# US 12,109,304 B1 · Oral patch for treating mouth ulcers

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- Number: US 12,109,304 B1
- Document ID: US12109304B1
- Status: Granted
- Kind: B1
- Application number: 18/522,062
- Filed: 2023-11-28
- Granted: 2024-10-08
- Earliest claimed: 2023-11-13
- Assignees: Xiamen LP Pharmaceutical Co., Ltd.
- Applicants: Xiamen LP Pharmaceutical Co., Ltd.
- Inventors: Haijian Zhu; Rongbin Ling; Avinash Singh; Liyan Xie; Xiaojin Xiao
- Web page: https://patentgrep.com/patent/US12109304B1

## CPC

- A61K 9/006: {Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays}
- A61K 9/7046: {the adhesive comprising macromolecular compounds}
- A61K 9/7053: {obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene}
- A61K 9/7061: {Polyacrylates}
- A61K 9/7069: {obtained otherwise than by reactions only involving carbon to carbon unsaturated bonds, e.g. polysiloxane, polyesters, polyurethane, polyethylene oxide}
- A61K 31/167: having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
- A61K 31/245: Amino benzoic acid types, e.g. procaine, novocaine (salicylic acid esters A61K31/60)
- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61K 31/58: containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin (digitoxin {A61K31/7048})
- A61K 47/08: containing oxygen, {e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides}
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- 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 47/34: Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers (A61K47/10 takes precedence)
- A61K 47/36: Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K 47/38: Cellulose; Derivatives thereof
- A61K 47/42: Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein (oligopeptides having up to five amino acids {A61K47/183}; polyamino acids A61K47/34)
- 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 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention provides an oral patch for localized treatment of mouth ulcers containing combination of tetracaine and triamcinolone as active drugs. The patch is a bilayer structure containing a drug layer with amorphous tetracaine hydrochloride and amorphous triamcinolone acetonide and a water-soluble backing layer without a drug. The oral patch with combination of drugs has improved efficacy over each individual drug. The drug layer comprises 3-20% by weight of amorphous tetracaine hydrochloride, or a pharmaceutical acceptable salt thereof, 0.1-2.0% by weight of amorphous triamcinolone acetonide or a pharmaceutical acceptable salt thereof, 20-95% by weight of a first film-forming material, 1-12% by weight of an adhesive, 1-20% by weight of one or more cooling agent, and optionally 1-12% by weight of a plasticizer. The backing layer comprises 70-95% by weight of one or more film-forming agents, 2-10% by weight of a plasticizer and optionally 1-8% by weight of a flavoring agent.

## Claims

### Claim 1

A bilayer oral patch, comprising:
(a) a drug layer comprising 3%-20% by weight (w/w) of amorphous tetracaine or a pharmaceutically acceptable salt thereof, 0.1%-2.0% w/w of amorphous triamcinolone or a pharmaceutically acceptable salt thereof, 20-90% w/w of a first film-forming material, 1-12% w/w of an adhesive, and 1-20% w/w of a cooling excipient; and
(b) a backing layer comprising 70-95% by weight of a second film-forming material and 2-10% by weight of a plasticizer, wherein the backing layer prevents the tetracaine, the triamcinolone, or their pharmaceutically acceptable salts, from diffusing into the oral cavity;
wherein the first film-forming material comprises (a) hypromellose acetate succinate (HPMCAS) and povidone (PVP), (b) ethyl cellulose and PVP, (c) HPMCAS and polyethylene glycol (PEG), or (d) HPMCAS and hydroxypropyl cellulose (HPC);
the adhesive is selected from the group consisting of: polyacrylic acid, sodium alginate, copolymer of ethyl acrylate methyl methacrylate, guar gum, sodium carboxyl methyl cellulose, 5-methyl pyrrolidone chitosan, polyglutamic acid, polycarbophil, dextran sulfate, and any combination thereof;
the cooling excipient is selected from the group consisting of: camphor, menthol, mint oil, clove oil, menthyl acetate, xylitol, sorbitol, thymol, and any combination thereof; and
the second film-forming material is selected from the group consisting of: HPMC, HPC, hydroxyethyl cellulose (HEC), hydroxypropylated high amylose starch, methylmethacrylate-based copolymer, povidone, collagen, gelatin, pectin, cellulose acetate phthalate (CAP), polyvinyl alcohol (PVA), polyvinyl alcohol phthalate (PVAP), and any combination thereof.

### Claim 2 (depends on 1)

The bilayer oral patch according to claim 1, wherein the first film-forming material comprises HPMCAS and PVP.

### Claim 3 (depends on 1)

The bilayer oral patch according to claim 1, wherein the second film-forming material is selected from the group consisting of: HPMC, HPC, HEC, hydroxypropylated high amylose starch, methylmethacrylate-based copolymer, povidone, and any combination thereof.

### Claim 4 (depends on 1)

The bilayer oral patch according to claim 1, wherein the drug layer further comprises a plasticizer in an amount of 1-12% w/w.

### Claim 5 (depends on 4)

The bilayer oral patch according to claim 4, wherein the plasticizer in the drug layer and the plasticizer in the backing layer are independently selected from the group consisting of: glycerin, triethyl citrate, propylene glycol, and any combination thereof.

### Claim 6 (depends on 1)

The bilayer oral patch according to claim 1, wherein the thickness of the backing layer is 100-200 μm.

### Claim 7 (depends on 1)

The bilayer oral patch according to claim 1, wherein the amount of the tetracaine or its pharmaceutically acceptable salt is 1-6 mg.

### Claim 8 (depends on 1)

The bilayer oral patch according to claim 1, wherein the amount of the triamcinolone or its pharmaceutically acceptable salt is 0.03-0.65 mg.

### Claim 9 (depends on 1)

The bilayer oral patch according to claim 1, wherein the drug layer further comprises 1-8% w/w of one or more flavoring agents.

### Claim 10 (depends on 1)

The bilayer oral patch according to claim 1, wherein the backing layer further comprises 1-8% w/w of one or more flavoring agents.

### Claim 11 (depends on 1)

The bilayer oral patch according to claim 1, wherein the drug layer comprises amorphous tetracaine hydrochloride and amorphous triamcinolone acetonide.

### Claim 12 (depends on 11)

The bilayer oral patch according claim 11, wherein the drug layer comprises 3%-20% w/w of amorphous tetracaine hydrochloride, 0.1%-2.0% w/w of amorphous triamcinolone acetonide, 30-90% w/w of the first film-forming material, 1-8% w/w of the adhesive, 1-15% w/w of the cooling excipient, and 1-12% w/w of a plasticizer; and
(b) the backing layer comprises 80%-95% by weight of the second film-forming material and 2-8% by weight of the plasticizer.

### Claim 13 (depends on 1)

The bilayer oral patch according claim 1, having a size from 1 cm×1 cm to 2 cm×2 cm.

### Claim 14 (depends on 1)

A method for treating mouth ulcer in a subject, comprising the steps of:
identifying a subject in need thereof, and
attaching the bilayer oral patch of claim 1 onto the mucosa of the mouth ulcer of the subject.

### Claim 15 (depends on 1)

The bilayer oral patch according to claim 1, wherein the first film-forming material comprises ethyl cellulose and PVP.

### Claim 16 (depends on 1)

The bilayer oral patch according to claim 1, wherein the first film-forming material comprises HPMCAS and PEG.

### Claim 17 (depends on 1)

The bilayer oral patch according to claim 1, wherein the first film-forming material comprises HPMCAS and HPC.