Irie T, Fukunaga K, Yoshida A, Uekama K, Fales H M, Pitha J
National Institutes of Health, Baltimore, Maryland 21224.
Pharm Res. 1988 Nov;5(11):713-7. doi: 10.1023/a:1015907927950.
The pharmaceutical usefulness of natural, crystalline cyclodextrins can be improved by chemical conversions into water-soluble, amorphous mixtures of their derivatives. Reaction of beta-cyclodextrin with 2-chloroethanol, 3-chloropropanol, isobutylene oxide, or iodoacetamide yielded the title compounds. Distributions of the substitution degree were close to symmetrical and relatively narrow. The average substitution degrees increased with the amount of alkylating reagent used in the preparation. The number of components (half-width of distribution) increased with increasing average substitution degree. Further, distributions of the substitution degree were measured in glucose derivatives after hydrolysis of 2-hydroxyethyl, 2-hydroxypropyl, and 2-hydroxyisobutyl-beta-cyclodextrin. The results show an uneven distribution of substituents around the cyclodextrins, suggesting that growth of oligoglycol side chains and/or clustering of substituents on one glucose residue occurs.
天然结晶环糊精的药用价值可通过化学转化为其衍生物的水溶性无定形混合物来提高。β-环糊精与2-氯乙醇、3-氯丙醇、环氧异丁烷或碘乙酰胺反应生成了标题化合物。取代度分布接近对称且相对较窄。平均取代度随制备中所用烷基化试剂的量增加而增加。组分数量（分布半宽）随平均取代度增加而增加。此外，在2-羟乙基、2-羟丙基和2-羟异丁基-β-环糊精水解后的葡萄糖衍生物中测量了取代度分布。结果表明环糊精周围取代基分布不均匀，这表明寡糖侧链的生长和/或一个葡萄糖残基上取代基的聚集发生了。
