US2014112988A1PendingUtilityA1
Pharmaceutical Composition and Administrations Thereof
Est. expiryAug 13, 2028(~2.1 yrs left)· nominal 20-yr term from priority
Inventors:William RowePatricia HurterChristopher R. YoungKirk DinehartMarinus Jacobus VerwijsKirk OverhoffPeter D.J. GrootenhuisMartyn BotfieldAlfredo Grossi
A61P 43/00A61P 3/00A61P 29/00A61P 19/00A61P 19/08A61P 11/00A61P 11/08A61P 19/10A61K 9/1635A61K 9/0053A61K 9/2054A61K 31/44A61K 9/2009A61K 9/284A61K 9/1652A61K 9/28A61K 9/2013A61K 9/2027A61K 31/47A61K 9/282A61K 9/2018A61K 9/14
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Claims
Abstract
The present invention relates to pharmaceutical compositions comprising a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, methods of manufacturing pharmaceutical compositions of the present invention, and methods of administering pharmaceutical compositions of the present invention.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A pharmaceutical composition comprising:
a. a solid dispersion comprising substantially amorphous Compound 1 and a polymer; b. a filler; c. a disintegrant; d. a surfactant; e. a binder; f. a glidant; and g. a lubricant.
2 . The pharmaceutical composition of claim 1 , wherein the solid dispersion comprises substantially amorphous Compound 1 and a polymer, and the polymer comprises HPMC, HPMCAS, PVP/VA, PVP, methacrylic acid/methacrylate copolymer, HPC, or any combination thereof.
3 . The pharmaceutical composition of claim 2 , wherein the solid dispersion has a mean particle diameter of greater than about 5 μm.
4 . The pharmaceutical composition of claim 2 , wherein the solid dispersion has a bulk density of about 0.10 g/cc or greater.
5 . The pharmaceutical composition of claim 2 , wherein the solid dispersion comprises substantially amorphous Compound 1, and Compound 1 is present in a concentration of at least 20 wt % by weight of the solid dispersion.
6 . The pharmaceutical composition of claim 5 , wherein the solid dispersion comprises 80 wt % or less of HPMCAS or PVP/VA.
7 . The pharmaceutical composition of claim 5 , wherein the solid dispersion comprises a surfactant.
8 . The pharmaceutical composition of claim 7 , wherein the solid dispersion comprises less than 10 wt % of surfactant by weight of solid dispersion.
9 . The pharmaceutical composition of claim 8 , wherein the solid dispersion comprises a surfactant, and the surfactant is SLS.
10 . The pharmaceutical composition of claim 9 , wherein the solid dispersion comprises amorphous Compound 1.
11 . The pharmaceutical composition of claim 1 , wherein the solid dispersion comprises from about 45 wt % to about 85 wt % of substantially amorphous Compound 1, from about 0.45 wt % to about 0.55 wt % of SLS, and from about 14.45 wt % to about 55.55 wt % of HPMCAS or PVP/VA by weight of the solid dispersion.
12 . The pharmaceutical composition of claim 1 , wherein the solid dispersion comprises from about 40 wt % to about 60 wt % of substantially amorphous Compound 1 by weight of the solid dispersion and from about 60 wt % to about 40 wt % of polymer by weight of the solid dispersion.
13 . The pharmaceutical composition of claim 1 , wherein the solid dispersion comprises from about 65 wt % to about 95 wt % of substantially amorphous Compound 1 by weight of the solid dispersion and from about 45 wt % to about 5 wt % of polymer by weight of the solid dispersion.
14 . The pharmaceutical composition of any of claims 1 - 13 , wherein the filler is lactose, sorbitol, cellulose, calcium phosphate, starch, sugar, or any combination thereof.
15 . The pharmaceutical composition of any of claims 1 - 14 , wherein the filler is lactose and has a concentration of at least about 10 wt % by weight of the composition.
16 . The pharmaceutical composition of any of claims 1 - 15 , wherein the disintegrant is sodium croscarmellose, sodium starch glycolate, or a combination thereof.
17 . The pharmaceutical composition of any of claims 1 - 16 , wherein the disintegrant is sodium croscarmellose and has a concentration of about 10 wt % or less by weight of the composition.
