Sustained release formulation containing tacrolimus or its hydrate is provided.
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. The time is measured in accordance
to the Japanes Pharmacopocia, the 13-th edition, Dissolution Test, No. 2 (Puddles
method, 50 rpm) using an aqueous 0.005% hydroxypropyl cellulose solution. This
aqueous test solution is adjusted to pH 4.5, accordingly. The formulation further
comprises a solid base which is a water-soluble or water-insoluble polymer. The
formulation is in the form of a powder, fine powder, granule, tablet or capsule.
The formulation is administered to a patient once a day for preventing organ or
tissue rejection by transplantation or autoimmune disease. In addition, a solid
dispersion composition is provided. The solid dispersion comprises tacrolimus or
its hydrate in a mixture containing water-soluble or water-insoluble polymer and
an excipient.
