# US 12,285,488 B2 · Oral dosage form containing theobromine-free cocoa

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- Number: US 12,285,488 B2
- Document ID: US12285488B2
- Status: Granted
- Kind: B2
- Application number: 16/977,018
- Filed: 2018-03-01
- Published: 2021-01-07
- Granted: 2025-04-29
- Earliest claimed: 2018-03-01
- Assignees: LTS Lohmann Therapie-Systeme AG
- Applicants: Lts Lohmann Therapie-Systeme AG
- Inventors: Thomas Hille; Gabriel Wauer; Frank Seibertz
- Web page: https://patentgrep.com/patent/US12285488B2

## CPC

- A61K 9/0056: {Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals}
- A61K 47/46: Ingredients of undetermined constitution or reaction products thereof, e.g. skin, bone, milk, cotton fibre, eggshell, oxgall or plant extracts
- A23G 1/02: Preliminary treatment, e.g. fermentation of cocoa
- A23G 1/42: containing microorganisms or enzymes; containing paramedical or dietetical agents, e.g. vitamins (containing dairy products A23G1/46)
- A23G 3/364: {containing microorganisms or enzymes; containing paramedical or dietetical agents, e.g. vitamins}
- A23G 4/12: containing microorganisms or enzymes; containing paramedical or dietetical agents, e.g. vitamins (containing dairy products A23G4/16)
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/006: {Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays}
- A61K 31/4178: not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
- A61K 31/4196: 1,2,4-Triazoles
- A61K 31/465: Nicotine; Derivatives thereof
- A61K 36/5777: {Theobroma, e.g. cocao or cocoa}
- A61K 47/02: Inorganic compounds
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/186: {Quaternary ammonium compounds, e.g. benzalkonium chloride or cetrimide}
- 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 47/38: Cellulose; Derivatives thereof
- 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)
- A23G: COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF

## Abstract

Disclosed are stable dosage forms for oral administration of active pharmaceutical ingredients in which any unpleasant taste sensation, caused by release of the active pharmaceutical ingredient and/or of the excipients in the oral and pharyngeal cavity of the patient, is masked by the use of theobromine-free cocoa.

## Claims

### Claim 1

An oral dosage form in the form of an oral film which, when administered, releases an active pharmaceutical ingredient into the oral and pharyngeal cavity, said oral dosage form containing:
a) at least one active pharmaceutical ingredient;
b) at least one excipient; and
c) theobromine-free cocoa, wherein the oral dosage form contains at most 10% by weight of theobromine-free cocoa.

### Claim 2 (depends on 1)

The oral dosage form according to claim 1, characterised in that the dosage form contains at most 5% by weight of theobromine-free cocoa.

### Claim 3 (depends on 1)

The oral dosage form according to claim 1, characterised in that the dosage form contains at least 2% by weight of theobromine-free cocoa.

### Claim 4 (depends on 1)

The oral dosage form according to claim 1, characterised in that the dosage form contains less than a total of 5% by weight of one or more further taste correctors.

### Claim 5 (depends on 4)

The oral dosage form according to claim 4, characterised in that the taste correctors are sweetening agents and/or flavourings.

### Claim 6 (depends on 1)

The oral dosage form according to claim 1, characterised in that the theobromine-free cocoa contains less than 0.6% by weight of theobromine.

### Claim 7 (depends on 1)

The oral dosage form according to claim 1, characterised in that the active pharmaceutical ingredient is present in the dosage form in a content which, without the use of a taste corrector, leads to an unpleasant taste sensation when ingested.

### Claim 8 (depends on 1)

The oral dosage form according to claim 1, characterised in that the active pharmaceutical ingredient is present in a content of at least 2% by weight and at most 20% by weight.

### Claim 9 (depends on 1)

The oral dosage form according to claim 1, characterised in that the excipient or excipients are selected from the group comprising disintegrants, binders, solvents, fillers, emulsifiers, solubilisers, buffers, preservatives, sweetening agents, flavourings, absorption antioxidants, accelerators, or combinations thereof.

### Claim 10 (depends on 1)

A method to mask an unpleasant taste sensation when using oral dosage forms which release at least one active pharmaceutical ingredient in the oral and pharyngeal cavity, said method comprising the administration of the oral dosage form of claim 1.

### Claim 11 (depends on 1)

The oral dosage form according to claim 1, characterised in that the theobromine-free cocoa contains less than 0.3% by weight of theobromine.

### Claim 12 (depends on 1)

The oral dosage form according to claim 1, characterised in that the theobromine-free cocoa contains less than 0.15% by weight of theobromine.

### Claim 13

An oral dosage form in the form of an oral film which, when administered, releases an active pharmaceutical ingredient into the oral and pharyngeal cavity, said oral dosage form containing
a) at least one active pharmaceutical ingredient selected from the group consisting of acetaminophen, adlupulon, agomelatine, albuterol, alverine, amitriptyline, amphetamine sulfate, amygdalin D, apomorphine, artemisinin, aspirin, atorvastatin, atropine, azathioprine, barbiturates, amobarbital, cyclobarbital, pentobarbital, phenobarbital, benzaldehyde, benzamine, benzoin, brucine, caffeine, caprolactam, carisoprodol, cascarillin, catechin, cetirizine, quinidine, quinine, chlordiazepoxide, chlorhexidine, chloroquine, chlorpheniramine maleate, chlorpromazine, cinnamedrine, cinchonine, clarithromycin, clobutinol, clonixin, codamine, codeine, colchicine, cycloheximide, deferiprone, demerol, dexamethasone, dextromethorphan, diclofenac, diphenhydramine, diphenylhydantoin, dorzolamide, doxepin, doxylamine, enalapril, epinephrine, erythromycin, falcarindiol, famotidine, fentanyl citrate, glimepiride, guaifenesin, haloperidol, hydrocortisone, ibuprofen, lidocaine, lincomycin, lomotil, loperamide, lupolone, methacholine, methadone, 6-methyl-2-thiouracil, miconazole, morphine hydrochloride, sodium benzoate, neostigmine, nicotine, omeprazole, ondansetron, orphenadrine, pantoprazole, papaverine, pemirolast, penicillin, peroxide, phenacetin, phenothiazine, phenytoin, prednisolone, prednisolone sodium phosphate, prednisone, propylthiouracil, pseudoephedrine hydrochloride, rizatriptan, salicylamide, salicylic acid, salsalate, sildenafil citrate, streptomycin, sulfonamide, terfenadine, topiramate, tramadol, trapidil, trimethadione, trimethoprim, valpromide, vitamins, thiamine, warfarin, and salts thereof, arbutin, coumarin, cucurbitacin B, ginkgolide A, ginkgolide B, ginkgolide C, harman, helenalin, helicin, humulone, lupinine, noscapine, parthenolide, picrotoxinin, taurine, acesulfame-K, magnesium sulfate and saccharin;
b) at least one excipient; and
c) theobromine-free cocoa, wherein the oral dosage form contains at most 15% by weight of theobromine-free cocoa.

### Claim 14 (depends on 13)

The oral dosage form according to claim 13, characterized in that the active pharmaceutical ingredient comprises ondansetron, nicotine or rizatriptan.