18 . The pharmaceutical composition of any of claims 1 - 17 , wherein the surfactant is sodium lauryl sulfate, sodium stearyl fumarate, polyoxyethylene 20 sorbitan mono-oleate, or any combination thereof.
19 . The pharmaceutical composition of any of claims 1 - 18 , wherein the surfactant is sodium lauryl sulfate and has a concentration of about 10 wt % or less by weight of the composition.
20 . The pharmaceutical composition of any of claims 1 - 19 , wherein the binder is microcrystalline cellulose, dibasic calcium phosphate, sucrose, corn starch, modified cellulose, or any combination thereof.
21 . The pharmaceutical composition of any of claims 1 - 20 , wherein the binder is microcrystalline cellulose and has a concentration of at least about 1 wt % by weight of the composition.
22 . The pharmaceutical composition of any of claims 1 - 21 , wherein the glidant is colloidal silicon dioxide, talc, or a combination thereof.
23 . The pharmaceutical composition of any of claims 1 - 22 , wherein the glidant is colloidal silicon dioxide and has a concentration of 2 wt % or less by weight of the composition.
24 . The pharmaceutical composition of any of claims 1 - 23 , wherein the lubricant is magnesium stearate, stearic acid, hydrogenated oil, sodium stearyl fumarate, or any combination thereof.
25 . The pharmaceutical composition of any of claims 1 - 24 , wherein the lubricant is magnesium stearate and has a concentration of about 2 wt % by weight of the composition.
26 . The pharmaceutical composition of any of claims 1 - 25 , further comprising a colorant.
27 . The pharmaceutical composition of any of claims 1 - 26 , wherein the colorant is a blue pigment having a concentration of less than 1 wt % by weight of the composition.
28 . A pharmaceutical composition comprising
a. from about 5 wt % to about 50 wt % of a solid dispersion, by weight of the composition, comprising from about 40 wt % to about 60 wt % of substantially amorphous Compound I, by weight of the dispersion, and from about 60 wt % to about 40 wt % of a polymer, by weight of the dispersion; b. from about 25 wt % to about 50 wt % of a filler; c. from about 1 wt % to about 10 wt % of a disintegrant; d. from about 2 wt % to about 0.3 wt % of a surfactant; e. from about 5 wt % to about 50 wt % of a binder; f. from about 2 wt % to about 0.05 wt % of a glidant; and h. from about 2 wt % to about 0.1 wt % of a lubricant.
29 . A pharmaceutical composition comprising
a. from about 5 wt % to about 50 wt % of a solid dispersion, by weight of the composition, comprising from about 70 wt % to about 90 wt % of substantially amorphous Compound 1, by weight of the dispersion, and from about 30 wt % to about 10 wt % of a polymer, by weight of the dispersion; b. from about 25 wt % to about 50 wt % of a filler; c. from about 1 wt % to about 10 wt % of a disintegrant; d. from about 2 wt % to about 0.3 wt % of a surfactant; e. from about 5 wt % to about 50 wt % of a binder; f. from about 2 wt % to about 0.05 wt % of a glidant; and h. from about 2 wt % to about 0.1 wt % of a lubricant.
30 . The pharmaceutical composition of any of claims 1 - 29 , further comprising a tablet, a capsule, or a suspension.
31 . The pharmaceutical composition of claim 30 , further comprising a tablet, and the tablet has a hardness of at least 5 Kp.
32 . A pharmaceutical composition consisting of a tablet that comprises a solid dispersion, a filler, a disintegrant, a surfactant, a binder, a glidant, and a lubricant, wherein the tablet has a dissolution of at least about 50% in about 30 minutes, and the solid dispersion comprises substantially amorphous Compound 1.
33 . The pharmaceutical composition of claim 32 , wherein the solid dispersion comprises substantially amorphous Compound 1 and HPMCAS or PVP/VA.
34 . The pharmaceutical composition of claim 33 , wherein the solid dispersion comprises at least about 25 mg of substantially amorphous Compound 1, and PVP/VA and SLS.
35 . The pharmaceutical composition of claim 33 , wherein the solid dispersion comprises at least about 25 mg of substantially amorphous Compound 1, and HPMCAS and SLS.
