JP7230080B2 - 低pHを有する皮膚用組成物 - Google Patents
低pHを有する皮膚用組成物 Download PDFInfo
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- JP7230080B2 JP7230080B2 JP2021027240A JP2021027240A JP7230080B2 JP 7230080 B2 JP7230080 B2 JP 7230080B2 JP 2021027240 A JP2021027240 A JP 2021027240A JP 2021027240 A JP2021027240 A JP 2021027240A JP 7230080 B2 JP7230080 B2 JP 7230080B2
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- hyaluronic acid
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Description
化粧用として許容可能な活性成分は、使用される緩衝剤のpKaの約1単位以内のpKaを有する。一実施形態では、化粧用として許容可能な活性成分は、緩衝剤のpKaの約0.7単位以内のpKaを有する。
緩衝剤は、約2.8~約4.2、好ましくは約3.5~約4のpKaを有する。
一実施形態では、本組成物は、水相、油相、及び非イオン性脂質相を含むエマルションである。
R5--(OCH2CH2)y--OH 式I
式中、R5は、約6~約22個の炭素原子を有する分枝状又は非分枝状アルキル基であり、yは、約4~約100、好ましくは約10~約100である。好ましいアルコキシル化アルコールは、R5がラウリル基である種であり、yは、23の平均値を有し、これはラウレス23として知られ、商品名「BRIJ 35」でICI Americas,Inc.(Wilmington,Del)から入手可能である。
本発明の組成物は、ヒトの皮膚又は毛髪に局所的に塗布される。したがって、本組成物は、組成物の約50重量%~約99.99重量%(例えば、組成物の約80重量%~約99重量%)であってよい化粧用として許容可能な局所用キャリアを更に含み得る。本発明の好ましい実施形態では、化粧用として許容可能な局所用キャリアには水が含まれる。
一実施形態では、本組成物は、追加の化粧用として許容可能な活性剤を含有する。
様々な他の材料も、当該技術分野において既知のように、本組成物中に存在してもよい。これらは、湿潤剤、pH調整剤、キレート剤(例えば、EDTA)、香料、染料、及び防腐剤(例えば、パラベン)を含む。
一実施形態では、本発明は、約3.3~約4のpH、少なくとも約0.15の緩衝能を有し、かつ約2.8~約4.2のpKaを有する緩衝剤を含有する組成物中の化粧用として許容可能な活性成分を局所投与することを含む、約2.8~約4のpKaを有する化粧用として許容可能な活性成分の局所送達を増加させる方法を提供する。
表1に示される成分を使用して、一連の本発明の組成物及び比較組成物を作製した。本発明の組成物及び比較組成物は全て、主である水相、油相、及び非イオン性脂質相の3つの相からなった。以下の実施例に論じられるように、乳酸(緩衝剤)及び乳酸ナトリウム(pH調整剤)の量を変化させながら、以下の手順を用いて組成物を調製した。
6つの組成物2A~2Fを実施例1に記載されるように作製し、上述のヒアルロン酸貫通試験を用いてヒアルロン酸(HA)貫通に関して試験した。乳酸なしで、pHを変更して組成物を作製した。組成物の全ては、0.002未満の緩衝能を有した。
実施例1に記載されるように4つの組成物を作製し、ヒアルロン酸貫通試験を用いてヒアルロン酸(HA)貫通に関して試験した。組成物のpHは3.3に固定したが、異なる量の乳酸及び異なる量の緩衝能を有した。
実施例1に従い作製した6つの組成物を、ヒアルロン酸貫通試験を用いてヒアルロン酸(HA)貫通に関して試験した。組成物は各々6重量%の乳酸を含有したが、3.0~6.0の範囲のpH及び0.096~0.37の緩衝能を有した。
実施例1に従い作製した4つの組成物を、ヒアルロン酸貫通試験を用いてヒアルロン酸(HA)貫通に関して試験した。本組成物は、緩衝能が0.001~0.021の様々な量の乳酸を含有した。各組成物はpH6を有した。
この実施例は、他の緩衝剤が本発明に従い使用することができることを示す。
皮膚pHに対する作用は、組成物3B及び3Dを用いて試験された。乳酸を含有しないことを除き他は同じである、非緩衝対照配合物と共に、各組成物を3人のヒト志願者の前腕に適用した。両試験組成物は、pH3.3を有した。
表7の成分を用いて、本発明による一連の組成物を作製した。下の表8に示される様々な増粘剤を組成物中に入れ替えた。
以下に記載されるプロセスにより、表9に示される成分を用いて、太陽光濾過剤を含有する本発明による日常装用組成物を作製した。
1つが<0.001の緩衝能を有する0%乳酸を含有し(比較組成物11A)、もう1つが0.26の緩衝能を有する6%乳酸を含有した(本発明の組成物11B)ことを除き、表9に従い2つの日常装用組成物を作製した。各組成物のpHは3.3であった。
(1) 局所用組成物であって、
(a)約2.8~約4.2のpKaを有する緩衝剤と、
(b)前記緩衝剤の前記pKaの約1単位以内のpKaを有する化粧用として許容可能な活性成分と、を含み、
前記組成物が、約3.3~約4のpH、及び少なくとも約0.15の緩衝能を有する、局所用組成物。
(2) 前記化粧用として許容可能な活性成分が、前記緩衝剤の前記pKaの約0.7単位以内のpKaを有する、実施態様1に記載の局所用組成物。
(3) 前記化粧用として許容可能な活性成分が、ヒアルロン酸を含む、実施態様1に記載の局所用組成物。
