Rao C T, Fales H M, Pitha J
NIA/GRC, National Institutes of Health, Baltimore, Maryland 21224.
Pharm Res. 1990 Jun;7(6):612-5. doi: 10.1023/a:1015818211518.
A series of hydroxypropyl-beta-cyclodextrins was prepared by a method that leads to a preferential substitution on the secondary hydroxyls, mainly O-2, of beta-cyclodextrin with (S)-2-hydroxypropyl groups. The series consisted of mixtures of compounds with average degrees of substitution of 8, 3, and 1.6 and of a specially isolated monosubstituted compound; thus, the number of components progressively decreased in this series. The crystallinity in the series increased progressively, the first member being fully amorphous and the last one fully crystalline. All members of the series formed clear aqueous solutions at concentrations of greater than 50.0, 2.0, 0.6, and 0.3%, respectively. Therefore, pharmaceutically useful hydroxypropylcyclodextrin preparations are those containing a large number of chemically individual compounds--a feature resulting in an amorphous state and high water solubility.
通过一种方法制备了一系列羟丙基-β-环糊精，该方法导致β-环糊精的仲羟基（主要是O-2）优先被(S)-2-羟丙基取代。该系列由平均取代度为8、3和1.6的化合物混合物以及一种特别分离出的单取代化合物组成；因此，该系列中组分的数量逐渐减少。该系列中的结晶度逐渐增加，第一个成员完全无定形，最后一个完全结晶。该系列的所有成员分别在浓度大于50.0%、2.0%、0.6%和0.3%时形成澄清的水溶液。因此，药学上有用的羟丙基环糊精制剂是那些含有大量化学上不同化合物的制剂——这一特征导致无定形状态和高水溶性。