36 . A pharmaceutical composition consisting of a tablet that comprises
a. a solid dispersion comprising substantially amorphous Compound 1, and HPMCAS or PVP/VA; b. a filler; c. a disintegrant; d. a surfactant; e. a binder; f. a glidant; and g. a lubricant.
37 . The pharmaceutical composition of claim 36 , wherein the solid dispersion further comprises SLS.
38 . A method of producing a pharmaceutical composition comprising
providing an admixture comprising a. a solid dispersion comprising substantially amorphous Compound 1; b. a binder; c. a glidant; d. a surfactant; e. a lubricant; f. a disintegrant; and g. a filler, and compressing the admixture into a tablet having a dissolution of at least about 50% in about 30 minutes.
39 . The method of claim 38 , wherein the admixture is compressed to produce a tablet having a hardness of at least 5 Kp.
40 . The method of claim 38 , further comprising mixing the admixture until the admixture is substantially homogenous.
41 . A method of administering a pharmaceutical composition comprising orally administering to a patient at least once per day at least one tablet comprising
a pharmaceutical composition comprising a. a solid dispersion comprising at least about 25 mg of substantially amorphous Compound 1; b. a filler; c. a binder; d. a glidant; e. a disintegrant; f. a surfactant; and g. a lubricant.
42 . The method of claim 41 , wherein the tablet comprising the pharmaceutical composition comprising the solid dispersion comprising substantially amorphous Compound 1, the filler, the binder, the glidant, the disintegrant, the surfactant, and the lubricant is orally administered to the patient once per day or about every 12 hours.
43 . The method of claim 42 , wherein the solid dispersion further comprises at least 75 mg of substantially amorphous Compound 1.
44 . A method of administering a pharmaceutical composition comprising orally administering to a patient at least once per day at least one tablet comprising
a pharmaceutical composition comprising
a. a solid dispersion comprising at least about 25 mg of substantially amorphous Compound 1;
b. a filler;
c. a binder;
d. a glidant;
e. a disintegrant;
f. a surfactant, and
g. a lubricant.
45 . A pharmaceutical composition consisting of a tablet comprising
a. a solid dispersion comprising from about 20 wt % to about 99 wt % of substantially amorphous Compound 1 by weight of the dispersion and a polymer selected from HPMCAS or PVP/VA; b. from about 27 wt % to about 45 wt % of a filler comprising lactose; c. from about 2.5 wt % to about 6.0 wt % of a disintegrant comprising sodium croscarmellose; d. from about 2.0 wt % to about 0.3 wt % of a surfactant comprising sodium lauryl sulfate; e. from about 20 wt % to about 45 wt % of a binder comprising microcrystalline cellulose; f. from about 1.0 wt % to about 0.09 wt % of a glidant comprising colloidal silicon dioxide; and g. from about 1.3 wt % to about 0.3 wt % of a lubricant comprising magnesium stearate.
46 . A pharmaceutical composition comprising
a. about 15 wt % of a solid dispersion by weight of the composition, wherein the dispersion comprises about 50 wt % of substantially amorphous Compound 1 by weight of the dispersion, about 49.5 wt % of HPMCAS by weight of the dispersion, and about 0.5 wt % SLS by weight of the dispersion; b. about 35 wt % of microcrystalline cellulose by weight of the composition; c. about 43 wt % of lactose by weight of the composition; about 5 wt % of sodium croscarmellose by weight of the composition; d. about 0.5 wt % of SLS by weight of the composition; e. about 0.125 wt % of colloidal silicon dioxide by weight of the composition; and f. about 0.5 wt % of magnesium stearate by weight of the composition.
47 . A pharmaceutical composition comprising
a. about 31 wt % of a solid dispersion by weight of the composition, wherein the dispersion comprises about 50 wt % of substantially amorphous Compound 1 by weight of the dispersion, about 49.5 wt % of HPMCAS by weight of the dispersion, and about 0.5 wt % SLS by weight of the dispersion; b. about 25 wt % of microcrystalline cellulose by weight of the composition; c. about 38 wt % of lactose by weight of the composition; d. about 5 wt % of sodium croscarmellose by weight of the composition; e. about 0.5 wt % of SLS by weight of the composition; f. about 0.125 wt % of colloidal silicon dioxide by weight of the composition; and g. about 0.5 wt % of magnesium stearate by weight of the composition.
