# US 2021/0275513 A1 · Shellac microcapsule formulations and compositions for topical intestinal delivery of vitamin b3

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- Number: US 2021/0275513 A1
- Document ID: US20210275513A1
- Status: Published application
- Kind: A1
- Application number: 16/343,083
- Filed: 2017-04-12
- Published: 2021-09-09
- Earliest claimed: 2016-04-19
- Assignees: Conaris Research Institute AG; Christian-Albrechts-Universität zu Kiel
- Applicants: Conaris Research Institute AG; Christian-Albrechts-UniversitäT Zu Kiel
- Inventors: Karin SCHWARZ; Julia KEPPLER; Eva-Maria THEISMANN; Jörg KNIPP; Daniela FANGMANN; Matthias LAUDES; Stefan SCHREIBER; Georg WÄTZIG
- Web page: https://patentgrep.com/patent/US20210275513A1

## CPC

- A61K 9/28: Dragees; Coated pills or tablets {, e.g. with film or compression coating (A61K9/2072 takes precedence, e.g. partially coated tablets A61K9/2072, coated multilayer tablets A61K9/2086, tablets with drug-coated core A61K9/209)}
- A61K 31/455: Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
- A23L 33/135: Bacteria or derivatives thereof, e.g. probiotics
- A23L 33/15: Vitamins
- A23L 33/16: Inorganic salts, minerals or trace elements
- A23L 33/40: {Complete food formulations for specific consumer groups or specific purposes, e.g. infant formula}
- A23P 20/10: Coating with edible coatings, e.g. with oils or fats
- A61K 9/145: {with organic compounds}
- A61K 9/148: {with compounds of unknown constitution, e.g. material from plants or animals (with oils, fats, waxes, shellac A61K9/145)}
- A61K 9/16: Agglomerates; Granulates; Microbeadlets {; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction (A61K9/20 takes precedence if the final form is a tablet; microspheres with drug-free outer coating, microcapsules A61K9/50; mixture of different granules, microcapsules, (coated) microparticles A61K9/5084; nanoparticles A61K9/51)}
- A61K 9/2886: {having two or more different drug-free coatings; Tablets of the type inert core-drug layer-inactive layer (of the type active core-drug layer-inactive layer A61K9/209)}
- A61K 9/4808: {characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release (capsules filled with granules or microparticles A61K9/16; filled with microcapsules or coated microparticles A61K9/50; with mixture of different granules, microcapsules, (coated) microparticles A61K9/5084)}
- A61K 9/4891: {Coated capsules; Multilayered drug free capsule shells (with drug coating for immediate release A61K9/4808; osmotic devices A61K9/0004)}
- A61K 9/50: Microcapsules {having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals (A61K9/2081 takes precedence; particles with a single coating comprising drug A61K9/167)}
- A61K 9/5015: {Organic compounds, e.g. fats, sugars}
- A61K 9/5073: {having two or more different coatings optionally including drug-containing subcoatings}
- A61K 31/22: of acyclic acids, e.g. pravastatin
- A61K 31/366: having six-membered rings, e.g. delta-lactones
- A61K 31/40: having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K 31/404: Indoles, e.g. pindolol
- A61K 31/4418: having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
- A61K 31/505: Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K 31/522: having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61K 31/616: by carboxylic acids, e.g. acetylsalicylic acid
- A61K 35/741: Probiotics (probiotic yeast, e.g. saccharomyces A61K36/06)
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 3/02: Nutrients, e.g. vitamins, minerals
- 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)
- A23L: FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF (preservation thereof A23B)
- A23P: SHAPING OR WORKING OF FOODSTUFFS, NOT FULLY COVERED BY A SINGLE OTHER SUBCLASS
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to microcapsules comprising a core containing vitamin B3, which are characterised by a coating layer system comprising two layers of shellac and a pH-modulating substance provided between the two layers of shellac.

## Claims

### Claim 1

A microcapsule comprising a core containing vitamin B3, wherein the microcapsule comprises a coating layer system comprising an inner layer of shellac, an outer layer of shellac, and a pH-modulating substance provided between the inner and outer layers of shellac.

### Claim 2 (depends on 1)

The microcapsule according to claim 1, wherein the vitamin B3 comprises or consists of nicotinic acid, and the pH-modulating substance comprises or consists of a basic substance, preferably selected from hydrogen carbonate, carbonate salts, acetate salts, and mixtures thereof.

### Claim 3 (depends on 1)

The microcapsule according to claim 1, wherein the vitamin B3 comprises or consists of nicotinamide, and the pH-modulating substance comprises or consists of an acidic substance, preferably selected from organic acids, inorganic acids, and mixtures thereof.

### Claim 4 (depends on 1)

The microcapsule according to claim 1, characterised in that the pH-modulating substance comprises or consists of sodium hydrogen carbonate (sodium bicarbonate).

### Claim 5 (depends on 1)

The microcapsule according to claim 1, wherein the pH-modulating substance comprises or consists of citric acid.

### Claim 6 (depends on 1)

The microcapsule according to claim 1, formulated as a medicament, nutraceutical, dietary supplement, food ingredient or food.

### Claim 7 (depends on 1)

A method for beneficially influencing the intestinal microbiota and/or for beneficially influencing or preventing unfavourable and/or abnormal and/or imbalanced blood and/or plasma and/or serum lipid levels and/or for beneficially influencing or preventing intestinal inflammation and/or other unfavourable and/or abnormal changes in the intestine, comprising orally administering a microcapsule according to claim 1 to a subject in need thereof, wherein the microcapsule releases vitamin B3 for at least partial topical efficacy in the lower small intestine, the terminal ileum, and/or in the colon.

