JPS6217973B2 - - Google Patents
Info
- Publication number
- JPS6217973B2 JPS6217973B2 JP13031583A JP13031583A JPS6217973B2 JP S6217973 B2 JPS6217973 B2 JP S6217973B2 JP 13031583 A JP13031583 A JP 13031583A JP 13031583 A JP13031583 A JP 13031583A JP S6217973 B2 JPS6217973 B2 JP S6217973B2
- Authority
- JP
- Japan
- Prior art keywords
- sulfur
- glycyrrhizinate
- nonionic surfactant
- eye drops
- drug
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired
Links
- 239000003889 eye drop Substances 0.000 claims description 21
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 20
- 239000011593 sulfur Substances 0.000 claims description 20
- 229910052717 sulfur Inorganic materials 0.000 claims description 20
- 229940079593 drug Drugs 0.000 claims description 15
- 239000003814 drug Substances 0.000 claims description 15
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims description 11
- LPLVUJXQOOQHMX-QWBHMCJMSA-N glycyrrhizinic acid Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@@H]1C([C@H]2[C@]([C@@H]3[C@@]([C@@]4(CC[C@@]5(C)CC[C@@](C)(C[C@H]5C4=CC3=O)C(O)=O)C)(C)CC2)(C)CC1)(C)C)C(O)=O)[C@@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O LPLVUJXQOOQHMX-QWBHMCJMSA-N 0.000 claims description 11
- 239000002736 nonionic surfactant Substances 0.000 claims description 9
- 239000002997 ophthalmic solution Substances 0.000 claims description 7
- 229940054534 ophthalmic solution Drugs 0.000 claims description 6
- VTAJIXDZFCRWBR-UHFFFAOYSA-N Licoricesaponin B2 Natural products C1C(C2C(C3(CCC4(C)CCC(C)(CC4C3=CC2)C(O)=O)C)(C)CC2)(C)C2C(C)(C)CC1OC1OC(C(O)=O)C(O)C(O)C1OC1OC(C(O)=O)C(O)C(O)C1O VTAJIXDZFCRWBR-UHFFFAOYSA-N 0.000 claims description 2
- LPLVUJXQOOQHMX-UHFFFAOYSA-N glycyrrhetinic acid glycoside Natural products C1CC(C2C(C3(CCC4(C)CCC(C)(CC4C3=CC2=O)C(O)=O)C)(C)CC2)(C)C2C(C)(C)C1OC1OC(C(O)=O)C(O)C(O)C1OC1OC(C(O)=O)C(O)C(O)C1O LPLVUJXQOOQHMX-UHFFFAOYSA-N 0.000 claims description 2
- 229960004949 glycyrrhizic acid Drugs 0.000 claims description 2
- 239000001685 glycyrrhizic acid Substances 0.000 claims description 2
- UYRUBYNTXSDKQT-UHFFFAOYSA-N glycyrrhizic acid Natural products CC1(C)C(CCC2(C)C1CCC3(C)C2C(=O)C=C4C5CC(C)(CCC5(C)CCC34C)C(=O)O)OC6OC(C(O)C(O)C6OC7OC(O)C(O)C(O)C7C(=O)O)C(=O)O UYRUBYNTXSDKQT-UHFFFAOYSA-N 0.000 claims description 2
- 235000019410 glycyrrhizin Nutrition 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 229940012356 eye drops Drugs 0.000 description 12
- GEHJYWRUCIMESM-UHFFFAOYSA-L sodium sulfite Chemical compound [Na+].[Na+].[O-]S([O-])=O GEHJYWRUCIMESM-UHFFFAOYSA-L 0.000 description 10
- 238000004040 coloring Methods 0.000 description 9
- -1 sodium thiosulfate Chemical class 0.000 description 8
- 229940074774 glycyrrhizinate Drugs 0.000 description 7
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 6
- 239000003795 chemical substances by application Substances 0.000 description 5
- 235000010265 sodium sulphite Nutrition 0.000 description 5
- 229920001214 Polysorbate 60 Polymers 0.000 description 4
- 230000002265 prevention Effects 0.000 description 4
- ZORQXIQZAOLNGE-UHFFFAOYSA-N 1,1-difluorocyclohexane Chemical compound FC1(F)CCCCC1 ZORQXIQZAOLNGE-UHFFFAOYSA-N 0.000 description 3
