JP2013227334A - 高い弾性付与活性を有する組成物 - Google Patents
高い弾性付与活性を有する組成物 Download PDFInfo
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- JP2013227334A JP2013227334A JP2013142834A JP2013142834A JP2013227334A JP 2013227334 A JP2013227334 A JP 2013227334A JP 2013142834 A JP2013142834 A JP 2013142834A JP 2013142834 A JP2013142834 A JP 2013142834A JP 2013227334 A JP2013227334 A JP 2013227334A
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- 230000008520 organization Effects 0.000 description 1
- 230000032696 parturition Effects 0.000 description 1
- 230000035515 penetration Effects 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 239000004033 plastic Substances 0.000 description 1
- 229920000223 polyglycerol Polymers 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- 230000007017 scission Effects 0.000 description 1
- 239000008159 sesame oil Substances 0.000 description 1
- 235000011803 sesame oil Nutrition 0.000 description 1
- KZJWDPNRJALLNS-VJSFXXLFSA-N sitosterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CC[C@@H](CC)C(C)C)[C@@]1(C)CC2 KZJWDPNRJALLNS-VJSFXXLFSA-N 0.000 description 1
- 229950005143 sitosterol Drugs 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 235000010268 sodium methyl p-hydroxybenzoate Nutrition 0.000 description 1
- 239000004071 soot Substances 0.000 description 1
- 239000003549 soybean oil Substances 0.000 description 1
- 235000012424 soybean oil Nutrition 0.000 description 1
- HCXVJBMSMIARIN-PHZDYDNGSA-N stigmasterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)/C=C/[C@@H](CC)C(C)C)[C@@]1(C)CC2 HCXVJBMSMIARIN-PHZDYDNGSA-N 0.000 description 1
- 229940032091 stigmasterol Drugs 0.000 description 1
- 235000016831 stigmasterol Nutrition 0.000 description 1
- BFDNMXAIBMJLBB-UHFFFAOYSA-N stigmasterol Natural products CCC(C=CC(C)C1CCCC2C3CC=C4CC(O)CCC4(C)C3CCC12C)C(C)C BFDNMXAIBMJLBB-UHFFFAOYSA-N 0.000 description 1
- 125000004434 sulfur atom Chemical group 0.000 description 1
- 230000009897 systematic effect Effects 0.000 description 1
- TUNFSRHWOTWDNC-UHFFFAOYSA-N tetradecanoic acid Chemical class CCCCCCCCCCCCCC(O)=O TUNFSRHWOTWDNC-UHFFFAOYSA-N 0.000 description 1
- TUNFSRHWOTWDNC-HKGQFRNVSA-N tetradecanoic acid Chemical compound CCCCCCCCCCCCC[14C](O)=O TUNFSRHWOTWDNC-HKGQFRNVSA-N 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 230000000472 traumatic effect Effects 0.000 description 1
- 230000000007 visual effect Effects 0.000 description 1
- 230000037303 wrinkles Effects 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 description 1
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Abstract
【解決手段】妊娠後期における膣及び会陰の弾性を改善するための組成物は、チオール化化合物又はその混合物と有機酸のエステル又はその混合物を組み合わせることを含む。
【選択図】なし
Description
