JP7369683B2 - 水溶性超分子複合体 - Google Patents
水溶性超分子複合体 Download PDFInfo
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- JP7369683B2 JP7369683B2 JP2020193393A JP2020193393A JP7369683B2 JP 7369683 B2 JP7369683 B2 JP 7369683B2 JP 2020193393 A JP2020193393 A JP 2020193393A JP 2020193393 A JP2020193393 A JP 2020193393A JP 7369683 B2 JP7369683 B2 JP 7369683B2
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- water
- acid
- soluble
- oxyalkylated
- agents
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Description
本出願は、2014年11月20日に出願された番号が第14/548,851号であり、標題が「水溶性超分子複合体」である米国非仮特許出願の利益を主張するものであり、当該米国非仮特許出願の内容はここで参照により本明細書に組み込まれる。
本発明は、医薬製剤または化粧料活性成分の輸送に用いられる水溶性超分子複合体に関し、具体的に、水和により透明なヒドロゲル又は溶液を形成することができる固体としての水溶性超分子複合体に関する。
(a)下記(i)~(v)からなる群から選ばれる、少なくとも2つのポリエチレンオキシドブロックおよび少なくとも1つのポリプロピレンオキシドブロックを含有する水溶性ブロックコポリマーと、
(i)一般式HO-(EO)a(PO)b(EO)a-H(式中、50≦a≦150、35≦b≦70を満たす)を有するトリブロックコポリマー、
(ii)一般式HO-[(PO)b(EO)a]m(PO)c[(EO)a(PO)b]m-H(式中、50≦a≦150、35≦b≦70、35≦c≦70、且つ、m>0を満たす)を有する線状マルチブロックコポリマー、
(iii)式{[An(EO)a(PO)b(EO)aAn]E}m(式中、Aがエステル、ヒドロキシル酸エステル、カーボネート、エーテル、シロキサンおよびアミドからなる群から選ばれるモノマーであり、Eが連鎖延長剤または架橋剤であり、また、50≦a≦150、35≦b≦70、0≦n≦50、且つ、m≧2を満たす)の鎖延長ブロックコポリマー、超分岐ブロックコポリマー、または星型ブロックコポリマー、
(iv)一般式R-G-(EO)a(PO)b(EO)a-G-R(式中、GがC-C、C-O、C(O)NH、S-C、C(O)-O又はSi-Oからなる群から選ばれ、RがC8-C36範囲のアルキル鎖長を有するアルキル基又はアラルキル基であり、また、50≦a≦150、35≦b≦70を満たす)の末端変性ブロックコポリマー、
(v)少なくとも2つのポリエチレンオキシドブロックおよび少なくとも1つのポリプロピレンオキシドブロックを含有し、かつ、一般式[A(EO)a(PO)b(EO)a]m(式中、Aがビニル、エステル、アミド、イミド、エーテル及びシロキサン結合からなる群から選ばれ、50≦a≦150、50≦b≦150、m≧2を満たす)を有するグラフトされた側鎖を含むグラフトブロックコポリマー、
上記各式において、(EO)はポリエチレンオキシドブロックであり、(PO)はポリプロピレンオキシドブロックであり、
(b)20℃の水中での溶解度が0.5g/100ml未満である、少なくとも1種類の結合性ゲル化アジュバントと、
を含む水溶性超分子複合体、を含有する組成物であって、
