TWI671082B - 陰離子性軟式隱形眼鏡用眼科用組成物 - Google Patents
陰離子性軟式隱形眼鏡用眼科用組成物 Download PDFInfo
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- TWI671082B TWI671082B TW103131935A TW103131935A TWI671082B TW I671082 B TWI671082 B TW I671082B TW 103131935 A TW103131935 A TW 103131935A TW 103131935 A TW103131935 A TW 103131935A TW I671082 B TWI671082 B TW I671082B
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- Prior art keywords
- anionic
- scl
- pranoprofen
- salt
- ophthalmic composition
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- 229960003101 pranoprofen Drugs 0.000 claims abstract description 69
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Abstract
本發明之目的在於提供一種針對含有普拉洛芬及/或其鹽之陰離子性SCL用眼科用組成物，抑制普拉洛芬及/或其鹽吸附於陰離子性SCL之技術。在含有普拉洛芬及/或其鹽之陰離子性SCL用眼科用組成物當中，使其含有牛磺酸及/或其鹽，且將pH設定為7.7以下，藉此能有效地抑制普拉洛芬及/或其鹽吸附於陰離子性SCL。
Description
本發明係有關於一種能抑制普拉洛芬及/或其鹽吸附於陰離子性軟式隱形眼鏡之陰離子性軟式隱形眼鏡用眼科用組成物。又，本發明係有關於一種抑制普拉洛芬及/或其鹽吸附於陰離子性軟式隱形眼鏡之方法。
近年來開發出拋棄式與可長時間連續配戴之軟式隱形眼鏡(以下亦簡稱為SCL)，SCL配戴者持續增加。作為SCL，以往已開發出表現有陰離子性、兩性離子性、非離子性等各種表面特性者，而陰離子性SCL具有透氧性優異、對於角膜負擔較少之優點，近年來受到廣泛使用。因此，為了提高陰離子性SCL配戴者之便利性，需要有在配戴陰離子性SCL之狀態下可以使用的點眼劑(陰離子性SCL用點眼劑)。
關於SCL用點眼劑，其製劑設計上必須發揮所欲藥效，還加上不會對SCL產生不良影響。特別是，SCL用點眼劑中的藥物若吸附在SCL，會造成鏡片變形、使用感低落等，還會有對於眼黏膜無法獲得所欲藥理效果之狀況，
故在SCL用點眼劑之製劑設計上，抑制藥物吸附在SCL上變成特別重要的課題。又，藥物之吸附特性會根據SCL表面特性而改變，故SCL用點眼劑之製劑設計上必須對應所適用SCL之材料。
另一方面，普拉洛芬及/或其鹽具有抑制造成發炎或疼痛原因之前列腺素的生物合成之作用，在眼科領域上，以眼睛充血或癢等症狀之緩和、及眼瞼炎、結膜炎、包含上鞏膜炎之鞏膜炎、術後發炎、前眼色素層炎等之預防或治療為目的被廣泛地使用。關於含有普拉洛芬及/或其鹽之SCL用點眼劑之製劑技術亦已有數種被提出。例如專利文獻1中，揭露了含有維生素A類與牛磺酸之非離子性聚矽氧水凝膠隱形眼鏡用之眼科組成物，能抑制脂質吸附在非離子性聚矽氧水凝膠隱形眼鏡表面。然而，專利文獻1中關於普拉洛芬吸附於SCL並無研討，且亦無揭露可適用在陰離子性SCL之技術。
