JP2014098030A - 蒸発亢進型ドライアイの予防又は改善用水性点眼剤 - Google Patents
蒸発亢進型ドライアイの予防又は改善用水性点眼剤 Download PDFInfo
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Images
Abstract
刺激が少なく安全で、べとつきがなく使用感の良い涙液の蒸発亢進に伴うドライアイ及びその諸症状の予防又は改善に有効な水性点眼剤を提供する。
【解決手段】
油分及びムコ多糖を含有することを特徴とする水性点眼剤。
【選択図】なし
Description
精製水に、塩化ナトリウム、塩化カリウム及びヒアルロン酸ナトリウムをそれぞれ0.05質量%、0.1質量%、0.05質量%になるように溶解し、ホウ酸、ホウ砂、グリセリンを用いて、pH7.4、浸透圧286mOsmの点眼剤100mLを調製した。
グリセリン(日本薬局方適合品)10.0gに精製水67.5gを加え均一にした後、70℃に加温して、撹拌しながらポリソルベート80(ニッコールTO−10M、日光ケミカルズ社製)10.0gを添加し分散させた。70℃で加温しながら、ヒマシ油(日本薬局方適合品)12.5gを添加し、ホモジナイザー(ヒスコトロン(商品名)、日立製作所製)で攪拌し、予備乳化物を得た。この乳化物を高圧ホモジナイザー(PANDA 2K型、Niro Soavi S.p.A)を用いて、微細な乳化物を得た。得られた乳化物を精製水で10倍に希釈する過程において、浸透圧調製のためにマンニトールを加え、浸透圧286mOsmの点眼剤を100mL調製した。
グリセリン(日本薬局方適合品)29.8gに精製水43.2gを加え均一にした後、70℃に加温して、撹拌しながらポリオキシエチレン硬化ヒマシ油60(ニッコールHCO−60、日光ケミカルズ社製)7.0gを添加した。70℃で加温しながら、ヒマシ油(日本薬局方適合品)20gを添加し、ホモジナイザー(ヒスコトロン(商品名)、日立製作所製)で攪拌し、予備乳化物を得た。この乳化物を高圧ホモジナイザー(PANDA 2K型、Niro Soavi S.p.A)を用いて、微細な乳化物を得た。
グリセリン(日本薬局方適合品)58.2gに精製水19.6gを加え均一にした後、70℃に加温し、撹拌しながら水素添加大豆レシチン(レシノールS−10M(商品名)、日光ケミカルズ社製)2.2gを添加し分散させた。70℃で加温しながら、ヒマシ油(日本薬局方適合品)20gを添加し、ホモジナイザー(ヒスコトロン(商品名)、日立製作所製)で攪拌し、予備乳化物を得た。この乳化物を高圧ホモジナイザー(ミニラボ830H(商品名)、ラニー社製)を用いて乳化し、微細な乳化物を得た。
製造例1及び2で得られた乳化物を精製水で希釈する過程において、表1に示す各成分を溶解させ、浸透圧調整のためグリセリンを加え、表1記載の点眼剤を各々100mLずつ調製した。
ヒマシ油をそれぞれ、大豆油、流動パラフィンに変更して製造例2と同様の方法で微細な乳化物を調製し、精製水で希釈する過程において、表2に示す各成分を溶解させ、浸透圧調整のためグリセリンを加え、表2記載の点眼剤を各々100mLずつ調製した。
ヒマシ油をオリーブ油に変更し、さらにポリソルベート80を加え、製造例2と同様の方法で微細な乳化物を調製し、精製水で希釈する過程において、表2に示す各成分を溶解させ、浸透圧調整のためグリセリンを加え、表2記載の点眼剤を100mL調製した。
ヒマシ油をスクワランに変更して製造例1と同様の方法で微細な乳化物を調製し、精製水で希釈する過程において、表2に示す各成分を溶解させ、浸透圧調整のためグリセリンを加え、表2記載の点眼剤を100mL調製した。
眼表面からの水分蒸散量は、TEWAMETER TM300(COURAGE+KHAZAKA electronic GmbH社製)を用いて測定した。体重約2.5kgの雄性日本白色ウサギ(北山ラベス)を押田式固定器にて固定後、ベノキシール0.4質量%点眼液(商品名、参天製薬)を50μL点眼し、眼表面麻酔を施した。5分後、結膜嚢内の涙液を拭き取り、被験点眼サンプルを50μL点眼し、10分後、20分後、30分後の眼表面からの水分蒸散量を測定した。水分蒸散量は、点眼直前の値を100%とし、下記の計算式より、変化率を算出した。なお各群の例数は5とした。
結果を表2に示す。
%X:水分蒸散量の変化率、x:各測定時間の水分蒸散量、y:点眼直前の蒸散量
涙液油層の観察には、ドライアイ観察装置DR−1(興和株式会社製)を用いた。DR−1は、角膜に白色光を照射し、その反射光をビデオカメラにより測定する装置である。涙液層は角膜表面から、粘液層、水層及び油層の三層構造からなっている。本装置は油層表面と油層裏面(水層との境界面)で反射される光の干渉像を測定している。すなわち、本装置により得られる干渉像は、涙液油層の状態を示している。一般に、本装置により得られる干渉像は、健常眼では、均一な灰色又は白色が観察され、蒸発亢進型ドライアイでは、油層が不均一になるため、赤や青の色が混ざった像が観察される。さらに重度なドライアイでは、油層が存在しないため干渉像が消失し、角膜が露出した状態になる(「あたらしい眼科」14(11)、1605−1612、1997、)
Am.J.Ophthalmol.、122、818−824、1996 参照)。
結果を図1〜図8に示す。
○:油層を形成した状態
△:一部角膜が露出した状態
×:角膜が露出した状態
Claims (2)
- 油分及びムコ多糖を含有することを特徴とする水性点眼剤。
- 油分及びムコ多糖を含有することを特徴とする蒸発亢進型ドライアイの予防又は改善用水性点眼剤。
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