Fujisawa Pharmaceutical Company, Ltd.

Astellas Pharma Gmbh

Takeo Hirose

Takashi Saitoh

Satoshi Ueda

Fumio Shimojo

Rinta Ibuki

Shigeki Tamura

Yukihiro Nomura

Sumihisa Kimura

Takehisa Hata

Eiji Hashimoto

Kazunari Yamashita

Toshio Ideno

Yuji Tokunaga

Norio Ohnishi

A sustained-release formulation is provided comprising a solid dispersion composition comprising a tricyclic compound or a pharmaceutically acceptable salt thereof in a mixture comprising a water-soluble polymer and a water-insoluble polymer, and an excipient.

Sustained-release formulation

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.

Sustained release formulation containing tacrolimus

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 Japanese Pharmacopoeia, the 13-th edition, Dissolution Test, No. 2 (Puddle 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 comprise a solid base which is a water-soluble polymer and/or wax. The formulation is in the form of a powder, fine powder, granule, tablet or capsule. Furthermore, the formulation is administered to a patient once a day for preventing organ or tissue rejection by transplantation or autoimmune diseases.

Sustained release formulations containing tacrolimus

Providing an oral formulation of a macrolide compound where the dissolution of the macrolide compound is under sustained release; and a sustained-release formulation containing a composition in solid solution, where the macrolide compound is present at an amorphous state in a solid base.

Sustained release preparations

To provide a pharmaceutical composition comprising a water-insoluble active substance, surfactant(s) and solid carrier(s), which is improved in dissolution and oral absorption characteristics.

Medicinal composition

Provided is a medicinal composition having a very satisfactory drug release profile and a very satisfactory drug absorption profile after oral administration characterized by its comprising an insoluble drug and two or more surfactants, at least one of the surfactants having as dissolved therein the insoluble drug and the other surfactant or surfactants.

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Kyoto, Japan

Takeo Hirose