上記複合体は水和と脱水を繰り返すことで溶液又は透明な逆的な熱可逆性ヒドロゲルを形成する可能であり、また、上記組成物が固体形態となり、上記溶液又は透明な逆的な熱可逆性ヒドロゲルは4~45℃で形成されてもよく、また、上記透明な逆的な熱可逆性ヒドロゲルが約4~40℃において調整可能なゾル-ゲル転移温度を有してもよい、組成物を提供する。
(a)下記(1)~(5)からなる群から選ばれる、少なくとも2つのポリエチレンオキシドブロックおよび少なくとも1つのポリプロピレンオキシドブロックを含有する水溶性ブロックコポリマーと、
(1)一般式HO-(EO)a(PO)b(EO)a-H(式中、50≦a≦150、35≦b≦70を満たす)を有するトリブロックコポリマー、
(2)一般式HO-[(PO)b(EO)a]m(PO)c[(EO)a(PO)b]m-H(式中、50≦a≦150、35≦b≦70、35≦c≦70、且つ、m>0を満たす)を有する線状マルチブロックコポリマー、
(3)式{[An(EO)a(PO)b(EO)aAn]E}m(式中、Aがエステル、ヒドロキシル酸エステル、カーボネート、エーテル、シロキサンおよびアミドからなる群から選ばれるモノマーであり、Eが連鎖延長剤または架橋剤であり、また、50≦a≦150、35≦b≦70、0≦n≦50、且つ、m≧2を満たす)の鎖延長ブロックコポリマー、超分岐ブロックコポリマー、または星型ブロックコポリマー、
(4)一般式R-G-(EO)a(PO)b(EO)a-G-R(式中、GがC-C、C-O、C(O)NH、S-C、C(O)-O又はSi-Oからなる群から選ばれ、RがC8-C36範囲のアルキル鎖長を有するアルキル基又はアラルキル基であり、また、50≦a≦150、35≦b≦70を満たす)の末端変性ブロックコポリマー、
(5)少なくとも2つのポリエチレンオキシドブロックおよび少なくとも1つのポリプロピレンオキシドブロックを含有し、かつ、一般式[A(EO)a(PO)b(EO)a]m(式中、Aがビニル、エステル、アミド、イミド、エーテル及びシロキサン結合からなる群から選ばれ、50≦a≦150、50≦b≦150、m≧2を満たす)を有するグラフトされた側鎖を含むグラフトブロックコポリマー、
上記各式において、(EO)はポリエチレンオキシドブロックであり、(PO)はポリプロピレンオキシドブロックであり、
(b)20℃の水中での溶解度が0.5g/100ml未満である、少なくとも1種類の結合性ゲル化アジュバントと、
から構成される組成物であって、
上記水溶性ブロックコポリマーと上記少なくとも1種類の結合性ゲル化アジュバントとから水溶性超分子複合体を形成し、当該水溶性超分子複合体は水和と脱水を繰り返すことで少なくとも1つの水溶液及び透明な逆的な熱可逆性ヒドロゲルを形成する可能であり、また、上記組成物が固体形態となる、組成物を提供する。なお、「基本的に…から構成される」とは、本発明によれば、前記組成物中の結合性ゲル化アジュバントと活性成分を溶解するために追加の添加剤を使用する必要とされていない。
少なくとも2つのポリエチレンオキシドブロックおよび少なくとも1つのポリプロピレンオキシドブロックを含有する水溶性ブロックコポリマー
結合性ゲル化アジュバント
(a)20℃未満の温度で、少なくとも2つのポリエチレンオキシドブロックおよび少なくとも1つのポリプロピレンオキシドブロックを含有する上記水溶性ブロックコポリマーを水中に溶解する工程と、
(b)次に、好適な温度で、少なくとも1種類の結合性ゲル化アジュバントを混合して、透明なヒドロゲルまたは溶液を形成する工程と、
(c)上記透明なヒドロゲルまたは溶液を、少なくとも45%、より好ましくは少なくとも75%、最も好ましくは少なくとも95%の水が透明なヒドロゲルまたは溶液から除去されるまで、乾燥させる工程と、
を含む、湿式法を提供する。
(a)上記水溶性ブロックコポリマーを55~120℃の温度に加熱する工程と、
(b)加熱されたコポリマーを少なくとも1種類の結合性ゲル化アジュバントと55~120℃の温度で混合して混合物を形成する工程と、