(4) 前記化粧用として許容可能な活性成分が、架橋ヒアルロン酸を含む、実施態様1に記載の局所用組成物。
(5) 前記緩衝剤が、乳酸、グリコール酸、クエン酸、酒石酸、グルコン酸、及びグルコノラクトンからなる群から選択される、実施態様1に記載の局所用組成物。
(7) 局所用組成物であって、
(a)ヒアルロン酸と、
(b)乳酸と、
(c)ステアレス10と、
(d)ジラウリン酸グリセロールと、
(e)グリセリンと、を含む、局所用組成物。
(8) 前記ヒアルロン酸は、架橋ヒアルロン酸を含む、実施態様7に記載の局所用組成物。
(9) ケイ酸アルミニウムマグネシウム、アクリル酸ヒドロキシエチル/アクリロイルジメチルタウリン酸ナトリウムコポリマー、キサンタンガム、シリカ、セチルヒドロキシエチルセルロース、及びポリアクリレート-13/ポリイソブチレン/ポリソルベート-20ブレンド、並びにこれらの混合物からなる群から選択される増粘剤を更に含む、実施態様7に記載の局所用組成物。
(10) 前記増粘剤が、アクリル酸ヒドロキシエチル/アクリロイルジメチルタウリン酸ナトリウムコポリマーを含む、実施態様9に記載の局所用組成物。
(12) 前記局所送達が、4を超えるpHを有することを除いて同じ組成物中に含有される場合の前記化粧用として許容可能な活性成分の局所送達と比較して、少なくとも2倍である、実施態様11に記載の方法。
(13) 前記局所送達が、前記緩衝剤を含まないことを除いて同じ組成物中に含有される場合の前記化粧用として許容可能な活性成分の局所送達と比較して、少なくとも2倍である、実施態様11に記載の方法。
(14) 前記化粧用として許容可能な活性成分が、ヒアルロン酸を含む、実施態様11に記載の方法。
(15) 前記化粧用として許容可能な活性成分が、架橋ヒアルロン酸を含む、実施態様11に記載の方法。
(a)乳酸と、
(b)ステアレス10と、
(c)ジラウリン酸グリセロールと、
(d)グリセリンと、を含む、局所用組成物。
(17) ケイ酸アルミニウムマグネシウム、アクリル酸ヒドロキシエチル/アクリロイルジメチルタウリン酸ナトリウムコポリマー、キサンタンガム、シリカ、セチルヒドロキシエチルセルロース、及びポリアクリレート-13/ポリイソブチレン/ポリソルベート-20ブレンド、並びにこれらの混合物からなる群から選択される増粘剤を更に含む、実施態様16に記載の局所用組成物。
(18) 前記増粘剤が、アクリル酸ヒドロキシエチル/アクリロイルジメチルタウリン酸ナトリウムコポリマーを含む、実施態様17に記載の局所用組成物。
Claims (4)
- 皮膚用局所用組成物であって、
(a)架橋ヒアルロン酸と、
(b)3~6重量%の乳酸と、
(c)ステアレス10と、
(d)ジラウリン酸グリセロールと、
(e)グリセリンと、を含み、
3.3~4のpH及び少なくとも0.15の緩衝能を有する、皮膚用局所用組成物。 - 3.3~3.5のpHを有する、請求項1に記載の皮膚用局所用組成物。
- ケイ酸アルミニウムマグネシウム、アクリル酸ヒドロキシエチル/アクリロイルジメチルタウリン酸ナトリウムコポリマー、キサンタンガム、シリカ、セチルヒドロキシエチルセルロース、及びポリアクリレート-13/ポリイソブチレン/ポリソルベート-20ブレンド、並びにこれらの混合物からなる群から選択される増粘剤を更に含む、請求項1又は2に記載の皮膚用局所用組成物。
- 前記増粘剤が、アクリル酸ヒドロキシエチル/アクリロイルジメチルタウリン酸ナトリウムコポリマーを含む、請求項3に記載の皮膚用局所用組成物。
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ES2892958T3 (es) | 2022-02-07 |
RU2016129158A (ru) | 2018-01-23 |
BR122021018243A2 (ja) | 2017-01-31 |
BR102016017090A2 (pt) | 2017-01-31 |
CN106361592A (zh) | 2017-02-01 |
BR102016017090B1 (pt) | 2022-01-18 |
KR20170012086A (ko) | 2017-02-02 |
DK3120831T3 (da) | 2021-10-11 |
JP6884522B2 (ja) | 2021-06-09 |
MX2016009666A (es) | 2017-05-01 |
CA2935367A1 (en) | 2017-01-23 |
AU2016206278B2 (en) | 2021-08-19 |
BR102016017090B8 (pt) | 2022-08-16 |
BR122021018243A8 (pt) | 2022-07-26 |
MX361590B (es) | 2018-12-11 |
KR102656735B1 (ko) | 2024-04-15 |
US10130578B2 (en) | 2018-11-20 |
EP3120831B1 (en) | 2021-08-25 |
US20170020799A1 (en) | 2017-01-26 |
EP3120831A1 (en) | 2017-01-25 |
JP2017025062A (ja) | 2017-02-02 |
JP2023009045A (ja) | 2023-01-19 |
JP2021080278A (ja) | 2021-05-27 |
AU2016206278A1 (en) | 2017-02-09 |
CA2935367C (en) | 2023-10-10 |
RU2727807C2 (ru) | 2020-07-24 |
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