- HZAXFHJVJLSVMW-UHFFFAOYSA-N 2-Aminoethan-1-ol Chemical compound NCCO HZAXFHJVJLSVMW-UHFFFAOYSA-N 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 3
- BIVBRWYINDPWKA-VLQRKCJKSA-L Glycyrrhizinate dipotassium Chemical compound [K+].[K+].O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@H]1CC[C@]2(C)[C@H]3C(=O)C=C4[C@@H]5C[C@](C)(CC[C@@]5(CC[C@@]4(C)[C@]3(C)CC[C@H]2C1(C)C)C)C(O)=O)C([O-])=O)[C@@H]1O[C@H](C([O-])=O)[C@@H](O)[C@H](O)[C@H]1O BIVBRWYINDPWKA-VLQRKCJKSA-L 0.000 description 3
- 229940101029 dipotassium glycyrrhizinate Drugs 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 238000002156 mixing Methods 0.000 description 3
- 239000000203 mixture Substances 0.000 description 3
- 239000001593 sorbitan monooleate Substances 0.000 description 3
- 235000011069 sorbitan monooleate Nutrition 0.000 description 3
- 229940035049 sorbitan monooleate Drugs 0.000 description 3
- 229960005404 sulfamethoxazole Drugs 0.000 description 3
- JLKIGFTWXXRPMT-UHFFFAOYSA-N sulphamethoxazole Chemical compound O1C(C)=CC(NS(=O)(=O)C=2C=CC(N)=CC=2)=N1 JLKIGFTWXXRPMT-UHFFFAOYSA-N 0.000 description 3
- 206010015946 Eye irritation Diseases 0.000 description 2
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 2
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 description 2
- DWAQJAXMDSEUJJ-UHFFFAOYSA-M Sodium bisulfite Chemical compound [Na+].OS([O-])=O DWAQJAXMDSEUJJ-UHFFFAOYSA-M 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- ZBCBWPMODOFKDW-UHFFFAOYSA-N diethanolamine Chemical compound OCCNCCO ZBCBWPMODOFKDW-UHFFFAOYSA-N 0.000 description 2
- 231100000013 eye irritation Toxicity 0.000 description 2
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 2
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 2
- 229920000053 polysorbate 80 Polymers 0.000 description 2
- BHZRJJOHZFYXTO-UHFFFAOYSA-L potassium sulfite Chemical compound [K+].[K+].[O-]S([O-])=O BHZRJJOHZFYXTO-UHFFFAOYSA-L 0.000 description 2
- 235000019252 potassium sulphite Nutrition 0.000 description 2
- 235000010267 sodium hydrogen sulphite Nutrition 0.000 description 2
- 150000003467 sulfuric acid derivatives Chemical class 0.000 description 2
- CIVCELMLGDGMKZ-UHFFFAOYSA-N 2,4-dichloro-6-methylpyridine-3-carboxylic acid Chemical compound CC1=CC(Cl)=C(C(O)=O)C(Cl)=N1 CIVCELMLGDGMKZ-UHFFFAOYSA-N 0.000 description 1
- SLXKOJJOQWFEFD-UHFFFAOYSA-N 6-aminohexanoic acid Chemical compound NCCCCCC(O)=O SLXKOJJOQWFEFD-UHFFFAOYSA-N 0.000 description 1
- 239000004354 Hydroxyethyl cellulose Substances 0.000 description 1
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- 229920001213 Polysorbate 20 Polymers 0.000 description 1
- 239000004372 Polyvinyl alcohol Substances 0.000 description 1
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 1
- NHUHCSRWZMLRLA-UHFFFAOYSA-N Sulfisoxazole Chemical compound CC1=NOC(NS(=O)(=O)C=2C=CC(N)=CC=2)=C1C NHUHCSRWZMLRLA-UHFFFAOYSA-N 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 229960002684 aminocaproic acid Drugs 0.000 description 1
- SOYKEARSMXGVTM-UHFFFAOYSA-N chlorphenamine Chemical compound C=1C=CC=NC=1C(CCN(C)C)C1=CC=C(Cl)C=C1 SOYKEARSMXGVTM-UHFFFAOYSA-N 0.000 description 1
- 229960003291 chlorphenamine Drugs 0.000 description 1
