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1. WO2021005478 - COMPRESSED MACITENTAN COMPOSITIONS, METHODS AND USES THEREOF

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[ EN ]

C L A I M S

1. A compressed composition comprising a therapeutically effective amount of macitentan;

a sugar alcohol diluent selected from a list consisting of: maltitol, xylitol, mannitol or mixtures thereof;

a surfactant selected from a list consisting of: sodium dodecyl sulfate, polysorbate 80, or a mixture thereof.

2. The compressed composition according to previous claim comprising 0.1% to 15% (wtSurfactant/wttotal) of Surfactant.

3. The compressed composition according to previous claim comprising 0.5% to 15% (wtSurfactant/wttotal) of Surfactant.

4. The compressed composition according to any of the previous claims comprising from 0.9% to 10% (wtSurfactant/wttotal) of surfactant, preferably from 2 % to 10 % (wtSurfactant/wttotal), more preferably from 2% to 5% (wtSurfactant/wttotal).

5. The compressed composition according to any of the previous claims comprising from 0.5 to 2% (wtSurfactant/wttotal) of surfactant.

6. The compressed composition according to the previous claims comprising

maltitol as sugar alcohol diluent and sodium dodecyl sulfate as surfactant; or maltitol as sugar alcohol diluent and polysorbate 80 as surfactant;

xylitol as sugar alcohol diluent and sodium dodecyl sulfate as surfactant; or xylitol as sugar alcohol diluent and polysorbate 80 as surfactant;

mannitol as sugar alcohol diluent and sodium dodecyl sulfate as surfactant; or mannitol as sugar alcohol diluent and polysorbate 80 as surfactant.

7. The compressed composition according to any of the previous claims wherein the Compressed Composition Comprises from 5% to 65% (wtnon-sugar alcoh ol dil uent/wttotal) non-sugar alcohol diluent, preferably from 10% to 50% (wtnon-sugar alcohol diiuent/wttotai),

more preferably from 15% to 35% (wtnon-sugar alcoh ol dil uent/wttotal)

8. The compressed composition according to any of the previous claims further

comprising microcrystalline cellulose as a non-sugar alcohol diluent.

9. The compressed composition according to any of the previous claims comprising

from 15% to 85% (wtsugar alcohol dii uent/wttota l) of sugar alcohol diluent, preferably from

25% to 75% (wtsugar alcohol dii uent/wttota l), more preferably from 35% to 65% (wtsugar alcohol dii uent/wttota l)

10. The compressed composition according to any of the previous claims comprising

from 1% to 45% (wtmacitentan/wttotai) of macitentan, preferably from 5% to 35%

(wtmacitentan/wttotal), more preferably from 5 % to 25 % (wtmacitentan/wttotal) .

11. The compressed composition according to any of the previous claims wherein the

compressed composition comprises from 5% to 65% (wtnon-sugar alcoh ol dil uent/wttotal)

non-sugar alcohol diluent, preferably from 10% to 50% (wtnon-sugar alcoh ol dil uent/wttotal)

more preferably from 15% to 35% (wtnon-sugar alcoh ol dil uent/wttotal)

12. The compressed composition according to any of the previous claims wherein the

compressed composition comprises from 5% to 25% (wtmacitentan/wttotai) of

macitentan, from 35% to 65% (wtsugar alcohol dii uent/wttota l) of sugar alcohol diluent, and

from 0.5% to 5% (wtSurfactant/wttotal) of surfactant.

13. The compressed composition according to any of the previous claims further

comprising at least one excipient selected from a disintegrant, a binder or a

lubricant.

14. The compressed composition according to any of the previous claims wherein the

non-sugar alcohol diluent is microcrystalline cellulose, the disintegrant is

crospovidone or sodium starch glycolate, the binder is povidone, and the lubricant is magnesium stearate.

15. The compressed composition according to any of the previous claims wherein the composition is prepared by wet granulation.

16. The compressed composition according to any of the previous claims for use in the treatment of pulmonary arterial hypertension.

17. A process for preparing a compressed composition, or a solid oral pharmaceutical composition, or a solid oral pharmaceutical composition for use in the treatment of pulmonary arterial hypertension, comprising:

mixing macitentan, a sugar alcohol diluent, and optionally one or more excipients selected from a non-sugar alcohol diluent, a disintegrant, a binder, a glidant;

granulating the mixture obtained in the previous step with an aqueous solution of a surfactant wherein the surfactant is sodium dodecyl sulfate, or polysorbate 80, or combinations thereof;

lubricating the granulate obtained in the previous step, preferably with magnesium stearate;

compressing the lubricated granulate obtained in the previous step.

18. A solid oral pharmaceutical composition comprising a compressed composition according to any of the claims 1 to 15 or a compressed composition prepared according the previous claim 16, preferably for use in the treatment of pulmonary arterial hypertension.