又，以往亦有研討關於抑制藥物吸附於SCL之製劑技術。例如，專利文獻2中，揭露了包含有(A)於具有2級胺基及/或3級胺基之胺及其鹽中所選出之鹼性藥物、及(B)含有從胺基酸及其鹽、酸性黏多醣及其鹽、及環糊精中所選出1種或2種以上之物質，且pH3.5~4.8之軟式隱形眼鏡用組成物，其可抑制鹼性藥物吸附於SCL。然而，專利文獻2中並無研討任何有關於抑制普拉洛芬吸附於陰離子性SCL，且因pH值不得不設定為3.5~4.8，故在製劑設計上的限制上也有問題。
專利文獻1：日本專利特開2011-111425號公報
專利文獻2：國際公開第2007/77783號
在以往已對普拉洛芬及/或其鹽有所注目，但關於其對於陰離子性SCL之吸附特性完全沒有討論。在此狀況下，透過本發明者確認到普拉洛芬及/或其鹽之吸附性對陰離子性SCL相較於對非離子性SCL為高(參照後述試驗例1)。因此，若欲將含有普拉洛芬及/或其鹽之陰離子性SCL用眼科用組成物進行實用化，則當務之急為確立能抑制普拉洛芬及/或其鹽吸附於陰離子性SCL。
在此，本發明係針對含有普拉洛芬及/或其鹽之陰離子性SCL用眼科用組成物，以提供一種抑制普拉洛芬及/或其鹽吸附於陰離子性SCL之技術為目的。
本發明者為了解決前述課題而進行深入研討時，發現了在含有普拉洛芬及/或其鹽之陰離子性SCL用眼科用組成物中，使其含有牛磺酸及/或其鹽，且將pH設定為7.7以下，藉此能有效地抑制普拉洛芬及/或其鹽吸附於陰離子性SCL。此外，發現了藉由將前述陰離子性SCL用眼科用組成物之pH設定為5.5以上，能實現清澈之外觀性狀。本發明
係以該見解為基礎，加上反覆研討而完成者。
亦即，本發明提供下述揭示態樣之發明。
項1.一種陰離子性軟式隱形眼鏡用眼科用組成物，其特徵在於含有普拉洛芬及/或其藥學上容許之鹽、與牛磺酸及/或其藥學上容許之鹽，且pH為7.7以下。
項2.如項1之陰離子性軟式隱形眼鏡用眼科用組成物，其pH為5.5~7.7。
項3.如項1或項2之陰離子性軟式隱形眼鏡用眼科用組成物，其中含0.01~3w/v%牛磺酸及/或其藥學上容許之鹽。
項4.如項1至3中任一項之陰離子性軟式隱形眼鏡用眼科用組成物，其中含0.001~0.5w/v%普拉洛芬及/或其藥學上容許之鹽。
項5.如項1至4中任一項之陰離子性軟式隱形眼鏡用眼科用組成物，其為陰離子性軟式隱形眼鏡用點眼劑。
項6.一種抑制普拉洛芬及/或其藥學上容許之鹽吸附於陰離子性軟式隱形眼鏡之方法，其特徵在於在含有普拉洛芬及/或其藥學上容許之鹽的陰離子性軟式隱形眼鏡用眼科用組成物當中，添加牛磺酸及/或其藥學上容許之鹽，且將pH調整為7.7以下。
項7.一種液劑用於製造陰離子性軟式隱形眼鏡用眼科用組成物之用途，該液劑含有普拉洛芬及/或其藥學上容許之鹽、與牛磺酸及/或其藥學上容許之鹽，且pH為7.7以下。
藉由本發明之陰離子性SCL用眼科用組成物，能
抑制普拉洛芬及/或其鹽吸附於陰離子性SCL，故對於陰離子性SCL不會產生壞影響，而能有效發揮普拉洛芬及/或其鹽之藥效。又，藉由本發明之陰離子性SCL用眼科用組成物，其中牛磺酸及/或其鹽不僅發揮抑制普拉洛芬及/或其鹽吸附於陰離子性SCL之作用，亦發揮眼睛之新陳代謝促進作用，故與普拉洛芬及/或其鹽之藥效相輔相成，亦能達到優異的預防眼疾與回復效果。
