US7915275B2
Active / In Force
US
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Use of polymorphic forms of rifaximin for medical preparations
Assignee: Alfasigma SpA
•
Filing: 2007-10-17
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Granted: 2011-03-29
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Expires: 2027-10-17
Abstract
Abstract The present invention relates to Rifaximin polymorphic forms α, β and γ, to their use in medicinal preparations for the oral or topical route and to therapeutic methods using them.
Inventors
- 👤 Giuseppe C. Viscomi
- 👤 Manuela Campana
- 👤 Donatella Confortini
- 👤 Miriam Barbanti
- 👤 Fiorella Calanni
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 11:35
CPC Classifications
C; C07; C07D; C07D498/00; C07D498/22; H; H05; H05B; H05B6/00; H05B6/02; H05B6/10; H05B6/12; H05B6/1209; H05B6/1236; A; A61; A61P; A61P1/00; A61P1/12; A61P31/00; A61P31/04; A61P31/06; H05B6/1245; H05B6/1263
Claims Analysis
Total Claims: 31
Claim 1
Independent Claim
144 words
A method of treating bacterial infection in a patient suffering from a bowel related disorder comprising administering to a patient in need thereof a solid pharmaceutical composition comprising a therapeutically effective amount of one or more of Form α, Form β, or Form γ polymorph of rifaximin and a pharmaceutically acceptable excipient or carrier, wherein the amount of each of Form α, Form β, or Form γ polymorph of rifaximin present in said pharmaceutical composition is an amount to control the amount of systemic absorption of said rifaximin, wherein the rifaximin Form α has x-ray powder diffraction pattern peaks at about 7.4°; 19.7°; 21.0° and 22.1° 2-θ, wherein the rifaximin Form β has x-ray powder diffraction pattern peaks at about 5.4°; 9.0°; and 20.9° 2-θ, and wherein the rifaximin Form γ has x-ray powder diffraction pattern peaks at about 5.0°, 7.1°, and 8.4° 2-θ.
Claim 2
Independent Claim
144 words
A method of treating bacterial infection in a patient suffering from a bowel related disorder comprising administering to a patient in need thereof a solid pharmaceutical composition comprising a therapeutically effective amount of one or more of Form α, Form β, or Form γ polymorph of rifaximin and a pharmaceutically acceptable excipient or carrier, wherein the amount of each of Form α, Form β, or Form γ polymorph of rifaximin present in said pharmaceutical composition is an amount to control the amount of systemic absorption of said rifaximin, wherein the rifaximin Form α has x-ray powder diffraction pattern peaks at about 7.4°; 19.7°; 21.0° and 22.1° 2-θ, wherein the rifaximin Form β has x-ray powder diffraction pattern peaks at about 5.4°; 9.0°; and 20.9° 2-θ, and wherein the rifaximin Form γ has x-ray powder diffraction pattern peaks at about 5.0°, 7.1°, and 8.4° 2-θ.
Claim 3
Dependent Claim
34 words
The method of claim 1 , wherein bowel related disorder is selected from the group consisting of irritable bowel syndrome, traveler's diarrhea, small intestinal bacterial overgrowth, Crohn's disease, chronic pancreatitis, pancreatic insufficiency, and colitis.
Claim 4
Dependent Claim
13 words
The method of claim 1 , wherein the pharmaceutical composition is administered orally.
Claim 5
Dependent Claim
13 words
The method of claim 1 , wherein the pharmaceutical composition is administered topically.
Claim 6
Dependent Claim
49 words
The method of claim 1 , wherein the rifaximin Form α has a water content of less than 4.5%; the rifaximin Form β has a water content of greater than or equal to 4.5%; and the rifaximin Form γ has a water content from about 0% to about 2%.
Claim 7
Dependent Claim
22 words
The method of claim 5 , wherein the rifaximin Form β has a water content of greater than or equal to 4.5%.
Claim 8
Dependent Claim
21 words
The method of claim 5 , wherein the rifaximin Form γ has a water content from about 0% to about 2%.
Claim 9
Dependent Claim
38 words
The method of claim 1 , wherein after administering the polymorph Form α to a patient, the bioavailable plasma concentration of the rifaximin reaches a maximum value (C max ) from about 0.0 ng/ml to about 5.5 ng/ml.
Claim 10
Dependent Claim
26 words
The method of claim 8 , wherein the C max is reached within a time (t max ) from about 1.0 h to about 6.0 h.
Claim 11
Dependent Claim
33 words
The method of claim 8 , wherein the bioavailable plasma AUC 0-24h is between about 0.0 and about 100 ng·h/ml, and the bioavailable plasma AUC 0-inf is between about 0.0 and 110 ng·h/ml.
