IP Library Granted Patent US 10,258,694
Granted Patent B2
US 10,258,694 · App. 15/312,985 · Granted Apr 16, 2019

Skin external preparation and skin irritation-reducing method

Inventors: Kenichi Suzuki (Fuji, JP); Haruki Nakagawa (Fuji, JP); Yoshihiro Yamakita (Fuji, JP); Eiichi Ozeki (Kyoto, JP); Takashi Kawabe (Kyoto, JP); Eri Matsutani (Kyoto, JP)
Assignee: Shimadzu Corporation
A61K47/34A61K9/0014A61K9/107A61K9/1075A61K9/50A61K31/13A61K31/325A61K31/47C08G63/912C08G2230/00
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Quick Facts
Patent No.
US 10,258,694
App. No.
15/312,985
Granted
Apr 16, 2019
Kind
B2
Abstract

Provided is a skin external preparation including a drug and nanometer-size molecular assemblies. The molecular assemblies contain an amphiphilic block copolymer having a hydrophilic block chain including a sarcosine-derived structural unit and a hydrophobic block chain including a hydroxy acid-derived structural unit. The skin external preparation according to the present invention may reduce skin irritation caused by the drug, be very safe, and have excellent pharmacological effects, even when a drug that is generally difficult to be transdermally administered due to its strong skin irritation is contained therein.

Claims (14)

1. A method for reducing skin irritation caused by a drug, comprising:

administering, to a subject in need of the drug, a skin external preparation comprising the drug, and an amphiphilic block copolymer having a hydrophilic block chain including sarcosine monomer units and a hydrophobic block chain including hydroxy acid monomer units,

wherein the drug is one of a statin and an Alzheimer-type dementia treatment drug.

2. The method of claim 1 , wherein the amphiphilic block copolymer forms a molecular assembly.

3. The method of claim 1 , wherein the hydrophilic block chain has 20 or more of sarcosine monomer units.

4. The method of claim 1 , wherein the hydrophobic block chain has 10 or more of hydroxy acid monomer units.

5. The method of claim 1 , wherein a hydroxy acid of the hydroxy acid-derived structural unit is lactic acid.

6. The method of claim 1 , wherein the amphiphilic block copolymer is represented by formula (3),

where R1 is a hydrogen or a methyl group, R2 is a single bond or methylene group, R3 is a divalent hydrocarbon group having 1 to 6 carbons, m is an integer in a range of 20 to 200, and n is an integer in a range of 10 to 100.

7. The method of claim 2 , wherein the molecular assembly and the drug coexist in a mixed state.

8. The method of claim 2 , wherein a region containing the molecular assembly and a region containing the drug are present in the skin external preparation.

9. The method of claim 6 , wherein in the formula (3), m is an integer of 30 to 150, and n is an integer of 15 to 80.

10. The method of claim 1 , wherein the molecular assemblies have an average particle diameter in a range of 15 to 60 nm.

11. The method of claim 1 , wherein the molecular assemblies have an average particle diameter in a range of 20 to 45 nm.

Assignments (2)
CONFIRMATORY LICENSE Recorded Sep 26, 2022
From: HARVARD UNIVERSITY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 061536/0698 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 21, 2016
From: SUZUKI, KENICHI; NAKAGAWA, HARUKI; YAMAKITA, YOSHIHIRO; OZEKI, EIICHI; KAWABE, TAKASHI; MATSUTANI, ERI
To: SHIMADZU CORPORATION
Reel/Frame 040394/0170 →
Priority Claims (1)
JP 2014-107070 · May 23, 2014 · national
Continuity (1)
Related Publication 20170151335A1 · Jun 1, 2017