Study on Usefulness of Novel Itraconazole Solid Dispersion when Administered as a Suspension

In the treatment of tinea unguium (pulse therapy) using itraconazole preparations,the dose is large and can vary widely.For example,it could be 200mg (4 capsules) per single dose or 400mg (8 capsules) per day.In this study,we developed a novel solid dispersion preparation of itraconazole (itraconazole SD) that could be taken easily and safely even by elderly patients with limited swallowing ability.We also investigated dosage forms of itraconazole SD that can be taken by the standard method of swallowing tablets with a glass of water or as a suspension of disintegrated tablets in a glass of water.Further,in a bioequivalence study in humans,we found that itraconazole SD (test product) was bioequivalent to an innovator product (Itrizole capsule 50)when ingested orally in the normal way or as a suspension in water.Our results suggested that the test product would be useful for patients who find it difficult to take several capsules or tablets at one time.In addition,the rapid disintegration of the test product enabled a suspension to be prepared easily and quickly.Furthermore,a suspension of the test product did not obstruct a thin tube (8 French) because the solid dispersion includes an enteric polymer,which does not dissolve in water,and the mean particle diameter is maintained at less than 120 μm in its preparation.Therefore,the test product would also be useful in the case of tube administration.