48 . A pharmaceutical composition comprising
a. about 40 wt % of a solid dispersion by weight of the composition, wherein the dispersion comprises about 80 wt % of substantially amorphous Compound 1 by weight of the dispersion, about 19.5 wt % of PVP/VA by weight of the dispersion, and about 0.5 wt % SLS by weight of the dispersion; b. about 27 wt % of microcrystalline cellulose by weight of the composition; c. about 27 wt % of lactose by weight of the composition; d. about 3 wt % of sodium croscarmellose by weight of the composition; e. about 0.5 wt % of SLS by weight of the composition; f. about 1 wt % of colloidal silicon dioxide by weight of the composition; g. about 1 wt % of magnesium stearate by weight of the composition; and h. about 0.4 wt % of colorant by weight of the composition.
49 . A pharmaceutical composition comprising
a. about 40 wt % of a solid dispersion by weight of the composition, wherein the dispersion comprises about 80 wt % of substantially amorphous Compound 1 by weight of the dispersion, about 19.5 wt % of HPMCAS by weight of the dispersion, and about 0.5 wt % SLS by weight of the dispersion; b. about 27 wt % of microcrystalline cellulose by weight of the composition; c. about 27 wt % of lactose by weight of the composition; d. about 3 wt % of sodium croscarmellose by weight of the composition; e. about 0.5 wt % of SLS by weight of the composition; f. about 1 wt % of colloidal silicon dioxide by weight of the composition; g. about 1 wt % of magnesium stearate by weight of the composition; and h. about 0.4 wt % of colorant by weight of the composition.
50 . A pharmaceutical composition comprising:
a. a solid dispersion comprising amorphous Compound 1 and a polymer; b. a filler; c. a disintegrant; d. a surfactant; e. a binder; f. a glidant; and g. a lubricant.
51 . The pharmaceutical composition of claim 50 , wherein the solid dispersion comprises substantially amorphous Compound 1 and a polymer, and the polymer comprises HPMC, HPMCAS, PVP/VA, PVP, methacrylic acid/methacrylate copolymer, HPC, or any combination thereof.
52 . The pharmaceutical composition of claim 51 , wherein the solid dispersion has a mean particle diameter of greater than about 5 μm.
53 . The pharmaceutical composition of claim 51 , wherein the solid dispersion has a bulk density of about 0.10 g/cc or greater.
54 . The pharmaceutical composition of claim 51 , wherein the solid dispersion comprises amorphous Compound 1, and Compound 1 is present in a concentration of at least 20 wt % by weight of the solid dispersion.
55 . The pharmaceutical composition of claim 54 , wherein the solid dispersion comprises 80 wt % or less of HPMCAS or PVP/VA.
56 . The pharmaceutical composition of claim 55 , wherein the solid dispersion comprises a surfactant.
57 . The pharmaceutical composition of claim 56 , wherein the solid dispersion comprises less than 10 wt % of surfactant by weight of solid dispersion.
58 . The pharmaceutical composition of claim 57 , wherein the solid dispersion comprises a surfactant, and the surfactant is SLS.
59 . The pharmaceutical composition of claim 50 , wherein the solid dispersion comprises from about 45 wt % to about 85 wt % of amorphous Compound 1, from about 0.45 wt % to about 0.55 wt % of SLS, and from about 14.45 wt % to about 55.55 wt % of HPMCAS or PVP/VA by weight of the solid dispersion.
60 . The pharmaceutical composition of claim 50 , wherein the solid dispersion comprises from about 40 wt % to about 60 wt % of amorphous Compound 1 by weight of the solid dispersion and from about 60 wt % to about 40 wt % of polymer by weight of the solid dispersion.
61 . The pharmaceutical composition of claim 50 , wherein the solid dispersion comprises from about 65 wt % to about 95 wt % of amorphous Compound 1 by weight of the solid dispersion and from about 45 wt % to about 5 wt % of polymer by weight of the solid dispersion.
62 . The pharmaceutical composition of any of claims 50 - 61 , wherein the filler is lactose, sorbitol, cellulose, calcium phosphate, starch, sugar, or any combination thereof.