又，在本發明之陰離子性SCL用眼科用組成物中，藉由將pH設定為5.5以上，亦能抑制起因於普拉洛芬及/或其鹽之白濁，能夠提供呈現清澈之外觀性狀的陰離子性SCL用眼科用組成物。又，本說明書中，所謂「清澈」係指沒有產生起因於普拉洛芬及/或其鹽之白濁的狀態，係不限於無色清澈，亦包含了根據其他含有成份而呈現顏色之有色清澈之概念。
1.陰離子性SCL用眼科用組成物
本發明之陰離子性SCL用眼科用組成物之特徵在於含有普拉洛芬及/或其藥學上容許之鹽、與牛磺酸及/或其藥學上容許之鹽，且pH為7.7以下。以下將詳細說明本發明之陰離子性SCL用眼科用組成物。又，本說明書中，所謂「陰離子性SCL用眼科用組成物」係指使用於眼科領域，且係
以與陰離子性SCL接觸之態樣所使用之組成物。又，本說明書中，各成份之濃度單位「w/v%」係指質量對容量百分率，其與g/100mL同義。
本發明之陰離子性SCL用眼科用組成物含有普拉洛芬及/或其鹽。所謂普拉洛芬，亦被稱為α-甲基-5H-[1]苯并吡喃[2,3-b]吡啶-7-醋酸，係已知在眼科領域具有消炎作用之周知化合物。
作為普拉洛芬之鹽，只要在藥學上被容許為限，則並無特別限制，可舉例如鈉鹽、鉀鹽、鈣鹽、鎂鹽、鋁鹽等金屬鹽；三乙胺鹽、二乙胺鹽、嗎福林鹽、哌嗪鹽等有機鹼鹽等。該等普拉洛芬之鹽可單獨使用1種，亦可組合2種以上來使用。
本發明之陰離子性SCL用眼科用組成物中，可由普拉洛芬及其鹽之中選擇1種單獨使用，亦可組合2種以上來使用。普拉洛芬及其鹽當中可舉出普拉洛芬為較佳者。
本發明之陰離子性SCL用眼科用組成物中，關於普拉洛芬及/或其鹽之濃度，可因應該陰離子性SCL用眼科用組成物之用途等來作適宜設定，可舉例如0.001~0.5w/v%，較佳為0.01~0.2w/v%，更佳為0.01~0.1w/v%。
本發明之陰離子性SCL用眼科用組成物更含有牛磺酸及/或其鹽。本發明之陰離子性SCL用眼科用組成物藉由使前述普拉洛芬及/或其鹽與牛磺酸及/或其鹽共存，使抑制普拉洛芬及/或其鹽吸附於陰離子性SCL變得可行。
牛磺酸亦被稱作胺基乙磺酸，化學名為2-胺基乙
磺酸。在眼科領域中，係亦以促進眼睛新陳代謝之目的等而被使用之公知化合物。
作為牛磺酸之鹽，只要在藥學上被容許為限，則並無特別限制，可舉例如鈉鹽、鉀鹽等鹼金屬鹽等。該等牛磺酸之鹽可單獨使用1種，亦可組合2種以上來使用。
本發明之陰離子性SCL用眼科用組成物中，可由牛磺酸及其鹽之中選擇1種單獨使用，亦可組合2種以上來使用。牛磺酸及其鹽當中可舉出牛磺酸為較佳者。
本發明之陰離子性SCL用眼科用組成物中，關於牛磺酸及/或其鹽之濃度，可舉例如0.01~3w/v%。特別是，從更有效地抑制普拉洛芬及/或其鹽吸附於陰離子性SCL之觀點來看，作為牛磺酸及/或其鹽之濃度，可舉出0.1~3w/v%，較佳為0.1~1w/v%。
本發明之陰離子性SCL用眼科用組成物的pH設定為7.7以下。本發明之陰離子性SCL用眼科用組成物藉由使前述普拉洛芬及/或其鹽與牛磺酸及/或其鹽共存，且設定成如此之pH範圍，會使抑制普拉洛芬及/或其鹽吸附於陰離子性SCL變得可行。
又，如後述試驗例所示，在含有普拉洛芬及/或其鹽之組成物中，確認到若pH變為4.5以下會產生起因於普拉洛芬及/或其鹽之白濁，但將pH設定成5.5以上則會呈現清澈之外觀性狀。有鑑於此點，作為本發明之陰離子性SCL用眼科用組成物之pH值，從更有效地抑制普拉洛芬及/或其鹽吸附於陰離子性SCL，同時使其具有清澈之外觀性狀的
觀點來看，係以5.5~7.7為佳，可舉出6.5~7.7為較佳，更佳為6.5~7.4，最佳為6.5~7.0。
