JP2018138605A5 - - Google Patents
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- Publication number
- JP2018138605A5 JP2018138605A5 JP2018094298A JP2018094298A JP2018138605A5 JP 2018138605 A5 JP2018138605 A5 JP 2018138605A5 JP 2018094298 A JP2018094298 A JP 2018094298A JP 2018094298 A JP2018094298 A JP 2018094298A JP 2018138605 A5 JP2018138605 A5 JP 2018138605A5
- Authority
- JP
- Japan
- Prior art keywords
- acid
- transdermal
- functional group
- containing compound
- absorption enhancer
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 238000010521 absorption reaction Methods 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 7
- 239000003623 enhancer Substances 0.000 claims 7
- 230000002708 enhancing Effects 0.000 claims 7
- 125000000524 functional group Chemical group 0.000 claims 7
- 230000002378 acidificating Effects 0.000 claims 5
- 239000004480 active ingredient Substances 0.000 claims 5
- GHVNFZFCNZKVNT-UHFFFAOYSA-N Decanoic acid Chemical compound CCCCCCCCCC(O)=O GHVNFZFCNZKVNT-UHFFFAOYSA-N 0.000 claims 4
- OYHQOLUKZRVURQ-IXWMQOLASA-N Linoleic acid Natural products CCCCC\C=C/C\C=C\CCCCCCCC(O)=O OYHQOLUKZRVURQ-IXWMQOLASA-N 0.000 claims 4
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N Oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 claims 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- 238000009472 formulation Methods 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- WPYMKLBDIGXBTP-UHFFFAOYSA-N Benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 2
- 239000005632 Capric acid (CAS 334-48-5) Substances 0.000 claims 2
- 229960001231 Choline Drugs 0.000 claims 2
- JFCQEDHGNNZCLN-UHFFFAOYSA-N Glutaric acid Chemical compound OC(=O)CCCC(O)=O JFCQEDHGNNZCLN-UHFFFAOYSA-N 0.000 claims 2
- 239000005642 Oleic acid Substances 0.000 claims 2
- QIQXTHQIDYTFRH-UHFFFAOYSA-N Stearic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 2
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Chemical compound OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 claims 2
- CRBHXDCYXIISFC-UHFFFAOYSA-N choline Chemical compound C[N+](C)(C)CC[O-] CRBHXDCYXIISFC-UHFFFAOYSA-N 0.000 claims 2
- AEMRFAOFKBGASW-UHFFFAOYSA-N glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 claims 2
- 235000020778 linoleic acid Nutrition 0.000 claims 2
- OFOBLEOULBTSOW-UHFFFAOYSA-N malonic acid Chemical compound OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims 2
- 230000001737 promoting Effects 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000011780 sodium chloride Substances 0.000 claims 2
- 239000005711 Benzoic acid Substances 0.000 claims 1
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 claims 1
- 206010047461 Viral infection Diseases 0.000 claims 1
- 208000001756 Virus Disease Diseases 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 150000007513 acids Chemical class 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 230000000240 adjuvant Effects 0.000 claims 1
- 150000001413 amino acids Chemical class 0.000 claims 1
- 235000010233 benzoic acid Nutrition 0.000 claims 1
- 125000004432 carbon atoms Chemical group C* 0.000 claims 1