63 . The pharmaceutical composition of any of claims 50 - 62 , wherein the filler is lactose and has a concentration of at least about 10 wt % by weight of the composition.
64 . The pharmaceutical composition of any of claims 50 - 63 , wherein the disintegrant is sodium croscarmellose, sodium starch glycolate, or a combination thereof.
65 . The pharmaceutical composition of any of claims 50 - 64 , wherein the disintegrant is sodium croscarmellose and has a concentration of about 10 wt % or less by weight of the composition.
66 . The pharmaceutical composition of any of claims 50 - 65 , wherein the surfactant is sodium lauryl sulfate, sodium stearyl fumarate, polyoxyethylene 20 sorbitan mono-oleate, or any combination thereof.
67 . The pharmaceutical composition of any of claims 50 - 66 , wherein the surfactant is sodium lauryl sulfate and has a concentration of about 10 wt % or less by weight of the composition.
68 . The pharmaceutical composition of any of claims 50 - 67 , wherein the binder is microcrystalline cellulose, dibasic calcium phosphate, sucrose, corn starch, modified cellulose, or any combination thereof.
69 . The pharmaceutical composition of any of claims 50 - 68 , wherein the binder is microcrystalline cellulose and has a concentration of at least about 1 wt % by weight of the composition.
70 . The pharmaceutical composition of any of claims 50 - 69 , wherein the glidant is colloidal silicon dioxide, talc, or a combination thereof.
71 . The pharmaceutical composition of any of claims 50 - 70 , wherein the glidant is colloidal silicon dioxide and has a concentration of 2 wt % or less by weight of the composition.
72 . The pharmaceutical composition of any of claims 50 - 71 , wherein the lubricant is magnesium stearate, stearic acid, hydrogenated oil, sodium stearyl fumarate, or any combination thereof.
73 . The pharmaceutical composition of any of claims 50 - 72 , wherein the lubricant is magnesium stearate and has a concentration of about 2 wt % by weight of the composition.
74 . The pharmaceutical composition of any of claims 50 - 73 , further comprising a colorant.
75 . The pharmaceutical composition of any of claims 50 - 74 , wherein the colorant is a blue pigment having a concentration of less than 1 wt % by weight of the composition.
76 . The pharmaceutical composition of any of claims 31 - 37 and 45 , wherein the tablet further comprises a coating.
77 . The pharmaceutical composition of claim 76 , wherein the coating comprises a colorant.
78 . The pharmaceutical composition of claim 77 , wherein the colorant comprises OPADRY® II.
79 . The pharmaceutical composition of claims 76 - 78 , wherein the coating further comprises a wax coating.
80 . The pharmaceutical composition of claim 79 , wherein the wax coating comprises a Carnauba wax powder.
81 . The pharmaceutical composition of claims 76 - 80 , wherein the tablet further comprises ink images or ink text printed on the coating.
82 . A caplet shaped pharmaceutical tablet composition having a hardness of 9.5 Kp±15 percent, comprising
a. about 34 wt % of a solid dispersion by weight of the composition, wherein the dispersion comprises about 80 wt % of substantially amorphous Compound 1 by weight of the dispersion, about 19.5 wt % of HPMCAS by weight of the dispersion, and about 0.5 wt % SLS by weight of the dispersion;
b. about 30 wt % of microcrystalline cellulose by weight of the composition;
c. about 30 wt % of lactose by weight of the composition;
d. about 3 wt % of sodium croscarmellose by weight of the composition;
e. about 0.5 wt % of SLS by weight of the composition;
f. about 1 wt % of colloidal silicon dioxide by weight of the composition; and
g. about 1 wt % of magnesium stearate by weight of the composition.
83 . The caplet shaped pharmaceutical tablet composition of claim 82 , wherein the tablet contains 150 mg of Compound 1.
84 . The caplet shaped pharmaceutical tablet composition of claim 82 , wherein the tablet contains 100 mg of Compound 1.