本發明之陰離子性SCL用眼科用組成物的pH欲調整成前述範圍時，使用在眼科用組成物中一般被使用之pH調整劑或緩衝劑即可。作為pH調整劑，可舉例如氫氧化鈉、氫氧化鉀等鹼；醋酸、檸檬酸、鹽酸、磷酸、酒石酸等酸。該等pH調整劑可單獨使用1種，亦可組合2種以上來使用。又，作為緩衝劑，可舉例如磷酸緩衝劑、硼酸緩衝劑、檸檬酸緩衝劑、酒石酸緩衝劑、醋酸緩衝劑、胺基酸、三羥甲基氨基甲烷等。該等緩衝劑可單獨使用1種，亦可組合2種以上來使用。
本發明之陰離子性SCL用眼科用組成物中除了前述成份之外，還可因應需要而含有普拉洛芬及/或其鹽以外之藥理成份。作為該藥理成份，可舉例如甘草酸二鉀、尿囊素、□-胺己酸、溴芬酸、酮咯酸氨丁三醇、奈帕芬胺、氯化小蘖鹼、硫酸鹽小蘗鹼、薁磺酸鈉、硫酸鋅、乳酸鋅、溶菌酶鹽酸鹽等消炎劑；馬來酸氯苯那敏、鹽酸苯海拉明等抗組織胺劑；色甘酸鈉、富馬酸酮替芬、阿扎司特、氨來呫諾、吡嘧司特鉀、曲尼司特、異丁司特等抗過敏劑；諾氟沙星、氧氟沙星、洛美沙星、左氟沙星、見大黴素、加替沙星等抗菌劑；抗壞血酸、黃素腺嘌呤二核苷酸鈉、氰鈷胺、鹽酸吡哆醇、乙酸生育酚、視黃醇乙酸酯、視黃醇棕櫚酸酯、泛醇、泛酸鈣、泛酸鈉等維生素類；天門冬醯胺、硫酸軟骨素鈉等胺基酸類，硫酸甲酯新斯狄明等抗
膽鹼酯酶劑；奈甲嘧唑啉、四氫唑啉、腎上腺素、麻黃素、脫羥腎上腺素、dl-甲基麻黃鹼等血管收縮劑；玻糖醛酸鈉等角結膜上皮障礙治療藥；磺胺嘧啶、磺胺異惡唑、磺胺二甲嘧啶、磺胺二甲氧嘧啶、磺胺甲氧嗒肼、磺胺甲氧惡唑、球磺胺、磺胺甲氧甲嘧啶、磺胺苯唑、磺胺胍、鄰苯二甲醯磺胺塞唑、琥珀醯磺胺塞唑等磺胺劑等。此處所例示之化合物只要以藥學上容許為限，可為鹽之型態，亦可為其他鹽之型態。該等藥理成份可單獨使用1種，亦可組合2種以上來使用。
關於該等藥理成份之濃度，可因應藥理成份之種類或陰離子性SCL用眼科用組成物之用途等來作適宜設定。
又，本發明之陰離子性SCL用眼科用組成物中，除了前述成份之外，還可因應需要而含有等張度劑、溶解輔助劑、黏稠劑、鉗合劑、清涼劑、防腐劑、安定劑、界面活性劑等添加劑。
作為等張度劑，可舉出山梨醇、葡萄糖、甘露醇等糖類；甘油、丙二醇等多價醇類；氯化鈉等鹽類；硼酸等。該等等張度劑可單獨使用1種，亦可組合2種以上來使用。
作為溶解輔助劑，可舉例如單油酸山梨醇多乙烯、聚氧乙烯硬化蓖麻油、泰洛沙泊、普朗尼克等非離子性界面活性劑；甘油、聚乙烯二醇等多價醇等。該等溶解輔助劑可單獨使用1種，亦可組合2種以上來使用。
作為黏稠劑，可舉例如聚乙烯吡咯烷酮、聚乙二醇、聚乙烯醇、羧基乙烯聚合物、三仙膠、硫酸軟骨素鈉、玻糖醛酸鈉等水溶性高分子；羥丙基甲基纖維素、羥乙基纖維素、甲基纖維素、羥丙基纖維素、羥丙基甲基纖維素、羧甲基纖維素鈉等纖維素類等。該等黏稠劑可單獨使用1種，亦可組合2種以上來使用。
作為鉗合劑，可舉出依地酸鹽、檸檬酸或其鹽等。該等鉗合劑可單獨使用1種，亦可組合2種以上來使用。
作為清涼劑，可舉出1-薄荷腦、龍腦、樟腦、桉樹油等。該等清涼劑可單獨使用1種，亦可組合2種以上來使用。
作為防腐劑，可舉出山梨酸或其鹽、苯甲酸或其鹽、對羥苯甲酸甲酯、對羥苯甲酸乙酯、對羥苯甲酸丙酯、氯丁醇、葡萄糖酸洛赫西定、硼酸、脫氫醋酸或其鹽、氯化苄烷銨、氯化苄乙氧銨、苄醇、氯化鋅、對氯間二甲苯酚、氯甲苯酚、苄甲醇、泊利氯銨、乙汞硫柳酸鈉、二丁基羥基甲苯等。該等防腐劑可單獨使用1種，亦可組合2種以上來使用。
作為安定劑，可舉出聚乙烯吡咯烷酮、亞硫酸鹽、單乙醇胺、甘油、丙二醇、環糊精、聚葡萄醣、抗壞血酸、依地酸鹽、生育酚、二丁基羥基甲苯等。該等安定劑可單獨使用1種，亦可組合2種以上來使用。
