FORMULATIONS OF RIFAXIMIN AND USES THEREOF
The present invention relates to new rifaximin forms comprising solid dispersions of rifaximin, methods of making same and to their use in medicinal preparations and therapeutic methods.
1 . A pharmaceutical composition comprising
from about 33 wt % to about 35 wt % rifaximin;
from about 33 wt % to about 35 wt % HPMC-AS;
from about 3 wt % to about 5 wt % poloxamer 407;
from about 4 wt % to about 14 wt % croscarmellose sodium;
from about 10 wt % to about 19 wt % microcrystalline cellulose;
from about 0.15 wt % to about 0.25 wt % colloidal silicon dioxide; and
from about 0.45 wt % to about 0.55 wt % magnesium stearate.
2 . The pharmaceutical composition of claim 1 , wherein the croscarmellose sodium is present in an amount of from about 12 wt % to about 14 wt %.
3 . The pharmaceutical composition of claim 1 , wherein the croscarmellose sodium is present in an amount of about 13%.
4 . The pharmaceutical composition of claim 1 , wherein the microcrystalline cellulose is present in an amount from about 10 wt % to about 12 wt %.
5 . The pharmaceutical composition of claim 1 , wherein the microcrystalline cellulose is present in an amount of about 11 wt %.
6 . The pharmaceutical composition of claim 1 , wherein the croscarmellose sodium is present in an amount from about 4 wt % to about 6 wt %.
7 . The pharmaceutical composition of claim 1 , wherein the croscarmellose sodium is present in an amount of about 5 wt %
8 . The pharmaceutical composition of claim 1 , wherein the microcrystalline cellulose is present in an amount from about 17 wt % to about 19 wt %.
9 . The pharmaceutical composition of claim 1 , wherein the microcrystalline cellulose is present in an amount of about 18 wt %.
10 . The pharmaceutical composition of claim 1 , wherein the poloxamer 407 is present in an amount of about 4%.
11 . The pharmaceutical composition of claim 1 , wherein the colloidal silicon dioxide is present in an amount of about 0.20 wt %.
12 . The pharmaceutical composition of claim 1 , wherein the magnesium stearate is present in an amount of about 0.50 wt %.
13 . The pharmaceutical composition of claim 1 , wherein the rifaximin is present in an amount of about 34%.
14 . The pharmaceutical composition of claim 1 , wherein the HPMC-AS is present in an amount of about 34%.
15 . The pharmaceutical composition of claim 1 , wherein the total amount of rifaximin is about 80 mg.
16 . A pharmaceutical composition comprising
from about 16 wt % to about 18 wt % rifaximin;
from about 16 wt % to about 18 wt % HPMC-AS;
from about 1 wt % to about 2 wt % poloxamer 407;
from about 4 wt % to about 10 wt % croscarmellose sodium;
from about 49 wt % to about 55 wt % microcrystalline cellulose;
from about 0.15 wt % to about 0.25 wt % colloidal silicon dioxide; and
from about 0.45 wt % to about 0.55 wt % magnesium stearate.
17 . The pharmaceutical composition of claim 16 , wherein the croscarmellose sodium is present in an amount from about 8 wt % to about 10 wt %.
18 . The pharmaceutical composition of claim 16 , wherein the croscarmellose sodium is present in an amount of about 9 wt %.
19 . The pharmaceutical composition of claim 16 , wherein the microcrystalline cellulose is present in an amount from about 49 wt % to about 51 wt %.
20 . The pharmaceutical composition of claim 16 , wherein the microcrystalline cellulose is present in an amount of about 51 wt %.
21 . The pharmaceutical composition of claim 16 , wherein the croscarmellose sodium is present in an amount from about 4 wt % to about 6 wt %.
22 . The pharmaceutical composition of claim 16 , wherein the croscarmellose sodium is present in an amount of about 5 wt %
23 . The pharmaceutical composition of claim 16 , wherein the microcrystalline cellulose is present in an amount from about 53 wt % to about 55 wt %.
24 . The pharmaceutical composition of claim 16 , wherein the microcrystalline cellulose is present in an amount of about 54 wt %.
25 . The pharmaceutical composition of claim 16 , wherein colloidal silicon dioxide is present in an amount of about 0.20 wt %.
26 . The pharmaceutical composition of claim 16 , wherein the magnesium stearate is present in an amount of about 0.50 wt %.
27 . The pharmaceutical composition of claim 16 , wherein the rifaximin is present in an amount of about 17 wt %.
28 . The pharmaceutical composition of claim 16 , wherein the HMPC-AS is present in an amount of about 17 wt %.
29 . The pharmaceutical composition of claim 16 , wherein the total amount of rifaximin is 40 mg.
30 . The pharmaceutical composition of claim 1 , wherein the composition is in the form of a tablet.
31 . The pharmaceutical composition of claim 16 , wherein the composition is in the form of a tablet.
32 . The pharmaceutical composition of claim 30 , wherein the composition is immediate release or sustained extended release.
33 . The pharmaceutical composition of claim 31 , wherein the composition is immediate release or sustained extended release.
34 . A method of reducing the time to hospitalization associated with a complication of liver disease in a subject, comprising administering to the subject a composition of any claim 1 .
35 . The method of claim 34 , wherein the complication of liver disease is selected from one or more of HE, EVB, SBP, and HRS.
36 . A method of reducing the time to hospitalization associated with a complication of liver disease in a subject, comprising administering to the subject a composition of any claim 16 .
37 . The method of claim 36 , wherein the complication of liver disease is selected from one or more of HE, EVB, SBP, and HRS.
38 . A method of reducing the time to development of refractory ascites in a subject, comprising administering to the subject a composition of claim 1 .
39 . A method of reducing the time to development of refractory ascites in a subject, comprising administering to the subject a composition of claim 16 .