Antimycotic drug composition
AssigneeTakeda Chemical Industries, Ltd.
InventorsHidetoshi Horibe, Yoko Nishida, Masao Nagao
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Abstract
The composition of the present invention comprises a quaternized nitrogen-containing imidazole-1-yl or 1,2,4-triazole-1-yl compound wherein one of the nitrogen atoms constituting the azole ring is quaternized with a group eliminating in vivo and represented by the formula: wherein R1 represents a hydrocarbon or heterocyclic group which may be substituted, R2 represents a hydrogen atom or a lower alkyl group, and n is 0 or 1, and a saccharide, said compound being capable of being converted into an anti-fungal azole compound upon elimination of said group in vivo. The composition of the present invention is stable and usable particularly as a pharmaceutical preparation for an injection composition.
Claims15
A composition comprising
- a lyophilized quaternized nitrogen-containing imidazole-1-yl or 1,2,4-triazole-1-yl compound wherein one of the nitrogen atoms constituting the azole ring is quaternized with a group eliminating in vivo and represented by the formula:
- wherein
- R1 represents a hydrocarbon or heterocyclic group which may be substituted,
- R2 represents a hydrogen atom or a lower alkyl group, and
- n is 0 or 1, and
- a saccharide,
- said compound being capable of being converted into an anti-fungal azole compound upon elimination of said group in vivo.
A process for producing a lyophilized product, which comprises adding a saccharide to an aqueous solution of a quaternized nitrogen-containing imidazole-1-yl or 1,2,4-triazole-1-yl compound wherein one of the nitrogen atoms constituting the azole ring is quaternized with a group of formula:
- wherein R1 represents a hydrocarbon or heterocyclic group which may be substituted, R2 represents a hydrogen atom or a lower alkyl group, and n is 0 or 1, eliminating in vivo, and then lyophilizing the mixture, said compound being capable of being converted into an anti-fungal azole compound upon elimination of said group in vivo.
A method of stabilizing a quaternized nitrogen-containing imidazole-1-yl or 1,2,4-triazole-1-yl compound in a lyophilized product, which comprises adding a saccharide to an aqueous solution of a quaternized nitrogen-containing imidazole-1-yl or 1,2,4-triazole-1-yl compound wherein one of the nitrogen atoms constituting the azole ring is quaternized with a group of formula:
- wherein R1 represents a hydrocarbon or heterocyclic group which may be substituted, R2 represents a hydrogen atom or a lower alkyl group, and n is 0 or 1, eliminating in vivo, and then lyophilizing the mixture, said compound being capable of being converted into an anti-fungal azole compound upon elimination of said group in vivo.
A method of making a pharmaceutical preparation for injection comprising mixing
- a lyophilized quaternized nitrogen-containing imidazole-1-yl or 1,2,4-triazole-1-yl compound wherein one of the nitrogen atoms constituting the azole ring is quaternized with a group eliminating in vivo and represented by the formula:
- wherein
- R1 represents a hydrocarbon or heterocyclic group which may be substituted,
- R2 represents a hydrogen atom or a lower alkyl group, and
- n is 0 or 1,
- and a saccharide,
- said compound being capable of being converted into an anti-fungal azole compound upon elimination of said group in vivo.
Dependencies are inferred from the claim text.