作為界面活性劑，可舉出泰洛沙泊、聚氧乙烯硬化蓖麻油、聚氧乙烯聚氧丙烯嵌段共聚物、聚氧乙烯山梨
醇酐脂肪酸酯、辛苯聚醇等非離子性界面活性劑；烷基二胺乙基甘胺酸、月桂基二甲基胺乙酸芐鹼等兩性界面活性劑；烷基硫酸鹽、N-醯基牛磺酸鹽、聚氧乙烯烷基醚磷酸鹽、聚氧乙烯烷基醚硫酸鹽等陰離子性界面活性劑；烷基吡啶鹽、烷基胺鹽等陽離子性界面活性劑等。該等界面活性劑可單獨使用1種，亦可組合2種以上來使用。
關於該等添加劑之濃度，可因應添加劑之種類或陰離子性SCL用眼科用組成物之用途等來作適宜設定。
關於本發明之陰離子性SCL用眼科用組成物之製劑型態，係為含有水作為基劑之液劑即可，例如水溶液狀、乳液狀等任一者皆可，可舉出水溶液狀為較佳者。
本發明之陰離子性SCL用眼科用組成物可因應其用途，依據本身周知之調製法來製造即可，例如可使用第十六改正日本藥局方之製劑總則所記載之方法來製造。
本發明之陰離子性SCL用眼科用組成物可使用作為陰離子性SCL配戴中亦可點眼之點眼劑(陰離子性SCL用點眼劑)；陰離子性SCL配戴中亦可洗眼之洗眼劑(陰離子性SCL用洗眼劑)；陰離子性SCL用配戴用液、陰離子性SCL用多功能溶液、陰離子性SCL用洗淨液、陰離子性SCL用保存液等隱形眼鏡保養用品等。該等之中，可舉出較佳為陰離子性SCL用點眼劑、陰離子性SCL用洗眼劑，更佳為陰離子性SCL用點眼劑。
作為本發明適用對象之陰離子性SCL係以包含有含陰離子性基單體之聚合物作為構成材料之SCL。作為
陰離子性SCL，可舉例如以含羧基、磺基、磷酸基等陰離子性基之聚合物作為構成材料之SCL，更具體來說，可舉出伊他富康A(etafilconA)、維富康A(vifilconA)、歐庫富康D(ocufilcon D)、瑪西富康A(methafilconA)等材料之SCL。陰離子性SCL之材料及製法係屬周知。
又，作為本發明適用對象之陰離子性SCL可為高含水率或低含水率之任一者，可舉出高含水率者，亦即被分類在美國食藥管理局(FDA)之群組IV(離子性單體1莫耳%以上，含水率50%以上)者為較佳。
2.抑制普拉洛芬及/或其鹽吸附於陰離子性SCL之方法(1)
另外，本發明提供一種抑制普拉洛芬及/或其鹽吸附於陰離子性SCL之方法，其特徵在於在含有普拉洛芬及/或其藥學上容許之鹽的陰離子性SCL用眼科用組成物當中，添加牛磺酸及/或其藥學上容許之鹽，且將pH調整為7.7以下。該抑制吸附方法有益於對陰離子性SCL用眼科用組成物賦予抑制普拉洛芬及/或其鹽吸附於陰離子性SCL的作用。
於本發明之抑制吸附方法中，關於所使用之普拉洛芬及/或其藥學上容許之鹽的種類及濃度、牛磺酸及/或其藥學上容許之鹽的種類及濃度、陰離子性SCL用眼科用組成物之pH值，添加於陰離子性SCL用眼科用組成物之藥理成份與添加劑之種類、陰離子性SCL用眼科用組成物之製劑型態與用途、作為適用對象之陰離子性SCL之種類等，係如同前述「1.陰離子性SCL用眼科用組成物」之欄所記
載。
3.抑制普拉洛芬及/或其鹽吸附於陰離子性SCL之方法(2)
另外，本發明提供一種抑制普拉洛芬及/或其鹽吸附於陰離子性SCL之方法，其包含將含有普拉洛芬及/或其藥學上容許之鹽、牛磺酸及/或其藥學上容許之鹽，且pH為7.7以下的液劑與陰離子性SCL接觸之步驟。
