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Claims for Patent: 6,583,174

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Claims for Patent: 6,583,174

Title: Composition and method for stabilizing the same
Abstract:Disclosed is a novel composition comprising a novel bi-cyclic compound, which is expected to be pharmaceutically active, and a glyceride. The stability of the bi-cyclic compound can be improved significantly by dissolving the same in a glyceride.
Inventor(s): Ueno; Ryuji (Montgomery, MD), Habe; Tsuyoshi (Sasayama, JP)
Assignee: Sucampo, A.G. (Zurich, CH)
Application Number:09/688,351
Patent Claims: 1. A composition comprising a bi-cyclic compound represented by the formula (I): ##STR21##

wherein, A is --CH.sub.2 OH, --COCH.sub.2 OH, --COOH or a functional derivative thereof, X.sub.1 and X.sub.2 are hydrogen atom, lower alkyl or halogen atom; V.sub.1 and V.sub.2 are carbon atoms; W.sub.1 and W.sub.2 are ##STR22## wherein R.sub.4 and R.sub.5 are hydrogen atom, hydroxy, halogen atom, lower alkyl, lower alkoxy or hydroxy (lower) alkyl with the proviso that R.sub.4 and R.sub.5 are not hydroxy or lower alkoxy at the same time; Z is an oxygen atom; R.sub.1 is a saturated or unsaturated bivalent lower-medium aliphatic hydrocarbon residue which is unsubstituted or substituted with halogen atom, an alkyl group, hydroxy, oxo, aryl or heterocyclic group; R.sub.2 is a saturated or unsaturated, lower or medium aliphatic hydrocarbon residue which is unsubstituted or substituted with halogen atom, oxo, hydroxy, lower alkyl, lower alkoxy, lower alkanoyloxy, lower cycloalkyl, lower cycloalkyloxy, aryl, aryloxy, heterocyclic group or heterocyclic-oxy group; lower cycloalkyl; lower cycloalkyloxy; aryl, aryloxy, heterocyclic group or heterocyclic-oxy group; R.sub.3 is a hydrogen atom, a lower alkyl, lower cycloalkyl, aryl or heterocyclic group, and a glyceride, in which the bi-cyclic compound is present in a ratio of at least 50:50 with respect to its tautomeric monocyclic compound.

2. The composition of claim 1, in which the bi-cyclic compound is the compound of the formula (I), wherein A is --COOH or functional derivative thereof, X.sub.1 and X.sub.2 are halogen atoms, W.sub.1 is .dbd.O, or where one of R.sub.4 and R.sub.5 is hydrogen, and the other is hydroxy, W.sub.2 is where R.sub.4 and R.sub.5 are both hydrogen atoms, R.sub.1 is a saturated or unsaturated bivalent unsubstituted lower-medium aliphatic hydrocarbon residue, R.sub.2 is a saturated or unsaturated unsubstituted lower-medium aliphatic hydrocarbon residue, R.sub.3 is a hydrogen atom.

3. The composition of claim 1, in which the glyceride is a glyceride of a fatty acid having 6-24 carbon atoms.

4. The composition of claim 3, wherein said glyceride is a glyceride of a fatty acid having 6-20 carbon atoms.

5. The composition of claim 1, in which the glyceride is a mixture of 2 or more glycerides.

6. The composition of claim 1, wherein said glyceride is admixed with another oil solvent.

7. The composition of claim 6, wherein said other oil solvent is mineral oil.

8. The composition of claim 1, which is in a dosage form suitable for oral administration.

9. The composition of claim 8, which is formulated as a capsule.

10. The composition of claim 1, which is in a dosage form suitable for topical administration.

11. The composition of claim 10, which is formulated as an eye drop.

12. A method for stabilizing a bi-cyclic compound represented by the formula (I): ##STR23##

wherein, A is --CH.sub.2 OH, --COCH.sub.2 OH, --COOH or a functional derivative thereof, X.sub.1 and X.sub.2 are hydrogen atom, lower alkyl or halogen atom; V.sub.1 and V.sub.2 are carbon atoms; W.sub.1 and W.sub.2 are ##STR24## wherein R.sub.4 and R.sub.5 are hydrogen atom, hydroxy, halogen atom, lower alkyl, lower alkoxy or hydroxy (lower) alkyl with the proviso that R.sub.4 and R.sub.5 are not hydroxy or lower alkoxy at the same time; Z is an oxygen atom; R.sub.1 is a saturated or unsaturated bivalent lower-medium aliphatic hydrocarbon residue which is unsubstituted or substituted with halogen atom, an alkyl group hydroxy, oxo, aryl or heteroyclic group; R.sub.2 is a saturated or unsaturated, lower or medium aliphatic hydrocarbon residue which is unsubstituted or substituted with halogen atom, oxo, hydroxy, lower alkyl, lower alkoxy, lower alkanoyloxy, lower cycloalkyl, lower cycloalkyloxy, aryl, aryloxy, heterocyclic group or heterocyclic-oxy group; lower cycloalkyl; lower cycloalkyloxy; aryl, aryloxy, heterocyclic group or heterocyclic-oxy group; R.sub.3 is a hydrogen atom, a lower alkyl, lower cycloalkyl, aryl or heterocyclic group, comprising the step of admixing the same with a glyceride.

13. The method of claim 12, in which said bicyclic compound is the compound of formula (I), wherein A is --COOH or functional derivative thereof, X.sub.1 and X.sub.2 are halogen atoms, W.sub.1 is .dbd.O, or where one of R.sub.4 and R.sub.5 is hydrogen, and the other is hydroxy, W.sub.2 is where R.sub.4 and R.sub.5 are both hydrogen atoms, R.sub.1 is a saturated or unsaturated bivalent unsubstituted lower-medium aliphatic hydrocarbon residue, R.sub.2 is a saturated or unsaturated unsubstituted lower-medium aliphatic hydrocarbon residue, R.sub.3 is a hydrogen atom.

14. The method of claim 12, in which the glyceride is a glyceride of a fatty acid having 6-24 carbon atoms.

15. The method of claim 14, in which said glyceride is a glyceride of a fatty acid having 6-20 carbon atoms.

16. The method of claim 12, in which the glyceride is a mixture of 2 or more glycerides.

17. The method of claim 12, wherein said glyceride is admixed with another oil solvent.

18. The method of claim 17, wherein said other oil solvent is mineral oil.

19. The method of claim 12, which is in a dosage form suitable for oral administration.

20. The method of claim 19, which is formulated as a capsule.

21. The method of claim 12, which is in a dosage form suitable for topical administration.

22. The method of claim 21, which is formulated as an eye drop.

23. The composition of claim 1, in which the ratio of bi-cyclic mono-cyclic compound is at least 90:10.

24. The composition of claim 1, in which the ratio of bi-cyclic mono-cyclic compound is substantially 100:0.

25. The composition of claim 1, in which the bi-cyclic compound is 7-[(1R,3R,6R,7R)-3-(1,1-difluoropentyl)-3-hydroxy-2-oxabicyclo[4,3,0]nonan e-8-one-7-yl ]heptanoic acid.
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