- 150000001860 citric acid derivatives Chemical class 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- 229940043237 diethanolamine Drugs 0.000 description 1
- 229960000525 diphenhydramine hydrochloride Drugs 0.000 description 1
- YKZPPPNXRZHVGX-PXYKVGKMSA-L dipotassium;(2s)-2-aminobutanedioate;hydron;hydrate Chemical compound [H+].[H+].O.[K+].[K+].[O-]C(=O)[C@@H](N)CC([O-])=O.[O-]C(=O)[C@@H](N)CC([O-])=O YKZPPPNXRZHVGX-PXYKVGKMSA-L 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- IPCSVZSSVZVIGE-UHFFFAOYSA-M hexadecanoate Chemical compound CCCCCCCCCCCCCCCC([O-])=O IPCSVZSSVZVIGE-UHFFFAOYSA-M 0.000 description 1
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 239000011976 maleic acid Substances 0.000 description 1
- OSZNNLWOYWAHSS-UHFFFAOYSA-M neostigmine methyl sulfate Chemical compound COS([O-])(=O)=O.CN(C)C(=O)OC1=CC=CC([N+](C)(C)C)=C1 OSZNNLWOYWAHSS-UHFFFAOYSA-M 0.000 description 1
- 229960002253 neostigmine methylsulfate Drugs 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 229920000259 polyoxyethylene lauryl ether Polymers 0.000 description 1
- 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 description 1
- 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 description 1
- 239000000249 polyoxyethylene sorbitan monopalmitate Substances 0.000 description 1
- 235000010483 polyoxyethylene sorbitan monopalmitate Nutrition 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 235000019422 polyvinyl alcohol Nutrition 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 229940068988 potassium aspartate Drugs 0.000 description 1
- 239000001103 potassium chloride Substances 0.000 description 1
- 235000011164 potassium chloride Nutrition 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000001509 sodium citrate Substances 0.000 description 1
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
- 229940079827 sodium hydrogen sulfite Drugs 0.000 description 1
- 229940083608 sodium hydroxide Drugs 0.000 description 1
- AKHNMLFCWUSKQB-UHFFFAOYSA-L sodium thiosulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=S AKHNMLFCWUSKQB-UHFFFAOYSA-L 0.000 description 1
- 235000019345 sodium thiosulphate Nutrition 0.000 description 1
- 238000010186 staining Methods 0.000 description 1
- 150000005846 sugar alcohols Polymers 0.000 description 1
- 229960000654 sulfafurazole Drugs 0.000 description 1
- LSNNMFCWUKXFEE-UHFFFAOYSA-L sulfite Chemical class [O-]S([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-L 0.000 description 1
- XOAAWQZATWQOTB-UHFFFAOYSA-N taurine Chemical compound NCCS(O)(=O)=O XOAAWQZATWQOTB-UHFFFAOYSA-N 0.000 description 1
- 150000004764 thiosulfuric acid derivatives Chemical class 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
本発明はスルフアメトキサゾール等のサルフア
剤を含有した点眼液に関し、更に詳述すると着色
防止力の優れたサルフア剤含有点眼液に関する。
従来、点眼液にスルフアメトキサゾール等のサ
ルフア剤を配合することは公知であり、またこの
種のサルフア剤含有点眼液に着色防止力を与える
ため、クエン酸ナトリウム等のクエン酸塩又は、
亜硫酸ナトリウムなどの還元性硫酸塩を添加する
ことも公知である。しかしながら、クエン酸塩又
は、還元性硫酸塩を添加したサルフア剤含有点眼
液の着色防止力は高いものではなく、極めて不十
分なものであつた。この場合、クエン酸塩又は、
還元性硫酸塩の添加量を増やすことには眼刺激な
どの点で問題があり、さらにサルフア剤にグリチ
ルリチン酸塩を配合した点眼液では、着色が激し
く従来のクエン酸塩又は、還元性硫酸塩を添加し
ても着色は防止することができない。このため、
サルフア剤含有点眼液の機能を損なうことなく着
色防止力を効果的に高めることが要望されてい
た。
本発明者らは、上記事情に鑑み、サルフア剤含
有点眼液の着色防止力を向上させることについて