於本發明之抑制吸附方法中，關於所使用之普拉洛芬及/或其藥學上容許之鹽的種類及濃度、牛磺酸及/或其藥學上容許之鹽的種類及濃度、液劑之pH值，添加於液劑之藥理成份與添加劑之種類、液劑之製劑型態與用途、作為適用對象之陰離子性SCL之種類等，係如同前述「1.陰離子性SCL用眼科用組成物」之欄所記載。又，於本發明之抑制吸附方法中，使前述液劑與陰離子性SCL接觸之方法係依據該液劑之用途來作適宜設定即可。例如，若前述液劑為點眼劑時，將前述液劑對著配戴有陰離子性SCL之眼進行點眼即可。
以下將舉出實施例並具體說明本發明，然而本發明並非受該等實施例所限定者。
試驗例1
將表1所示各成份以常規方法進行混合，藉此調製試驗液。對所獲得之各試驗液之外觀進行觀察，並測定濁度(660nm下的吸光度)，評價有無白濁。
另外，將各試驗液3mL裝入小瓶(vial container)，將1枚SCL浸漬於其中，在25℃下震盪2小時以上。又，將各試驗液3mL裝入小瓶並在無SCL浸漬於其中的狀態下，在25℃下震盪2小時以上。震盪後以液相色層分析法測定各試驗液中的普拉洛芬含量，依據下述之式算出於SCL上之普拉洛芬吸附量。又，已確認到在SCL浸漬於試驗液之條件下進行震盪時，因於SCL上普拉洛芬之吸附會在2小時內達成平衡狀態，如將震盪時間設定為2小時以上，於SCL上之普拉洛芬吸附量的測定值不會有影響。
[數1]吸附於1枚SCL之普拉洛芬的量(μg)=(CC-CT)×V
CC：無SCL浸漬之試驗液中的普拉洛芬含量(μg/mL)
CT：有SCL浸漬之試驗液中的普拉洛芬含量(μg/mL)
V：試驗所使用之試驗液的量(mL)
又，本試驗中使用下述2種SCL，求出對於各SCL之普拉洛芬的吸附量。
鏡片1：群組IV，販售名「1-day acuvue(註冊商標)」(Johnson & Johnson株式會社製)，陰離子性，USAN名：etafilcon A
鏡片2：聚矽氧水凝膠隱形眼鏡，群組I，販售名「AIR OPTIX 2-week(註冊商標)」(CIBA Vision株式會社製)，USAN名：lotrafilcon B
所得結果顯示於表1。由比較例5之結果可知，已確認到陰離子性SCL相較於非離子性聚矽氧水凝膠隱形眼
鏡，普拉洛芬的吸附量較多。另一方面，含有普拉洛芬及牛磺酸、且pH為7.7以下之試驗液(實施例1~3)中，顯著地抑制了普拉洛芬吸附於陰離子性SCL。相對於此，pH在8.0以上、且含有普拉洛芬及牛磺酸之試驗液(比較例2及4)中，相較於不含牛磺酸之情況，不僅沒有抑制普拉洛芬吸附於陰離子性SCL，反而還有助長之現象。由以上結果來看，可清楚瞭解到藉由含有普拉洛芬與牛磺酸及/或其鹽、且pH設定為7.7以下，能抑制普拉洛芬吸附於陰離子性SCL。又，pH為5.5以上的所有試驗液都沒有確認到白濁，呈現清澈之外觀性狀。
表中，各添加成份之添加量的單位為「w/v%」。又，n.m.表示未測定。
試驗例2
將表2及3所示各成份以常規方法進行混合，藉此調製試驗液。對所獲得之各試驗液之外觀進行觀察，並測定濁度(660nm下的吸光度)，藉此評價有無白濁。又，對於所獲得之各試驗液，以與前述試驗例1相同之方法測定對於陰離子性SCL之普拉洛芬吸附量。
所得結果顯示於表2及3。由此結果可知，在pH5.5~7.7之間，藉由使之含有將普拉洛芬與各種濃度之牛磺酸組合者，確認到能抑制普拉洛芬吸附於陰離子性SCL。又，pH為5.5~7.7的所有試驗液都沒有確認到白濁，呈現清澈之外觀性狀。
表中，各添加成份之添加量的單位為「w/v%」。
表中，各添加成份之添加量的單位為「w/v%」。
試驗例3
將表4所示各成份以常規方法進行混合，藉此調製試驗液。對所獲得之各試驗液之外觀進行觀察，並測定濁度(660nm下的吸光度)，藉此評價有無白濁。
