# US 12,109,312 B2 · Oral tablet for taste masking of active ingredients

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- Number: US 12,109,312 B2
- Document ID: US12109312B2
- Status: Granted
- Kind: B2
- Application number: 17/341,785
- Filed: 2021-06-08
- Published: 2021-09-23
- Granted: 2024-10-08
- Earliest claimed: 2018-05-17
- Assignees: Fertin Pharma A/S
- Applicants: Fertin Pharma A/S
- Inventors: Helle Wittorff
- Web page: https://patentgrep.com/patent/US12109312B2

## CPC

- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates}
- 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 9/0058: {Chewing gums (non-medicinal aspects, preparing chewing gum A23G4/00; chewing gum for care of the teeth or oral cavity, e.g. with breath freshener A61Q11/00)}
- A61K 9/006: {Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays}
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/2077: {Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets}
- A61K 9/2095: {Tabletting processes}
- A61K 31/167: having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
- A61K 31/43: Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula [IMAGE cpc-sch-A61K-0952.gif], e.g. penicillins, penems
- A61K 31/485: Morphinan derivatives, e.g. morphine, codeine
- A61K 31/522: having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
- 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 9/2086: {Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat (active cores with a complete drug-free outer coat A61K9/28)}
- 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

An oral tablet for taste masking of active ingredients includes a population of particles and an active ingredient with off-note taste. The population of particles includes directly compressible (DC) and non-directly compressible (non-DC) sugar alcohol particles, the non-DC particles providing the tablet with a plurality of discrete non-DC areas, and the non-DC areas resulting at least partly in induced taste masking of the active ingredient upon mastication of the tablet.

## Claims

### Claim 1

An oral direct compression tablet for taste masking of active ingredients, the tablet comprising a population of particles and an active ingredient with off-note taste, the population of particles comprising directly compressible (DC) and non-directly compressible (non-DC) sugar alcohol particles, the non-DC particles consisting essentially of pure non-DC sugar alcohol, the non-DC particles providing the direct compression tablet with a plurality of discrete non-DC areas formed by single non-DC particles or small groups of non-DC particles distributed between the DC particles, and the non-DC areas resulting at least partly in induced taste masking upon mastication of the tablet, wherein said active ingredient with off-note taste is selected from the group consisting of an active ingredient with bitter taste, an active ingredient with metallic taste, an active ingredient with astringent taste, an active ingredient with chalky taste, an active ingredient with salty taste, and combinations thereof.

### Claim 2

An oral direct compression tablet for taste masking of active ingredients, the tablet comprising a population of particles and an active ingredient with off-note taste, the population of particles comprising directly compressible (DC) and non-directly compressible (non-DC) sugar alcohol particles, the non-DC particles consisting essentially of pure non-DC sugar alcohol, the non-DC particles providing the direct compression tablet with a plurality of discrete non-DC areas distributed between the DC particles, and the non-DC areas resulting at least partly in induced taste masking of the active ingredient upon mastication of the tablet, wherein said active ingredient with off-note taste is selected from the group consisting of an active ingredient with bitter taste, an active ingredient with metallic taste, an active ingredient with astringent taste, an active ingredient with chalky taste, an active ingredient with salty taste, and combinations thereof.

### Claim 3 (depends on 2)

The tablet according to claim 2, wherein the tablet comprises said non-DC sugar alcohol particles in an amount of at least 10% by weight of the tablet.

### Claim 4 (depends on 2)

The tablet according to claim 2, wherein at least 30% by weight of the non-DC sugar alcohol particles have a particles size above 500 μm.

### Claim 5 (depends on 2)

The tablet according to claim 2, wherein the tablet has a weight ratio between said non-DC sugar alcohol particles and said DC sugar alcohol particles, which is between 0.3 and 0.7.

### Claim 6 (depends on 2)

The tablet according to claim 2, wherein the non-DC sugar alcohol particles are selected from non-DC particles of erythritol, maltitol, mannitol, xylitol, lactitol, isomalt, and combinations thereof.

### Claim 7 (depends on 2)

The tablet according to claim 2, wherein the tablet is a chewable tablet.

### Claim 8 (depends on 2)

The tablet according to claim 2, wherein said active ingredient with off-note taste is an analgesic selected from the group consisting of ibuprofen, acetaminophen, dextromethorphan, ampicillin, clarithromycin, metronidazole, loperamide, caffeine, sumatriptan, ascorbic acid, and combinations thereof.

### Claim 9 (depends on 2)

The tablet according to claim 2, wherein said active ingredient with off-note taste is an antihistamine selected from the group consisting of cimetidine, ranitidine, famotidine, nizatidine, desloratadine, and combinations thereof.

### Claim 10 (depends on 2)

The tablet according to claim 2, wherein said active ingredient with off-note taste is a gastrointestinal active selected from the group consisting of omeprazole, ondansetron, loperamide, simethicone, calcium carbonate, metoclopramide, cisapride, docusate, and combinations thereof.

