Solid dosage forms of elafibranor

Abstract

The present invention relates to formulations of elafibranor or a pharmaceutically acceptable salt or ester thereof; and uses thereof. In particular, the present invention relates to an oral solid dosage form comprising at least elafibranor or a pharmaceutically acceptable salt or ester thereof; a filler, a disintegrating agent and a binder.

Description

Abstract This invention relates to formulations of irafenox or its pharmaceutically acceptable salts or esters and their uses. Specifically, this invention relates to an oral solid dosage form comprising at least irafenox or its pharmaceutically acceptable salts or esters, a filler, a disintegrant, and a binder.

Claims

CLAIMS1 . An oral solid dosage form, comprising: i) elafibranor or a pharmaceutically acceptable salt or ester thereof; ii) a filler selected in the group consisting of mannitol, microcrystalline cellulose and lactose monohydrate; iii) a disintegrating agent selected in the group consisting of crospovidone and croscarmellose sodium; iv) a binder selected in the group consisting of hydroxypropylcellulose, copovidone, povidone and hydroxypropylmethyl cellulose.

2. The oral solid dosage form according to claim 1 , wherein elafibranor or a pharmaceutically acceptable salt or ester thereof is micronized.

3. The oral solid dosage form according to claim 1 or 2, wherein elafibranor or a pharmaceutically acceptable salt or ester thereof is in the form of particles, and wherein at least 90% of the particles have a diameter of 15 pm or less.

4. The oral solid dosage form according to any one of claims 1 to 3, wherein at least 50% of the particles have a diameter of 5 pm or less.

5. The oral solid dosage form according to any one of claims 1 to 4, wherein the dosage form comprises from 20 to 60 % by weight of elafibranor or a pharmaceutically acceptable salt or ester thereof.

6. The oral solid dosage form according to any onf of claims 1 to 5, wherein the dosage form comprises from 35 to 40% by weight of elafibranor or a pharmaceutically acceptable salt or ester thereof.

7. The oral solid dosage form according to any one of claims 1 to 6, wherein the dosage form comprises from 35 mg to 180 mg of elafibranor or a pharmaceutically acceptable salt or ester thereof.

8. The oral solid dosage form according to any one of claims 1 to 7, wherein the dosage form comprises from 40 mg to 120 mg of elafibranor or a pharmaceutically acceptable salt or ester thereof.

9. The oral solid dosage form according to any one of claims 1 to 8, said dosage form being a tablet.

10. The oral solid dosage form according to any one of claims 1 to 9, said dosage form being a tablet comprising:(a) an internal phase comprising:(i) from 30% to 60 % by weight of elafibranor or a pharmaceutically acceptable salt or ester thereof;(ii) from 20% to 55 % by weight of microcrystalline cellulose;(iii) from 0.8% to 6 % by weight of croscarmellose sodium; and(iv) from 2% to 6 % by weight of povidone; and(b) an external phase comprising: from 0.2% to 4 % by weight of croscarmellose sodium; from 0.1 % to 0.4 % by weight of colloidal silica; and from 0.1 % to 2% by weight of magnesium stearate; relative to the total weight of the tablet.

11. The oral solid dosage form according to claim 9 or 10, wherein the tablet is obtained by carried out a step of wet granulation followed by tablet compression and optionnaly coating.

12. The oral solid dosage form according to any one of claims 9 to 11 , said dosage form comprising an external coating.

13. The oral solid dosage form according to claim 12, wherein the external coating comprises a coloring agent.

14. The oral solid dosage form of any of claims 1 to 13, for use in treating or preventing primary biliary cholangitis (PBC), primary sclerosing cholangitis (PSC), nonalcoholic fatty liver disease (NAFLD), nonalcoholic steatohepatitis (NASH), cirrhosis, hepatitis C infection, alcoholic liver disease, liver damage due to progressive fibrosis, liver fibrosis or cirrhosis in a patient in need thereof.

15. The oral solid dosage form for use according to claim 14, wherein said composition is for oral administration once a day.

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