JP2019142974A5 - - Google Patents

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JP2019142974A5
JP2019142974A5 JP2019096298A JP2019096298A JP2019142974A5 JP 2019142974 A5 JP2019142974 A5 JP 2019142974A5 JP 2019096298 A JP2019096298 A JP 2019096298A JP 2019096298 A JP2019096298 A JP 2019096298A JP 2019142974 A5 JP2019142974 A5 JP 2019142974A5
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aqueous solution
combination
water
salt
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ブリモニジン及び/又はその塩、水溶性高分子、及びクロルヘキシジングルコン酸塩を含有する水性液剤であって、
ブリモニジン及び/又はその塩の含有量が0.05w/v%〜0.2w/v%であり、水溶性高分子の含有量が0.05w/v%〜3w/v%であり、クロルヘキシジングルコン酸塩の含有量が0.001w/v%〜0.01w/v%である、水性液剤
An aqueous solution containing brimonidine and / or a salt thereof, a water-soluble polymer, and chlorhexidine gluconate ,
The content of brimonidine and / or a salt thereof is 0.05 w / v% to 0.2 w / v%, the content of a water-soluble polymer is 0.05 w / v% to 3 w / v%, and chlorhexidine glucone An aqueous solution, wherein the content of the acid salt is 0.001 w / v% to 0.01 w / v% .
ブリモニジン及び/又はその塩と、水溶性高分子と、クロルヘキシジングルコン酸塩との重量比が1:1〜15:0.01〜0.1である、請求項に記載の水性液剤。 The aqueous liquid preparation according to claim 1 , wherein the weight ratio of brimonidine and / or a salt thereof, the water-soluble polymer, and chlorhexidine gluconate is 1: 1 to 15: 0.01 to 0.1. 該水溶性高分子が、ポリビニル系高分子化合物、セルロース系高分子化合物、及び天然高分子化合物から選択される1種又は2種以上の組合せを含む、請求項1または2に記載の水性液剤。The aqueous liquid preparation according to claim 1, wherein the water-soluble polymer includes one or a combination of two or more selected from a polyvinyl polymer compound, a cellulose polymer compound, and a natural polymer compound. 該ポリビニル系高分子化合物が、ポリビニルピロリドン、ポリビニルアルコール、及びカルボキシビニルポリマーからなる群より選択される1種又は2種以上の組合せを含み、The polyvinyl polymer compound includes one or a combination of two or more selected from the group consisting of polyvinylpyrrolidone, polyvinyl alcohol, and carboxyvinyl polymer,
該セルロース系高分子化合物が、カルボキシメチルセルロース、ヒドロキシエチルセルロース、メチルセルロース、ヒドロキシプロピルセルロース、及びヒドロキシプロピルメチルセルロースからなる群より選択される1種又は2種以上の組合せを含み、  The cellulosic polymer compound includes one or a combination of two or more selected from the group consisting of carboxymethylcellulose, hydroxyethylcellulose, methylcellulose, hydroxypropylcellulose, and hydroxypropylmethylcellulose,
該天然高分子が、キサンタンガム、コンドロイチン硫酸ナトリウム、及びヒアルロン酸ナトリウムからなる群より選択される1種又は2種以上の組合せを含む、請求項1〜3のいずれか一項に記載の水性液剤。  The aqueous solution according to any one of claims 1 to 3, wherein the natural polymer comprises one or a combination of two or more selected from the group consisting of xanthan gum, sodium chondroitin sulfate, and sodium hyaluronate.
水性液剤を60℃で4週間保管した後の該水性液剤の粘度を当該4週間保管する前の該水性液剤の粘度で除して算出した粘度安定性が、90%以上である、請求項1〜のいずれか一項に記載の水性液剤。 The viscosity stability calculated by dividing the viscosity of the aqueous solution after storing the aqueous solution at 60 ° C. for 4 weeks by the viscosity of the aqueous solution before storage for 4 weeks is 90% or more. The aqueous liquid preparation according to any one of claims 4 to 4 . 該水性液剤が眼科用である、請求項1〜のいずれか一項に記載の水性液剤。 The aqueous solution according to any one of claims 1 to 5 , wherein the aqueous solution is for ophthalmology. 該眼科用の水性液剤が点眼剤である、請求項に記載の水性液剤。 The aqueous solution according to claim 6 , wherein the ophthalmic aqueous solution is an eye drop. 緑内障を治療するための、請求項1〜のいずれか一項に記載の水性液剤。 The aqueous solution according to any one of claims 1 to 7 , for treating glaucoma. 水性液剤の粘度低下を抑制する方法であって、水溶性高分子を含有する水性液剤中にブリモニジン及び/又はその塩と、クロルヘキシジングルコン酸塩と両方を共存させる工程を含ブリモニジン及び/又はその塩の含有量が0.05w/v%〜0.2w/v%であり、水溶性高分子の含有量が0.05w/v%〜3w/v%であり、クロルヘキシジングルコン酸塩の含有量が0.001w/v%〜0.01w/v%である、粘度低下を抑制する方法。 A method of inhibiting the viscosity reduction of aqueous solutions, see containing a brimonidine and / or its salt in an aqueous solution containing a water-soluble polymer, a process to co-exist both chlorhexidine gluconate, brimonidine and / Or the content of a salt thereof is 0.05 w / v% to 0.2 w / v%, the content of a water-soluble polymer is 0.05 w / v% to 3 w / v%, and the content of chlorhexidine gluconate is A method for suppressing a decrease in viscosity, wherein the content is 0.001 w / v% to 0.01 w / v% . ブリモニジン及び/又はその塩と、水溶性高分子と、クロルヘキシジングルコン酸塩との重量比が1:1〜15:0.01〜0.1である、請求項に記載の方法。 