(c)混合物を冷却する工程と、
を含む、ホットメルト加工法を提供する。
医薬製剤
(1) セフォキシチン、n-ホルムアミドイル-チエナマイシンおよび他のチエナマイシン誘導体、テトラサイクリン、クロラムフェニコール、ネオマイシン、カルベニシリン、コリスチン、ペニシリンG、ポリミクシンB、バンコマイシン、セファゾリン、セファロリジン、チブロリファマイシン、グラミシジン、バシトラシン、スルホンアミド;ゲンタマイシン、カナマイシン、アミカシン、シソマイシンおよびトブラマイシンなどのアミノグリコシド抗生物質;ノルフロキサシンおよびflucalanine/ペンチジドンの抗菌剤組合せなどのナリジクス酸および類似体;ニトロフラゾンなど。
(2) ピリラミン、クロルフェニラミン、テトラヒドラゾリン、アンタゾンリン(antazonline)などの抗ヒスタミン剤と充血除去剤。
(3) コルチゾン、ヒドロコルチゾン、酢酸ヒドロコルチゾン、ベータメタゾン、デキサメタゾン、リン酸デキサメタゾンナトリウム、プレドニゾン、メチルプレドニゾロン、メドリゾン、フルオロメトロン、フルオコルトロン、プレドニゾロン、リン酸プレドニゾロンナトリウム、トリアムシノロン、インドメタシン、スリンダク、その塩およびその対応するスルフィドなど。
(4) エコチオフェート、ピロカルピン、サリチル酸フィソスチグミン、ジイソプロピルフルオロリン酸、エピネフリン、ジピボリルエピネフライン(dipivolyl epinephraine)、ネオスチグミン、エコチオフェーヨウ化物、デメカリウム臭化物、カルバコール、メタコリン、ベタネコールなど。
(5) アトロピン、ホマトロピン、スコポラミン、ヒドロキシアンフェタミン、エフェドリン、コカイン、トロピカミド、フェニレフリン、シクロペントラート、オキシフェノニウム、オイカトロピンなどの散瞳剤;および目の症状または疾患の治療に用いられる他の薬。
(6) たとえば、特に、マレイン酸塩およびR-チモロール、ならびに、ピロカルピンおよびチモロールまたはR-チモロールの組合せとしての、ベタキソロール、ピロカルピン、チモロールなどの抗緑内障薬。さらに、酒石酸水素塩、ホウ酸塩、塩酸塩およびジピベフリン誘導体などのエピネフリンおよびエピネフリン複合体またはプロドラッグ、ならびにグリセリン、マンニトールおよび尿素などの高浸透圧剤も含まれる。
(7) イベルメクチンなどの抗寄生虫化合物および/または抗原生動物化合物;ピリメタミン、トリスルファピリミジン、クリンダマイシンおよびコルチコステロイド調剤。
(8) アシクロビル、5-ヨード-2’-デオキシウリジン(IDU)、アデノシンアラビノシド(Ara-A)、トリフルオロチミジン、ならびにインターフェロンおよびポリI:Cなどのインターフェロン誘発剤などの抗ウイルス効果化合物。
(9) アセタゾラミド、ジクロフェナミド、2-(p-ヒドロキシフェニル)チオ-5-チオフェンスルホンアミド、6-ヒドロキシ-2-ベンゾチアゾールスルホンアミドおよび6-ピバロイルオキシ-2-ベンゾチアゾールスルホンアミドなどの炭酸脱水酵素阻害剤。
(10) アムホテリシンB、ナイスタチン、フルシトシン、ナタマイシン、およびミコナゾールなどの抗真菌剤。
(11) エチドカインコカイン、へノキシネート(henoxinate)、ジブカイン塩酸塩、ジクロニン塩酸塩、ナエパイン、フェナカイン塩酸塩、ピペロカイン、プロパラカイン塩酸塩、テトラカイン塩酸塩、ヘキシルカイン、ブピカイン、リドカイン、メピバカインおよびプリロカインなどの麻酔剤。
(12) 以下のような眼診断剤:(a)網膜を検査するために用いるものおよびクロリド-ナトリウムフルオレセイン;(b)フルオレセインおよびローズベンガルなどの結膜、角膜および涙器を検査するのに用いるもの;および(c)メタコリン、コカイン、アドレナリン、アトロピン、ヒドロキシアンフェタミンおよびピロカルピンなどの異常な瞳孔反射を検査するために用いるもの。
