C-met modulator pharmaceutical compositions

Patent metadata

Field	Value
Publication number	US-9724342-B2
Application number	US-201113810537-A
Country	US
Kind code	B2
Filing date	Jul 18, 2011
Priority date	Jul 16, 2010
Publication date	Aug 8, 2017
Grant date	Aug 8, 2017

Abstract

Pharmaceutical compositions and unit dosage forms comprising Compound I are disclosed.

First claim

What is claimed is:

1. A tablet pharmaceutical composition comprising about:

Ingredient
(% w/w)

Compound I, L-malate salt
31.68

Microcrystalline Cellulose
38.85

Lactose anhydrous
19.42

Hydroxypropyl Cellulose
3.00

Croscarmellose Sodium
3.00

Total Intra-granular
95.95

Silicon dioxide, Colloidal
0.30

Croscarmellose Sodium
3.00

Magnesium Stearate
0.75

Total
100.00

wherein Compound I is:

Compound I.

2. A tablet pharmaceutical composition comprising:
30-32 percent by weight of Compound I, L-malate salt wherein Compound I is:

38-40 percent by weight of microcrystalline cellulose;
18-22 percent by weight of lactose;
2-4 percent by weight of hydroxypropyl cellulose;
4-8 percent by weight of croscarmellose sodium;
0.2-0.6 percent by weight of colloidal silicon dioxide; and
0.5-1 percent by weight of magnesium stearate.

3. The tablet pharmaceutical composition of claim 2 , further comprising a film coating containing hypromellose, titanium dioxide, triacetin, and iron oxide yellow.

4. The tablet pharmaceutical composition of claim 1 , further comprising a film coating containing hypromellose, titanium dioxide, triacetin, and iron oxide yellow.

5. The table pharmaceutical composition of claim 1 , containing 20 to 100 mg of Compound I.

6. The tablet pharmaceutical composition of claim 1 , containing 20, 25, 50, 60, 75, 80, or 100 mg of Compound I.

7. A tablet pharmaceutical composition comprising, based on 100 weight/weight percent:
30-32 percent by weight of Compound I, L-malate salt wherein Compound I is:

38-40 percent by weight of microcrystalline cellulose;
18-22 percent by weight of lactose
2-4 percent by weight of hydroxypropyl cellulose;
4-8 percent by weight of croscarmellose sodium;
0.2-0.6 percent by weight of colloidal silicon dioxide; and
0.5-1 percent by weight of magnesium stearate;
and further comprising a film coating containing hypromellose, titanium dioxide, triacetin, and iron oxide yellow.

8. The tablet pharmaceutical composition of claim 7 , containing 20 to 100 mg of Compound I.

9. The tablet pharmaceutical composition of claim 7 , containing 20, 25, 50, 60, 75, 80, or 100 mg of Compound I.

10. A tablet pharmaceutical composition comprising:

Ingredient
(% w/w)

Compound I, L-malate
31.68

salt

Microcrystalline Cellulose
38.85

Lactose anhydrous
19.42

Hydroxypropyl Cellulose
3.00

Croscarmellose Sodium
6.00

Silicon dioxide, Colloidal
0.30

Magnesium Stearate
0.75

Total
100.00.

wherein Compound I is:

11. The tablet pharmaceutical composition of claim 2 , containing 20 to 100 mg of Compound I.

12. The tablet pharmaceutical composition of claim 2 , containing 20, 25, 50, 60, 75, 80, or 100 mg of Compound I.

Assignees

• Wilson Jo Ann
• Shah Khalid
• Exelixis Inc

Inventors

• Wilson Jo Ann
• Shah Khalid

Classifications

• A61K9/2004

  Excipients; Inactive ingredients · CPC title

• A61K9/28

  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 title

• A61K45/06

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title

• A61K9/2095

  Tabletting processes · CPC title

• A61K9/2893

  Tablet coating processes (mechanical aspects A61J3/06) · CPC title