The method according to claim 9 , wherein the weight ratio of brimonidine and / or a salt thereof, the water-soluble polymer, and chlorhexidine gluconate is 1: 1 to 15: 0.01 to 0.1. 該水溶性高分子が、ポリビニル系高分子化合物、セルロース系高分子化合物、及び天然高分子化合物から選択される1種又は2種以上の組合せを含む、請求項9または10に記載の方法。The method according to claim 9, wherein the water-soluble polymer includes one or a combination of two or more selected from a polyvinyl-based polymer compound, a cellulose-based polymer compound, and a natural polymer compound. 該ポリビニル系高分子化合物が、ポリビニルピロリドン、ポリビニルアルコール、及びカルボキシビニルポリマーからなる群より選択される1種又は2種以上の組合せを含み、The polyvinyl polymer compound includes one or a combination of two or more selected from the group consisting of polyvinylpyrrolidone, polyvinyl alcohol, and carboxyvinyl polymer,
該セルロース系高分子化合物が、カルボキシメチルセルロース、ヒドロキシエチルセルロース、メチルセルロース、ヒドロキシプロピルセルロース、及びヒドロキシプロピルメチルセルロースからなる群より選択される1種又は2種以上の組合せを含み、  The cellulosic polymer compound includes one or a combination of two or more selected from the group consisting of carboxymethylcellulose, hydroxyethylcellulose, methylcellulose, hydroxypropylcellulose, and hydroxypropylmethylcellulose,
該天然高分子が、キサンタンガム、コンドロイチン硫酸ナトリウム、及びヒアルロン酸ナトリウムからなる群より選択される1種又は2種以上の組合せを含む、請求項9〜11のいずれか一項に記載の方法。  The method according to any one of claims 9 to 11, wherein the natural polymer comprises one or a combination of two or more selected from the group consisting of xanthan gum, sodium chondroitin sulfate, and sodium hyaluronate.
水溶性高分子を含有する水性液剤の粘度低下を抑制するための、ブリモニジン及び/又はその塩と、クロルヘキシジングルコン酸塩と両方を含有する粘度低下抑制剤であって、
水溶性高分子の濃度が0.05w/v%〜3w/v%となるように用いられ、
ブリモニジン及び/又はその塩の含有量が0.05w/v%〜0.2w/v%であり、クロルヘキシジングルコン酸塩の含有量が0.001w/v%〜0.01w/v%となるように配合される、粘度低下抑制剤
To suppress the reduction viscosity of the aqueous solution containing a water-soluble polymer, brimonidine and / or a salt thereof, a viscosity reducing inhibitor comprising both chlorhexidine gluconate,
Used so that the concentration of the water-soluble polymer is 0.05 w / v% to 3 w / v%,
The content of brimonidine and / or a salt thereof is 0.05 w / v% to 0.2 w / v%, and the content of chlorhexidine gluconate is 0.001 w / v% to 0.01 w / v%. A viscosity reduction inhibitor that is blended in .
ブリモニジン及び/又はその塩と、水溶性高分子と、クロルヘキシジングルコン酸塩との重量比が1:1〜15:0.01〜0.1となるように配合される、請求項13に記載の粘度低下抑制剤。 14. The composition according to claim 13 , wherein the weight ratio of brimonidine and / or a salt thereof, the water-soluble polymer, and chlorhexidine gluconate is 1: 1 to 15: 0.01 to 0.1. Viscosity reduction inhibitor. 該水溶性高分子が、ポリビニル系高分子化合物、セルロース系高分子化合物、及び天然高分子化合物から選択される1種又は2種以上の組合せを含む、請求項13または14に記載の粘度低下抑制剤 15. The method according to claim 13, wherein the water-soluble polymer comprises one or a combination of two or more selected from a polyvinyl polymer, a cellulose polymer, and a natural polymer. Agent . 該ポリビニル系高分子化合物が、ポリビニルピロリドン、ポリビニルアルコール、及びカルボキシビニルポリマーからなる群より選択される1種又は2種以上の組合せを含み、
該セルロース系高分子化合物が、カルボキシメチルセルロース、ヒドロキシエチルセルロース、メチルセルロース、ヒドロキシプロピルセルロース、及びヒドロキシプロピルメチルセルロースからなる群より選択される1種又は2種以上の組合せを含み、
該天然高分子が、キサンタンガム、コンドロイチン硫酸ナトリウム、及びヒアルロン酸ナトリウムからなる群より選択される1種又は2種以上の組合せを含む、請求項13〜15いずれか一項に記載の粘度低下抑制剤
The polyvinyl polymer compound includes one or a combination of two or more selected from the group consisting of polyvinylpyrrolidone, polyvinyl alcohol, and carboxyvinyl polymer,
The cellulosic polymer compound includes one or a combination of two or more selected from the group consisting of carboxymethylcellulose, hydroxyethylcellulose, methylcellulose, hydroxypropylcellulose, and hydroxypropylmethylcellulose,
The viscosity reduction inhibitor according to any one of claims 13 to 15, wherein the natural polymer includes one or a combination of two or more selected from the group consisting of xanthan gum, sodium chondroitin sulfate, and sodium hyaluronate. .
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WO2020175525A1 (en) * 2019-02-27 2020-09-03 参天製薬株式会社 Ophthalmic composition containing diquafosol or salt thereof, vinyl-based polymer and cellulose-based polymer
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