(13) アルファキモトリプシンおよびヒアルロニダーゼなどの手術で補助剤として用いられる眼剤。
(14) エチレンジアミンテトラアセテート(EDTA)およびデフェロキサミンなどのキレート剤。
(15) メトトレキセート、シクロホスファミド、6-メルカプトプリン、およびアザチオプリンなどの免疫抑制剤および抗代謝物質。
(16) 心房性ナトリウム利尿因子、カルシトニン-遺伝子関連因子、黄体化ホルモン、放出ホルモン、ニューロテリシン(neuroterisin)、血管活性腸ペプチド、バソプレシン、シクロスポリン、ボツリヌス毒素、インターフェロン、P物質エンケファリン、表皮成長因子、目由来の成長因子、フィブロネクチン、インシュリン様成長因子および中胚葉成長因子。
(17) サリチル酸およびその誘導体、硫黄、乳酸、グリコール酸、ピルビン酸、アゼライン酸、尿素、レゾルシノールおよびN-アセチルシステイン、ならびに、レチノイン酸およびその誘導体などのレチノイドなどの、ざ瘡治療剤。
(18) ヒアルロン酸ナトリウムまたはポリビニルアルコールなどの潤滑剤。
(19) ネオマイシン硫酸塩-リン酸デキサメタゾンナトリウム、マレイン酸チモロール-アセクリジンなどの併用抗緑内障療法におけるような抗生物質-抗炎症剤などの上記の組合せ。
化粧料活性成分
(1) 限定されないが、アーモンドオイル、イランイランオイル、ネロリオイル、サンダルウッドオイル、フランキンセンスオイル、ペパーミントオイル、ラベンダーオイル、純ジャスミン、ゼラニウムオイルバーボン、スペアミントオイル、クローブオイル、レモングラスオイル、セダーウッドオイル、バルサムオイル、ティーツリーオイルおよびタンジェリンオイルを含む精油。また、限定されないが、1-シトロネロール、α-アミルシンナムアルデヒド、ライラル、ゲラニオール、ファルネソール、ヒドロキシシトロネラール、イソオイゲノール、オイゲノール、ユーカリオイルおよびオイカリプトール、レモンオイル、リナロールおよびシトラールなどの精油に存在する活性成分を使用してもよい。それらのフレグランスまたは香味料としての効果以外に、このような化合物は抗菌剤としても組成物において有用であり得る。精油または単離された成分の濃度は、約0.3~1重量%の間、または約0.1~0.5重量%の間、または0.5~2重量%の間であり得る。
(2) 保湿保持剤は、グリセリン、ソルビトール、プロピレングリコール、ジプロピレングリコール、1,3-ブチレングリコール、ペンチレングリコール、グルコース、キシリトール、マルチトール、ポリエチレングリコール、ヒアルロン酸、コンドロイチン硫酸、ピロリドンカルボキシラート、ポリオキシエチレングリコシド、およびポリオキシプロピレンメチルグリコシドなどを含む。
(3) 胎盤抽出物、アルブチン、グルタチオンおよびユキノシタ抽出物、コウジ酸、胎盤抽出物、硫黄、エラグ酸、リノール酸、トラネキサム酸などの美白剤;ローヤルゼリー、光増感剤、コレステロール誘導体、子牛血抽出物、α-ヒドロキシル酸およびβ-ヒドロキシル酸などの細胞活性剤;荒れ肌および乾燥肌改善剤;ノニル酸、バニリルアミド、ニコチン酸ベンジル、ニコチン酸β-ブトキシエチル、カプサイシン、ジンゲロン、カンタリスチンキ、イクタモール、カフェイン、タンニン酸、α-ボルネオール、ニコチン酸トコフェリル、ヘキサニコチン酸イノシトール、シクランデラート、シンナリジン、トラゾリン、アセチルコリン、ベラパミル、セファランチンおよびγ-オリザノールなどの血液循環改善剤;酸化亜鉛およびタンニン酸などの皮膚収れん剤;硫黄およびチアントールなどの抗脂漏剤;ならびにα-ヒドロキシアセトンなどの皮膚着色剤などを含む、皮膚美容剤。
