abstract |
A sustained release formulation of tacrolimus or its hydrate is disclosed, wherein: the time (T63.2%) required for 63.2% of the maximum amount of tacrolimus or its hydrate to be dissolved is 0.7 to 15 hours, as measured according to the Japanese Pharmacopoeia, 13th edition, Dissolution Test, No. 2 (Puddle method, 50 rpm) using a test solution which is an aqueous 0.005% hydroxypropyl cellulose solution adjusted to pH 4.5 which comprises: 1) a solid dispersion composition, wherein tacrolimus or its hydrate is present as an amorphous state in water-soluble base; or 2) a solid dispersion composition, wherein tacrolimus or its hydrate is present as an amorphous state in water-soluble polymer, no disintegrator is contained, and the particle size of the solid dispersion composition is equal to or smaller than 350 mm; or 3) a fine powder of tacrolimus or its hydrate which is characterised by a particle size distribution within the range of 0.1 to 50 mm and/or a mean particle diameter within the range of 0.2 to 20 mm. |