US2021379050A1PendingUtilityA1
C-Met Modulator Pharmaceutical Compositions
Est. expiryJul 16, 2030(~4 yrs left)· nominal 20-yr term from priority
A61K 9/2031A61K 9/2866A61K 9/2018A61K 9/28A61K 31/47A61K 9/2013A61K 31/33A61K 9/2054A61K 31/395A61K 9/2009A61K 9/2095A61K 31/435A61K 9/2833A61K 45/06A61K 31/00A61K 9/2004A61K 9/2893A61K 9/00
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Claims
Abstract
Pharmaceutical compositions and unit dosage forms comprising Compound (I) are disclosed.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A pharmaceutical composition comprising:
Ingredient
(% w/w)
Compound I
31.68
Microcrystalline Cellulose
38.85
Lactose anhydrous
19.42
Hydroxypropyl Cellulose
3.00
Croscarmellose Sodium
3.00
Total Intro-granular
95.95
Silicon dioxide, Colloidal
0.30
Croscarmellose Sodium
3.00
Magnesium Stearate
0.75
Total
100.00
2 . A pharmaceutical composition comprising:
Ingredient
(% w/w)
Compound I
25.0-33.3
Microcrystalline Cellulose
q.s
Hydroxypropyl Cellulose
3
Poloxamer
0-3
Croscarmellose Sodium
6.0
Colloidal Silicon Dioxide
0.5
Magnesium Stearate
0.5-1.0
Total
100
3 . A pharmaceutical composition comprising:
Theoretical
Quantity (mg/unit
Ingredient
dose)
Compound I
100.0
Microcrystalline Cellulose
155.4
PH-102
Lactose Anhydrous 60M
77.7
Hydroxypropyl Cellulose,
12.0
EXF
Croscarmellose Sodium
24
Colloidal Silicon Dioxide
1.2
Magnesium Stearate (Non-
3.0
Bovine)
Opadry Yellow
16.0
Total
416
4 . A pharmaceutical composition comprising:
30-32 percent by weight of Compound I in at least one of the forms disclosed herein; 50-70 percent by weight of a filler; 2-4 percent by weight of a binder; 4-8 percent by weight of a disintegrant; and 0.2-0.6 percent by weight of a glidant; and 0.5-1 percent by weight of a lubricant.
5 . The pharmaceutical composition of claim 4 , wherein Compound I is the free base.
6 . The pharmaceutical composition of claim 4 , wherein Compound I is a pharmaceutically acceptable salt.
7 . The pharmaceutical composition of claim 4 , wherein Compound I is the malate salt.
8 . The pharmaceutical composition of claim 4 , wherein Compound I is the L-, D-, or D,L malate salt, or mixtures thereof.
9 . The pharmaceutical composition of claim 8 , wherein the Compound I malate salt is in amorphous, substantially amorphous, crystalline, or substantially crystalline form.
10 . The pharmaceutical composition of claim 8 , wherein the Compound I malate salt is in crystalline or amorphous form.
11 . The pharmaceutical composition of claim 4 , wherein the filler is selected from the group consisting of sodium starch glycolate, corn starch, talc, sucrose, dextrose, glucose, lactose, xylitol, fructose, sorbitol, calcium phosphate, calcium sulfate, calcium carbonate, and microcrystalline cellulose, or mixtures thereof.
12 . The pharmaceutical composition of claim 11 , wherein the filler is comprises lactose and microcrystalline cellulose.
13 . The pharmaceutical composition of claim 2 , wherein the binder is selected from the group consisting of acacia, alginic acid, carbomer, carboxymethylcellulose sodium, dextrin, ethylcellulose, gelatin, guar gum, hydrogenated vegetable oil (type I), hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, liquid glucose, magnesium aluminium silicate, maltodextrin, methylcellulose, polymethacrylates, povidone, pregelatinized starch, sodium alginate, starch, and zein, or mixtures thereof.
14 . The pharmaceutical composition of claim 13 , wherein the binder is hydroxypropyl cellulose.
15 . The pharmaceutical composition of claim 14 , wherein the disintegrant is selected from the group consisting of alginic acid, carboxymethylcellulose calcium, carboxymethylcellulose sodium, colloidal silicon dioxide, croscarmellose sodium, crospovidone, guar gum, magnesium aluminum silicate, methylcellulose, microcrystalline cellulose, polyacrilin potassium, powdered cellulose, pregelatinized starch, sodium alginate, and starch, or mixtures thereof.
16 . The pharmaceutical composition of claim 15 , wherein the disintegrant is croscarmellose sodium.
17 . The pharmaceutical composition of claim 4 , wherein the glidant is colloidal silicon dioxide.
18 . The pharmaceutical composition of claim 4 , wherein the lubricant is selected from the group consisting of magnesium stearate, Lubritab®, stearic acid, and talc, or mixtures thereof.
19 . The pharmaceutical composition of claim 4 , wherein the lubricant is magnesium stearate.
20 . The pharmaceutical composition of claim 4 , further comprising a film coating.
21 . The pharmaceutical composition of claim 20 , wherein the film coating comprises Opadry Yellow.
22 . The pharmaceutical formulation of claims 1 - 4 which is a tablet formulation.
23 . A pharmaceutical composition comprising:
Weight/Weight
Component
Percent
Compound I
25-29
Microcrystalline Cellulose
q.s.
Lactose Anhydrous
40-44
Hydroxypropyl Cellulose
2-4
Croscarrnellose Sodium
2-8
Colloidal Silicon Dioxide
0.1-0.4
Magnesium Stearate
0.7-0.9
Total
100
24 . The pharmaceutical composition of claim 22 , further comprising a film coating.
25 . The pharmaceutical composition of claim 24 , wherein the film coating comprises Opadry yellow.
26 . A method for treating cancer, comprising administering to a patient in need of such treatment a pharmaceutical composition of claim 1 - 4 or 23 , alone or in combination with another therapeutic agent.
27 . The method of claim 26 , wherein the cancer is selected from the group consisting of pancreatic cancer, kidney cancer, liver cancer, prostate cancer, gastric cancer, gastroesophageal cancer, melanoma, lung cancer, breast cancer, thyroid cancer, and astrocytic tumors.
28 . The method of claim 27 , wherein the cancer is pancreatic cancer, hepatocellular carcinoma (HCC), renal cell carcinoma, castration-resistant prostate cancer (CRPC), gastric or gastroesophageal junction cancer, melanoma, small cell lung cancer (SCLC), ovarian cancer, primary peritoneal or fallopian tube carcinoma, estrogen receptor positive breast cancer, estrogen receptor/progesterone receptor/HER2-negative (triple-negative) breast cancer, inflammatory (regardless of receptor status) breast cancer, non-small cell lung cancer (NSCLC), or medullary thyroid cancer.
29 . A process for manufacturing a pharmaceutical composition comprising Compound I, comprising the steps of:
a. Delumping unmilled Compound I; b. Premixing the delumped Compound I with microcrystalline cellulose, anhydrous lactose, and croscarmellose sodium to form a binder solution; c. Wet high shear granulation of the binder solution to produce wet granules; d. Wet screening of the wet granules to produce wet screened granules; e. Fluid bed drying of the wet screened granules to produce dried granules; f. Dry milling of the dried granules to produce dried milled granules; g. Blending the dried milled granules with colloidal silicon and croscarmellose to produce an extragranular Wend; h. Lubricant blending of the extragranular blend and magnesium stearate to produce a final blend; and i. Tablet compression of the final blend to form an uncoated core tablet.
30 . The process of claim 29 , further comprising the step of film coating of the uncoated core tablet.Cited by (0)
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