(4) 日焼け止めは、p-アミノ安息香酸、エチルジヒドロキシプロピルp-アミノベンゾアート、グリセリルp-アミノベンゾアート、およびオクチルp-ジメチルアミノベンゾアートなどのベンゾアート型のUV吸収剤;アントラニル酸メチルなどのアントラニル酸型UV吸収剤;サリチル酸メチル、サリチル酸オクチル、およびトリエタノールアミン塩またはサリチル酸などのサリチル酸型のUV吸収剤;p-メトキシけい皮酸オクチル、p-メトキシヒドロキシけい皮酸のジエタノールアミン塩、およびジメトキシヒドロキシけい皮酸(dimethocycinnamic acid)/イソオクタン酸グリセリド(isooctanoic acid gryceride);2,4-ジヒドロキシベンゾフェノン、2,2’,4,4’-テトラヒドロキシベンゾフェノン、2-ヒドロキシ-4-メトキシベンゾフェノン、2-ヒドロキシ-4-メトキシペンゾフェノン-5-スルホン酸(2-hydroxy-4-methoxypenzophenon-5-sulfonic acid)、2,2’-ジヒドロキシ-4-メトキシペンゾフェノン、および2-ヒドロキシ-4-N-オクトオキシベンゾフェノンなどのベンゾフェノン型UV吸収剤;ウロカニン酸エチルなどのウロカニン酸型のUV吸収剤;4-tert-ブチル-4’-メトキシジベンゾイルメタン、4-イソプロピルジベンゾイルメタンなどのジベンゾイルメタン型のUV吸収剤;3-(4-メチルベンジリデン)カンファー、オクチルトリアゾン、e-エチルヘキシル-2-シアノ-3,3-ジフェニルアクリレート、2-フェニル-ベンゾイミダゾール-5-スルフェート、4-(3,4-ジメトキシフェニルメチレン)-2,5-ジオキソ-1-イミダゾリジン(4-(3,4-dimethoxypnehylmethylene)-2,5-dioxo-1-imidazolidine)、および2-エチルヘキシルプロピオネートを含む。UV吸収剤は、ポリマー粉末内にカプセル化され得る。たとえば、酸化チタン微粉末、鉄を含有する酸化チタンの微粉末、酸化亜鉛微粉末、酸化セリウム微粉末およびこれらの混合物などの紫外線を吸収または散乱させる上述の粉末を使用し得る。
(5) 制汗剤は、アルミニウムクロロ水和物、塩化アルミニウム、アルミニウムセスキクロロ水和物、ジルコニルヒドロキシクロリド、アルミニウムジルコニウムヒドロキシクロリドおよびアルミニウムジルコニウムグリシンなどを含む。
(6) ビタミンAオイル、レチノール、酢酸レチニルおよびパルミチン酸レチニルなどのビタミンA;リボフラビン、酪酸リボフラビンおよびフラビンアデニンヌクレオチドなどのビタミンB2、塩酸ピリドキシン、ジオクタン酸ピリドキシンおよびトリパルミチン酸ピリドキシンなどのビタミンB6、ビタミンB12およびその誘導体、ならびにビタミンB15およびその誘導体;L-アスコルビン酸、L-アスコルビン酸ジパルミタート、ナトリウム(L-アスコルビン酸)-2-スルフェートおよび二カリウムL-アスコルビン酸ジホスファートなどのビタミンC;エルゴカルシフェロールおよびコレカルシフェロールなどのビタミンD;α-トコフェロール、β-トコフェロール、γ-トコフェロール、酢酸dl-α-トコフェリル、ニコチン酸dl-α-トコフェリルおよびコハク酸dl-α-トコフェリル;ビタミンH;ビタミンP;ニコチン酸、ニコチン酸ベンジルおよびニコチン酸アミドなどのニコチン酸;パントテン酸カルシウム、D-パントテニルアルコール、パントテニルエチルエーテルおよびアセチルパントテニルエチルエーテルなどのパントテン酸;ビオチン、などのビタミン。
(7) アミノ酸は、グリシン、バリン、ロイシン、イソロイシン、セリン、トレオニン、フェニルアラニン(phenylaranine)、アルギニン、リジン、アスパラギン酸、グルタミン酸、シスチン、システイン、メチオニンおよびトリプトファンを含む。例または核酸は、デオキシリボ核酸を含み、ホルモンの例は、エストラジオールおよびエテニルエストラジオールなどを含む。
