# US 2016/0256552 A1 · Transdermal colloidal solution agent

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- Number: US 2016/0256552 A1
- Document ID: US20160256552A1
- Status: Published application
- Kind: A1
- Application number: 15/156,244
- Filed: 2016-05-16
- Published: 2016-09-08
- Earliest claimed: 2013-11-17
- Assignees: Medrx Co., Ltd.
- Applicants: MEDRx CO., LTD
- Inventors: Keiko YAMASAKI
- Web page: https://patentgrep.com/patent/US20160256552A1

## CPC

- A61K 47/24: containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 9/10: Dispersions; Emulsions
- A61K 9/7069: {obtained otherwise than by reactions only involving carbon to carbon unsaturated bonds, e.g. polysiloxane, polyesters, polyurethane, polyethylene oxide}
- A61K 31/13: Amines {(A61K31/04 takes precedence)}
- A61K 31/135: having aromatic rings {, e.g. ketamine, nortriptyline (methadone A61K31/137)}
- A61K 31/343: condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
- A61K 31/405: Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
- A61K 31/4196: 1,2,4-Triazoles
- A61K 31/445: Non condensed piperidines, e.g. piperocaine
- A61K 31/473: ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
- A61K 31/55: having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/18: Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

Disclosed is a transdermal absorptive liquid preparation in which a medicament or a salt thereof is colloidally dispersed in propylene glycol or a propylene glycol-containing solvent, whose transdermal permeability of the medicament is excellent, problem of skin irritation is reduced. This transdermal absorptive liquid formulation has a mode of particle diameter at around 100 nm, and an average particle size of 50 to 500 nm. This transdermal absorptive liquid formulation makes marked improvement in the transdermal permeability by further containing an absorption promoter such as triethanolamine.

## Claims

### Claim 1

A transdermal absorptive colloidal liquid formulation comprising a medicament or a salt thereof colloidally dispersed in propylene glycol or a propylene glycol-containing solvent in the presence of phosphatidyl choline.

### Claim 2 (depends on 1)

The transdermal absorptive colloidal liquid formulation according to claim 1, further comprising an alkanolamine.

### Claim 3 (depends on 2)

The transdermal absorptive colloidal liquid formulation according to claim 2, wherein the alkanolamine is triethanolamine.

### Claim 4 (depends on 1)

The transdermal absorptive colloidal liquid formulation according to claim 1, wherein the medicament contains a six-membered ring skeleton and a nitrogen-containing group in a structure of the medicament.

### Claim 5 (depends on 1)

The transdermal absorptive colloidal liquid formulation according to claim 1, wherein an amount of the phosphatidyl choline is from 0.1 to 5 w/w % based on a total amount of the transdermal absorptive colloidal liquid formulation.

### Claim 6 (depends on 1)

The transdermal absorptive colloidal liquid formulation according to claim 1, wherein the phosphatidyl choline is an unsaturated phosphatidyl choline.

### Claim 7 (depends on 2)

The transdermal absorptive colloidal liquid formulation according to claim 2, wherein an amount of the alkanolamine is from 0.01 to 10 w/w % based on a total amount of the transdermal absorptive colloidal liquid formulation.

### Claim 8 (depends on 1)

The transdermal absorptive colloidal liquid formulation according to claim 1, wherein the phosphatidyl choline is at least one selected from the group consisting of an egg yolk phosphatidyl choline and soybean phosphatidyl choline.

### Claim 9

A transdermal absorptive liquid formulation comprising a medicament or a salt thereof, propylene glycol, phosphatidyl choline, and a higher alcohol.

### Claim 10 (depends on 9)

The transdermal absorptive liquid formulation of claim 9, wherein the higher alcohol is oleyl alcohol and/or isostearyl alcohol.

### Claim 11 (depends on 9)

The transdermal absorptive liquid formulation of claim 9, wherein an amount of the higher alcohol is 0.1 to 10 weight % based on a total weight of the transdermal absorptive liquid formulation.

### Claim 12 (depends on 9)

The transdermal absorptive liquid formulation of claim 9, wherein an amount of the higher alcohol is 0.2 to 5 weight % based on a total weight of the transdermal absorptive liquid formulation.

### Claim 13 (depends on 9)

The transdermal absorptive liquid formulation of claim 9, wherein an amount of the propylene glycol is 40 to 98 weight % based on a total weight of the transdermal absorptive liquid formulation.

### Claim 14 (depends on 9)

The transdermal absorptive liquid formulation of claim 9, wherein an amount of the propylene glycol is 60 to 90 weight % based on a total weight of the transdermal absorptive liquid formulation.

### Claim 15 (depends on 9)

The transdermal absorptive liquid formulation of claim 9, wherein an amount of the phosphatidyl choline is 0.1 to 5 weight % based on a total weight of the transdermal absorptive liquid formulation.

### Claim 16 (depends on 9)

The transdermal absorptive liquid formulation of claim 9, further comprising an alkanolamine.

### Claim 17 (depends on 16)

The transdermal absorptive colloidal liquid formulation according to claim 16, wherein the alkanolamine is triethanolamine.
