METHODS OF TREATMENT OF PARTIAL ONSET SEIZURES USING ESLICARBAZEPINE ACETATE.

• US 20170143736A1
• Filed: 02/01/2017
• Published: 05/25/2017
• Est. Priority Date: 05/06/2005
• Status: Active Grant

• Current Assignee: BIAL Portela & Ca, SA
• Original Assignee: BIAL Portela & Ca, SA
• Inventors: de ALMEIDA, Jos Luis, Araujo Soares Da Silva, Patricio Manuel Vieria
• Granted Patent: US 10,702,536 B2
• Time in Patent Office: Days
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/19 Carboxylic acids, e.g. valproic acid salicylic acid A61K31/60
• CPC Class Codes: A61K 31/55 having seven-membered rings, e.g. azelastine, pentylenetetrazole
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/06 Antimigraine agents
• CPC Class Codes: A61P 25/08 Antiepileptics; Anticonvulsants
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia

Abstract

The present disclosure relates to the treatment of various diseases and conditions with eslicarbazepine acetate. The present disclosure also relates to the use of eslicarbazepine acetate in a method for reducing or decreasing epileptic seizures in a patient. The present disclosure also relates to a method for increasing the exposure to eslicarbazepine in a patient. The present disclosure also relates to a method of preparing a pharmaceutical composition comprising eslicarbazepine acetate.

Claims

1. A method for treating a patient with partial-onset seizures, comprising:

administering once-daily to a patient in need thereof a pharmaceutical composition consisting essentially of eslicarbazepine acetate, wherein the once-daily administration is pharmacologically effective to treat partial-onset seizures in the patient, and wherein the patient is a human.

2. The method according to claim 1, wherein the pharmaceutical composition is administered once-daily in an amount consisting essentially of at least about 400 mg of eslicarbazepine acetate.

3. The method according to claim 1, wherein the pharmaceutical composition is administered once-daily in an amount consisting essentially of at least about 800 mg of eslicarbazepine acetate.

4. The method according to claim 1, wherein the pharmaceutical composition is administered once-daily in an amount consisting essentially of at least about 1200 mg of eslicarbazepine acetate.

5. The method according to claim 1, wherein the pharmaceutical composition is administered once-daily in an amount consisting essentially of from about 800 mg to about 2400 mg of eslicarbazepine acetate.

6. The method according to claim 1, wherein the pharmaceutical composition is administered once-daily in an amount consisting essentially of about 200 mg of eslicarbazepine acetate.

7. The method according to claim 1, wherein the pharmaceutical composition is administered once-daily in an amount consisting essentially of about 400 mg of eslicarbazepine acetate.

8. The method according to claim 1, wherein the pharmaceutical composition is administered once-daily in an amount consisting essentially of about 600 mg of eslicarbazepine acetate.

9. The method according to claim 1, wherein the pharmaceutical composition is administered once-daily in an amount consisting essentially of about 800 mg of eslicarbazepine acetate.

10. The method according to claim 1, wherein the pharmaceutical composition is administered once-daily in an amount consisting essentially of about 1200 mg of eslicarbazepine acetate.

11. The method according to claim 1, wherein the pharmaceutical composition is administered once-daily in an amount consisting essentially of about 2400 mg of eslicarbazepine acetate.

12. The method according to claim 1, wherein the pharmaceutical composition is administered once-daily in an initial dosage consisting essentially of about 400 mg of eslicarbazepine acetate and increased to a dosage consisting essentially of about 800 mg, or to a dosage consisting essentially of about 1200 mg.

13. The method according to claim 1, wherein the amount of the pharmaceutical composition consisting essentially of eslicarbazepine acetate is administered once-daily as adjunctive therapy to a patient being treated with at least one other anti-epileptic drug.

14. The method according to claim 13, where the serum concentration of the at least one other anti-epileptic drug is not significantly decreased by the once-daily administration of the pharmaceutical composition consisting essentially of eslicarbazepine acetate.

15. The method according to claim 13, wherein the at least one other anti-epileptic drug is chosen from valproate, lamotrigine, topiramate, and combinations thereof.

16. The method according to claim 1, wherein the pharmaceutical composition is administered once-daily in the form of a tablet or an oral suspension.

17. The method according to claim 1, wherein upon once-daily administration of the pharmaceutical composition, the number, duration, or frequency of seizures in the patient decreases relative to the number, duration, or frequency of seizures in a patient without treatment.

18. The method according to claim 1, wherein the pharmaceutical composition is administered once-daily orally.

19. The method according to claim 1, wherein steady-state plasma concentrations of eslicarbazepine are attained after 4 to 5 days of once-daily administration.

20. The method according to claim 1, wherein a full daily dose is contained in a single dosage unit.

21. The method according to claim 1, wherein the pharmaceutical composition is administered once-daily in an amount that results in an area under the concentration curve, AUC_0-τ

, of eslicarbazepine from about 2,400 ng·

h/mL to about 507,600 ng·

h/mL, wherein τ

is the dosing interval, which is 24 hours.

22. The method according to claim 1, wherein the pharmaceutical composition is administered once-daily in an amount that results in an area under the concentration curve, AUC_0-τ

, of eslicarbazepine from about 126,300 ng·

h/mL to about 905,900 ng·

h/mL, wherein τ

is the dosing interval, which is 24 hours.

23. The method according to claim 1, wherein the pharmaceutical composition is administered once-daily in an amount that results in a maximum observed plasma concentration, C_max, of eslicarbazepine up to about 56,500 ng/mL.

24. The method according to claim 1, wherein the pharmaceutical composition is administered once-daily in an amount that results in a mean maximum plasma concentration, C_max, of eslicarbazepine from about 8,800 ng/mL to about 56,500 ng/mL.

25. The method according to claim 1, wherein the pharmaceutical composition is administered once-daily in an amount that results in a mean maximum plasma concentration, C_max, of eslicarbazepine from about 18,000 ng/mL to about 34,600 ng/mL.

26. The method according to claim 1 wherein the pharmaceutical composition is administered once-daily in an amount that results in a maximum plasma concentration, C_max, of eslicarbazepine from about 8,500 to about 18,600.

27. The method according to claim 1, wherein the pharmaceutical composition is administered once-daily in an amount that results in a maximum observed plasma concentration, C_max, of eslicarbazepine from about 2,900 to about 15,000.

28. A method for treating a patient with partial-onset seizures, comprising exposing the patient in need thereof to a higher rate of exposure to eslicarbazepine, in terms of C_max, wherein the rate of exposure is increased by providing the patient a once-daily amount of eslicarbazepine, rather than providing the same total amount of eslicarbazepine divided twice-daily.

29. The method according to claim 28, wherein the C_max of eslicarbazepine is up to about 56,500 ng/mL.

30. The method according to claim 28, wherein the Cmax of eslicarbazepine is from 1,500 ng/mL to 35,900 ng/mL.