鋭意研究を行なつた結果、サルフア剤にグリチル
リチン酸塩を加えた系に対し、亜硫酸ナトリウム
等の還元性硫酸塩にポリオキシエチレンソルビタ
ンモノオレエート等の親水性ノニオン界面活性剤
を併用する場合には長期保存においても着色せ
ず、この点眼液はその着色防止力が非常に高いも
のであることを知見し、本発明をなすに至つたも
のである。
以下、本発明につき更に詳しく説明する。
本発明に係る点眼液は、サルフア剤、グリチル
リチン酸塩、それに還元性硫酸塩及び親水性ノニ
オン界面活性剤を含有してなるものである。
ここで、サルフア剤としては、スルフアメトキ
サゾール、スルフイソキサゾール等が挙げられ、
これらの１種又は２種以上が使用される。これら
のサルフア剤の配合量は特に制限されないが、通
常点眼液全体の３〜５％（重量／容量％、以下同
じ）である。
また、グリチルリチン酸塩としては、グリチル
リチン酸ジカリウム、グリチルリチン酸アンモニ
ウム等が挙げられ、これらの１種又は２種以上が
使用される。その配合量は特に制限されないが、
通常点眼液全体の0.05〜0.2％である。
なお、サルフア剤にグリチルリチン酸塩を加え
た本発明の点眼液はモノエタノールアミン、ジエ
タノールアミン、水酸化ナトリウム等でPHを7.5
〜9.0とすることが好ましく、PHが低すぎるとサ
ルフア剤の溶解度が減少して析出が生じ、PHが高
すぎると点眼液としての安定性及び安全性に問題
が生じる。
本発明の点眼液は、サルフア剤及びグリチルリ
チン酸塩を含む系に還元性硫酸塩及び親水性ノニ
オン界面活性剤を配合するもので、これにより透
明で顕著な着色防止力を有する点眼液を得ること
ができる。
ここで、還元性硫酸塩としては、亜硫酸ナトリ
ウム、亜硫酸水素ナトリウム、亜硫酸カリウム等
の亜硫酸塩、チオ硫酸ナトリウム等のチオ硫酸塩
等が挙げられ、これらの１種又は２種以上が使用
されるが、特に亜硫酸ナトリウム、亜硫酸水素ナ
トリウム、亜硫酸カリウムが好ましく用いられ
る。また、親水性ノニオン界面活性剤としては、
ポリオキシエチレンソルビタンモノオレエート、
ポリオキシエチレンソルビタンモノパルミテー
ト、ポリオキシエチレンソルビタンモノラウレー
ト等のポリオキシエチレンソルビタンモノ脂肪
酸、ポリオキシエチレンモノステアレート、ポリ
オキシエチレンモノオレエート、ポリオキシエチ
レンモノパルミテート等のポリオキシエチレンモ
ノ脂肪酸類、ポリオキシエチレンラウリルエーテ
ル等のポリオキシエチレンアルコールエーテルな
どの親水性のものが挙げられ、これらの１種又は
２種以上が使用され得る。なお、ポリオキシエチ
レンモル数は使用感の点で10モル以上とすること
が望ましい。
還元性硫酸塩の配合量は、サルフア剤、グリチ
ルリチン酸塩、更にはノニオン界面活性剤の種類
や配合量、還元性硫酸塩の種類等により相違する
が、全体の0.02〜0.2％とすることが好ましい。
0.02％より少ないと十分な着色防止力が得られな
い場合があり、0.2％より多いと安全性及び眼刺
激の点で問題がある場合がある。またノニオン界
面活性剤の配合量は0.05〜0.5％、特に0.05〜0.2
％とすることが好ましい。
本発明の点眼液には、更に必要に応じ、サルフ
ア剤に加えてモノエタノールアミン、ジエタノー
ルアミン、水酸化ナトリウム、塩酸ジフエンヒド
ラミン、アスパラギン酸カリウム、アミノエチル
スルフオン酸、ε−アミノカプロン酸、マレイン
酸クロルフエニラミン、メチル硫酸ネオスチグミ
ン等を配合することができ、また塩化ナトリウ
ム、塩化カリウムなどの等張化剤、多価アルコー
ル、ポリビニルアルコール、ポリビニルピロリド
ン、ハイドロキシエチルセルロース、ハイドロキ
シプロピルセルロースなどの高分子添加剤等を配
合することもできる。
以下、実施例と比較例を示し、本発明を具体的
に説明するが、本発明は下記の実施例に限定され
るものではない。
実施例
第１表に示す処方の点眼液を調製し（なお表中
％はいずれも重量／容量％を示す。）、50℃１ケ月
保存後の着色度合を調べた。
結果を第１表に併記する。
なお評価基準は下記の通りである。
〇：変化を認めず
△：やや褐変
×：褐変
The present invention relates to an ophthalmic solution containing a sulfur drug such as sulfamethoxazole, and more specifically to an ophthalmic solution containing a sulfur drug that has excellent anti-staining properties. Conventionally, it has been known to incorporate sulfur drugs such as sulfur amethoxazole into eye drops, and in order to give this type of sulfur drug-containing eye drops anti-coloring power, citrate salts such as sodium citrate or
It is also known to add reducing sulfates such as sodium sulfite. However, the coloring prevention power of sulfur drug-containing eye drops to which citrate or reducing sulfate was added was not high and was extremely insufficient. In this case, citrate or
Increasing the amount of reducing sulfate added causes problems such as eye irritation, and eye drops containing glycyrrhizinate in addition to sulfur drugs are severely colored, compared to conventional citrate or reducing sulfate. Coloring cannot be prevented even with the addition of . For this reason,
