓释模式。结果表明，2可作为硝酸异山梨酯缓释的疏水性药物载体。