### Claim 8 (depends on 7)

The method of claim 7, wherein the method is for the therapy and/or prophylaxis of
a disease and/or syndrome associated with and/or accompanied by unfavourable or abnormal or imbalanced intestinal microbiota and/or
a disease and/or syndrome associated with and/or accompanied by unfavourable or abnormal or imbalanced blood and/or plasma and/or serum lipid levels, preferably in non-alcoholic fatty liver disease (NAFLD) and/or non-alcoholic steatohepatitis (NASH), for decreasing the liver fat content and/or beneficially influencing blood and/or plasma and/or serum lipid levels, and/or
a disease and/or syndrome associated with and/or accompanied by intestinal inflammation, preferably in inflammatory bowel diseases (IBD), and/or
other unfavourable or abnormal changes in the intestine, and/or
one or more selected from the group consisting of lipid metabolism disorders, dyslipidemia, NAFLD, NASH, cardiovascular diseases, arteriosclerosis, atherosclerosis, metabolic syndrome, obesity, diabetes, inflammatory diseases of the small intestine and/or colon, IBD, Crohn's disease, ulcerative colitis, indeterminate colitis, irritable bowel syndrome, colon carcinoma, psoriasis, allergy, atopic eczema, asthma, chronic obstructive pulmonary disease, cystic fibrosis, and other diseases and/or syndromes associated with and/or accompanied by unfavourable or abnormal or imbalanced blood and/or plasma and/or serum lipid levels and/or intestinal inflammation and/or other unfavourable or abnormal changes in the intestine and/or unfavourable or abnormal changes in the intestinal microbiota and/or an impaired interaction between the intestinal microbiota and the intestine.

### Claim 9 (depends on 1)

The microcapsule according to claim 1, comprising nicotinic acid and/or nicotinamide as the vitamin B3 component and further comprising one or more other active substances within the core selected from probiotics; prebiotics; synbiotics; polyphenols; substances, proteins and/or enzymes supporting probiotics; antibiotic, antimycotic, antiprotozoal, antihelminthic, antiviral or anti-inflammatory agents; aminosalicylates; acetylsalicylic acid; prostaglandin D2 antagonists; short-chain fatty acids; medium-chain fatty acids; systemic or topical corticosteroids; β2-adrenergic receptor agonists; theophylline and other substances of the xanthine family; statins; small molecules; peptides, biologicals, fusion proteins, monoclonal antibodies, or derivatives thereof.

### Claim 10 (depends on 1)

A composition comprising a microcapsule according to claim 1.

### Claim 11 (depends on 10)

The composition according to claim 10, formulated for oral administration with controlled and/or delayed release of vitamin B3.

### Claim 12 (depends on 11)

The composition according to claim 11, in the form of a finished oral dosage form having an active substance content of nicotinic acid and/or nicotinamide of 1-5000 mg each per finished dosage form.

### Claim 13 (depends on 10)

The composition according to claim 10, further comprising one or more other active substances selected from probiotics; prebiotics; synbiotics; polyphenols; substances, proteins and/or enzymes supporting probiotics; antibiotic, antimycotic, antiprotozoal, antihelminthic, antiviral or anti-inflammatory agents; aminosalicylates; acetylsalicylic acid; prostaglandin D2 antagonists; short-chain fatty acids; medium-chain fatty acids; systemic or topical corticosteroids; β2-adrenergic receptor agonists; theophylline and other substances of the xanthine family; statins; small molecules; peptides, biologicals, fusion proteins, monoclonal antibodies or derivatives thereof.

### Claim 14 (depends on 10)

A method for beneficially influencing the intestinal microbiota and/or for beneficially influencing or preventing unfavourable and/or abnormal and/or imbalanced blood and/or plasma and/or serum lipid levels and/or for beneficially influencing or preventing intestinal inflammation and/or other unfavourable and/or abnormal changes in the intestine, and/or for use in the therapy and/or prophylaxis of
a disease and/or syndrome associated with and/or accompanied by unfavourable or abnormal or imbalanced intestinal microbiota and/or
a disease and/or syndrome associated with and/or accompanied by unfavourable or abnormal or imbalanced blood and/or plasma and/or serum lipid levels, preferably in non-alcoholic fatty liver disease (NAFLD) and/or non-alcoholic steatohepatitis (NASH), for decreasing the liver fat content and/or beneficially influencing blood and/or plasma and/or serum lipid levels, and/or
a disease and/or syndrome associated with and/or accompanied by intestinal inflammation, preferably in inflammatory bowel diseases (IBD), and/or
other unfavourable or abnormal changes in the intestine, and/or
one or more selected from the group consisting of lipid metabolism disorders, dyslipidemia, NAFLD, NASH, cardiovascular diseases, arteriosclerosis, atherosclerosis, metabolic syndrome, obesity, diabetes, inflammatory diseases of the small intestine and/or colon, IBD, Crohn's disease, ulcerative colitis, indeterminate colitis, irritable bowel syndrome, colon carcinoma, psoriasis, allergy, atopic eczema, asthma, chronic obstructive pulmonary disease, cystic fibrosis, and other diseases and/or syndromes associated with and/or accompanied by unfavourable or abnormal or imbalanced blood and/or plasma and/or serum lipid levels and/or intestinal inflammation and/or other unfavourable or abnormal changes in the intestine and/or unfavourable or abnormal changes in the intestinal microbiota and/or an impaired interaction between the intestinal microbiota and the intestine,
comprising orally administering a composition according to claim 10 to a subject in need thereof.

### Claim 15 (depends on 1)

A method for producing a microcapsule according to claim 1, comprising:
a. providing a core material comprising or consisting of vitamin B3,
b. coating the core material with a first shellac layer,
c. providing a pH-modulating substance,
d. applying the pH-modulating substance onto the first shellac layer, and
e. applying a second shellac layer.