以下のw/w%組成を有するリポゲル(=均一な疎水性軟膏)製剤を調製した。
1)システイン酸リシンカルボキシメチル1 5.00%
2)ポリグリセリル−3蜜ろう2 7.50%
3)甘扁桃油(Prunus amygdalus var. dulcis)3 12.00%
4)トコフェロール、レシチン、パルミチン酸アスコルビル、クエン酸4 0.05%
5)ワセリン5 15.00%
6)水素化ヒマシ油6 2.00%
7)鉱物油7 100.00%まで適量
1Elastocell(登録商標);2Cera Bellina(遊離脂肪酸がポリグリセロールエステルに変換された蜜ろうの親水性誘導体);3スイートアーモンド油(約65%のオレイン酸由来のグリセリドを含有する);4Aperoxid TLA;5白色軟パラフィン;6Cutina(登録商標)HR粉末(ヒドロキシステアリン酸(C18)のトリグリセリドから主に構成される);7Pharma 55
鉱物油、ポリグリセリル−3蜜ろう、甘扁桃油、Aperoxid TLA及びワセリンをターボエマルサー(turboemulsor)で混合し、70℃で加熱した。塊が溶融したときに、完全に分散するまで穏やかに撹拌しながら水素化ヒマシ油を加えた。次いで、溶融した塊を45℃に冷却し、均一なゲルが得られるまで撹拌しながらシステイン酸リシンカルボキシメチルを加えた。
以下のw/w%組成を有するリポゲル(=均一な疎水性軟膏)製剤を調製した。
1)システイン酸リシンカルボキシメチル 7.50%
2)ポリグリセリル−3蜜ろう 5.00%
3)アセチル化ラノリン* 2.00%
4)トコフェロール、レシチン、パルミチン酸アスコルビル、クエン酸 0.05%
5)ワセリン 38.50%
6)鉱物油 14.00%
7)水素化ヒマシ油 3.00%
8)ダイズ油** 100.00%まで適量
*Modulan(商標)ラノリン誘導体(Noveon)アセチル化ラノリンアルコール;**リノール酸(50〜57%)、リノレン酸(5〜10%)、オレイン酸(17〜26%)、パルミチン酸(9〜13%)及びステアリン酸(3〜6%)のグリセリドからなる。
以下のw/w%組成を有するリポゲル(=均一な疎水性軟膏)製剤を調製した。
1)システイン酸リシンカルボキシメチル 5.00%
2)ポリグリセリル−3蜜ろう 5.00%
3)甘扁桃油 12.00%
4)トコフェロール、レシチン、パルミチン酸アスコルビル、クエン酸 0.10%
5)ワセリン 15.00%
6)フィトステロールエステル* 15.00%
7)水素化ヒマシ油 3.50%
8)シリカ 1.50%
9)鉱物油 100.00%まで適量
*Vegapure(Cognis)
得られたゲルは、本発明による35.5%のエステルを含有する。
以下のw/w%組成を有するリポゲル(=均一な疎水性軟膏)製剤を調製した。
1)システイン酸リシンカルボキシメチル 5.00%
2)ポリグリセリル−3蜜ろう 7.50%
3)甘扁桃油 7.00%
4)ミリスチン酸イソプロピル* 5.00%
5)トコフェロール、レシチン、パルミチン酸アスコルビル、クエン酸 0.10%
6)ワセリン 15.00%
7)水素化ヒマシ油 4.50%
8)シリカ 1.50%
9)鉱物油 100.00%まで適量
*Crodamol IPM(Croda、イソプロピルアルコールと飽和脂肪酸であるミリスチン酸とのエステル)
得られたゲルは、本発明による24.00%のエステルを含有する。
以下のw/w%組成を有するリポゲル(=均一な疎水性軟膏)製剤を調製した。
1)L−メチオニン 5.00%
2)合成蜜ろう* 8.50%
3)甘扁桃油 12.00%
4)トコフェロール、レシチン、パルミチン酸アスコルビル、クエン酸 0.05%
5)ワセリン 15.00%
6)水素化ヒマシ油 4.00%
7)シリカ 2.50%
8)ニーム油** 1.00%
9)ゴマ油*** 2.00%
10)鉱物油 100.00%まで適量
*Syncrowax BB4(Croda)
**リノール酸、オレイン酸、パルミチン酸及びステアリン酸のトリグリセリドの混合物を含有
***アラキドン酸(0.8%)、リノール酸(40.4%)、オレイン酸(45.4%)、パルミチン酸(9.1%)及びステアリン酸(4.3%)のグリセリドを含有
得られたゲルは、本発明による27.50%のエステルを含有する。
以下のw/w%組成を有するリポゲル(=均一な疎水性軟膏)製剤を調製した。
1)メチルスルホニルメタン 5.00%
2)合成蜜ろう 5.00%
3)甘扁桃油 12.00%
4)トコフェロール、レシチン、パルミチン酸アスコルビル、クエン酸 0.10%
5)ワセリン 15.00%
6)水素化植物油* 3.50%
7)シリカ 1.50%
8)鉱物油 100.00%まで適量
*CEGESOFT(登録商標)HF62(Cognis、C16〜C24トリグリセリドの混合物を含有)
得られたゲルは、本発明による20.50%のエステルを含有する。
以下のw/w%組成を有するリポゲル(=均一な疎水性軟膏)製剤を調製した。
1)システイン酸リシンカルボキシメチル 5.00%
2)合成蜜ろう 5.00%
3)甘扁桃油 6.00%
4)トコフェロール、レシチン、パルミチン酸アスコルビル、クエン酸 0.10%
5)ワセリン 15.00%
6)ラノリンアルコール* 3.50%
7)ラノリンUSP** 6.00%
8)シリカ 1.50%
9)鉱物油 100.00%まで適量
*Super Hartolan(Croda、医薬品等級のラノリンのコレステロールに富む固体画分);**Medilan(商標)(Croda、コレステロールと数種の脂肪酸のエステルとの混合物を含有)
得られたゲルは、本発明による20.50%のエステルを含有する。
比較臨床試験
白色軟パラフィンからなる標準対照製品と比較して、急性試験において3種の組成物の皮膚弾性化活性を調査することを目的とした健常志願者に対する臨床試験を実施した。本試験の目的は、カルボキシメチルシステイン酸塩等のチオール化化合物及び脂肪酸とグリセロールとのエステルの混合物を含有する製剤の活性を、チオール化化合物のみ又はエステル混合物のみを含有する異なる製剤の活性と比較することであった。
Ue:即時伸展性
Uf:最大伸展性
Uv:粘弾性
