# US 11,992,562 B2 · Percutaneous absorption preparation for treating dementia comprising donepezil

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- Number: US 11,992,562 B2
- Document ID: US11992562B2
- Status: Granted
- Kind: B2
- Application number: 16/957,774
- Filed: 2018-11-07
- Published: 2021-03-04
- Granted: 2024-05-28
- Earliest claimed: 2017-12-27
- Assignees: Dong-A St Co., Ltd.; Km Transderm Ltd.
- Applicants: Dong-A St Co., Ltd.; Km Transderm Ltd.
- Inventors: Sun-Woo Jang; Chang-Yell Shin; Jeong-Soo Kim; Hae-Sun Kim; Kwang-Ho Cha; Hyun-Jung Kim; Masaoki Goto
- Web page: https://patentgrep.com/patent/US11992562B2

## CPC

- A61K 9/7053: {obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene}
- A61K 9/7084: {Transdermal patches having a drug layer or reservoir, and one or more separate drug-free skin-adhesive layers, e.g. between drug reservoir and skin, or surrounding the drug reservoir; Liquid-filled reservoir patches}
- A61F 13/0276: {Apparatus or processes for manufacturing adhesive dressings or bandages}
- A61K 31/445: Non condensed piperidines, e.g. piperocaine
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- A61K 47/32: Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone}
- A61K 47/44: Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin (synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14)
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61F 2013/0296: {for making transdermal patches (chemical processes excluded)}
- B29D 7/01: Films or sheets
- B29K 2071/02: {Polyalkylene oxides, e.g. PEO, i.e. polyethylene oxide, or derivatives thereof}
- B29L 2031/753: {Medical equipment; Accessories therefor (bloodbags, medical bags B29L2031/7148; artificial eyes B29L2011/0008)}
- 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)
- A61F: FILTERS IMPLANTABLE INTO BLOOD VESSELS; PROSTHESES; DEVICES PROVIDING PATENCY TO, OR PREVENTING COLLAPSING OF, TUBULAR STRUCTURES OF THE BODY, e.g. STENTS; ORTHOPAEDIC, NURSING OR CONTRACEPTIVE DEVICES; FOMENTATION; TREATMENT OR PROTECTION OF EYES OR EARS; BANDAGES, DRESSINGS OR ABSORBENT PADS; FIRST-AID KITS (dental prosthetics A61C)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- B29D: PRODUCING PARTICULAR ARTICLES FROM PLASTICS OR FROM SUBSTANCES IN A PLASTIC STATE (making granules B29B9/00; making preforms B29B11/00)
- B29K: INDEXING SCHEME ASSOCIATED WITH SUBCLASSES B29B, B29C OR B29D, RELATING TO MOULDING MATERIALS OR TO MATERIALS FOR {MOULDS, } REINFORCEMENTS, FILLERS OR PREFORMED PARTS, e.g. INSERTS
- B29L: INDEXING SCHEME ASSOCIATED WITH SUBCLASS B29C, RELATING TO PARTICULAR ARTICLES

## Abstract

A percutaneous absorption preparation is disclosed. The percutaneous absorption preparation contains donepezil for treatment of dementia, wherein the preparation includes: (a) donepezil or its pharmaceutically acceptable salt as active component, (b) propylene glycol monocaprylate as solubilizer, and (c) styrene-isoprene-styrene block copolymer (“SIS”) as adhesive. The percutaneous absorption preparation has low skin irritation and high skin penetration.

## Claims

### Claim 1

A percutaneous absorption preparation for the treatment of dementia comprising a backing layer, a drug-containing layer, and a release liner,
wherein the drug-containing layer of the percutaneous absorption preparation comprises (a) donepezil or a pharmaceutically acceptable salt thereof as an active component, (b) a propylene glycol monocaprylate as a solubilizer, (c) a styrene-isoprene-styrene block copolymer as an adhesive, and (d) a plasticizer,
wherein a ratio of donepezil or the pharmaceutically acceptable salt thereof: the propylene glycol monocaprylate is not less than 1:1.5 by weight,
wherein the styrene-isoprene-styrene block copolymer makes up 10-70 wt % of a total weight of the drug-containing layer, and
wherein the plasticizer (d) is selected from the group consisting of paraffin process oil, naphthalene process oil, aromatic process oil, olive oil, camellia oil, tall oil, castor oil, isopropyl myristate, hexyl lauric acid, mineral oil, octyldodecyl myristate, propylene glycol, and a combination thereof.

### Claim 2 (depends on 1)

The percutaneous absorption preparation according to claim 1, wherein the donepezil as an active component is donepezil free base.

### Claim 3 (depends on 1)

The percutaneous absorption preparation according to claim 1, wherein the propylene glycol monocaprylate makes up 1-40 wt % of the total weight of the drug-containing layer.

### Claim 4 (depends on 3)

The percutaneous absorption preparation according to claim 3, wherein the propylene glycol monocaprylate makes up 3-30 wt % of the total weight of the drug-containing layer.

### Claim 5 (depends on 4)

The percutaneous absorption preparation according to claim 4, wherein the propylene glycol monocaprylate makes up 5-25 wt % of the total weight of the drug-containing layer.

### Claim 6 (depends on 1)

A process for preparing the percutaneous absorption preparation of claim 1, wherein the process comprises the following steps:
(a) dissolving propylene glycol monocaprylate, styrene-isoprene-styrene block copolymer and doenpezil free base in an organic solvent;
(b) casting the solution obtained in step (a) on a release linear, followed by drying, to form a drug-containing layer; and
(c) laminating the drug-containing layer with a backing layer.

### Claim 7 (depends on 1)

The percutaneous absorption preparation according to claim 1, wherein the ratio of donepezil or the pharmaceutically acceptable salt thereof: the propylene glycol monocaprylate is 1:1.5-1:4.5 by weight.