- 150000001735 carboxylic acids Chemical class 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N fumaric acid Chemical compound OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims 1
- 150000001261 hydroxy acids Chemical class 0.000 claims 1
- 230000001861 immunosuppresant Effects 0.000 claims 1
- 239000003018 immunosuppressive agent Substances 0.000 claims 1
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 claims 1
- 150000004668 long chain fatty acids Chemical class 0.000 claims 1
- 239000011976 maleic acid Substances 0.000 claims 1
- 238000002844 melting Methods 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 239000001384 succinic acid Substances 0.000 claims 1
- 230000017613 viral reproduction Effects 0.000 claims 1
Claims (10)
- ａ）分子量が５０〜１２０、融点が５０〜３５０℃であって、コリンまたはその誘導体である塩基性官能基含有化合物と、
ｂ）ＬｏｇＰが−４〜７．３である酸性官能基含有化合物
との等モル塩を含み、
ｂ）酸性官能基含有化合物が、アミノ酸、カルボン酸、ヒドロキシ酸、置換基を有していてもよい炭素数が１２〜２０の長鎖脂肪酸、及び糖酸からなる群から選択される１種である、経皮吸収促進助剤又は経皮吸収促進剤。 - ｂ）酸性官能基含有化合物のＬｏｇＰが２．５〜７．３である、請求項１に記載の経皮吸収促進助剤又は経皮吸収促進剤。
- ｂ）酸性官能基含有化合物が、ヒスチジン、グリコール酸、乳酸塩、マロン酸、酢酸、マレイン酸、コハク酸、グルタル酸、安息香酸、カプリン酸、オレイン酸、リノール酸、及び、イソステアリン酸からなる群から選択される１種である、請求項１又は２に記載の経皮吸収促進助剤又は経皮吸収促進剤。
- ａ）塩基性官能基含有化合物が、コリンである、請求項３に記載の経皮吸収促進助剤又は経皮吸収促進剤。
- ｂ）酸性官能基含有化合物が、カプリン酸、オレイン酸、リノール酸、イソステアリン酸から選択される１種である、請求項４に記載の経皮吸収促進助剤又は経皮吸収促進剤。
- 活性成分、及び、請求項１〜５いずれか一項に記載の経皮吸収促進助剤又は経皮吸収促進剤を含む経皮製剤。
- 前記活性成分の分子量が１万以下、ＬｏｇＰが３．５以下である、請求項６に記載の経皮製剤。
- 前記活性成分の分子量が１万以下、ＬｏｇＰが０．５以下である、請求項６に記載の経皮製剤。
- 前記活性成分が塩ではない、請求項６〜８いずれか一項に記載の経皮製剤。
- 前記活性成分が、ウイルス感染症治療薬、または免疫抑制剤である、請求項６〜９いずれか一項に記載の経皮製剤。
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2014221315 | 2014-10-30 | ||
| JP2014221315 | 2014-10-30 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016556223A Division JP6482570B2 (ja) | 2014-10-30 | 2015-10-30 | 経皮吸収促進剤及び経皮吸収促進助剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018138605A JP2018138605A (ja) | 2018-09-06 |
| JP2018138605A5 true JP2018138605A5 (ja) | 2018-12-06 |
| JP6693999B2 JP6693999B2 (ja) | 2020-05-13 |
Family
ID=55857668
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016556223A Active JP6482570B2 (ja) | 2014-10-30 | 2015-10-30 | 経皮吸収促進剤及び経皮吸収促進助剤 |
| JP2018094298A Active JP6693999B2 (ja) | 2014-10-30 | 2018-05-16 | 経皮吸収促進剤及び経皮吸収促進助剤 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016556223A Active JP6482570B2 (ja) | 2014-10-30 | 2015-10-30 | 経皮吸収促進剤及び経皮吸収促進助剤 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US20170239173A1 (ja) |
| EP (3) | EP3395368A1 (ja) |
| JP (2) | JP6482570B2 (ja) |
| WO (1) | WO2016068336A1 (ja) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2019131480A (ja) * | 2018-01-29 | 2019-08-08 | 旭化成株式会社 | 経皮吸収促進剤及び経皮製剤 |
| US11446257B2 (en) | 2018-09-27 | 2022-09-20 | BioPhysics Pharma, Inc. | Transdermal drug delivery system |
| BR112022000767A2 (pt) | 2019-07-16 | 2022-03-15 | Donaghys Ltd | Sistema de solvente transdérmico e métodos de uso |
| EP4043007A4 (en) | 2019-10-11 | 2023-11-08 | Toray Industries, Inc. | PHARMACEUTICAL COMPOSITION COMPRISING A TEMPERATURE SENSITIVE IONIC LIQUID |