Ur:即時弾性回復
Ur/Ue:弾性回復
Ur/Uf:皮膚弾性
Uv/Uc:粘性
τon及びτoffは「前進」及び「戻り」曲線上の時定数
製品1:実施例1による組成を有するリポゲルLPOL514
製品2:以下のw/w%組成を有するヒドロゲルLPOL513
1)システイン酸リシンカルボキシメチル1 7.50%
2)プロピルパラベンナトリウム 0.04%
3)メチルパラベンナトリウム 0.37%
4)イミダゾリジニルウレア2 0.20%
5)EDTA二ナトリウム 0.10%
6)ヒドロキシエチルセルロース3 1.50%
7)カラゲニンゲル4 5.00%
8)クエン酸 pH5.5まで適量
9)水 100.00%まで適量
1Elastocell(登録商標);2Gram 1;3Natrosol 250M;4Seamollient
製品3:以下のw/w%組成を有するヒドロゲルLPOL520
1)水素化ダイズホスファチジルコリン1 1.03%
2)コレステロールUSP 0.26%
3)ブチル化ヒドロキシアニソール(BHA) 0.10%
4)アスコルビン酸 7.10%
5)グリセロール 5.00%
6)EDTA二ナトリウム2 0.10%
7)メチルパラベンナトリウム3 0.37%
8)プロピルパラベンナトリウム4 0.04%
9)イミダゾリジニルウレア5 0.21%
10)ヒドロキシエチルセルロース6 0.70%
11)キサンタンゴム7 1.00%
12)水 100.00%まで適量
1Lipoid S 100−3;2Dissolvine NA−2;3Nipagin M ナトリウム;4Nipasol M ナトリウム;5Gram 1;6Natrosol 250M;7Rhodigel Ultra
製品4:以下の組成を有する対照標準
1)ワセリン(=白色軟パラフィン)CAS番号8009−03−8 100%
結果を以下の表1に要約する。
** ベースラインに対してP<0.01
***: ベースラインに対してP<0.001
比較臨床試験
妊娠の最後の2ヵ月間に実施例3による製剤を定期的に適用することにより、会陰組織における弾性付与活性及び分娩時の会陰の外傷を予防する能力を調査することを目的として、妊娠女性における臨床試験を実施した。試験は、既存群と比較した、オープンラベルであった。
Claims (13)
- 妊娠女性における膣及び会陰の弾性を改善するための局所組成物の製造のための、
a)混合物の全重量に対する0.1から25重量%の少なくともチオール化化合物、及び
b)混合物の全重量に対する1.0から95重量%の少なくとも6から18個の炭素原子を有する有機酸のエステル又はその混合物、
の使用。 - 成分a)は、硫酸化アミノ酸及びその誘導体から選択されることを特徴とする請求項1に記載の使用。
- 成分a)は、1−メチオニン、1−システイン、1−シスチン、タウリン、4−チアゾリジンカルボン酸、カルボキシメチルシステイン及び/又はメチルスルホニルメタン、並びにそれらの生理学的に許容される塩から選択されることを特徴とする請求項1に記載の使用。
- 成分a)は、0.5から15重量%の量で存在することを特徴とする請求項1に記載の使用。
- 成分a)は、1.0から10重量%の量で存在することを特徴とする請求項1に記載の使用。
- 成分b)は、グリセロールのエステル又は動物若しくは植物ステロールのエステル又はそれらの混合物であることを特徴とする請求項1に記載の使用。
- 前記ステロールが、コレステロールであることを特徴とする請求項6に記載の使用。
- 前記有機酸は、12から18個の炭素原子を含むことを特徴とする請求項1に記載の使用。
- 前記有機酸は、飽和又は不飽和であることを特徴とする請求項1に記載の使用。
- 成分b)は、5から70重量%の量で存在することを特徴とする請求項1に記載の使用。
- 成分b)は、10から45重量%の量で存在することを特徴とする請求項1に記載の使用。
- 1又は複数の薬剤学的に許容できる賦形剤を含むことを特徴とする請求項1に記載の使用。
- 前記賦形剤は、イオン化剤、酸化防止剤、キレート化剤、湿潤剤、熱粘着化剤(thermoviscosizing agent)、うっ血除去剤、消毒剤及び/又は抗菌剤、香味料及び着色剤からなる群から選択されることを特徴とする請求項12に記載の使用。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP06118649.0 | 2006-08-09 | ||
EP20060118649 EP1886676A1 (en) | 2006-08-09 | 2006-08-09 | Compositions with enhanced elasticizing activity |
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JP2009523211A Division JP2010500309A (ja) | 2006-08-09 | 2007-04-18 | 高い弾性付与活性を有する組成物 |
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JP2013227334A true JP2013227334A (ja) | 2013-11-07 |
JP5771649B2 JP5771649B2 (ja) | 2015-09-02 |
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JP2009523211A Pending JP2010500309A (ja) | 2006-08-09 | 2007-04-18 | 高い弾性付与活性を有する組成物 |
JP2013142834A Active JP5771649B2 (ja) | 2006-08-09 | 2013-07-08 | 高い弾性付与活性を有する組成物 |
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JP2009523211A Pending JP2010500309A (ja) | 2006-08-09 | 2007-04-18 | 高い弾性付与活性を有する組成物 |
