JP2013227300A5 - - Google Patents

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Publication number
JP2013227300A5
JP2013227300A5 JP2013068407A JP2013068407A JP2013227300A5 JP 2013227300 A5 JP2013227300 A5 JP 2013227300A5 JP 2013068407 A JP2013068407 A JP 2013068407A JP 2013068407 A JP2013068407 A JP 2013068407A JP 2013227300 A5 JP2013227300 A5 JP 2013227300A5
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Japan
Prior art keywords
aqueous composition
fatty acid
polyoxyethylene sorbitan
sorbitan fatty
acid ester
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JP2013068407A
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Japanese (ja)
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JP5922609B2 (en
JP2013227300A (en
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Publication of JP2013227300A5 publication Critical patent/JP2013227300A5/ja
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Claims (25)

2−アミノ−3−(4−ブロモベンゾイル)フェニル酢酸又はその塩、そして場合によりベンザルコニウム塩化物及び/又はポリオキシエチレンソルビタン脂肪酸エステルを含有する水性組成物であって、2−アミノ−3−(4−ブロモベンゾイル)フェニル酢酸100質量部に対するベンザルコニウム塩化物の含有量A(質量部)とポリオキシエチレンソルビタン脂肪酸エステルの含有量B(質量部)が、
0≦A<1のとき、0≦B<96A+5
A=1のとき、1<B≦100
1<A<3のとき、5<B≦100
3≦A≦10のとき、20<B≦100
の範囲内である、水性組成物、但し
ゲンタマイシン塩酸塩またはトブラマイシンを含有しない
An aqueous composition comprising 2-amino-3- (4-bromobenzoyl) phenylacetic acid or a salt thereof, and optionally benzalkonium chloride and / or polyoxyethylene sorbitan fatty acid ester, comprising 2-amino-3 The content A (parts by mass) of benzalkonium chloride and the content B (parts by mass) of polyoxyethylene sorbitan fatty acid ester with respect to 100 parts by mass of-(4-bromobenzoyl) phenylacetic acid,
When 0 ≦ A <1, 0 ≦ B <96A + 5
When A = 1, 1 <B ≦ 100
When 1 <A <3, 5 <B ≦ 100
When 3 ≦ A ≦ 10, 20 <B ≦ 100
An aqueous composition , wherein
Contains no gentamicin hydrochloride or tobramycin .
ベンザルコニウム塩化物の含有量Aとポリオキシエチレンソルビタン脂肪酸エステルの含有量B が、
0≦A<1のとき、0≦B<26A+5
A=1のとき、2≦B≦30
1<A<3のとき、5<B≦30
3≦A≦5のとき、20<B≦30
の範囲内である、請求項1記載の水性組成物。
Benzalkonium chloride content A and polyoxyethylene sorbitan fatty acid ester content B
When 0 ≦ A <1, 0 ≦ B <26A + 5
When A = 1, 2 ≦ B ≦ 30
When 1 <A <3, 5 <B ≦ 30
When 3 ≦ A ≦ 5, 20 <B ≦ 30
The aqueous composition of claim 1, which is within the range of
ベンザルコニウム塩化物の含有量Aとポリオキシエチレンソルビタン脂肪酸エステルの含有量B が、
1<A<3、及び5<B≦30
の範囲内である、請求項1記載の水性組成物。
Benzalkonium chloride content A and polyoxyethylene sorbitan fatty acid ester content B
1 <A <3 and 5 <B ≦ 30
The aqueous composition of claim 1, which is within the range of
ベンザルコニウム塩化物の含有量Aとポリオキシエチレンソルビタン脂肪酸エステルの含有量B が、
1.2≦A≦2.5、及び7≦B≦20
の範囲内である、請求項1記載の水性組成物。
Benzalkonium chloride content A and polyoxyethylene sorbitan fatty acid ester content B
1.2 ≦ A ≦ 2.5 and 7 ≦ B ≦ 20
The aqueous composition of claim 1, which is within the range of
ベンザルコニウム塩化物の含有量Aとポリオキシエチレンソルビタン脂肪酸エステルの含有量B が、  Benzalkonium chloride content A and polyoxyethylene sorbitan fatty acid ester content B
A=0、及びB=0である、請求項1記載の水性組成物。  The aqueous composition of claim 1, wherein A = 0 and B = 0.
2−アミノ−3−(4−ブロモベンゾイル)フェニル酢酸又はその塩、そして場合によりベンザルコニウム塩化物及び/又はポリオキシエチレンソルビタン脂肪酸エステルを含有する水性組成物であって、ベンザルコニウム塩化物の濃度X(w/v%)とポリオキシエチレンソルビタン脂肪酸エステルの濃度Y(w/v%)が、
0≦X<0.001のとき、0≦Y<96X+0.005
X=0.001のとき、0.001<Y≦0.1
0.001<X<0.003のとき、0.005<Y≦0.1
0.003≦X≦0.01のとき、0.02<Y≦0.1
の範囲内である、水性組成物、但し
ゲンタマイシン塩酸塩またはトブラマイシンを含有しない
An aqueous composition comprising 2-amino-3- (4-bromobenzoyl) phenylacetic acid or a salt thereof, and optionally benzalkonium chloride and / or polyoxyethylene sorbitan fatty acid ester, comprising benzalkonium chloride Concentration X (w / v%) and polyoxyethylene sorbitan fatty acid ester concentration Y (w / v%)
When 0 ≦ X <0.001, 0 ≦ Y <96X + 0.005
When X = 0.001, 0.001 <Y ≦ 0.1
When 0.001 <X <0.003, 0.005 <Y ≦ 0.1
When 0.003 ≦ X ≦ 0.01, 0.02 <Y ≦ 0.1
An aqueous composition , wherein
Contains no gentamicin hydrochloride or tobramycin .
ベンザルコニウム塩化物の濃度Xとポリオキシエチレンソルビタン脂肪酸エステルの濃度Yが、
0≦X<0.001のとき、0≦Y<26X+0.005
X=0.001のとき、0.002≦Y≦0.03
0.001<X<0.003のとき、0.005<Y≦0.03
0.003≦X≦0.005のとき、0.02<Y≦0.03
の範囲内である、請求項記載の水性組成物。
Benzalkonium chloride concentration X and polyoxyethylene sorbitan fatty acid ester concentration Y
When 0 ≦ X <0.001, 0 ≦ Y <26X + 0.005
When X = 0.001, 0.002 ≦ Y ≦ 0.03
When 0.001 <X <0.003, 0.005 <Y ≦ 0.03
When 0.003 ≦ X ≦ 0.005, 0.02 <Y ≦ 0.03
The aqueous composition of claim 6 , which is within the range of
