Spray base material including low-molecular gelator

Patent metadata

Field	Value
Publication number	US-9333158-B2
Application number	US-201013256765-A
Country	US
Kind code	B2
Filing date	Mar 12, 2010
Priority date	Mar 16, 2009
Publication date	May 10, 2016
Grant date	May 10, 2016

Abstract

A spray base material containing an aqueous medium that is gelled by a low-molecular gelator in the medium, wherein the low-molecular gelator includes one or more compounds selected from low-molecular compounds capable of gelling the aqueous medium via self-assembly.

First claim

The invention claimed is:

1. A spray base material comprising:
an aqueous medium that is gelled by a low-molecular gelator in the medium, wherein:
the molecular weight of the low-molecular gelator is not higher that 1000; and
the low-molecular gelator is capable of gelling the aqueous medium via self-assembly and comprises at least one lipid peptide of Formula (1) or a pharmaceutically usable salt thereof:

where:
R 1 is a C 9-23 aliphatic group,
R 2 is a hydrogen atom or a C 1-4 alkyl group that optionally contains a C 1-2 branched chain,
R 3 is a —(CH 2 ) n —X group,
n is a number of 1 to 4, and
X is an:
amino group,
a guanidino group,
a —CONH 2 group,
a 5-membered ring optionally containing 1 to 3 nitrogen atoms,
a 6-membered ring optionally containing 1 to 3 nitrogen atoms, or
a condensed heterocycle that contains a 5-membered ring and a 6-membered ring optionally containing 1 to 3 nitrogen atoms.

2. The spray base material according to claim 1 , wherein a concentration of the low-molecular gelator in the gelled aqueous medium is 0.0001 to 20% (w/v).

3. The spray base material according to claim 1 , wherein the low-molecular gelator contains a hydrophobic moiety and a hydrophilic moiety.

4. The spray base material according to claim 1 , wherein in Formula (1), R 3 is a —(CH 2 ) n —X group, n is a number of 1 to 4, and X is an amino group, a guanidino group, a —CONH 2 group, a 5-membered ring optionally containing 1 or 2 nitrogen atoms, or a condensed heterocycle that contains a 5-membered ring and a 6-membered ring optionally containing 1 or 2 nitrogen atoms.

5. The spray base material according to claim 1 , wherein in Formula (1), R 1 is a linear C 11-21 aliphatic group that optionally contains 0 to 2 unsaturated bonds.

6. The spray base material according to claim 1 , wherein in Formula (1), R 2 is a hydrogen atom or a C 1-3 alkyl group that optionally contains a C 1 branched chain.

7. The spray base material according to claim 4 , wherein in Formula (1), n is a number of 1 to 4 and X is an amino group, a guanidino group, or a —CONH 2 group, or n is 1 and X is a pyrrole group, an imidazole group, a pyrazole group, or an imidazole group.

8. The spray base material according to claim 1 , further comprising a physiologically active substance or a functional substance.

9. A thin film comprising:
at least one compound having a molecular weight that is not higher that 1000 that is capable of gelling an aqueous medium via self-assembly, the at least one compound comprising at least one lipid peptide of Formula (1) or a pharmaceutically usable salt thereof:

where:
R 1 is a C 9-23 aliphatic group,
R 2 is a hydrogen atom or a C 1-4 alkyl group that optionally contains a C 1-2 branched chain,
R 3 is a —(CH 2 ) n —X group,
n is a number of 1 to 4, and
X is an:
amino group,
a guanidino group,
a —CONH 2 group,
a 5-membered ring optionally containing 1 to 3 nitrogen atoms,
a 6-membered ring optionally containing 1 to 3 nitrogen atoms, or
a condensed heterocycle that contains a 5-membered ring and a 6-membered ring optionally containing 1 to 3 nitrogen atoms; and

the aqueous medium.

10. The thin film according to claim 9 , wherein the self-assembled at least one compound has a fibrous structure.

11. A sol obtained by mechanically disintegrating an aqueous medium that is gelled by a low-molecular gelator in the medium, wherein:
the molecular weight of the low-molecular gelator is not higher than 1000; and
the low-molecular gelator is capable of gelling the aqueous medium via self-assembly and comprises at least one lipid peptide of Formula (1) or a pharmaceutically usable salt thereof:

where:
R 1 is a C 9-23 aliphatic group,
R 2 is a hydrogen atom or a C 1-4 alkyl group that optionally contains a C 1-2 branched chain,
R 3 is a —(CH 2 ) n —X group,
n is a number of 1 to 4, and
X is an:
amino group,
a guanidino group,
a —CONH 2 group,
a 5-membered ring optionally containing 1 to 3 nitrogen atoms,
a 6-membered ring optionally containing 1 to 3 nitrogen atoms, or
a condensed heterocycle that contains a 5-membered ring and a 6-membered ring optionally containing 1 to 3 nitrogen atoms.

12. A spray base material comprising the sol of claim 11 .

13. The spray base material according to claim 12 , wherein in Formula (1), R 3 is a —(CH 2 ) n —X group, n is a number of 1 to 4, and X is an amino group, a guanidino group, a —CONH 2 group, a 5-membered ring optionally containing 1 or 2 nitrogen atoms, or a condensed heterocycle that contains a 5-membered ring and a 6-membered ring optionally containing 1 or 2 nitrogen atoms.

14. The spray base material according to claim 12 , wherein in Formula (1), R 1 is a linear C 11-21 aliphatic group that optionally contains 0 to 2 unsaturated bonds.

15. The spray base material according to claim 12 , wherein in Formula (1), R 2 is a hydrogen atom or a C 1-3 alkyl group that optionally contains a C 1 branched chain.

16. The spray base material according to claim 13 , wherein in Formula (1), n is a number of 1 to 4 and X is an amino group, a guanidino group, or a —CONH 2 group, or n is 1 and X is a pyrrole group, an imidazole group, a pyrazole group, or an imidazole group.

17. A sol comprising:
a compound of Formula (1):

where:
R 1 is a C 9-23 aliphatic group,
R 2 is a hydrogen atom or a C 1-4 alkyl group that optionally contains a C 1-2 branched chain,
R 3 is a —(CH 2 ) n —X group,
n is a number of 1 to 4, and
X is an:
amino group,
a guanidino group,
a —CONH 2 group,
a 5-membered ring optionally containing 1 to 3 nitrogen atoms,
a 6-membered ring optionally containing 1 to 3 nitrogen atoms, or
a condensed heterocycle that contains a 5-membered ring and a 6-membered ring optionally containing 1 to 3 nitrogen atoms; and

an aqueous medium;
wherein the molecular weight of the compound of Formula (1) is not higher than 1000.

18. A spray base material comprising the sol as claimed in claim 17 .

19. A process for preparing a thin film comprising applying the spray base material as claimed in claim 1 by a spray method.

Assignees

• Miyamoto Misao
• Iwama Takehisa
• Miyachi Nobuhide
• Gotoh Masahiro
• Nissan Chemical Ind Ltd
• Univ Kyushu

Inventors

• Miyamoto Misao
• Iwama Takehisa
• Miyachi Nobuhide
• Gotoh Masahiro

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61Q19/00

  Preparations for care of the skin · CPC title

• A61K9/7015

  Drug-containing film-forming compositions, e.g. spray-on · CPC title

• A61K2800/48

  Thickener, Thickening system · CPC title

• A61K8/64 Primary

  Proteins; Peptides; Derivatives or degradation products thereof · CPC title