Country Status (23)
Country | Link |
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US (1) | US9125806B2 (ja) |
EP (2) | EP1886676A1 (ja) |
JP (2) | JP2010500309A (ja) |
KR (2) | KR101521166B1 (ja) |
CN (1) | CN101500550B (ja) |
AR (1) | AR062304A1 (ja) |
AT (1) | ATE457723T1 (ja) |
BR (1) | BRPI0715182C1 (ja) |
CA (1) | CA2655472C (ja) |
CY (1) | CY1110032T1 (ja) |
DE (1) | DE602007004857D1 (ja) |
DK (1) | DK2049092T3 (ja) |
EA (1) | EA014971B1 (ja) |
ES (1) | ES2340335T3 (ja) |
HK (1) | HK1126956A1 (ja) |
HR (1) | HRP20100212T1 (ja) |
MX (1) | MX2009000869A (ja) |
NO (1) | NO343143B1 (ja) |
PL (1) | PL2049092T3 (ja) |
PT (1) | PT2049092E (ja) |
RS (1) | RS51282B (ja) |
SI (1) | SI2049092T1 (ja) |
WO (1) | WO2008017521A2 (ja) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
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EP3081212A1 (en) | 2015-04-16 | 2016-10-19 | Polichem SA | Carboxymethylcysteine for topical treatment of stretch marks |
EP3442501A1 (en) | 2016-04-15 | 2019-02-20 | Fairhaven Health, LLC | Compositions and methods for maintaining or enhancing homeostasis or function of female lower reproductive tract |
IT202100002285A1 (it) * | 2021-02-03 | 2022-08-03 | Farm Dott Ferretti Stefano | Nuova composizione |
Citations (3)
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WO2006045584A1 (en) * | 2004-10-25 | 2006-05-04 | Unilever Plc | Personal care compositions with glycerin and hydroxypropyl quaternary ammonium salts |
WO2006045428A1 (en) * | 2004-10-25 | 2006-05-04 | Unilever Plc | Personal care compositions with salts of hydroxypropyl trialkylammonium substituted mono-saccharide |
WO2006045364A1 (en) * | 2004-10-25 | 2006-05-04 | Unilever Plc | Personal care compositions with salts of dihydroxypropyltri(c1-c3 alkyl) ammonium monosubstituted polyols |
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DE1617639A1 (de) * | 1966-09-12 | 1972-04-20 | Mini Ind Chimice | Verfahren zur Herstellung eines Arzneimittels zur Behandlung von physiologischen Hautkrankheiten |
US4296130A (en) * | 1979-08-30 | 1981-10-20 | Herschler R J | Methylsulfonylmethane and methods of use |
GB9213472D0 (en) * | 1992-06-25 | 1992-08-12 | Unilever Plc | Cosmetic composition |
WO1995034280A1 (en) * | 1994-06-15 | 1995-12-21 | The Procter & Gamble Company | Methods of lightening hyperpigmented regions in mammalian skin |
JP3542665B2 (ja) * | 1995-07-07 | 2004-07-14 | 株式会社資生堂 | 抗老化皮膚外用剤、コラーゲン架橋阻害皮膚外用剤及び抗紫外線皮膚外用剤 |
FR2740340B1 (fr) * | 1995-10-30 | 1997-12-05 | Oreal | Utilisation d'acides carboxyliques porteurs d'une fonction soufree pour favoriser la desquamation de la peau ou stimuler le renouvellement epidermique |