ベンザルコニウム塩化物の濃度Xとポリオキシエチレンソルビタン脂肪酸エステルの濃度Yが、
0.001<X<0.003、及び0.005<Y≦0.03
の範囲内である、請求項記載の水性組成物。
Benzalkonium chloride concentration X and polyoxyethylene sorbitan fatty acid ester concentration Y
0.001 <X <0.003 and 0.005 <Y ≦ 0.03
The aqueous composition of claim 6 , which is within the range of
ベンザルコニウム塩化物の濃度Xとポリオキシエチレンソルビタン脂肪酸エステルの濃度Yが、
0.0012≦X≦0.0025、及び0.008≦Y≦0.02
の範囲内である、請求項記載の水性組成物。
Benzalkonium chloride concentration X and polyoxyethylene sorbitan fatty acid ester concentration Y
0.0012 ≦ X ≦ 0.0025 and 0.008 ≦ Y ≦ 0.02
The aqueous composition of claim 6 , which is within the range of
ベンザルコニウム塩化物の濃度Xとポリオキシエチレンソルビタン脂肪酸エステルの濃度Yが、  Benzalkonium chloride concentration X and polyoxyethylene sorbitan fatty acid ester concentration Y
X=0、及びY=0である、請求項6記載の水性組成物。  The aqueous composition according to claim 6, wherein X = 0 and Y = 0.
ポリオキシエチレンソルビタン脂肪酸エステルが、ポリソルベート80である、請求項1〜10のいずれか一項に記載の水性組成物。 The aqueous composition according to any one of claims 1 to 10 , wherein the polyoxyethylene sorbitan fatty acid ester is polysorbate 80. 水性組成物中の2−アミノ−3−(4−ブロモベンゾイル)フェニル酢酸の濃度が、0.01〜1.0%(w/v)である、請求項1〜11のいずれか一項に記載の水性組成物。 The concentration of 2-amino-3- (4-bromobenzoyl) phenylacetic acid in the aqueous composition is a 0.01 to 1.0% (w / v), to any one of claims 1 to 11 The aqueous composition described. 0.01〜3.0%(w/v)の塩化ナトリウムを更に含有する、請求項1〜12のいずれか一項に記載の水性組成物。 The aqueous composition according to any one of claims 1 to 12 , further comprising 0.01 to 3.0% (w / v) sodium chloride. ホウ酸及び/又はホウ砂を更に含有する、請求項1〜13のいずれか一項に記載の水性組成物。  The aqueous composition according to any one of claims 1 to 13, further comprising boric acid and / or borax. 0.01〜15%(w/v)のホウ酸及び/又はホウ砂を更に含有する、請求項1〜14のいずれか一項に記載の水性組成物。  The aqueous composition according to any one of claims 1 to 14, further comprising 0.01 to 15% (w / v) boric acid and / or borax. 水性組成物のpHが、7.0より大きく9.5以下である、請求項1〜15のいずれか一項に記載の水性組成物。 The aqueous composition according to any one of claims 1 to 15 , wherein the pH of the aqueous composition is greater than 7.0 and not more than 9.5. 医薬的に許容される期間の貯蔵後、水性組成物の外観に変化が認められない、医薬的に安定な請求項1〜16のいずれか一項に記載の水性組成物。  The aqueous composition according to any one of claims 1 to 16, wherein no change is observed in the appearance of the aqueous composition after storage for a pharmaceutically acceptable period. 25℃で3か月間の貯蔵後、水性組成物の外観に変化が認められない、医薬的に安定な請求項1〜17のいずれか一項に記載の水性組成物。  The aqueous composition according to any one of claims 1 to 17, wherein no change is observed in the appearance of the aqueous composition after storage at 25 ° C for 3 months. 40℃で1か月間の貯蔵後、水性組成物の外観に変化が認められない、医薬的に安定な請求項1〜18のいずれか一項に記載の水性組成物。  The aqueous composition according to any one of claims 1 to 18, wherein no change in the appearance of the aqueous composition is observed after storage for 1 month at 40 ° C. 60℃で1か月間の貯蔵後、水性組成物の外観に変化が認められない、医薬的に安定な請求項1〜19のいずれか一項に記載の水性組成物。  The aqueous composition according to any one of claims 1 to 19, wherein no change is observed in the appearance of the aqueous composition after storage at 60 ° C for 1 month. 水性組成物が澄明、黄色、沈殿不含有である、医薬的に安定な請求項1〜20のいずれか一項に記載の水性組成物。  21. A pharmaceutically stable aqueous composition according to any one of the preceding claims, wherein the aqueous composition is clear, yellow, precipitate-free. 水性組成物が、注射剤、輸液、点鼻剤、点耳剤又は点眼剤である請求項1〜21のいずれか一項に記載の水性組成物。 The aqueous composition according to any one of claims 1 to 21 , wherein the aqueous composition is an injection, an infusion solution, a nasal drop, an ear drop or an eye drop. 眼科用注射剤である、請求項22記載の水性組成物。 The aqueous composition according to claim 22 , which is an ophthalmic injection. 点眼剤である、請求項22記載の水性組成物。 The aqueous composition according to claim 22 , which is an eye drop. 請求項1〜24のいずれか一項記載の水性組成物の製造方法であって、2−アミノ−3−(4−ブロモベンゾイル)フェニル酢酸若しくはその塩又はそれらの水和物、並びに場合によりベンザルコニウム塩化物及び/又はポリオキシエチレンソルビタン脂肪酸エステルを水性溶媒に溶解させることを特徴とする製造方法。 25. A method for producing an aqueous composition according to any one of claims 1 to 24 , comprising 2-amino-3- (4-bromobenzoyl) phenylacetic acid or a salt thereof or a hydrate thereof, and optionally benza. A production method comprising dissolving a ruthenium chloride and / or a polyoxyethylene sorbitan fatty acid ester in an aqueous solvent.
JP2013068407A 2012-03-28 2013-03-28 Aqueous composition containing 2-amino-3- (4-bromobenzoyl) phenylacetic acid Expired - Fee Related JP5922609B2 (en)