It has been desired to effectively increase the coloring prevention power of sulfur drug-containing eye drops without impairing their functionality. In view of the above circumstances, the present inventors conducted intensive research on improving the coloring prevention power of ophthalmic solutions containing sulfur drugs, and as a result, compared to the system in which glycyrrhizinate was added to sulfur drugs, sodium sulfite, etc. When a hydrophilic nonionic surfactant such as polyoxyethylene sorbitan monooleate is used in combination with a reducing sulfate, no coloration occurs even during long-term storage, and this eye drop has an extremely high ability to prevent coloration. This discovery led to the present invention. The present invention will be explained in more detail below. The eye drops according to the present invention contain a sulfur drug, a glycyrrhizinate, a reducing sulfate, and a hydrophilic nonionic surfactant. Here, examples of sulfur drugs include sulfamethoxazole, sulfisoxazole, etc.
One or more of these may be used. The blending amount of these sulfur drugs is not particularly limited, but is usually 3 to 5% (weight/volume %, hereinafter the same) of the entire eye drop. Furthermore, examples of the glycyrrhizinate include dipotassium glycyrrhizinate, ammonium glycyrrhizinate, and the like, and one or more of these may be used. There are no particular restrictions on its blending amount, but
It is usually 0.05-0.2% of the total eye drops. The ophthalmic solution of the present invention, which is a sulfur drug with glycyrrhizinate added, has a pH of 7.5 with monoethanolamine, diethanolamine, sodium hydroxide, etc.
It is preferable to set it to ~9.0; if the pH is too low, the solubility of the sulfur agent will decrease and precipitation will occur, and if the pH is too high, problems will arise in the stability and safety of the ophthalmic solution. The eye drops of the present invention contain a reducing sulfate and a hydrophilic nonionic surfactant in a system containing a sulfur drug and a glycyrrhizinate, thereby obtaining a transparent eye drop having remarkable anti-coloring power. I can do it. Here, examples of reducing sulfates include sulfites such as sodium sulfite, sodium bisulfite, and potassium sulfite, and thiosulfates such as sodium thiosulfate, and one or more of these may be used. In particular, sodium sulfite, sodium hydrogen sulfite, and potassium sulfite are preferably used. In addition, as a hydrophilic nonionic surfactant,
polyoxyethylene sorbitan monooleate,
Polyoxyethylene sorbitan monofatty acids such as polyoxyethylene sorbitan monopalmitate, polyoxyethylene sorbitan monolaurate, polyoxyethylene monostearate, polyoxyethylene monooleate, polyoxyethylene monopalmitate, etc. Examples include hydrophilic ones such as fatty acids and polyoxyethylene alcohol ethers such as polyoxyethylene lauryl ether, and one or more of these may be used. Note that the number of moles of polyoxyethylene is desirably 10 moles or more from the viewpoint of feeling in use. The amount of the reducing sulfate varies depending on the type and amount of the sulfur agent, glycyrrhizinate, nonionic surfactant, type of reducing sulfate, etc., but it can be 0.02 to 0.2% of the total. preferable.
If it is less than 0.02%, sufficient anti-coloring power may not be obtained, and if it is more than 0.2%, there may be problems in terms of safety and eye irritation. In addition, the amount of nonionic surfactant added is 0.05 to 0.5%, especially 0.05 to 0.2%.
