JP5209827B2 - 薬物徐放性医療用デバイス - Google Patents
薬物徐放性医療用デバイス Download PDFInfo
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- JP5209827B2 JP5209827B2 JP2012545418A JP2012545418A JP5209827B2 JP 5209827 B2 JP5209827 B2 JP 5209827B2 JP 2012545418 A JP2012545418 A JP 2012545418A JP 2012545418 A JP2012545418 A JP 2012545418A JP 5209827 B2 JP5209827 B2 JP 5209827B2
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
前記薬物の徐放率が、薬物の放出開始から24時間経過時では50wt%以下である、前記薬物徐放性医療用デバイスが提供される。
前記薬物の徐放率が、薬物の放出開始から4時間経過時では25wt%以下であり、かつ、薬物の放出開始から24時間経過時では50wt%以下であることを特徴とする前記薬物徐放方法が提供される。
本発明の薬物徐放性医療用デバイスは、薬物を保持する両親媒性ハイドロゲルを含むものである。また、本発明の薬物徐放性医療用デバイスにおいて、薬物の徐放率は、薬物の放出開始から24時間経過時では50wt%以下であり、好ましくは薬物の放出開始から4時間経過時では25wt%以下であり、かつ、薬物の放出開始から24時間経過時では50wt%以下である。
薬物の徐放率(wt%)=(所定時間経過後の薬物放出量/薬物取込量全量)×100
との関係式により求められる。
両親媒性ハイドロゲルを構成するモノマーの混合物に重合開始剤を添加し、撹拌および溶解することによりモノマー混合液を得る工程、得られたモノマー混合液を所望の成形型に入れ、共重合反応により共重合体を得る工程、共重合体を冷却および成形型から剥離し、必要に応じて切削、研磨した後に、成形した共重合体を水和膨潤させてハイドロゲルを得る工程、および、得られたハイドロゲルを、薬物を溶解させた溶液中に浸漬して、ハイドロゲルの内部に薬物を保持させた薬物徐放性医療用デバイスを得る工程。
医療用デバイスを膨潤させ余分な水分を拭き取った後、含水状態のデバイスの重量(W1)を測定した。その後、60℃の乾燥機にて一晩乾燥させ、乾燥状態のデバイスの重量(W2)を測定し、各々の重量より含水率を算出した。
含水率(重量%)=[(W1−W2)/W1]×100
医療用デバイスを25℃、10mLのメタノール中に浸漬させ、24時間静置した。デバイスを取出した後、メタノール中に含有された薬物量をHPLC(日本分光(株)社製;カラム Phenomenex Luna C18 5μ 150×4.6mm)を用いて定量し、得られた値を薬物取込量とした。
医療用デバイスを25℃または37℃、10mLの整理食塩水中に浸漬させ、各々について一定時間(4,8,24,72時間)経過後の浸漬液をサンプリングし、その浸漬液に含有される薬物量をHPLC(日本分光(株)社製;カラム Phenomenex Luna C18 5μ 150×4.6mm)を用いて定量した。その値を取込量全量に対する100分率で表し、薬物徐放性に対する評価を行った。
徐放率(%)=(各時間経過後徐放量/取込量全量)×100
得られた医療用デバイスについて評価を行った結果を表1、ならびに図1および図2に示す。実施例1〜3では、初期バーストが抑えられ、また、72時間以上の薬物徐放が可能であり、薬物の徐放性が制御された。
MAA;メタクリル酸
MOESA;2−メタクリロイルオキシエチルコハク酸
TM0701;サイラプレーンTM−0701(チッソ社製:3−トリス(トリメチルシロキシ)シリルプロピルメタクリレート)
FM0711;サイラプレーンFM−0711(チッソ社製:末端メタクリロイルオキシポリジメチルシロキサン)
SIA0198;3−メチルジメトキシシリルプロピルアクリレート(Gelest社製)
8F;1H、1H、5H−オクタフルオロペンチルアクリレート
DMAA;ジメチルアクリルアミド
NVP;N−ビニルピロリド ン
HEMA;2−ヒドロキシエチルメタクリレート
DNBAAm;N,N−ジ−n−ブチルメタクリルアミド
EDMA;エチレングリコールジメタクリレート
1,9−NDA;1,9−ノナンジオールジメタクリレート
AIBN;アゾビスイソブチロニトリル。
Claims (5)
- カチオン性官能基を有する水溶性薬物を保持する両親媒性ハイドロゲルを含む薬物徐放性医療用コンタクトレンズであって、
前記薬物の徐放率が、薬物の放出開始から24時間経過時では50wt%以下であり、かつ、