(8) サリチル酸およびその誘導体、硫黄、乳酸、グリコール酸、ピルビン酸、アゼライン酸、尿素、ティーツリーオイル、レゾルシノールおよびN-アセチルシステイン、ならびに、レチノイン酸またはその誘導体などのレチノイドなどの抗ざ瘡剤。
(9) 防腐剤または抗菌剤は、パラオキシ安息香酸アルキル、安息香酸、安息香酸ナトリウム、ソルビン酸、ソルビン酸カリウム、およびフェノキシエタノールを含み、用いられ得る。抗菌剤については、安息香酸、過酸化ベンジル(benzyl peroxide)、サリチル酸およびその誘導体、石炭酸、ソルビン酸、パラオキシ安息香酸アルキルエステル、パラクロロメタクレゾール、ヘキサクロロフェン、塩化ベンザルコニウム、塩化クロルヘキシジン(chlorohexydine chloride)、トリクロロカルボアニリド、トリクロサン、光増感剤、フェノキシエタノールなど。
(10) 抗ウイルス剤および抗菌剤として、さらに、皮膚の刺激を緩和または予防するための亜鉛塩。亜鉛塩の例は、その開示内容がここに引用により援用される米国特許第5,208,031号に記載されるもののような、酢酸亜鉛、乳酸亜鉛、プロピオン酸亜鉛、グルコン酸亜鉛および酸化亜鉛を含む。亜鉛塩は、0.5~25%の間の濃度にある。
(11) 歯のホワイトニング剤は、限定されないが、過酸化水素、過酸化カルボイミド、過酸化カルシウム、過炭酸塩、過炭酸ナトリウム、過ホウ酸塩、過硫酸塩、およびこれらの混合物を含む。シュウ酸、マロン酸、酒石酸およびこれらの塩。好適なジカルボン酸塩は、限定されないが、たとえば、シュウ酸、マロン酸および酒石酸などのナトリウム、カリウム、亜鉛、鉄、カルシウム、マグネシウムおよび銅塩を含む。
(12) 脱毛剤は、限定されないが、1以上のチオール酸(たとえば、チオグリコール酸、チオ乳酸、およびβ-メルカプトプロピオン酸など)などのチオール系脱毛剤、または、これらの酸のアルカリ塩および/またはアルカリ土類金属塩を含む。さらに、他の活性チオール剤も使用できる。これらは、β-メルカプトエタノール、チオグリセロール、1,3-ジチオ-2-プロパノール、1,4-ジチオ-2-ブタノール、1,4-ジメルカプト-2,3-ブタンジオール、1,3-diexthio(ジエキスチオ)-2-メトキシプロパン、1,3-ジメルカプト-2-アミノプロパン、1,4-ジメルカプト-2,3-ジアミノブタン、アミノエタンチオール、および関連する有効なチオール活性物質などを含む。
(13) フレグランス油は、合成、天然、およびこれらの混合物からのフレグランス油を含む。香料ヒドロゲル組成物は、アルコールの有無を問わないフレグランスの香りの徐放のために、ヒドロゲルを擦るか、またはスプレーのいずれかとして適用され得る。
(14) 防虫剤は、ブチルアセチルアミノプロピン酸エチル、N,N-ジエチルトルアミド(DEET)、N,N-ジエチルベンズアミド、フィチン酸ジメチル、エチルベキサンジオール(ethyl bexanediol)、インダロン、ビシクロヘプテンジカルボキシド、テトラヒドロフルアルデヒドなどを含む。
(15) 酸化防止剤は、トコフェロール、ブチルヒドロキシアニソール、ジブチルヒドロキシトルエンおよびフィチン酸を含む。
(16) キレート剤の例は、アラニン、エチレンジアミン四酢酸ナトリウム、ポリリン酸ナトリウム、メタリン酸ナトリウムおよびリン酸を含む。
(17) 冷媒の例は、L-メントールおよびカンファーを含む。
(18) 抗炎症剤の例は、アラントイン、グリチルリチンおよびその塩、グリシレチン酸およびグリシレチン酸ステアリル、トラネキサム酸、アズレンなどを含む。
(19) 無機塩、有機酸の塩、アミン塩およびアミノ酸の塩などの塩。無機塩の例は、ナトリウム、カリウム、マグネシウム、カルシウム、アルミニウム、ジルコニウム、および塩酸の亜鉛塩、硫酸、炭酸塩酸、および硝酸を含む。有機酸塩の例は、酢酸、デヒドロ酢酸、クエン酸、マレイン酸、コハク酸、アスコルビン酸およびステアリン酸の塩を含む。アミン塩の例は、トリエタノールアミンの塩であり、アミノ酸塩の例は、グルタミン酸の塩である。他の例は、化粧料に組込むことの可能なヒアルロン酸、コンドロイチン硫酸、アルミニウム・ジルコニウム・グリシン複合体および酸塩基反応によりつくられる塩である。
