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combination

An aqueous composition and compound technology, applied in the directions of drug combination, drug delivery, amide active ingredients, etc., can solve the problem of undisclosed storage stability, and achieve the effect of inhibiting discoloration

Inactive Publication Date: 2020-07-28
KOWA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, Patent Document 5 only discloses that a solution containing 0.4% Ripasudil and an eye drop containing 0.05% latanoprost are sequentially dripped into the same eye of a cynomolgus monkey. Or storage it in a container, and its storage stability over time, etc. are not disclosed at all.

Method used

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Examples

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Embodiment

[0111] Hereinafter, the present invention will be further described with reference to examples, but the present invention is not limited to these examples at all.

[0112] However, in the following test examples, Ripasudil 1 hydrochloride dihydrate can be produced, for example, by the method described in International Publication No. 2006 / 057397 pamphlet.

manufacture example 1～27

[0137] An aqueous composition containing the components and quantities (amount (g) per 100 mL of the aqueous composition) shown in Tables 4 to 6 was produced according to a conventional method.

[0138]

[0139]

[0140]

manufacture example 28～54

[0142] Instead of Ripasudil 1 hydrochloride dihydrate in Production Examples 1 to 27, an equivalent amount of 4-bromo-5-{[(2S)-2-methyl-1,4-diazepane-1 -yl]sulfonyl}isoquinoline, the aqueous compositions of Production Examples 28 to 54 can be produced by a conventional method.

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Abstract

The present invention provides a technique for suppressing discoloration of an aqueous composition containing a halogenated isoquinoline derivative during high-temperature storage. An aqueous composition containing a compound represented by the following general formula (1) [wherein, X represents a halogen atom], a salt thereof, or a solvate thereof, and prostaglandins.

Description

technical field [0001] The present invention relates to aqueous compositions and the like. Background technique [0002] The following structural formulas are known: [0003] [0004] The shown Ripasudil (chemical name: 4-fluoro-5-{[(2S)-2-methyl-1,4-diazepan-1-yl]sulfonyl}isoquinoline) and the following structural formula : [0005] [0006] The halogenated isoquinoline derivatives such as 4-bromo-5-{[(2S)-2-methyl-1,4-diazepan-1-yl]sulfonyl}isoquinoline have Pharmacological actions such as Rho kinase inhibitory action (for example, Patent Documents 1 and 2) are useful for the prevention and treatment of eye diseases. Specifically, it is reported that it is suitable for the prevention or treatment of ocular hypertension and glaucoma (for example, Patent Document 3), or the prevention or treatment of fundus diseases such as age-related macular degeneration (for example, Patent Document 4). [0007] Therefore, it is extremely useful to establish a technique for stab...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/551A61K9/08A61K31/5575A61K47/14A61P27/02A61P27/06A61P43/00
CPCA61K47/14A61K9/08A61K31/5575A61P27/06A61K31/551A61K31/18A61K31/502A61K2300/00A61K9/0048A61K45/06C08L23/12
Inventor 泽井勇
Owner KOWA CO LTD