前記両親媒性ハイドロゲルが、5〜15wt% シリコーン含有モノマーと5〜15wt% カルボキシル基およびメタクリル基を有するイオン性モノマーとを含むモノマー混合液を共重合して得られる共重合体である
前記薬物徐放性医療用コンタクトレンズ。 - 前記薬物の徐放率が、薬物の放出開始から4時間経過時では25wt%以下である、請求項1に記載の薬物徐放性医療用コンタクトレンズ。
- 前記両親媒性ハイドロゲルが10〜15wt% シリコーン含有モノマーと10〜15wt% カルボキシル基およびメタクリル基を有するイオン性モノマーとを含むモノマー混合液を共重合して得られる共重合体である、請求項1に記載の薬物徐放性医療用コンタクトレンズ。
- 前記両親媒性ハイドロゲルが1から3個のモノアルキルシロキシ基、ジアルキルシロキシ基、またはトリアルキルシロキシ基を有するシリコーン含有モノマーである、請求項1に記載の薬物徐放性医療用コンタクトレンズ。
- 前記イオン性モノマーがアニオン性モノマーである、請求項1に記載の薬物徐放性医療用コンタクトレンズ。
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JPS62103028A (ja) * | 1985-08-16 | 1987-05-13 | ボーシュ アンド ローム インコーポレイテイド | 疎水性ポリマ−系を含む持効性製剤 |
JPH01503072A (ja) * | 1987-01-07 | 1989-10-19 | チヤン,シン‐シウン | 湿潤性、親水性、軟性及び酸素透過性の共重合体組成物 |
JP2009204770A (ja) * | 2008-02-27 | 2009-09-10 | Toray Ind Inc | 眼用レンズ |
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IL50250A (en) * | 1975-08-27 | 1980-01-31 | Hydrophilics Int Inc | Sustained release compositions comprising slats of pharmaceutically acitve bases with polymers containing acid groups |
AU618817B2 (en) * | 1988-07-05 | 1992-01-09 | Novartis Ag | Dimethylacrylamide-copolymer hydrogels with high oxygen permeability |
JP3929014B2 (ja) * | 2000-02-24 | 2007-06-13 | Hoyaヘルスケア株式会社 | 側鎖にポリシロキサン構造を有するマクロマーからなるコンタクトレンズ材料 |
JP5238115B2 (ja) * | 2002-09-18 | 2013-07-17 | 株式会社シード | 薬物徐放性高分子ゲル及びそれからなる眼用レンズ |
JP4379778B2 (ja) | 2003-04-03 | 2009-12-09 | 株式会社シード | 薬物徐放性眼用レンズ |
JP2005218780A (ja) | 2004-02-09 | 2005-08-18 | Menicon Co Ltd | 薬物放出速度を制御し得る薬物徐放可能なヒドロゲル材料の製造方法 |
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JPS62103028A (ja) * | 1985-08-16 | 1987-05-13 | ボーシュ アンド ローム インコーポレイテイド | 疎水性ポリマ−系を含む持効性製剤 |
JPH01503072A (ja) * | 1987-01-07 | 1989-10-19 | チヤン,シン‐シウン | 湿潤性、親水性、軟性及び酸素透過性の共重合体組成物 |
JP2009204770A (ja) * | 2008-02-27 | 2009-09-10 | Toray Ind Inc | 眼用レンズ |
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CN103282053B (zh) | 2014-10-22 |
MY183421A (en) | 2021-02-18 |
EP2650021A4 (en) | 2013-12-04 |
EP2650021B1 (en) | 2015-12-09 |
KR20130023358A (ko) | 2013-03-07 |
SG187547A1 (en) | 2013-03-28 |
EP2650021A1 (en) | 2013-10-16 |
KR101311134B1 (ko) | 2013-09-25 |
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