Fujisawa Pharmaceutical Company, Ltd.

Nissho Corporation

Akira Kagayama

Takehisa Hata

Saburo Murata

Sachiyo Tanimoto

Hitoshi Futagawa

Sotoo Asakura

Seizo Sunago

Yuji Tokunaga

Sumihisa Kimura

Yoshio Murakami

Yasuto Koyama

Youhei Kiyota

Toshiomi Nakate

Mitsuo Murakami

Osamu Takahata

Kiyoko Akashi

Masashi Hashimoto

Hiroshi Kayakiri

Satoshi Ueda

Hidekazu Takeno

Kazumi Ohtomo

Seiji Sawai

Tetsuji Miyamoto

Tomohiko Kubo

Atsunori Kaibara

Kenji Nishiwaki

Tomoaki Iwasa

Process for producing a hydrochloride of a vancomycin antibiotic, comprising subjecting an aqueous solution of a hydrochloride of a vancomycin antibiotic to a primary freezing at from &minus;1&deg; C. to &minus;20&deg; C. for a time sufficient to grow ice crystals, to form a primarily frozen substance, then subjecting said primarily frozen substance to a secondary freezing at from &minus;25&deg; C. to &minus;80&deg; C. to form a completely frozen solid, and then drying the resulting frozen solid in vacuo; and product obtained by the process.

Hydrochlorides of vancomycin antibiotics and process for producing the same

Fluid vessel

A lotion comprising a tricyclic compound, typically 17-allyl-1,14-dihydroxy-12-�2-(4-hydroxy-3-methoxycyclohexyl)-1-methylviny l!-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo �22.3.1.0.sup.4,9 !octacos-18-ene-2,3,10,16-tetraone, or a pharmaceutically acceptable salt thereof, a solubilizing and/or absorption-promoting agent, a liquid medium, and optionally an emulsifier and/or a viscosity increasing agent. The lotion is stable, excellent in absorption and has less irritation against the skin and sustained release. Also, the lotion is effective for the treatment and/or prophylaxis of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses.

Lotion for FK 506

A liposome preparation containing an immunosuppresive tricylic compound or a pharmaceutically acceptable salt thereof. Since the tricyclic compound is entrapped stably and quantitatively into the liposomes, a broad variety of drug forms and pharmaceutical preparations insuring a long duration of efficacy can be provided.

Liposome preparation containing a tricyclic compound

The invention relates to a delayed action preparation which comprises a core comprising a drug and a swelling agent and an outer membrane comprising a biodegradable high molecular weight substance characterized in that the swelling agent is contained in a sufficient amount to cause a explosion of the outer membrane of biodegradable high molecular weight substance at a definite time after administration. This preparation provides for free control over the timing of drug release and is suited for administration not only by the oral route but also by the intramuscular, subcutaneous and other routes.

Delayed action preparation

Sustained release medicinal preparation

A suspendible composition comprising a tricyclic compound such as FK 506 substance which is 17-allyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylviny l]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo-[22.3. 1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone, or the like, and a pharmaceutically acceptable surfactant, which can be used as an orally administrable agent or eye drops and is useful for treating various diseases.

Suspendible composition and process for preparing the same

A suspendible composition comprising a tricyclic compound such as FK 506 substance which is 17-allyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylviny 1]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1 .0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone, or the like, and a pharmaceutically acceptable surfactant, which can be used as an orally administrable agent or eye drops and is useful for treating various diseases.

The invention relates to a novel prodrug compound useful in the treatment of tumors, of the formula:

Prodrug compounds, process for the preparation thereof and sustained

Growing community of inventors

Ikoma, Japan

Akira Kagayama