所獲得之結果顯示於表4。由表4可知，在pH4.5以下之情況，在任一含有普拉洛芬之試驗液中皆確認到白濁。根據上述試驗例1及2之結果，明白到藉由使之含有普拉洛芬與牛磺酸及/或其鹽、且pH設定為5.5以上，能呈現清澈之外觀性狀，且能抑制普拉洛芬吸附於陰離子性SCL。
表中，各添加成份之添加量的單位為「w/v%」。
Claims (9)
- 一種抑制普拉洛芬及/或其藥學上容許之鹽吸附於陰離子性軟式隱形眼鏡之方法，其特徵在於在含有普拉洛芬及/或其藥學上容許之鹽的陰離子性軟式隱形眼鏡用眼科用組成物當中，添加牛磺酸及/或其藥學上容許之鹽，且將pH調整為7.7以下。
- 一種液劑用於製造陰離子性軟式隱形眼鏡用眼科用組成物之用途，該液劑含有普拉洛芬及/或其藥學上容許之鹽、與牛磺酸及/或其藥學上容許之鹽，且pH為7.7以下。
- 如請求項2之用途，其中陰離子性軟式隱形眼鏡根據美國食藥管理局所規定之分類屬於群組IV。
- 如請求項2或3之用途，其中陰離子性軟式隱形眼鏡在材料方面是含有伊他富康A(EtafilconA)。
- 如請求項2或3之用途，其中，在液劑中含有0.5~3w/v%牛磺酸及/或其藥學上容許之鹽。
- 如請求項2或3之用途，其中液劑之pH為5.5~7.7。
- 如請求項2或3之用途，其中，在前述液劑中含有0.001~0.5w/v%普拉洛芬及/或其藥學上容許之鹽。
- 如請求項2或3之用途，其中，前述陰離子性軟式隱形眼鏡用眼科用組成物為陰離子性軟式隱形眼鏡用點眼劑。
- 一種抑制普拉洛芬及/或其藥學上容許之鹽吸附於陰離子性軟式隱形眼鏡之方法，其特徵在於含有下述步驟：使含有普拉洛芬及/或其藥學上容許之鹽與牛磺酸及/或其藥學上容許之鹽、且pH為7.7以下之液劑，在活體外(in vitro)，接觸陰離子性軟式隱形眼鏡。
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| JP (1) | JP6449773B2 (zh) |
| CN (1) | CN105555268B (zh) |
| HK (1) | HK1220921A1 (zh) |
| RU (1) | RU2677665C2 (zh) |
| TW (1) | TWI671082B (zh) |
| WO (1) | WO2015041192A1 (zh) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2017105752A (ja) * | 2015-08-31 | 2017-06-15 | ロート製薬株式会社 | 眼科組成物 |
| CN114786726A (zh) * | 2019-11-29 | 2022-07-22 | 千寿制药株式会社 | 软性隐形眼镜用药物组合物 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010143882A (ja) * | 2008-12-19 | 2010-07-01 | Rohto Pharmaceut Co Ltd | シリコーンハイドロゲルコンタクトレンズ用点眼剤 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1905453E (pt) * | 2005-07-13 | 2012-12-04 | Santen Pharmaceutical Co Ltd | Composição conservante para utilização oftálmica |
