JP7053790B2 - ジクロフェナク含有乳化ゲル組成物 - Google Patents
ジクロフェナク含有乳化ゲル組成物 Download PDFInfo
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- JP7053790B2 JP7053790B2 JP2020503422A JP2020503422A JP7053790B2 JP 7053790 B2 JP7053790 B2 JP 7053790B2 JP 2020503422 A JP2020503422 A JP 2020503422A JP 2020503422 A JP2020503422 A JP 2020503422A JP 7053790 B2 JP7053790 B2 JP 7053790B2
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Description
[1]ジクロフェナクナトリウム、水、ゲル化剤、抗酸化剤、およびHLBが14以上である界面活性剤を含有し、ゲル化剤が非イオン性水溶性高分子である、乳化ゲル組成物。
[2]非イオン性水溶性高分子が、疎水化ヒドロキシプロピルメチルセルロースを含む、[1]に記載の乳化ゲル組成物。
[3]抗酸化剤が、2-メルカプトベンズイミダゾール、エデト酸ナトリウム、トコフェロール、ジブチルヒドロキシトルエンおよび没食子酸プロピルからなる群から選択される少なくとも1つの化合物を含む、[1]または[2]に記載の乳化ゲル組成物。
[4]HLBが14以上である界面活性剤が、モノヤシ油脂肪酸ポリオキシエチレンソルビタン、モノステアリン酸ポリエチレングリコール、ポリオキシエチレンフィトステロール、ポリオキシエチレンセチルエーテルおよびポリオキシエチレンベヘニルエーテルからなる群から選択される少なくとも1つの化合物を含む、[1]~[3]のいずれかに記載の乳化ゲル組成物。
[5]乳化ゲル組成物のpHが7.0以上である、[1]~[4]のいずれかに記載の乳化ゲル組成物。
ゲル組成物の調製において、水溶性成分を混合して水相を形成した後に、疎水性成分を加えて混合してもよく、疎水性成分を混合して油相を形成した後に、水溶性成分を加えて混合してもよく、他の方法であってもよい。
ゲル組成物の乳化方法は、単に混合してもよく、混合時に高圧ホモジナイザーまたは高速撹拌機を使用することにより、組成物に高い剪断力を付加してもよい。また、組成物を加温または冷却して乳化させてもよい。乳化方法は、水溶性成分と疎水性成分の組み合わせ、乳化剤の有無を考慮して、当業者は適宜選択すればよい。
表1および2の記載にしたがい、各成分を混和して、参考例1~22の組成物を調製した。表1に記載の「成分A」およびその含有量は、表2の記載にしたがい、精製水の含有量は、組成物全体が100質量%となるように設定した。表1中のその他の成分は、ジクロフェナクナトリウム以外の生理活性物質、および任意成分である。
表3にしたがい、各成分を混合した後、乳化ゲル組成物を調製した。表3中の数字は、「質量%」を意味する。疎水化HPMCとして、ステアリルオキシHPMC(ステアリルオキシヒドロキシプロピルオキシ基=0.3~0.6質量%)を使用した。表3中のその他の成分は、ジクロフェナクナトリウム以外の生理活性物質、および任意成分である。
表5および表6にしたがい、各成分を混合した後、ゲル組成物を調製した。表5中の数字は、「質量%」を意味し、成分Cとして表6に記載の成分を使用した。精製水と無水エタノールに関して、最終的なゲル組成物の総質量がジクロフェナクナトリウムの質量の100倍となるように、精製水と無水エタノールの混合溶液(質量比=1:1)を加えた。疎水化HPMCとして、ステアリルオキシHPMC(ステアリルオキシヒドロキシプロピルオキシ基=0.3~0.6質量%)を使用した。表5中のその他の成分は、ジクロフェナクナトリウム以外の生理活性物質、および任意成分である。
表8にしたがい、各成分を混合した後、乳化ゲル組成物を調製した。表8中の数字は、「質量%」を意味する。使用した疎水化HPMCは、試験例2に記載のとおりである。表8中のその他の成分は、ジクロフェナクナトリウム以外の生理活性物質、および任意成分である。乳酸は、ゲル組成物のpHが所望の値となるような量で加えられた。ポリソルベート80のHLB値は、15.0である。
表10にしたがい、各成分を混合した後、乳化ゲル組成物を調製した。表10中の数字は、「質量%」を意味する。使用した疎水化HPMCは、試験例2に記載のとおりである。表10中のその他の成分は、ジクロフェナクナトリウム以外の生理活性物質、および任意成分である。乳酸およびジエタノールアミンは、ゲル組成物のpHが所望の値となるような量で加えられた。POE(30)ベヘニルエーテルのHLB値は、18.0である。
Claims (5)
- ジクロフェナクナトリウム、水、ゲル化剤、抗酸化剤、およびHLBが14以上である界面活性剤を含有し、
前記ゲル化剤が、非イオン性水溶性高分子であり、
前記非イオン性水溶性高分子が、ヒドロキシプロピルセルロースおよび疎水化ヒドロキシプロピルメチルセルロースからなる群から選択される一種以上の化合物であり、
低級アルコールをさらに含有する、乳化ゲル組成物(但し、カルボキシビニルポリマーを含有する乳化ゲル組成物を除く。)。 - 前記非イオン性水溶性高分子が、疎水化ヒドロキシプロピルメチルセルロースを含む、請求項1に記載の乳化ゲル組成物。
- 前記抗酸化剤が、2-メルカプトベンズイミダゾール、エデト酸ナトリウム、トコフェロール、ジブチルヒドロキシトルエンおよび没食子酸プロピルからなる群より選択される少なくとも1つの化合物を含む、請求項1または2に記載の乳化ゲル組成物。
- 前記HLBが14以上である界面活性剤が、モノヤシ油脂肪酸ポリオキシエチレンソルビタン、モノステアリン酸ポリエチレングリコール、ポリオキシエチレンフィトステロール、ポリオキシエチレンセチルエーテル、ポリオキシエチレンベヘニルエーテルおよびポリオキシエチレンオレイルエーテルからなる群より選択される少なくとも1つの化合物を含む、請求項1~3のいずれか一項に記載の乳化ゲル組成物。
- 前記乳化ゲル組成物のpHが7.0以上である、請求項1~4のいずれか一項に記載の乳化ゲル組成物。
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KR102390748B1 (ko) | 2022-04-25 |
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TW202000190A (zh) | 2020-01-01 |
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EP3760198B1 (en) | 2023-09-06 |
WO2019167728A1 (ja) | 2019-09-06 |
KR20200112919A (ko) | 2020-10-05 |
EP3760198A1 (en) | 2021-01-06 |
US20210077393A1 (en) | 2021-03-18 |
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