Nippon Kayaku Kabushiki Kaisha

Dai Kawamura

Keiichirou Yamamoto

Manami Okazaki

It is an object of the present invention to provide a pharmaceutical composition which can suppress a reduction in the content of an active ingredient caused by oxidation or decomposition of the rapamycin or a derivative thereof, can ensure long-term stability, and has high safety. The present invention provides a pharmaceutical composition comprising (A) rapamycin or a derivative thereof and (B) trehalose, and a method for producing a pharmaceutical composition comprising rapamycin or a derivative thereof, which comprises adding a solution containing rapamycin or a derivative thereof to sugars having a critical relative humidity at 25&#xb0; C. of 95% or more.

Pharmaceutical composition comprising rapamycin or derivative thereof, and method for producing the same

[Problem]To provide a novel polymer derivative of a cytidine metabolic antagonist which allows release of a medicament irrespective of enzymes of the living body and is expected to have high therapeutic effects. [Solution] The polymer derivative of a cytidine metabolic antagonist in which a substituent represented by the general formula (I) or the general formula (II) [wherein Rand Reach independently represent a hydrogen atom or an optionally substituted (C1-C6)alkyl group, Rrepresents a hydrogen atom, an optionally substituted (C1-C40)alkyl group, an optionally substituted (C1-C40)aralkyl group, an optionally substituted aromatic group, an amino acid residue in which the carboxy group is protected, or an optionally substituted sugar residue, CX&#x2014;CY represents CH&#x2014;CH or C&#x2550;C (double bond), and A represents the residue of the cytidine metabolic antagonist except the amino group at the position 4] is bonded to the side-chain carboxy group of a block copolymer of a polyethylene-glycol structural moiety and a polymer having 10 or more carboxy groups.

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Saitama, Japan

Dai Kawamura