85 . A caplet shaped pharmaceutical tablet composition having an initial hardness of 11 Kp±20 percent, comprising
a. about 40 wt % of a solid dispersion by weight of the composition, wherein the dispersion comprises about 80 wt % of substantially amorphous Compound 1 by weight of the dispersion, about 19.5 wt % of HPMCAS by weight of the dispersion, and about 0.5 wt % SLS by weight of the dispersion;
b. about 30 wt % of microcrystalline cellulose by weight of the composition;
c. about 30 wt % of lactose by weight of the composition;
d. about 3 wt % of sodium croscarmellose by weight of the composition;
e. about 0.5 wt % of SLS by weight of the composition;
f. about 1 wt % of colloidal silicon dioxide by weight of the composition; and
g. about 1 wt % of magnesium stearate by weight of the composition.
86 . The caplet shaped pharmaceutical tablet composition of claim 85 , wherein the tablet contains 150 mg of Compound 1.
87 . The caplet shaped pharmaceutical tablet composition of claim 85 , wherein the tablet contains 100 mg of Compound 1.
88 . A caplet shaped pharmaceutical tablet composition having an initial hardness of 11 Kp±20 percent, comprising
a. about 34.1 wt % of a solid dispersion by weight of the composition, wherein the dispersion comprises about 80 wt % of substantially amorphous Compound 1 by weight of the dispersion, about 19.5 wt % of HPMCAS by weight of the dispersion, and about 0.5 wt % SLS by weight of the dispersion;
b. about 30 wt % of microcrystalline cellulose by weight of the composition;
c. about 30.4 wt % of lactose by weight of the composition;
d. about 3 wt % of sodium croscarmellose by weight of the composition;
e. about 0.5 wt % of SLS by weight of the composition;
f. about 1 wt % of colloidal silicon dioxide by weight of the composition; and
g. about 1 wt % of magnesium stearate by weight of the composition.
89 . The caplet shaped pharmaceutical tablet composition of claim 88 , wherein the tablet contains 100 mg of Compound 1.
90 . The caplet shaped pharmaceutical tablet composition of claim 88 , wherein the tablet contains 150 mg of Compound 1.
91 . The caplet shaped pharmaceutical tablet composition of claim 88 , wherein the tablet includes a colorant coating and a printed logo or text.
92 . The caplet shaped pharmaceutical tablet composition of claim 91 , wherein the tablet includes a blue OPADRY® II coating and a water or solvent based ink logo or text.
93 . A caplet shaped pharmaceutical tablet composition having an initial hardness of between about 6 and 16 Kp, comprising
a. about 34.1 wt % of a solid dispersion by weight of the composition, wherein the dispersion comprises about 80 wt % of substantially amorphous Compound 1 by weight of the dispersion, about 19.5 wt % of HPMCAS by weight of the dispersion, and about 0.5 wt % SLS by weight of the dispersion; b. about 30.5 wt % of microcrystalline cellulose by weight of the composition; c. about 30.4 wt % of lactose by weight of the composition; d. about 3 wt % of sodium croscarmellose by weight of the composition; e. about 0.5 wt % of SLS by weight of the composition; f. about 0.5 wt % of colloidal silicon dioxide by weight of the composition; and g. about 1 wt % of magnesium stearate by weight of the composition.
94 . The caplet shaped pharmaceutical tablet composition of claim 93 , wherein the composition contains 100 mg of Compound 1.
95 . The caplet shaped pharmaceutical tablet composition of claim 93 , wherein the composition contains 150 mg of Compound 1.
96 . The caplet shaped pharmaceutical tablet composition of claim 93 , wherein the tablet further comprises a colorant coated, a wax coating, and a printed logo or text.
97 . The caplet shaped pharmaceutical tablet composition of claim 96 , wherein the tablet includes a blue OPADRY® II coating and a water or solvent based ink logo or text.
98 . The caplet of claim 96 , wherein the wax coating comprises Carnauba wax.
99 . The caplet of claim 96 , wherein the ink for the printed logo or text is a solvent based ink.
