HIGH DRUG LOAD TABLET

• US 20100203133A1
• Filed: 04/21/2010
• Published: 08/12/2010
• Est. Priority Date: 04/23/2002
• Status: Abandoned Application

• Current Assignee: Novartis Ag
• Original Assignee: Novartis Ag
• Inventors: LUFTENSTEINER, Christian-Peter, Ogorka, Jörg, Kalb, Oskar, Bianchi, Jean-Claude
• Application Number:
  US12/764,696
• Publication Number:
  US 20100203133A1
• Time in Patent Office: Days
• US Class Current: 424/474
• CPC Class Codes: A61K 31/185 Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids hydroxamic acids A61K31/16; peroxy acids A61K31/327
• CPC Class Codes: A61K 31/505 Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
• CPC Class Codes: A61K 31/506 not condensed and containing further heterocyclic rings
• CPC Class Codes: A61K 9/2009 Inorganic compounds
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• 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 9/2072 characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms A61K9/0004, A61K9/0056, A61K9/0065 take precedence
• 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 9/28 Dragees; Coated pills or tablets , e.g. with film or compression coating A61K9/2072 takes precedence, e.g. partially coated tablets A61K9/2072, coated multilayer tablets A61K9/2086, tablets with drug-coated core A61K9/209
• CPC Class Codes: A61P 13/08 of the prostate
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 35/02 specific for leukemia
• CPC Class Codes: B29C 43/003 characterised by the choice of material

Abstract

The present invention pertains to a high drug load tablet comprising as active ingredient Compound I of formula

or a pharmaceutically acceptable salt thereof in an amount from about 30% to 80% in weight of the active moiety based on the total weight of the tablet.

Claims

1. :

A tablet comprising a pharmacologically effective amount of Compound I of formula (1)

or a pharmaceutically acceptable salt thereof in an amount from about 30% to 80% in weight of the active moiety based on the total weight of the tablet.

2. :

A tablet according to claim 1 wherein Compound I of formula (1) or a pharmaceutically acceptable salt thereof is present in an amount from about 50% to 80% in weight of the active moiety based on the total weight of the tablet.

3. :

A tablet according to claim 2 wherein Compound I of formula (1) is in the monomesylate salt form.

4. :

A tablet according to claim 3 wherein Compound I of formula (1) monomesylate is in the beta crystal form thereof.

5. :

A tablet according to claim 1 wherein the tablet comprises one or more pharmaceutically acceptable excipients suitable for the preparation of tablets.

6. :

A tablet according to claim 5 wherein the excipient comprises at least one binder.

7. :

A tablet according to claim 5 wherein the excipients comprise;

at least one binder in a total amount of about 1% to 25% in weight based on the total weight of the tablet,

at least one disintegrant in a total amount of about 10% to 35% in weight based on the total weight of the tablet

at least one glidant in a total amount of about 0.5% to 3% in weight based on the total weight of the tablet, and/or

at least one lubricant in a total amount of about 0.5% to 2% in weight based on the total weight of the tablet.

8. :

A tablet according to claim 6 wherein the binder comprises microcrystalline cellulose or hydroxypropylmethyl cellulose or a mixture thereof.

9. :

A tablet according to claim 7 wherein the disintegrant comprises cross-linked polyvinylpyrrolidinone.

10. :

A tablet according to claim 7 wherein the glidant comprises colloidal silicon dioxide and/or colloidal anhydrous silica.

11. :

A tablet according to claim 7 wherein the lubricant comprises magnesium stearate.

12. :

A process for the preparation of a tablet according to claim 1, which process comprises

(i) mixing the Compound I of formula (1) or pharmaceutically acceptable salts thereof and pharmaceutically acceptable excipients;

(ii) wet-granulating;

(iii) mixing with pharmaceutically acceptable excipients to form a mixture; and

(iv) compressing the mixture obtained in step (iii) to form a tablet.

13. :

The process according to claim 12 wherein the tablet is coated.

14. :

A tablet according to claim 1 prepared by a wet-granulation process.

15. :

A method of treating a subject which comprises administering a tablet according to claim 1 comprising a pharmacologically effective amount of Compound I of formula (1) to a subject in need of such a treatment.