Pharmaceutical composition comprising licarbazepine acetate

• US 9,566,244 B2
• Filed: 12/17/2013
• Issued: 02/14/2017
• Est. Priority Date: 10/26/2007
• Status: Active Grant

• Current Assignee: BIAL Portela & Ca, SA
• Original Assignee: BIAL Portela & Ca, SA
• Inventors: Cardoso de Vasconcelos, Tefilo, dos Santos Lima, Ricardo Jorge, Cerdeira de Campos Costa, Rui
• Primary Examiner(s): Barham, Bethany
• Assistant Examiner(s): Anthopolos, Peter
• Application Number:
  US14/108,615
• Publication Number:
  US 20140343043A1
• Time in Patent Office: 1,155 Days
• Field of Search: None
• US Class Current: 1/1
• CPC Class Codes: A61K 31/55 having seven-membered rings, e.g. azelastine, pentylenetetrazole
• CPC Class Codes: A61K 9/0053 Mouth and digestive tract, i.e. intraoral and peroral administration rectal administration A61K9/0031
• CPC Class Codes: 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
• CPC Class Codes: A61K 9/16 Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction A61K9/20 takes precedence if the final form is a tablet; microspheres with drug-free outer coating, microcapsules A61K9/50; mixture of different granules, microcapsules, (coated) microparticles A61K9/5084; nanoparticles A61K9/51
• CPC Class Codes: A61K 9/1635 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/1652 Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin homeopathic globules A61K9/1623
• CPC Class Codes: A61K 9/1682 Processes
• CPC Class Codes: A61K 9/1694 resulting in granules or microspheres of the matrix type containing more than 5% of excipient
• CPC Class Codes: A61K 9/20 Pills, tablets, discs, rods A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095
• CPC Class Codes: A61K 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2095 Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing mechanical aspects A61J3/00
• CPC Class Codes: A61K 9/48 Preparations in capsules, e.g. of gelatin, of chocolate A61K9/0004 takes precedence; bite capsules A61K9/0056
• CPC Class Codes: A61K 9/4866 Organic macromolecular compounds
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/08 Antiepileptics; Anticonvulsants
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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.

Claims

1. A tablet or capsule consisting essentially of:

a granular phase comprising licarbazepine acetate and a super-disintegrant selected from the group consisting of croscarmellose sodium, crospovidone, sodium starch glycolate, and mixtures thereof;

an extragranular phase comprising a lubricant and a super-disintegrant selected from the group consisting of croscarmellose sodium, crospovidone, sodium starch glycolate, and mixtures thereof; and

optionally one or more additional excipients selected from the group consisting of (1) a binder selected from the group consisting of povidone, pregelatinized starch, gelatin, and mixtures thereof, (2) a diluent/filler, (3) a disintegrant, (4) a glidant, (5) a lubricant, and (6) mixtures thereof; and

wherein the amount of licarbazepine acetate present in the granular phase ranges from 70 to 90 percent by weight relative to the total weight of the tablet or capsule;

wherein the total amount of super-disintegrant ranges from 5 to 10 percent by weight relative to the total weight of the tablet or capsule; and

wherein 30 to 70 percent by weight of the total amount of super-disintegrant is present in the granular phase.

2. The tablet or capsule according to claim 1, wherein the licarbazepine acetate is eslicarbazepine acetate.

3. The tablet or capsule according to claim 2, wherein the amount of eslicarbazepine acetate ranges from 80 to 90% by weight relative to the total weight of the tablet or capsule, the amount of povidone ranges from 3 to 10% by weight relative to the total weight of the tablet or capsule, and the amount of croscarmellose sodium ranges from 3 to 10% by weight relative to the total weight of the tablet or capsule.

4. A tablet or capsule comprising:

a granular phase comprising licarbazepine acetate and a super-disintegrant selected from the group consisting of croscarmellose sodium, crospovidone, sodium starch glycolate, and mixtures thereof;

an extragranular phase comprising a lubricant and a super-disintegrant selected from the group consisting of croscarmellose sodium, crospovidone, sodium starch glycolate, and mixtures thereof; and

povidone; and

wherein the amount of licarbazepine acetate present in the granular phase ranges from 55 to 60 percent by weight relative to the total weight of the tablet or capsule;

wherein the total amount of super-disintegrant ranges from 5 to 10 percent by weight relative to the total weight of the tablet or capsule;

wherein the amount of povidone is 5 to 9 percent by weight relative to the total weight of the tablet or capsule;

wherein 30 to 70 percent by weight of the total amount of super-disintegrant is present in the granular phase; and

wherein the tablet or capsule exhibits a dissolution percentage of 67.9 to 81.5 at 30 minutes when using a paddle apparatus at a speed of 100 rpm under the following combination of conditions;

a dissolution medium temperature of 37±

0.5°

C. and a dissolution medium pH of 4.5.

5. The tablet or capsule according to claim 4, wherein the licarbazepine acetate is eslicarbazepine acetate.