JP2007169629A - 活性物質を安定化させるための水性ポリマー分散物 - Google Patents
活性物質を安定化させるための水性ポリマー分散物 Download PDFInfo
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Abstract
【解決手段】a)水性分散物中の固形分の重量基準で5〜99.9重量%の、10,000未満の数平均分子量を有する1以上のポリマー;b)水性分散物中の固形分の重量基準で0.1〜95重量%の、水溶性活性成分、部分的に水溶性の活性成分、水不溶性活性成分およびその組み合わせからなる群から選択される1以上の活性成分;およびc)30〜95重量%の水:を含む水性分散物。
【選択図】なし
Description
本発明は、水性分散物のブレンドを乾燥する追加の工程を含む、水性分散物で安定化された1以上の活性成分を放出させる方法も提供する。
エマルジョン重合による低分子量ポリマー分散物
エマルジョン重合は、メカニカルスターラー、温度調節装置、凝縮器、モノマーおよび開始剤フィードラインならびに窒素入口を備えた5リットル四口丸底フラスコ中で行った。
エマルジョン重合からの低分子量ポリマー
低分子量ポリマーを実施例1の分散物から水の蒸発により粘稠性油状物として単離した。この油状物をゼオライトを通して濾過し、透明油状物(アクリル油状物という(AO))を得た。
溶液重合からの低分子量ポリマー
メカニカルスターラー、温度調節装置、凝縮器、モノマーおよび開示剤供給ラインならびに窒素入口を備えた3リットルの丸底四口フラスコ中で溶液重合を行った。
溶液重合による低分子量ポリマー分散物
4gの低分子量ポリマー(実施例3、100BA/1.9iPrOH、Mn4191)、0.4gのNeodol 45−7、0.5gのRM8W(17.5%固形分)および5.1gの水を含む安定な水性分散物を調製した。混合物を1分間超音波処理して、粒子サイズが0.5〜1μであり、合計固形分が〜40%である分散物を得た。
低分子量ポリマーおよび部分的水溶性活性成分の水性分散物
実施例1Aの水性分散物(10g)をサリチル酸メチル(19g)と周囲条件下で混合した。水性分散物を光学顕微鏡下で観察した。粒子は30分以内に0.8〜1ミクロンに目に見えて膨張した。定量的膨張した理論的粒子サイズは830nmである。
低分子量ポリマーおよび水不溶性活性成分の水性分散物
イブプロフェン(商標)(2.5g)を低アクリル油(5g、実施例1A)中に40℃で溶解させた。油混合物溶液を、水(6g)、Tergital(商標)15−S−5(0.5g)およびラウリル硫酸ナトリウムSLS(1g)からなる水性溶液に60℃で添加した。水性混合物を60℃で1分間超音波処理し(最大500WのSonicator Processor、XLの40%電力設定)、〜200nmの粒子サイズを有する水中アクリル油/イブプロフェン(商標)の水性分散物を得た。調製された水性分散物は、水中、16.7重量%のイブプロフェン(商標)および33.3重量%のアクリル油を含んでいた。分散物は室温で30分間安定であり、その後、針状形態の結晶の形成を光学顕微鏡下で見ることができる。
低分子量ポリマー、水不溶性活性成分およびフィルム形成性ポリマーの水性分散物
実施例4からの水性分散物(6g)をフィルム形成性接着剤分散物、Robond(商標)PS−90(14g)と混合して、水中、5.4重量%のイブプロフェン(商標)、10.8重量%のアクリル油および34.7重量%の高分子量ポリマーからなる水性分散物を形成した。水性分散物は1週間にわたって光学顕微鏡下で結晶形成が観察されることなく安定であった。
ポリマー中の活性成分の組成物
実施例5における水性分散物のアリコート(8g)を直径8インチのテフロン(登録商標)製ペトリ皿に添加し、周囲条件下で乾燥した。最終乾燥組成物は、70%の高分子量ポリマー、10%のイブプロフェン(商標)および20%のアクリル油からなる。極低温条件下でマイクロトーニングし、RuO4で染色したサンプルを用いて、透過型電子顕微鏡により観察されるものとして、イブプロフェン(商標)はポリマー相中でドメイン(〜125nm)として観察された。
Claims (8)
- a)水性分散物中の固形分の重量基準で5〜99.9重量%の、10,000未満の数平均分子量を有する1以上のポリマー;b)水性分散物中の固形分の重量基準で0.1〜95重量%の、水溶性活性成分、部分的に水溶性の活性成分、水不溶性活性成分およびその組み合わせからなる群から選択される1以上の活性成分;およびc)30〜95重量%の水:を含む水性分散物。
- (a)水性分散物中の固形分の重量基準で5〜49.9重量%の、10,000未満の数平均分子量を有する1以上のポリマー;(b)水性分散物中の固形分の重量基準で0.1〜45重量%の、水溶性活性成分、部分的に水溶性の活性成分、水不溶性活性成分およびその組み合わせからなる群から選択される1以上の活性成分;および(c)水性分散物中の固形分の重量基準で94.9〜5.1重量%の、10,000より大きい数平均分子量を有する1以上のフィルム形成性ポリマー:を含み;
1以上の活性成分が、前記構成成分および水を組み合わせる前に(a)中に分配されている、水性分散物。 - (a)組成物の重量基準で5〜49.9重量%の、10,000未満の数平均分子量を有する1以上のポリマー;(b)組成物の重量基準で0.1〜45重量%の、水溶性活性成分、部分的に水溶性の活性成分、水不溶性活性成分およびその組み合わせからなる群から選択される1以上の活性成分;および(c)組成物の重量基準で94.9〜5.1重量%の、10,000より大きい数平均分子量を有する1以上のフィルム形成性ポリマー:を含み;
1以上の活性成分が、前記構成成分を組み合わせる前に(a)中に分配されている、組成物。 - 請求項2記載の水性分散物から製造されるフィルム。
- 請求項2記載の水性分散物から製造される接着剤。