(20) 着色剤は、さまざまな染料、有機および無機顔料を含む。染料の例は、D&CおよびFD&Cブルー、ブラウン、グリーン、オレンジ、レッド、イエロ-などと呼ばれている、アゾ、インジゴイド、トリフェニルメタン、アントラキノンおよびキサンチン染料を含む。有機顔料は、一般的に、レーキ、特に、D&CおよびFD&C色素のレーキと呼ばれる、法定色素添加剤の不溶性金属塩;およびカーボンブラックからなる。無機顔料は、酸化鉄、紺青、クロム、水酸化クロム色素、およびこれらの混合物を含む。好適な無機顔料は、酸化鉄を含む。
さらに、たとえば、ガラス、アクリル樹脂、ポリエステル、ポリウレタン、ポリエチレンテレフタレート、セラミックスまたはアルミナなどの天然または合成の有機または鉱物基材を含有する粒子など、効果を有する色素も挙げられ、上記基材は、たとえば、アルミニウム、金、銀、白金、銅もしくはブロンズなどの金属物質、または、たとえば、二酸化チタン、酸化鉄もしくは酸化クロム、およびこれらの混合物などの金属酸化物で被覆されていなくてもいてもよい。干渉顔料、特に、液晶または多層干渉顔料も用いられ得る。
水溶性染料は、たとえば、ビートルート・ジュースまたはメチレンブルーである。
他の着色剤は、水溶性材料または水不溶性材料によりカプセル化されてもよい。シリコーンによりカプセル化された、SUNSIL材料などの製品が、Sunjin Chemical Companyから入手可能である。ナイロンまたはポリメタクリル酸メチルで被覆された追加の染料もSunjin Chemical Companyから入手可能である。
(21) 微粒子フィラーは、着色または非着色であってよく(非着色は、無色であるか、白色を意味する)、好ましくは、微粒子フィラーは、0.02~100、好ましくは0.5~50ミクロンの粒径を有する。好適な微粒子フィラーは、オキシ塩化ビスマス、チタン酸マイカ、ヒュームドシリカ、球状シリカ、シリコーン粉末、ポリメチルメタクリレート、微粒子化テフロン(登録商標)、窒化ホウ素、アクリレートコポリマー、珪酸アルミニウム、アルミニウムスターチオクテニルスクシナート、ベントナイト、珪酸カルシウム、セルロース、チョーク、コーンスターチ、ケイソウ土、フラー土、グリセリルスターチ、ヘクトライト、水和シリカ、カオリン、珪酸アルミニウムマグネシウム、トリ珪酸マグネシウム、マルトデキストリン、モンモリロナイト、微結晶セルロース、コメデンプン、絹粉末、シリカ、タルク、マイカ、二酸化チタン、ラウリン酸亜鉛、ミリスチン酸亜鉛、ロジン酸亜鉛、アルミナ、アタパルジャイト、炭酸カルシウム、ケイ酸カルシウム、デキストラン、カオリン、ナイロン、シリル化シリカ、セリサイト、大豆粉、酸化錫、水酸化チタン、リン酸トリマグネシウム、クルミ殻粉末、またはこれらの混合物を含む。
(22) 上述の顔料および微粒子フィラーは、微粒子表面を被覆する、単独または組合されたレシチン、アミノ酸、鉱油、シリコーン油またはさまざまな他の試薬により表面処理されてもよい。表面処理のために用いられる被膜は、新油性または新水性のいずれであってもよい。
Claims (6)
- (a)少なくとも2つのポリエチレンオキシドブロックおよび少なくとも1つのポリプロピレンオキシドブロックを含有する水溶性ブロックコポリマーと、
(b)20℃の水中での溶解度が0.5g/100ml未満である、少なくとも1種類の結合性ゲル化アジュバントと、
からなる無水超分子複合体であって、
前記水溶性ブロックコポリマーは、一般式HO-(EO)a(PO)b(EO)a-H((EO) a はポリエチレンオキシドブロックであり、(PO) b はポリプロピレンオキシドブロックであり、aは50~150の範囲であり、bは35~70の範囲である)を有するトリブロックコポリマーであり、