% is preferable. The ophthalmic solution of the present invention further contains monoethanolamine, diethanolamine, sodium hydroxide, diphenhydramine hydrochloride, potassium aspartate, aminoethyl sulfonic acid, ε-aminocaproic acid, maleic acid, in addition to a sulfur agent, as necessary. It can contain acid chlorpheniramine, neostigmine methyl sulfate, etc., and isotonizing agents such as sodium chloride and potassium chloride, polymers such as polyhydric alcohol, polyvinyl alcohol, polyvinylpyrrolidone, hydroxyethyl cellulose, and hydroxypropyl cellulose. Additives etc. can also be blended. EXAMPLES Hereinafter, the present invention will be specifically explained by showing examples and comparative examples, but the present invention is not limited to the following examples. Example Eye drops having the formulations shown in Table 1 were prepared (all % in the table indicates weight/volume %), and the degree of coloration was examined after storage at 50°C for 1 month. The results are also listed in Table 1. The evaluation criteria are as follows. 〇: No change observed △: Slight browning ×: Browning
【表】【table】
【表】
第１表の結果より、サルフア剤（スルフアメト
キサゾール）とグリチルリチン酸又はその塩（グ
リチルリチン酸ジカリウム）を含有する系に還元
性硫酸塩（亜硫酸ナトリウム）と親水性ノニオン
界面活性剤を併用して配合することにより、優れ
た着色防止力を有する点眼液が得られることが知
見された。
実施例 ６
グリチルリチン酸ジカリウムをグリチルリチン
酸アンモニウムとしモノエタノールアミンにより
同一のPHに調製したほかは実施例１と同処方の点
眼液を調製した。
この点眼液の着色防止力は実施例１と同様に十
分満足できるものであつた。
実施例 ７、８
実施例１の処方において、POEソルビタンモ
ノオレート（＝20）の配合量を0.5％とした点
眼液（実施例７）、POEソルビタンモノオレート
（＝20）の代りにPOEソルビタンモノパルミテ
ート（＝20）とした点眼液（実施例８）をそれ
ぞれ調製した。
これらの点眼液も実施例６と同様な効果を有し
ていた。[Table] From the results in Table 1, it was found that a system containing a sulfur agent (sulfamethoxazole) and glycyrrhizic acid or its salt (dipotassium glycyrrhizinate) was combined with a reducing sulfate (sodium sulfite) and a hydrophilic nonionic surfactant. It has been found that an eye drop having excellent anti-coloring ability can be obtained by blending these together. Example 6 An eye drop having the same formulation as in Example 1 was prepared, except that dipotassium glycyrrhizinate was replaced with ammonium glycyrrhizinate and the pH was adjusted to the same level with monoethanolamine. The coloring prevention power of this eye drop was sufficiently satisfactory as in Example 1. Examples 7 and 8 In the formulation of Example 1, eye drops containing 0.5% POE sorbitan monooleate (=20) (Example 7), POE sorbitan monooleate (=20) was replaced with POE sorbitan monooleate (=20). Eye drops containing palmitate (=20) (Example 8) were prepared. These eye drops also had the same effects as in Example 6.
Claims (1)
を含有する点眼液に還元性硫酸塩と親水性ノニオ
ン界面活性剤を配合してなることを特徴とする点
眼液。 ２ 還元性硫酸塩の配合量が全体の0.02〜0.2重
量／容量％である特許請求の範囲第１項記載の点
眼液。 ３ 親水性ノニオン界面活性剤の配合量が全体の
0.05〜0.5重量／容量％である特許請求の範囲第
１項又は第２項記載の点眼液。[Scope of Claims] 1. An eye drop comprising a reducing sulfate and a hydrophilic nonionic surfactant in an eye drop containing a sulfur drug and glycyrrhizic acid or its salt. 2. The eye drop according to claim 1, wherein the amount of the reducing sulfate is 0.02 to 0.2% by weight/volume of the total weight. 3 The amount of hydrophilic nonionic surfactant
The ophthalmic solution according to claim 1 or 2, which contains 0.05 to 0.5% by weight/volume.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP13031583A JPS6023318A (en) | 1983-07-19 | 1983-07-19 | Eye drops |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP13031583A JPS6023318A (en) | 1983-07-19 | 1983-07-19 | Eye drops |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS6023318A JPS6023318A (en) | 1985-02-05 |
| JPS6217973B2 true JPS6217973B2 (en) | 1987-04-21 |
Family
ID=15031380
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP13031583A Granted JPS6023318A (en) | 1983-07-19 | 1983-07-19 | Eye drops |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS6023318A (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5414011A (en) * | 1987-09-11 | 1995-05-09 | Syntex (U.S.A.) Inc. | Preservative system for ophthalmic formulations |
| US5110493A (en) * | 1987-09-11 | 1992-05-05 | Syntex (U.S.A.) Inc. | Ophthalmic NSAID formulations containing a quaternary ammonium preservative and a nonionic surfactant |
-
1983
- 1983-07-19 JP JP13031583A patent/JPS6023318A/en active Granted
Also Published As
| Publication number | Publication date |
|---|---|
| JPS6023318A (en) | 1985-02-05 |
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