# US 2025/0144015 A1 · Pharmaceutical Compositions

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- Number: US 2025/0144015 A1
- Document ID: US20250144015A1
- Status: Published application
- Kind: A1
- Application number: 18/937,113
- Filed: 2024-11-05
- Published: 2025-05-08
- Earliest claimed: 2023-11-06
- Assignees: Extrovis AG; Athyna Pharma LLC
- Applicants: Extrovis AG; Athyna Pharma LLC
- Inventors: Kirankumar Kowkuntla
- Web page: https://patentgrep.com/patent/US20250144015A1

## 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 9/006: {Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays}
- A61K 9/2013: {Organic compounds, e.g. phospholipids, fats}
- A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates}
- A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 9/2059: {Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin}
- A61K 9/2095: {Tabletting processes}
- A61K 31/485: Morphinan derivatives, e.g. morphine, codeine
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- 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

The present disclosure relates to a stable, fast-disintegrating pharmaceutical tablet for buccal or sublingual administration, containing buprenorphine or its pharmaceutically acceptable salt, and naloxone or its pharmaceutically acceptable salt, providing enhanced ease of administration. The stable pharmaceutical tablet disintegrates in a patient's oral cavity, under the tongue, and helps in sublingual absorption of the buprenorphine or its pharmaceutically acceptable salt.

## Claims

### Claim 1

A stable pharmaceutical tablet for buccal or sublingual administration, comprising:
from about 1 mg to about 24 mg of buprenorphine in the form of its base or a pharmaceutically acceptable salt; and
from about 0.5 mg to about 6 mg of naloxone in the form of its base or a pharmaceutically acceptable salt; and pharmaceutically acceptable excipients,
wherein the tablet:
has an in vitro disintegration time of less than 120 seconds when tested by the disintegration test defined in the United States Pharmacopoeia (USP);
has a hardness of 2-10 kP;
has a friability of less than 1%;
exhibits an in vivo disintegration time of less than 20 minutes; and
releases more than 85% of the buprenorphine in less than 5 minutes and all of the naloxone in less than 20 minutes, when tested in vitro in a dissolution apparatus defined in the United States Pharmacopoeia (USP).

### Claim 2 (depends on 1)

The pharmaceutical tablet according to claim 1, wherein the amount of buprenorphine or pharmaceutically acceptable salt thereof is about 16 mg and the amount of naloxone or its pharmaceutically salt is about 4 mg.

### Claim 3 (depends on 1)

The pharmaceutical tablet according to claim 1, wherein the amount of buprenorphine or pharmaceutically acceptable salt thereof, in the tablet is about 12 mg and the amount of naloxone or its pharmaceutically salt is about 3 mg.

### Claim 4 (depends on 1)

The pharmaceutical tablet according to claim 1, wherein the amount of buprenorphine or pharmaceutically acceptable salt thereof, in the tablet is about 4 mg and the amount of naloxone or its pharmaceutically salt is about 1 mg.

### Claim 5 (depends on 1)

The pharmaceutical tablet according to claim 1, wherein the amount of buprenorphine or pharmaceutically acceptable salt thereof, in the tablet is about 24 mg and the amount of naloxone or its pharmaceutically salt is about 6 mg.

### Claim 6 (depends on 1)

The pharmaceutical tablet according to claim 1, wherein the in vivo disintegration time is less than 20 minutes when the tablet is administered without any pre-hydration of the mouth with water.

### Claim 7 (depends on 1)

The pharmaceutical tablet according to claim 1, wherein the in vivo disintegration time is less than 10 minutes when the tablet is administered with pre-hydration of the mouth with water.

### Claim 8 (depends on 1)

The pharmaceutical tablet according to claim 1, further comprising a score mark or separation mark to guide a user in breaking the tablet along the designated area or region indicated by said score or separation mark.

### Claim 9 (depends on 1)

The pharmaceutical tablet according to claim 1, further comprising pharmaceutically acceptable excipients selected from one or more of disintegrating agent, filler, lubricant, diluent, binder, pH adjusting agent, buffer, sweetening agent, flavouring agent, and a combination thereof.

### Claim 10 (depends on 9)

The pharmaceutical tablet according to claim 9, wherein the pH adjusting agent is citric acid and the buffer is sodium citrate.

### Claim 11 (depends on 10)

The stable pharmaceutical tablet according to claim 10, wherein upon storage under accelerated stability conditions of 40° C. and 75% relative humidity for at least one month, the tablet contains about 0.1% w/w of the tablet or less of 3-O-allyl naloxone impurity and about 0.1% or less of Buprenorphine Impurity G.

### Claim 12 (depends on 11)

The stable pharmaceutical tablet according to claim 11, further comprising a total amount of naloxone-related degradants of about 0.2% w/w of the tablet or less and a total amount of buprenorphine-related degradants of about 0.2% w/w of the tablet or less.