# US 2019/0167596 A1 · Sustained Release Compositions Comprising Micronized Tolcapone

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- Number: US 2019/0167596 A1
- Document ID: US20190167596A1
- Status: Published application
- Kind: A1
- Application number: 16/321,336
- Filed: 2017-07-28
- Published: 2019-06-06
- Earliest claimed: 2016-07-29
- Assignees: SOM Innovation Biotech, S.L.
- Applicants: Som Innovation Biotech, S.L.
- Inventors: Anna Nardi Ricart; Josep María Suñé Negre; Núria Reig Bolaño; Raúl Insa Boronat; Oscar Huertas Gambín; Santiago Esteva Gras; Gal·la Pericot Mohr
- Web page: https://patentgrep.com/patent/US20190167596A1

## CPC

- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/2009: {Inorganic compounds}
- A61K 9/2013: {Organic compounds, e.g. phospholipids, fats}
- A61K 9/2095: {Tabletting processes}
- A61K 31/12: Ketones
- A61K 31/122: having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
- A61P 25/16: Anti-Parkinson drugs
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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 relates to sustained release tablet comprising micronized tolcapone, a release retardant and a binder, to said tablet for use in the prevention and/or treatment of a transthyretin-associated amyloidosis, to a method for the prevention and/or treatment of a transthyretin-associated amyloidosis comprising administering to a subject in need thereof an effective amount of said tablet, to pharmaceutical composition in the form of said tablet which is used in the prevention and/or treatment of a transthyretin-associated amyloidosis and to a process for the manufacture of said tablet.

## Claims

### Claim 1

A sustained release tablet comprising micronized tolcapone, a release retardant and a binder.

### Claim 2 (depends on 1)

A tablet according to claim 1 wherein the release retardant is a cellulose polymer.

### Claim 3 (depends on 2)

A tablet according to claim 2 wherein the cellulose polymers is selected from the group consisting of cellulose ethers and cellulose esters.

### Claim 4 (depends on 3)

A tablet according to claim 3 wherein the cellulose polymer is hydroxypropyl methyl cellulose

### Claim 5 (depends on 1)

A tablet according to claim 1 wherein the binder is microcrystalline cellulose.

### Claim 6 (depends on 1)

A tablet according to claim 1 wherein the tolcapone used in the manufacture of the tablet has a particle size distribution characterized in that its DV,0.9 is not greater than 70 μm.

### Claim 7 (depends on 1)

A tablet according to claim 1 characterized in that it comprises from 5% to 80% by weight of tolcapone.

### Claim 8 (depends on 1)

A tablet according to claim 1 characterized in that the proportion of tolcapone dissolved after 5 hours in the conditions of USP36 Tolcapone monograph is not higher than 90% of the total amount of tolcapone in the tablet.

### Claim 9 (depends on 1)

A tablet according to claim 1 characterized in that it shows a release of tolcapone such that not greater than 90% is released during the period starting with oral ingestion and ending 5 hours after oral ingestion.

### Claim 10 (depends on 1)

A tablet according to claim 1 wherein the tolcapone used in the manufacture of the tablet has a particle size distribution characterized in that its DV,0.9 is greater than 10 μm but not greater than 80 μm.

### Claim 11 (depends on 1)

A tablet according to claim 1 comprising tolcapone, hydroxypropylmethyl cellulose and microcrystalline cellulose.

### Claim 12 (depends on 11)

A tablet according to claim 11 comprising tolcapone, hydroxypropylmethyl cellulose, microcrystalline cellulose, talc, magnesium stearate and anhydrous colloidal silica.

### Claim 13 (depends on 12)

A tablet according to claim 12 comprising:
a) 5 to 80% of tolcapone
b) 20 to 36% of hydroxypropylmethyl cellulose
c) 8 to 65% of microcrystalline cellulose
d) 0.1 to 3% of talc
e) 0.03 to 2% of magnesium stearate
f) 0.06 to 0.8% of anhydrous colloidal silica

### Claim 14

(canceled)

### Claim 15 (depends on 1)

A method for the prevention and/or treatment of a transthyretin-associated amyloidosis comprising administering to a subject in need thereof an effective amount of a tablet according to claim 1.

### Claim 16

(canceled)

### Claim 17

(canceled)

### Claim 18 (depends on 1)

A process for the manufacture of a tablet of claim 1 comprising:
a) providing tolcapone, a release retardant and a binder
b) optionally sieving the ingredients of step a) with a mesh having 5 mm openings
c) mixing the ingredients of step b)
d) compressing the ingredients of step c) to form tablets.