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JP2012073181 2012-03-28
JP2012073181 2012-03-28
JP2013068407A JP5922609B2 (en) 2012-03-28 2013-03-28 Aqueous composition containing 2-amino-3- (4-bromobenzoyl) phenylacetic acid

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JP2013227300A JP2013227300A (en) 2013-11-07
JP2013227300A5 true JP2013227300A5 (en) 2016-02-04
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JP (1) JP5922609B2 (en)
KR (1) KR20140139501A (en)
CN (1) CN104203224A (en)
IN (1) IN2014DN07767A (en)
MY (1) MY170840A (en)
PH (1) PH12014502171A1 (en)
SG (1) SG11201405837YA (en)
TW (1) TWI604858B (en)
WO (1) WO2013147000A1 (en)

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WO2016199854A1 (en) * 2015-06-10 2016-12-15 参天製薬株式会社 Ophthalmic solution and method for maintaining preservative efficacy of ophthalmic solution
WO2019117252A1 (en) * 2017-12-14 2019-06-20 参天製薬株式会社 Eye drop containing 2-amino-3-(4-bromobenzoyl) phenylacetic acid or salt thereof
CN114224830A (en) * 2021-12-24 2022-03-25 辰欣药业股份有限公司 Single-dose bacteriostatic-free ophthalmic preparation and preparation method thereof

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JP2002308764A (en) * 2001-02-09 2002-10-23 Taisho Pharmaceut Co Ltd Pharmaceutical composition for ophthalmic use
WO2005046700A1 (en) * 2003-11-14 2005-05-26 Senju Pharmaceutical Co., Ltd. Aqueous solution preparation containing aminoglycoside antibiotic and bromfenac
CN1823754A (en) * 2006-03-28 2006-08-30 卢秀莲 Sodium bromophenolate eye drops and its preparation method
CN101313899B (en) * 2007-06-01 2012-02-29 北京德众万全药物技术开发有限公司 Medicament composition for eyes containing sodium bromfenac
BRPI0908502A2 (en) * 2008-02-21 2017-05-23 Ista Pharmaceuticals ophthalmic aines as adjuvants
CN101322683B (en) * 2008-07-30 2013-01-16 浙江三叶药业有限公司 Gel for eye containing bromfenac sodium hydrate and preparation thereof
WO2012099142A1 (en) * 2011-01-18 2012-07-26 千寿製薬株式会社 Bromfenac aqueous liquid composition having preservative efficiency
JP6012231B2 (en) * 2011-04-08 2016-10-25 ロート製薬株式会社 Bromfenac-containing composition

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