PREPARATION OF DRUG - HYDROXYPROPYLCYCLODEXTRIN COMPLEXES BY A METHOD USING ETHANOL OR AQUEOUS AMMONIUM HYDROXIDE AS CO-SOLUBILIZERS

The dissolution of lipophilic drugs in aqueous solutions of hydroxypropylcyclodextrins can be accelerated by the addition of co-solubilizers such as ethanol or ammonia. These co-solubilizers can be removed later, together with water, by evaporation or freeze-drying, leaving drug: hydroxypropylcyclodextrin complexes. The co-solubilizer method was used successfully with steroid drugs (5-androstene-3-beta,17-beta-diol, 4-androstene-3,17-dione, dehydroepiandrosterone, dexamethasone, 5-alpha-dihydrotestosterone, 6-methylprednisolone and testosterone), peptides (gramicidin S) and a macrocyclic antibiotic (amphotericin B). The complexes prepared in this manner were amorphous and of satisfactory stability and solubility.