| JP5616617B2 (ja) * | 2008-12-10 | 2014-10-29 | ロート製薬株式会社 | シリコーンハイドロゲルコンタクトレンズ用点眼剤 |
| JP5709482B2 (ja) * | 2009-12-01 | 2015-04-30 | ロート製薬株式会社 | シリコーンハイドロゲルコンタクトレンズ用眼科組成物 |
| JP5650947B2 (ja) * | 2010-07-29 | 2015-01-07 | ロート製薬株式会社 | イオン性シリコーンハイドロゲルコンタクトレンズ用眼科組成物 |
| JP5340498B1 (ja) * | 2013-03-11 | 2013-11-13 | 千寿製薬株式会社 | ソフトコンタクトレンズ用眼科用組成物 |
-
2014
- 2014-09-16 CN CN201480050791.7A patent/CN105555268B/zh not_active Expired - Fee Related
- 2014-09-16 TW TW103131935A patent/TWI671082B/zh not_active IP Right Cessation
- 2014-09-16 RU RU2016111956A patent/RU2677665C2/ru not_active IP Right Cessation
- 2014-09-16 JP JP2015537911A patent/JP6449773B2/ja not_active Expired - Fee Related
- 2014-09-16 WO PCT/JP2014/074346 patent/WO2015041192A1/ja active Application Filing
-
2016
- 2016-08-01 HK HK16109147.5A patent/HK1220921A1/zh unknown
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010143882A (ja) * | 2008-12-19 | 2010-07-01 | Rohto Pharmaceut Co Ltd | シリコーンハイドロゲルコンタクトレンズ用点眼剤 |
Also Published As
| Publication number | Publication date |
|---|---|
| JPWO2015041192A1 (ja) | 2017-03-02 |
| RU2677665C2 (ru) | 2019-01-18 |
| CN105555268A (zh) | 2016-05-04 |
| WO2015041192A1 (ja) | 2015-03-26 |
| JP6449773B2 (ja) | 2019-01-09 |
| TW201542242A (zh) | 2015-11-16 |
| HK1220921A1 (zh) | 2017-05-19 |
| CN105555268B (zh) | 2019-05-10 |
| RU2016111956A3 (zh) | 2018-07-06 |
| RU2016111956A (ru) | 2017-10-23 |
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