- a)水性分散物中の固形分の重量基準で5〜99.9重量%の、10,000未満の数平均分子量を有する1以上のポリマーを含む水性分散物を調製する工程;およびb)前記水性分散物を、水性分散物中の固形分の重量基準で0.1〜95重量%の、水溶性活性成分、部分的に水溶性の活性成分、水不溶性活性成分およびその組み合わせからなる群から選択される1以上の活性成分と組み合わせる工程:を含む、1以上の活性成分を安定化させる方法。
- a)水性分散物中の固形分の重量基準で5〜49.9重量%の、10,000未満の数平均分子量を有する1以上のポリマーを含む第一水性分散物を調製し;b)前記水性分散物を、水性分散物中の固形分の重量基準で0.1〜45重量%の、水溶性活性成分、部分的に水溶性の活性成分、水不溶性活性成分およびその組み合わせからなる群から選択される1以上の活性成分と組み合わせ;c)第一水性分散物を、組成物の重量基準で94.9〜5.1重量%の、10,000より大きい数平均分子量を有する1以上のフィルム形成性ポリマーの第二水性分散物と組み合わせ(ここにおいて、1以上の活性成分は、第二水性分散物と組み合わせられる前に第一水性分散物中に分配される);およびd)水性分散物の混合物を乾燥して、フィルムまたはコーティングを形成すること:を含む、水性分散物から1以上の活性成分を放出させる方法。
- 水性分散物の組み合わせを乾燥した後にフィルムが形成される請求項7記載の方法。
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ES2562036T3 (es) * | 2007-07-30 | 2016-03-02 | Basf Corporation | Dispersiones basadas en agua de polímeros altamente ramificados |
CN107666902B (zh) | 2015-05-21 | 2021-09-21 | 德玛万科学有限责任公司 | 局部药物组合物 |
US11617724B2 (en) | 2015-05-21 | 2023-04-04 | Dermavant Sciences GmbH | Topical pharmaceutical compositions |
WO2022167974A1 (en) * | 2021-02-03 | 2022-08-11 | 3M Innovative Properties Company | Acrylate oligomers, acrylate oligomer emulsions, and fluorine-free stain-release compositions containing the same |
CN113881297A (zh) * | 2021-10-13 | 2022-01-04 | 广东青筑科技有限公司 | 一种渗透型封闭抗碱固化剂及其制备方法 |
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- 2006-11-23 KR KR1020060116284A patent/KR20070057660A/ko active Application Filing
- 2006-11-24 EP EP06256024.8A patent/EP1792921B1/en not_active Ceased
- 2006-11-28 US US11/605,150 patent/US20070128260A1/en not_active Abandoned
- 2006-11-29 BR BRPI0604969-9A patent/BRPI0604969B1/pt not_active IP Right Cessation
- 2006-11-30 JP JP2006324223A patent/JP4466962B2/ja not_active Expired - Fee Related
- 2006-12-01 CN CN201310430172.8A patent/CN103524966B/zh not_active Expired - Fee Related
- 2006-12-01 CN CNA2006101667234A patent/CN1978537A/zh active Pending
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WO2015151224A1 (ja) * | 2014-03-31 | 2015-10-08 | リンテック株式会社 | 粘着性組成物、粘着剤および粘着シート |
JPWO2015151224A1 (ja) * | 2014-03-31 | 2017-04-13 | リンテック株式会社 | 粘着性組成物、粘着剤および粘着シート |
Also Published As
Publication number | Publication date |
---|---|
CN103524966B (zh) | 2017-01-18 |
JP4466962B2 (ja) | 2010-05-26 |
BRPI0604969B1 (pt) | 2018-02-06 |
US20070128260A1 (en) | 2007-06-07 |
CN103524966A (zh) | 2014-01-22 |
EP1792921B1 (en) | 2015-08-12 |
KR100947490B1 (ko) | 2010-03-17 |
KR20070057660A (ko) | 2007-06-07 |
CN1978537A (zh) | 2007-06-13 |
KR20080053441A (ko) | 2008-06-13 |
BRPI0604969A (pt) | 2007-10-09 |
EP1792921A1 (en) | 2007-06-06 |
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