在水中难溶或不大稳定的药物难以做成制剂注射给药,这是一个长期存在的恼人的问题。有人曾用药物前体、有机助溶剂、乳剂、脂质体及胶束化等方法来解决药理活性成分的水不相容问题,但注射给药对低毒性的绝对需要阻碍了这些方法的应用。环糊精能与许多药物形成包含物,实质上能增加药物的水溶性,但由于环糊精有肾毒性,排除了用于注射剂的可能。羟基烃基-β-环糊精似乎比未取代或烃基化环糊精的毒性低,有可能应用于静脉注射。本文旨在说明羟基烃基环糊精在注射剂中应用的可 It is a longstanding and annoying problem that drugs that are poorly soluble or unstable in water are difficult to make by injection. Some methods such as prodrugs, organic cosolvents, emulsions, liposomes and micelles have been used to solve the water incompatibility issue of pharmacologically active ingredients, but the absolute need for low toxicity by injection for injection hinders the use of these methods . Cyclodextrins can form inclusions with many drugs that substantially increase the water solubility of the drug, but because of their nephrotoxicity, cyclodextrins eliminate the potential for injectables. Hydroxyhydrocarbyl-β-cyclodextrins appear to be less toxic than unsubstituted or hydrocylated cyclodextrins and are potentially useful for intravenous injection. This article aims to illustrate the use of hydroxy hydrocarbyl cyclodextrins in injectables