Claims for Patent: 10,912,781

Summary for Patent: 10,912,781

Title:	Pharmaceutical composition comprising licarbazepine acetate
Abstract:	A pharmaceutical composition comprising licarbazepine acetate, especially eslicarbazepine acetate, in combination with suitable excipients, in particular a binder, and a disintegrant. Also disclosed is a granulation process, especially a wet granulation process, for making the pharmaceutical composition.
Inventor(s):	Cardoso de Vasconcelos; Teofilo (S. Mamede do Coronado, PT), dos Santos Lima; Ricardo Jorge (S. Mamede do Coronado, PT), Cerdeira de Campos Costa; Rui (S. Mamede do Coronado, PT)
Assignee:	BIAL-Portela & C.A., S.A. (S. Mainede do Coronado, PT)
Application Number:	15/397,945
Patent Claims:	1. A pharmaceutical composition consisting essentially of eslicarbazepine acetate in combination with a binder and a disintegrant, wherein eslicarbazepine acetate is present in an amount of from 80 to 90 wt %, the binder is present in an amount of from 3 to 10 wt %, and the disintegrant is present in an amount of from 3 to 10 wt %, and wherein the pharmaceutical composition exhibits a dissolution of at least 60% at about 30 minutes at a temperature of 37.+-.0.5.degree. C. and a pH of about 4.5 using a paddle apparatus at a speed of about 100 rpm. 2. The pharmaceutical composition of claim 1, wherein the binder is povidone, which is present in an amount of from 5 to 9 wt %. 3. The pharmaceutical composition of claim 1, wherein the binder is povidone, hypromellose, hydroxypropyl cellulose, methyl-cellulose, pregelatinized maize starch or gelatine, or a mixture of one or more thereof. 4. The pharmaceutical composition of claim 3, wherein the binder is povidone. 5. The pharmaceutical composition of claim 1, wherein the disintegrant is croscarmellose sodium, which is present in an amount of from 5 to 8 wt %. 6. The pharmaceutical composition of claim 1, wherein the disintegrant is croscarmellose sodium, crospovidone, low substituted hydroxypropyl cellulose, microcrystalline cellulose, carboxymethyl cellulose sodium, carboxymethylcellulose calcium, sodium starch glycolate, or a mixture of one or more thereof. 7. The pharmaceutical composition of claim 6, wherein the disintegrant is croscarmellose sodium. 8. The pharmaceutical composition of claim 1, wherein the pharmaceutical composition is prepared by a wet granulation process and comprises granules of eslicarbazepine acetate. 9. The pharmaceutical composition of claim 8, wherein the disintegrant is intragranular or extragranular. 10. The pharmaceutical composition of claim 8, wherein at least part of the disintegrant is intragranular and at least part of the disintegrant is extragranular. 11. The pharmaceutical composition of claim 10, wherein from about 20 to about 80 wt % of the total amount of the disintegrant is present in the granules. 12. The pharmaceutical composition of claim 10, wherein from about 30 to about 70 wt % of the total amount of the disintegrant is present in the granules. 13. The pharmaceutical composition of claim 10, wherein from about 40 to about 60 wt % of the total amount of the disintegrant is in the granules. 14. The pharmaceutical composition of claim 10, wherein from about 45 to about 55 wt % of the total amount of the disintegrant is in the granules. 15. The pharmaceutical composition of claim 10, wherein about 50 wt % of the total amount of the disintegrant is in the granules. 16. The pharmaceutical composition of claim 10, wherein: eslicarbazepine acetate is present in the intragranular phase; the binder is povidone, which is present in an amount of from 5 to 9 wt %; and the disintegrant is croscarmellose sodium, which is present in an amount of from 5 to 8 wt %, and wherein about 50% of croscarmellose sodium is present in the intragranular phase and about 50% of croscarmellose sodium is present in the extragranular phase. 17. The pharmaceutical composition of claim 1, further comprising a lubricant, and/or a glidant. 18. The pharmaceutical composition of claim 1, further comprising a lubricant, which is magnesium stearate and is present in an amount of from about 0.1 to about 3 wt %. 19. The pharmaceutical composition of claim 1, wherein the pharmaceutical composition does not comprise a calcium carbonate, calcium phosphate dibasic anhydrous, calcium phosphate dibasic dihydrate, calcium phosphate tribasic, or calcium sulphate. 20. The pharmaceutical composition of claim 1, wherein the pharmaceutical composition is in an oral dosage form. 21. The pharmaceutical composition of claim 20, wherein the oral dosage form is a tablet or capsule. 22. A pharmaceutical composition consisting essentially of (i) from 80 to 90 wt % eslicarbazepine acetate, (ii) from 3 to 10 wt % povidone, and (iii) from 3 to 10 wt % croscarmellose sodium, wherein the pharmaceutical composition exhibits a dissolution of at least 60% at about 30 minutes at a temperature of 37.+-.0.5.degree. C. and a pH of about 4.5 using a paddle apparatus at a speed of about 100 rpm. 23. A pharmaceutical composition consisting essentially of (i) from 80 to 90 wt % eslicarbazepine acetate, (ii) from 3 to 10 wt % povidone, and (iii) from 3 to 10 wt % croscarmellose sodium, wherein the pharmaceutical composition is prepared by a wet granulation process and comprises granules of eslicarbazepine acetate, and wherein the pharmaceutical composition exhibits a dissolution of at least 60% at about 30 minutes at a temperature of 37.+-.0.5.degree. C. and a pH of about 4.5 using a paddle apparatus at a speed of about 100 rpm. 24. A pharmaceutical composition consisting essentially of (i) from 80 to 90 wt % eslicarbazepine acetate, (ii) from 3 to 10 wt % povidone, and (iii) from 3 to 10 wt % croscarmellose sodium, wherein the pharmaceutical composition has an apparent density of from about 0.5 to about 1.5 g/mL, and wherein the pharmaceutical composition exhibits a dissolution of at least 60% at about 30 minutes at a temperature of 37.+-.0.5.degree. C. and a pH of about 4.5 using a paddle apparatus at a speed of about 100 rpm. 25. The pharmaceutical composition of claim 24, wherein the pharmaceutical composition is in an oral dosage form.