US20040265268A1 (en) * | 2001-08-18 | 2004-12-30 | Deepak Jain | Compositions and methods for skin rejuvenation and repair |
CH697081A5 (de) * | 2002-01-22 | 2008-04-30 | Andreas F Dr Schaub | Zusammensetzung für die Unterstützung der Geburt eines menschlichen Föten. |
US6821524B2 (en) * | 2002-06-03 | 2004-11-23 | Jan Marini Skin Research, Inc. | Cosmetic skin care compositions |
US20050266064A1 (en) * | 2004-05-29 | 2005-12-01 | Mccarthy Kathryn J | Cosmetic compositions and methods |
DE102004054552A1 (de) * | 2004-11-11 | 2006-05-18 | Hcb Happy Child Birth Holding Ag | Neue Zusammensetzung zur Erleichterung der Humangeburt |
US7351745B2 (en) * | 2004-12-22 | 2008-04-01 | Avon Products, Inc | Compositions and methods of their use for improving the condition and appearance of skin |
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2007
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- 2007-04-18 PL PL07728255T patent/PL2049092T3/pl unknown
- 2007-04-18 WO PCT/EP2007/053793 patent/WO2008017521A2/en active Application Filing
- 2007-04-18 DK DK07728255T patent/DK2049092T3/da active
- 2007-04-18 DE DE200760004857 patent/DE602007004857D1/de active Active
- 2007-04-18 EP EP20070728255 patent/EP2049092B1/en active Active
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- 2007-04-18 CA CA 2655472 patent/CA2655472C/en active Active
- 2007-04-18 CN CN2007800296579A patent/CN101500550B/zh active Active
- 2007-04-18 PT PT07728255T patent/PT2049092E/pt unknown
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- 2007-04-18 US US12/310,032 patent/US9125806B2/en active Active
- 2007-04-18 BR BRPI0715182A patent/BRPI0715182C1/pt active IP Right Grant
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- 2007-04-18 EA EA200900293A patent/EA014971B1/ru not_active IP Right Cessation
- 2007-08-09 AR ARP070103525 patent/AR062304A1/es not_active Application Discontinuation
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2009
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- 2009-05-19 HK HK09104533A patent/HK1126956A1/xx unknown
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Patent Citations (3)
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WO2006045584A1 (en) * | 2004-10-25 | 2006-05-04 | Unilever Plc | Personal care compositions with glycerin and hydroxypropyl quaternary ammonium salts |
WO2006045428A1 (en) * | 2004-10-25 | 2006-05-04 | Unilever Plc | Personal care compositions with salts of hydroxypropyl trialkylammonium substituted mono-saccharide |
WO2006045364A1 (en) * | 2004-10-25 | 2006-05-04 | Unilever Plc | Personal care compositions with salts of dihydroxypropyltri(c1-c3 alkyl) ammonium monosubstituted polyols |
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