| WO2021192861A1 (ja) * | 2020-03-26 | 2021-09-30 | 国立大学法人九州大学 | イオン液体、溶媒、製剤および経皮吸収剤 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3551554A (en) | 1968-08-16 | 1970-12-29 | Crown Zellerbach Corp | Enhancing tissue penetration of physiologically active agents with dmso |
| DE2528516A1 (de) | 1974-07-05 | 1976-01-22 | Sandoz Ag | Neue galenische zubereitung |
| FR2314731A1 (fr) | 1975-06-19 | 1977-01-14 | Nelson Res & Dev | Azacycloalcan-2-ones 1-substituees et compositions pharmaceutiques contenant ces composes a titre d'excipients |
| JPS5283914A (en) | 1976-01-01 | 1977-07-13 | Sandoz Ag | Improvement of galenus medicine |
| JPS5781409A (en) * | 1980-11-10 | 1982-05-21 | Toko Yakuhin Kogyo Kk | External plaster |
| EP0189861A3 (en) * | 1985-01-26 | 1988-02-17 | Showa Denko Kabushiki Kaisha | Percutaneous absorption accelerator for ionic water-soluble medicine |
| JP2905210B2 (ja) | 1989-01-23 | 1999-06-14 | フロイント産業株式会社 | 経皮、経粘膜吸収促進剤および経皮、経粘膜製剤 |
| JP2651616B2 (ja) | 1989-02-03 | 1997-09-10 | リンテック株式会社 | 経皮吸収製剤 |
| DE4436764A1 (de) * | 1994-10-14 | 1996-04-18 | Henkel Kgaa | Verwendung von Guanidiniumsalzen ungesättigter Fettsäuren als Korrosionsschutzwirkstoff |
| FR2752421B1 (fr) * | 1996-08-13 | 2001-05-04 | Fabre Pierre Dermo Cosmetique | Sels de guanidines anti-seborrheiques |
| US6120779A (en) * | 1998-01-29 | 2000-09-19 | Soma Technologies | Use of partial and complete salts of choline and carboxylic acids for the treatment of skin disorders |
| AU6751000A (en) * | 1999-07-30 | 2001-02-19 | Maxim Pharmaceuticals, Inc. | Use of histamine as a drug delivery enhancing compound for use in transmucosal or transdermal delivery |
| JP2003160511A (ja) * | 2001-11-29 | 2003-06-03 | Shiseido Co Ltd | 経皮吸収促進剤 |
| US20030143195A1 (en) * | 2002-01-30 | 2003-07-31 | Pinsker Judy Senior | Use of histamine as a drug delivery enhancing compound for use in transmucosal or transdermal delivery |
| US20060147508A1 (en) * | 2002-10-04 | 2006-07-06 | Bioderm Research | Concurrent Enhancement of Skin Penetration of Organic Base Active Agents and Organic Hydroxy Acid Active Agents as Their Ion-Pair Complexes |
| JP4969065B2 (ja) | 2005-07-13 | 2012-07-04 | 株式会社 メドレックス | 常温性イオン性液体を含有する医薬組成物 |
| JP2008162899A (ja) | 2006-12-27 | 2008-07-17 | Tokyo Univ Of Agriculture & Technology | 生体関連化合物からなるイオン液体 |
| JP5117732B2 (ja) * | 2007-01-29 | 2013-01-16 | 株式会社 メドレックス | 外用剤用の低刺激性溶解助剤 |
| JP5333972B2 (ja) | 2007-11-22 | 2013-11-06 | 株式会社 メドレックス | 脂肪酸系イオン液体を有効成分とする外用剤組成物 |
| JP5550056B2 (ja) | 2012-09-05 | 2014-07-16 | 株式会社 メドレックス | 外用剤用の低刺激性溶解助剤 |
| JP2016535781A (ja) * | 2013-11-03 | 2016-11-17 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア | 経皮薬物送達のためのイオン性液体 |
-
2015
- 2015-10-30 EP EP18177251.8A patent/EP3395368A1/en not_active Withdrawn
- 2015-10-30 EP EP15855750.4A patent/EP3213769A4/en not_active Withdrawn
- 2015-10-30 JP JP2016556223A patent/JP6482570B2/ja active Active
- 2015-10-30 WO PCT/JP2015/080841 patent/WO2016068336A1/ja active Application Filing
- 2015-10-30 EP EP18177254.2A patent/EP3395369A1/en not_active Withdrawn
- 2015-10-30 US US15/519,246 patent/US20170239173A1/en not_active Abandoned
-
2018
- 2018-05-16 JP JP2018094298A patent/JP6693999B2/ja active Active
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