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Stable aqueous solution composition containing sulfonamide compound

An aqueous solution and composition technology, applied in the field of aqueous solution composition, can solve problems such as poor patient compliance

Inactive Publication Date: 2011-06-15
ASAHI KASEI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, in the case of concomitant use of multiple drugs, there is a problem that the patient's compliance deteriorates, and there is a demand for drugs that can achieve a strong intraocular pressure lowering effect with as few drugs as possible in the medical field.

Method used

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  • Stable aqueous solution composition containing sulfonamide compound
  • Stable aqueous solution composition containing sulfonamide compound
  • Stable aqueous solution composition containing sulfonamide compound

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0081] [Example 1] Preparation of (S)-1-(4-chloro-5-isoquinolinesulfonyl)-3-(methylamino)pyrrolidine monohydrochloride

[0082] According to the method described in International Patent Publication No. WO2007 / 026664 pamphlet, (S)-1-(4-chloro-5-isoquinolinesulfonyl)-3-(methyl amino)pyrrolidine, which was dissolved in water (52 mL). The solution was vigorously stirred, and a 2 mol / L sodium hydroxide aqueous solution (4.13 mL, manufactured by Wako Pure Chemical Industries, Ltd.) was slowly added dropwise under ice-cooling. After the resulting suspension was further stirred at room temperature for 1 hour, dichloromethane (30 mL) was added, and the organic layer was separated. The aqueous layer was further extracted with dichloromethane (30 mL), and the combined organic layers were washed with water (50 mL), and dried over anhydrous magnesium sulfate. The solvent was distilled off under reduced pressure, and ethyl acetate (10 mL) and n-hexane (20 mL) were added to the residue. T...

example 2

[0085] [Example 2] Preparation of (S)-1-(4-chloro-5-isoquinolinesulfonyl)-3-(methylamino)pyrrolidine monohydrochloride aqueous solution not containing citric acid or its salt

[0086] (1) Physiological saline solution

[0087] Make a solvent by dissolving 18g of sodium chloride in 2L of distilled water. Add 60 mL of solvent to dissolve 12 mg of (S)-1-(4-chloro-5-isoquinolinesulfonyl)-3-(methylamino)pyrrolidine monohydrochloride, and measure the pH.

[0088] (2) 10mM phosphate buffer (pH6) solution

[0089] Dissolve 0.78 g of sodium dihydrogen phosphate dihydrate in 500 mL of the solvent of Example 2 (1). A solution obtained by dissolving 1.432 g of disodium hydrogenphosphate dodecahydrate in 400 mL of the solvent of Example 2 (1) was added to 50 mL of this liquid to adjust the pH to 6.0, and this was prepared as a 10 mM phosphate buffer (pH 6) solvent. Add 60mL of 10mM phosphate buffer (pH6) solvent to 12mg of (S)-1-(4-chloro-5-isoquinolinesulfonyl)-3-(methylamino)pyrrolidi...

example 3

[0152] [Example 3] Preparation of (S)-1-(4-chloro-5-isoquinolinesulfonyl)-3-aminopyrrolidine monohydrochloride

[0153] Hydrochloride (5.500 g) of (S)-1-(4-chloro-5-isoquinolinesulfonyl)-3-aminopyrrolidine obtained by the method described in International Patent Publication No. WO2007 / 026664 pamphlet Dissolve in water (50mL). The solution was vigorously stirred, and a 1 mol / L sodium hydroxide aqueous solution (29.32 mL, manufactured by Wako Pure Chemical Industries, Ltd.) was slowly added dropwise under ice-cooling. Ethyl acetate (300 mL) and water (20 mL) were added, and the organic layer was distilled off. The aqueous layer was further extracted with dichloromethane, and the combined organic layers were washed with water and dried over anhydrous magnesium sulfate. The solvent was distilled off under reduced pressure, and ethyl acetate (35 mL) and n-hexane (105 mL) were added to the residue. The precipitated solid was filtered, washed with n-hexane / ethyl acetate mixture (4...

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Abstract

Disclosed is an aqueous solution composition which contains (S)-1-(4-chloro-5-isoquinolinesulfonyl)-3-aminopyrrolidine or (S)-1-(4-chloro-5-isoquinolinesulfonyl)-3- (methylamino)pyrrolidine as an active ingredient, does not contain citric acid or a salt thereof, and has high stability so that the composition can be stored at room temperature.

Description

technical field [0001] The present invention relates to an aqueous solution composition containing a sulfonamide compound or a pharmaceutically acceptable salt thereof excellent in lowering intraocular pressure, and having high stability for storage at room temperature. Background technique [0002] Normally, the aqueous humor circulates continuously in the eyeball to maintain a certain intraocular pressure. However, if the flow in the trabeculae, which is the outlet of the aqueous humor, gradually decreases, or if the anterior chamber angle narrows and the flow of the aqueous humor is blocked, the intraocular pressure in the eyeball rises, and as a result, the optic nerve is compressed causing Glaucoma with abnormal vision or ocular hypertension that is likely to develop into glaucoma over a long period of time without abnormal vision. In the treatment of glaucoma or ocular hypertension, it is necessary to reduce the increased intraocular pressure, although sympathomimetic...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4725A61K9/08A61K47/04A61K47/12A61K47/18A61P27/02
CPCA61K9/0048A61K31/4725A61K9/08A61P27/02A61P27/06A61K47/02
Inventor 神泽义仁片山和彦西尾文秀
Owner ASAHI KASEI PHARMA
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