Pitha J, Anaissie E J, Uekama K
NIA/GRC, Baltimore, MD 21224.
J Pharm Sci. 1987 Oct;76(10):788-90. doi: 10.1002/jps.2600761007.
A crystalline complex of testosterone with gamma-cyclodextrin was evaluated for solubility and dissolution rate. Whereas these parameters were at least an order of magnitude lower than those of testosterone complexes with amorphous derivatives of cyclodextrins, the properties of the crystalline complex enabled the preparation of a suitable pharmaceutical form for the sublingual administration of hormone to humans. This is in contrast to the situation with similar beta-cyclodextrin complexes, in which such administration was ineffective. Sublingual administration of the gamma-cyclodextrin complex, as shown in previous work using amorphous complexes, avoided rapid first-pass loss of hormone and directed it effectively into the circulation; administration of the complex into the stomach resulted in much lower circulatory hormone levels.
对睾酮与γ-环糊精的晶体复合物进行了溶解度和溶解速率评估。尽管这些参数比睾酮与环糊精无定形衍生物形成的复合物的参数至少低一个数量级，但该晶体复合物的特性使得能够制备出适合人类舌下给药的药物剂型。这与类似的β-环糊精复合物的情况形成对比，在后者中这种给药方式无效。如先前使用无定形复合物的研究所示，γ-环糊精复合物的舌下给药避免了激素的快速首过损失，并有效地将其导向循环系统；将该复合物给予胃会导致循环激素水平低得多。