100 . A caplet shaped pharmaceutical tablet composition having an initial hardness of between about 9 and 21 Kp, comprising
a. about 34.1 wt % of a solid dispersion by weight of the composition, wherein the dispersion comprises about 80 wt % of substantially amorphous Compound 1 by weight of the dispersion, about 19.5 wt % of HPMCAS by weight of the dispersion, and about 0.5 wt % SLS by weight of the dispersion; b. about 30.5 wt % of microcrystalline cellulose by weight of the composition; c. about 30.4 wt % of lactose by weight of the composition; d. about 3 wt % of sodium croscarmellose by weight of the composition; e. about 0.5 wt % of SLS by weight of the composition; f. about 0.5 wt % of colloidal silicon dioxide by weight of the composition; and g. about 1 wt % of magnesium stearate by weight of the composition.
101 . The caplet shaped pharmaceutical tablet composition of claim 100 , wherein the tablet contains 150 mg of Compound 1.
102 . The caplet shaped pharmaceutical tablet composition of claim 100 , wherein the composition contains 100 mg of Compound 1.
103 . The caplet shaped pharmaceutical tablet composition of claim 100 , wherein the tablet further comprises a colorant coated, a wax coating, and a printed logo or text.
104 . The caplet shaped pharmaceutical tablet composition of claim 103 , wherein the tablet includes a blue OPADRY® II coating and a water or solvent based ink logo or text.
105 . The caplet of claim 103 , wherein the wax coating comprises Carnauba wax.
106 . The caplet of claim 103 , wherein the ink for the printed logo or text is a solvent based ink.
107 . A method of treating or lessening the severity of a disease in a patient comprising administering to said patient a pharmaceutical composition according to claims 1 - 37 and 45 - 101 , wherein said disease is selected from cystic fibrosis, asthma, smoke induced COPD, chronic bronchitis, rhinosinusitis, constipation, pancreatitis, pancreatic insufficiency, male infertility caused by congenital bilateral absence of the vas deferens (CBAVD), mild pulmonary disease, idiopathic pancreatitis, allergic bronchopulmonary aspergillosis (ABPA), liver disease, hereditary emphysema, hereditary hemochromatosis, coagulation-fibrinolysis deficiencies, such as protein C deficiency, Type 1 hereditary angioedema, lipid processing deficiencies, such as familial hypercholesterolemia, Type 1 chylomicronemia, abetalipoproteinemia, lysosomal storage diseases, such as I-cell disease/pseudo-Hurler, mucopolysaccharidoses, Sandhof/Tay-Sachs, Crigler-Najjar type II, polyendocrinopathy/hyperinsulemia, Diabetes mellitus, Laron dwarfism, myleoperoxidase deficiency, primary hypoparathyroidism, melanoma, glycanosis CDG type 1, congenital hyperthyroidism, osteogenesis imperfecta, hereditary hypofibrinogenemia, ACT deficiency, Diabetes insipidus (DI), neurophyseal DI, neprogenic DI, Charcot-Marie Tooth syndrome, Perlizaeus-Merzbacher disease, neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, progressive supranuclear plasy, Pick's disease, several polyglutamine neurological disorders such as Huntington's, spinocerebullar ataxia type I, spinal and bulbar muscular atrophy, dentatorubal pallidoluysian, and myotonic dystrophy, as well as spongiform encephalopathies, such as hereditary Creutzfeldt-Jakob disease (due to prion protein processing defect), Fabry disease, Straussler-Scheinker syndrome, COPD, dry-eye disease, or Sjogren's disease, Osteoporosis, Osteopenia, Gorham's Syndrome, chloride channelopathies such as myotonia congenita (Thomson and Becker forms), Bartter's syndrome type III, Dent's disease, hyperekplexia, epilepsy, hyperekplexia, lysosomal storage disease, Angelman syndrome, and Primary Ciliary Dyskinesia (PCD), a term for inherited disorders of the structure and/or function of cilia, including PCD with situs inversus (also known as Kartagener syndrome), PCD without situs inversus and ciliary aplasia.
108 . The method of claim 107 , wherein said disease is cystic fibrosis.
109 . The method of claim 108 , wherein said patient has cystic fibrosis transmembrane receptor (CFTR) with a ΔF508 mutation.
110 . The method of claim 109 , wherein said patient has cystic fibrosis transmembrane receptor (CFTR) with a R117H mutation.
111 . The method of claim 109 , wherein said patient has cystic fibrosis transmembrane receptor (CFTR) with a G551D mutation.Join the waitlist — get patent alerts
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