Back to results
US 2009/0022787 A1Published application
Pharmaceutical composition comprising 11-deoxy- prostaglandin compound and method for stabilizing the compound
AssigneesR-Tech Ueno, Ltd., Sucampo AG
InventorsYasuhiro HARADA, Junichi Kawasaki, Yoshie Nishimura, Ryuji Ueno
Life of this patent
Estimating the term…
Abstract
Provided is a pharmaceutical composition comprising a 11-deoxy-prostaglandin compound represented by formula (I): and a fatty acid ester. By mixing the compound of formula (I) and a fatty acid ester, the compound of formula (I) will be stabilized.
Claims42
A pharmaceutical composition comprising a 11-deoxy-prostaglandin compound represented by formula (I):
- wherein L and N are hydrogen, hydroxy, halogen, lower alkyl, hydroxy(lower)alkyl, lower alkanoyloxy or oxo, wherein the five-membered ring may optionally have at least one double bond;
- A is —CH3, —CH2OH, —COCH2OH, —COOH or a functional derivative thereof;
- R1 is a saturated or unsaturated bivalent lower or medium aliphatic hydrocarbon, which is unsubstituted or substituted with halogen, lower alkyl, hydroxy, oxo, aryl or heterocyclic group, and at least one of carbon atom in the aliphatic hydrocarbon is optionally substituted by oxygen, nitrogen or sulfur;
- and
- R0 is a saturated or unsaturated lower or medium aliphatic hydrocarbon residue, which is unsubstituted or substituted with halogen, oxo, hydroxy, lower alkyl, lower alkoxy, lower alkanoyloxy, cyclo(lower)alkyl, cyclo(lower)alkyloxy, aryl, aryloxy, heterocyclic group or hetrocyclic-oxy group;
- lower alkoxy;
- lower alkanoyloxy;
- cyclo(lower)alkyl;
- cyclo(lower)alkyloxy;
- aryl;
- aryloxy;
- heterocyclic group;
- heterocyclic-oxy group, and at least one of carbon atom in the aliphatic hydrocarbon is optionally substituted by oxygen, nitrogen or sulfur, and
- a fatty acid ester.
11 more elements
A method for stabilizing a 11-deoxy-prostaglandin compound represented by formula (I):
- wherein L and N are hydrogen, hydroxy, halogen, lower alkyl, hydroxy(lower)alkyl, lower alkanoyloxy or oxo, wherein the five-membered ring may optionally have at least one double bond;
- A is —CH3, —CH2OH, —COCH2OH, —COOH or a functional derivative thereof;
- R1 is a saturated or unsaturated bivalent lower or medium aliphatic hydrocarbon, which is unsubstituted or substituted with halogen, lower alkyl, hydroxy, oxo, aryl or heterocyclic group, and at least one of carbon atom in the aliphatic hydrocarbon is optionally substituted by oxygen, nitrogen or sulfur;
- and
- R0 is a saturated or unsaturated lower or medium aliphatic hydrocarbon residue, which is unsubstituted or substituted with halogen, oxo, hydroxy, lower alkyl, lower alkoxy, lower alkanoyloxy, cyclo(lower)alkyl, cyclo(lower)alkyloxy, aryl, aryloxy, heterocyclic group or hetrocyclic-oxy group;
- lower alkoxy;
- lower alkanoyloxy;
- cyclo(lower)alkyl;
- cyclo(lower)alkyloxy;
- aryl;
- aryloxy;
- heterocyclic group;
- heterocyclic-oxy group, and at least one of carbon atom in the aliphatic hydrocarbon is optionally substituted by oxygen, nitrogen or sulfur,
- which comprises mixing the 11-deoxy-prostaglandin compound with a fatty acid ester.
11 more elements
A soft gelatin capsule formulation, which comprises:
- a soft gelatin capsule shell comprising a polyol and/or sugar alcohol as a plasticizer, and
- a pharmaceutical composition comprising a 11-deoxy-prostaglandin compound represented by formula (I):
- wherein L and N are hydrogen, hydroxy, halogen, lower alkyl, hydroxy(lower)alkyl, lower alkanoyloxy or oxo, wherein the five-membered ring may optionally have at least one double bond;
- A is —CH3, —CH2OH, —COCH2OH, —COOH or a functional derivative thereof;
- R1 is a saturated or unsaturated bivalent lower or medium aliphatic hydrocarbon, which is unsubstituted or substituted with halogen, lower alkyl, hydroxy, oxo, aryl or heterocyclic group, and at least one of carbon atom in the aliphatic hydrocarbon is optionally substituted by oxygen, nitrogen or sulfur;
- and
- R0 is a saturated or unsaturated lower or medium aliphatic hydrocarbon residue, which is unsubstituted or substituted with halogen, oxo, hydroxy, lower alkyl, lower alkoxy, lower alkanoyloxy, cyclo(lower)alkyl, cyclo(lower)alkyloxy, aryl, aryloxy, heterocyclic group or hetrocyclic-oxy group;
- lower alkoxy;
- lower alkanoyloxy;
- cyclo(lower)alkyl;
- cyclo(lower)alkyloxy;
- aryl;
- aryloxy;
- heterocyclic group;
- heterocyclic-oxy group, and at least one of carbon atom in the aliphatic hydrocarbon is optionally substituted by oxygen, nitrogen or sulfur, and
- a pharmaceutically acceptable vehicle,
- wherein said pharmaceutical composition is incorporated in the soft gelatin capsule shell.
14 more elements
Dependencies are inferred from the claim text.