### Claim 11 (depends on 2)

The tablet according to claim 2, wherein said active ingredient with off-note taste is selected from vitamins, minerals, supplements, and combinations thereof.

### Claim 12 (depends on 2)

The tablet according to claim 2, wherein said active ingredient with off-note taste is a hormone selected from the group consisting of progesterone, testosterone, melatonin, and combinations thereof.

### Claim 13 (depends on 2)

The tablet according to claim 2, wherein said active ingredient with off-note taste is a zinc salt selected from the group consisting of zinc acetate, zinc chloride, zinc gluconate, and combinations thereof.

### Claim 14 (depends on 2)

The tablet according to claim 2, wherein said population of particles is tableted into a first module and combined with a second population of particles that is tableted into a second module.

### Claim 15 (depends on 2)

The tablet according to claim 2, wherein said population of particles is tableted into a first module and combined with a second population of particles that is tableted into a second module, wherein the second population of particles includes particles comprising gum base.

### Claim 16 (depends on 2)

The tablet according to claim 2, wherein said population of particles is tableted into a first module together with particles comprising gum base and combined with a second population of particles that is tableted into a second module.

### Claim 17

An oral tablet for taste masking of active ingredients, the tablet comprising a population of particles and an active ingredient with off-note taste, the population of particles comprising directly compressible (DC) and non-directly compressible (non-DC) sugar alcohol particles, the non-DC particles consisting essentially of pure non-DC sugar alcohol, the non-DC particles providing the tablet with a plurality of discrete non-DC areas distributed between the DC particles, and the non-DC areas resulting at least partly in induced taste masking of the active ingredient upon mastication of the tablet, wherein said active ingredient with off-note taste is selected from the group consisting of an active ingredient with bitter taste, an active ingredient with metallic taste, an active ingredient with astringent taste, an active ingredient with chalky taste, an active ingredient with salty taste, and combinations thereof.

### Claim 18 (depends on 17)

The tablet according to claim 17, wherein said active ingredient with off-note taste is selected from active ingredients for the throat selected from the group consisting of acetylcysteine, ambroxol, amylmetacresol, benzocaine, bisacodyl, bismuth subsalicylate, bromhexine, cetirizine, cetylpyridinium, chlorhexidine, dextromethorphan hydrobromide, 2,4-dichlorobenzyl alcohol, doxylamine succinate, eucalyptus oil, flurbiprofen, glycerin, hexylresorcinol, lidocaine, menthol, myrrh, paracetamol, pectin, peppermint oil, phenol, phenylephrine, povidone-iodine, pseudoephedrine, ranitidine, simethicone, sodium docusate, spearmint, zinc, and any combination thereof; active ingredients for the gastrointestinal tract selected from the group consisting of alginate, atenolol, aspirin (acetylsalicylic acid), ampicillin, aminosalicylates, anhydrous citric acid, bisacodyl, bismuth subsalicylate, bupropion, caffeine, calcium, calcium carbonate, cetirizine, cimetidine, cisapride, clarithromycin, desloratadine, dexlansoprazole, diphenhydramine HCl, diphenhydramine citrate, dimenhydrinate, docusate erythromycin, dopamine, esomeprazole, famotidine, fexofenadine HCl, guaifenesin, hydrotalcite, ibuprofen, ketoprofen, lactase enzyme, lansoprazole, loratadine, lorcaserin, loperamide, loperamide HCl, magnesium, magnesium carbonate, magnesium hydroxide, melatonin, methamphetamine HCl, metoclopramide, metronidazole, montelukast, mycostatin, naltrexone, naproxen, naproxen sodium, nizatidine, omeprazole, ondansetrone, orlistat, pantoprazole, paracetamol (acetaminophen), pectin, phentermine HCl, polypodium leucotomos, prednisolone, prednisone, progesterone, propranolol, propantheline bromide, pseudoephedrine HCl, phentermine, rabeprazole, ranitidine, roflumilast, scopoloamine butyl hydroxide, simethicone, sodium, sodium bicarbonate, sodium docusate, sumatriptan, testosterone, tetracycline, topiramate, vitamin A, vitamin B, vitamin B12, vitamin C (ascorbic acid), vitamin D, and vitamin E, vitamin K, and any combination thereof, and active ingredients for buccal absorption selected from the group consisting of atenolol, baclofene, caffeine, carvedilol, chlorpheniramine, chlorpheniramine maleate, fluticasone propionate, maleate, desmopressine, diltiazem hydrochloride, doxylamine succinate, mycostatin, nicotine, nifedipine, nitroglycerin, omeprazole, ondansetrone, oxymetazoline HCl, oxytocin, phenylephrine, piroxicam, prednisone, propranolol, salbutamol sulphate, scopoloamine butyl hydroxide, sumatriptan, triamcinolonacetonid, and any combination thereof.