NOVEL DIACETYLDAPSONE-CONTAINING COMPOSITIONS AND THE USE THEREOF FOR THE TREATMENT OF VARIOUS DISEASE STATES

摘要

Diacetyldapsone has been demonstrated to be effective against Pneumocystis carinii in a mouse model. The solubility of this highly insoluble drug can be greatly enhanced by formulation in a molecular inclusion complex with a cyclodextrin (such as, for example, hydroxypropyl-beta-cyclodextrin). The formulation of diacetyldapsone in cyclodextrin enhances the stability thereof, presumably by protecting the drug against hydrolysis of the amide substituents thereof. Oral administration of the resulting formulation results in the absorption of diacetyldapsone and systemic conversion thereof to monoacetyldapsone and dapsone. These results illustrate the utility of a cyclodextrin formulation of diacetyldapsone as a chemoprophylactic adjunct in the management of disease states such as Pneumocystis pneumonia in acquired immune deficiency syndrome (AIDS).