Fujisawa Pharmaceutical Company, Ltd.

Astellas Pharma Gmbh

Fumio Shimojo

Takao Takaya

Hisashi Takasugi

Takashi Saitoh

Satoshi Ueda

Rinta Ibuki

Takeo Hirose

Shigeki Tamura

Yukihiro Nomura

Kazunari Yamashita

Toshio Ideno

Yoshio Ueda

Kazutake Kado

Masayuki Yamanaka

Takehisa Hata

Tsutomu Toyonaka Teraji

Ikuo Ueda

Shigetaka Nishino

Eiji Hashimoto

Toshihiko Toyoda

Sumihisa Kimura

Norio Ohnishi

Erika Yoshida

Sotoo Asakura

Kyoko Ishii

Yuji Tokunaga

Yoshio Murakami

Seiji Sawai

Toshiyasu Honbo

Masahiro Tsuji

Kenzo Toyoshima

Yasuo Shimazaki

Hiromitu Yoshida

Hideki Ito

Nobumitsu Nakahasi

Mitsuru Yasumara

Yoshio Uedo

Keiji Takai

Kiyoshige Yoshida

Takeo Chayamachi 525 Hirose

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

To provide a pharmaceutical composition comprising a macrolide compound, such as tricyclic compound (I) or its pharmaceutically acceptable salt, a dissolution/absorption promoter, a pharmaceutical base, and optionally a compatibilizing agent and/or a thickener. It is satisfactory in stability and absorption kinetics and/or a low irritation potential.

Medicinal compositions

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

A pharmaceutical composition comprising a tricyclic compound (I) or its pharmaceutically acceptable salt, an oil substance, a surfactant, a hydrophilic substance, water, and optionally a pH control agent, with enhanced stability, absorbability and/or a low irritation potential, is provided.

Pharmaceutical composition

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.

Two surfactant-containing medicinal composition

Aerosol composition containing middle-chain fatty acid triglyceride dispersant

Encapsulated medicine

A pharmaceutical composition which is a physical mixture of exifone and certain water soluble cellulose derivatives. The mixture exhibits surprisingly improved solubility and bio availability.

Novel pharmaceutical composition comprising exifone and water-soluble

This invention relates to a solid dispersion composition comprising FR-900506 substance and water-soluble hydroxypropyl methylcellulose which is capable of dispersing the FR-900506 substance, the FR-900506 substance and hydroxypropyl methylcellulose being in the ratio of 1:0:1 to 1:20 by weight.

Solid dispersion composition of FR-900506 substance

The invention relates to a sustained-release transdermal delivery preparation which comprises a slow-release microcapsule containing 2-nitroxymethyl-6-chloropyridine or its occlusion compound with .beta.-cyclodextrin and a skin-compatible base.

Sustained-release transdermal delivery preparations

An occlusion compound of 2-nitroxymethyl-6-chloropyridine with .beta.-cyclodextrin is disclosed herein as well as a process for preparing the occlusion compound thereof. The occlusion compound of the present invention has a molar ratio of 2-nitroxymethyl-6-chloropyridine to .beta.-cyclodextrin of between about 1:1 and about 3:1. The present occlusion compound is nonvolatile, thereby overcoming the problems associated with the volatility of the 2-nitroxymethyl-6-chloropyridine for pharmacuetical preparations. The process of the present invention is carried out by reacting 2-nitroxymethyl-6-chloropyridine with .beta.-cyclodextrin either by kneading both compounds together with a small amount of a solvent or by mixing both compounds in an appropriate solvent, such as water. The occlusion compound is then precipitated, separated and further purified by conventional methods.

Occlusion compound of 2-nitroxymethyl-6-chloropyridine with

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Kawanishi, Japan

Fumio Shimojo