Anti-infective compositions for the treatment of a human in need of therapy for a systemic or topical fungal infection which comprise a pharmaceutically acceptable carrier and a therapeutically effective amount of (2R,4S) itraconazole or a pharmaceutically acceptable salt thereof, substantially free of its (2S,4R) stereoisomer.

The present invention is concerned with the stereoisomeric forms of itraconazole (X=Cl) and saperconazole (X=F), which may be represented by the formula ##STR1## and the pharmaceutically acceptable acid addition salt forms thereof, processes for preparing said stereoisomeric forms, the complexes thereof with cyclodextrin derivatives, pharmaceutical compositions comprising said complexes and methods of preparing said complexes and pharmaceutical compositions.

Methods for preparing microspheres containing imidazole derivatives are provided. Also provided is the use of imidazole derivatives containing microspheres for treating fungal infections. Oral dosage forms for oral administration are also provided.

The present invention provides a polymorphic form of itraconazole.

Methods for preparing microspheres containing imidazole derivatives are provided. Also provided is the use of imidazole derivatives containing microspheres for treating fungal infections. Oral dosage forms for oral administration are also provided.

Solutions comprising itraconazole solubilized in a solvent comprising at least one volatile organic acid are provided. Methods for preparing microspheres containing imidazole derivatives are provided. Also provided is the use of imidazole derivatives containing microspheres for treating fungal infections. Oral dosage forms for oral administration are also provided.

The present invention relates to a method and composition of an oral preparation of itraconazole, an excellent azole antifungal drug. More particularly, it relates to an oral preparation of itraconazole having improved bioavailability, which is prepared by following steps of: i) dissolving itraconazole and bydrophilic polymer with solvent, ii) spray-drying said mixture, and iii) preparing the solid dispersions for oral preparation. The solid dispersions prepared in this invention may be useful i...

A method of manufacturing an itraconazole oral dosage form that is substantially free of residual methylene chloride comprises the steps of: (a) providing a working solution comprising an alcohol, a strong acid (preferably an inorganic acid or organic sulphonic acid), itraconazole, a water-soluble polymer, and water, with the itraconazole and the strong acid preferably present in the working solution in a ratio of 1 Mole itraconazole to 1-3 Moles acid; (b) providing particles formed from a pharm...

The invention provides novel soluble conazole crystalline forms (e.g. itraconazole, posaconazole and saperconazole) that include salts, co-crystals and related solvates useful as pharmaceuticals. The invention also provides pharmaceutical compositions comprising, and processes for making, these conazole crystalline forms. Methods of using such compositions for the treatment or prevention of systemic and local fungal, yeast, and dermatophyte infections are also provided.

An antifungal oral composition comprising a fused mixture of itraconazole and phosphoric acid provides a high in vivo bioavailability of itraconazole.