A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 47/40 (2006.01) A61K 31/515 (2006.01) A61P 11/06 (2006.01)
Patent
CA 2561660
It was surprisingly found that a-trioxopyrimidine-cyclodextrin-complex formed of a trioxopyrimidine derivative represented by the below-described formula (I) and a water-soluble cyclodextrin (further abbreviated as CD) exhibits enhanced water solubility, excellent stability, and low topical stimulation and is useful as a therapeutic agent. Accordingly, the present invention provides a trioxopyrimidine-cyclodextrin complex formed of a trioxopyrimidine derivative or a salt thereof and a cyclodextrin, preferably .alpha.-, .beta.- or .gamma.-cyclodextrin or a water-soluble cyclodextrin derivative (water- soluble being defined as a solubility of at least 0.5 gr/100ml water at 25~C), wherein the trioxopyrimidine derivative is represented by formula (I). It was furthermore found that such a trioxopyrimidine complex with cyclodextrin and an adjuvant such as L-lysine or L-arginine show improved water solubility and bioavailability, excellent stability, and low topical stimulation and is useful as a therapeutic agent.
L'invention concerne un complexe de trioxopyrimidine-cyclodextrine constitué d'un dérivé de trioxopyrimidine ou d'un sel de celui-ci et un dérivé de cyclodextrine hydrosoluble et possédant une solubilité améliorée.
Bartsch Pierre
Cataldo Didier
Endele Richard
Evrard Brigitte
Foidart Jean-Michel
Borden Ladner Gervais Llp
F. Hoffmann-La Roche Ag
Universite de Liege
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