前記少なくとも1種類の結合性ゲル化アジュバントに対する前記水溶性ブロックコポリマーの重量比は1:1~10:1であり;
前記無水超分子複合体は、水に可溶性であり、10~60℃の範囲の軟化点を有し、
前記無水超分子複合体は水との水和および脱水を繰り返すことで、水和後に溶液またはクリアかつ透明な逆的な熱可逆性ヒドロゲルを形成することが可能であり、および
前記無水超分子複合体は脱水後にワックス状固体またはペーストを形成することが可能である
、無水超分子複合体。 - 前記水溶性ブロックコポリマー(a)の一般式においてaが101であってbが56であるか、またはaが141であってbが44である、請求項1に記載の無水超分子複合体。
- 前記少なくとも1種類の結合性ゲル化アジュバントが、オキシアルキル化脂肪族アルコール、オキシアルキル化脂肪族アルコールのエステル、オキシアルキル化アルキルアルコール、オキシアルキル化アルキルアルコールのエステル、オキシアルキル化アルキルアリールアルコール、脂肪族ヒドロキシカルボン酸、脂肪族ヒドロキシカルボン酸のエステル、芳香族ヒドロキシカルボン酸、芳香族ヒドロキシカルボン酸のエステル、ポリ(ヒドロキシカルボン酸)、オキシアルキル化ソルビタンエステル、オキシアルキル化トリグリセリド、オキシアルキル化グリセリルエステル、オキシアルキル化ソルビトールのエステル、ポリオールエステル、ソルビタンエステルおよびこれらの混合物からなる群から選択され;
前記オキシアルキル化脂肪族アルコールはラウレス-2、ラウレス-3、ラウレス-4、ラウレス-5、およびラウレス-6、オレス-2、オレス-5、およびオレス-10からなる群から選択され、または
前記オキシアルキル化脂肪族アルコールはC12-13パレス-2、C12-13パレス-3、C12-13パレス-4、C12-13パレス-5、およびC12-13パレス-6からなる群から選択され、または前記オキシアルキル化脂肪族アルコールのエステルはアジピン酸ジ-PPG-2ミレス-9、アジピン酸ジ-PPG-2ミレス-10、およびアジピン酸ジ-PPG-2ミレス-11からなる群から選択される、請求項1に記載の無水超分子複合体。 - 請求項1に記載の無水超分子複合体とさらに有効量の少なくとも1つの医薬品、診断用化合物または化粧料活性成分を含む組成物。
- 前記少なくとも1つの医薬品、診断用化合物または化粧料活性成分が、抗生物質、抗ヒスタミン剤、充血除去剤、抗炎症剤、縮瞳剤、抗コリン作用剤、散瞳薬、抗緑内障化合物、抗寄生虫化合物、抗ウイルス化合物、炭酸脱水酵素阻害剤、診断剤、眼剤、キレート剤、免疫抑制剤、抗代謝物質、麻酔、抗真菌剤、タンパク質、ペプチド、ざ瘡治療剤、潤滑剤、ビタミン、アミノ酸、歯のホワイトニング剤、脱毛剤、防虫剤、酸化防止剤、抗炎症剤、およびそれらの混合物からなる群から選択され、
任意に、前記少なくとも1つの医薬品、診断用化合物または化粧料活性成分は組成物全体の0.01~70重量%の濃度範囲で存在し、または香味料、膜形成ポリマー、防腐剤、着色剤、塩およびフレグランスからなる群から選択される1つ以上の医薬上または化粧料上許容される賦形剤を含む、請求項4に記載の組成物。 - 請求項1に記載の無水超分子複合体を調製するための方法であって、
(a)20℃未満の温度で、前記水溶性ブロックコポリマーを水中に溶解する工程と、
(b)好適な温度で、溶解されたコポリマーと少なくとも1種類の結合性ゲル化アジュバントとを混合して、透明なヒドロゲルまたは溶液を形成する工程と、
(c)前記透明なヒドロゲルまたは溶液を、少なくとも95%の水が前記透明なヒドロゲルまたは溶液から除去されるまで乾燥して、無水物形態を得る工程と、
を含む、方法。
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