Claim 12
Dependent Claim
38 words
The method of claim 1 , wherein after administering the polymorph Form β to a patient, the bioavailable plasma concentration of the rifaximin reaches a maximum value (C max ) from about 0.0 ng/ml to about 3.7 ng/ml.
Claim 13
Dependent Claim
26 words
The method of claim 11 , wherein the C max is reached within a time (t max ) from about 1.0 h to about 6.0 h.
Claim 14
Dependent Claim
34 words
The method of claim 11 , wherein the bioavailable plasma AUC 0-24h comprises between about 0.0 and about 40 ng·h/ml and the bioavailable plasma AUC 0-inf comprises from about 0.0 to about 50 ng·h/ml.
Claim 15
Dependent Claim
25 words
The method of claim 1 , wherein the rifaximin Form β has a dissolution rate of from about 0.001 to about 0.016 mg/min/cm 2 .
Claim 16
Dependent Claim
38 words
The method of claim 1 , wherein after administering the polymorph Form γ to a patient, the bioavailable plasma concentration of the rifaximin reaches a maximum value (C max ) from about 0.0 ng/ml to about 5000 ng/ml.
Claim 17
Dependent Claim
26 words
The method of claim 15 , wherein the C max is reached within a time (t max ) from about 1.0 h to about 6.0 h.
Claim 18
Dependent Claim
34 words
The method of claim 15 , wherein the bioavailable plasma AUC 0-24h comprises between about 0.0 and about 22000 ng·h/ml and the bioavailable plasma AUC 0-inf comprises from about 0.0 to about 22000 ng·h/ml.
Claim 19
Dependent Claim
25 words
The method of claim 1 , wherein the rifaximin Form γ has a dissolution rate of from about 0.1 to about 0.16 mg/min/cm 2 .
Claim 20
Dependent Claim
19 words
The method of claim 5 , wherein the rifaximin Form α has a water content of less than 4.5%.
Claim 21
Dependent Claim
84 words
The method of claim 5 , wherein after administering the polymorph Form α to a patient, the bioavailable plasma concentration of the rifaximin reaches a maximum value (C max ) from about 0.0 ng/ml to about 5.5 ng/ml; the C max is reached within a time (t max ) from about 1.0 h to about 6.0 h; and the bioavailable plasma AUC 0-24h is between about 0.0 and about 100 ng·h/ml, and the bioavailable plasma AUC 0-inf is between about 0.0 and 110 ng·h/ml.
Claim 22
Dependent Claim
85 words
The method of claim 5 , wherein after administering the polymorph Form β to a patient, the bioavailable plasma concentration of the rifaximin reaches a maximum value (C max ) from about 0.0 ng/ml to about 3.7 ng/ml; the C max is reached within a time (t max ) from about 1.0 h to about 6.0 h; and the bioavailable plasma AUC 0-24h comprises between about 0.0 and about 40 ngh/ml and the bioavailable plasma AUC 0-inf comprises from about 0.0 to about 50 ng·h/ml.
Claim 23
Dependent Claim
25 words
The method of claim 5 , wherein the rifaximin Form β has a dissolution rate of from about 0.001 to about 0.016 mg/min/cm 2 .
Claim 24
Dependent Claim
85 words
The method of claim 5 , wherein after administering the polymorph Form γ to a patient, the bioavailable plasma concentration of the rifaximin reaches a maximum value (C max ) from about 0.0 ng/ml to about 5000 ng/ml; the C max is reached within a time (t max ) from about 1.0 h to about 6.0 h; and the bioavailable plasma AUC 0-24h comprises between about 0.0 and about 22000 ng·h/ml and the bioavailable plasma AUC 0-inf comprises from about 0.0 to about 22000 ng·h/ml.
Claim 25
Dependent Claim
25 words
The method of claim 5 , wherein the rifaximin Form γ has a dissolution rate of from about 0.1 to about 0.16 mg/min/cm 2 .
Claim 26
Dependent Claim
240 words
The method of claim 1 , wherein after administering the polymorph Form α to a patient, bioavailable plasma concentration of the rifaximin reaches a maximum value (C max ) from about 0.0 ng/ml to about 5.5 ng/ml; the C max is reached within a time (t max ) from about 1.0 h to about 6.0 h; and the bioavailable plasma AUC 0-24h is between about 0.0 and about 100 ng·h/ml, and the bioavailable plasma AUC 0-inf is between about 0.0 and 110 ng·h/ml; wherein after administering the polymorph Form β to a patient, bioavailable plasma concentration of the rifaximin reaches a maximum value (C max ) from about 0.0 ng/ml to about 3.7 ng/ml; the C max is reached within a time (t max ) from about 1.0 h to about 6.0 h; and the bioavailable plasma AUC 0-24h comprises between about 0.0 and about 40 ng·h/ml and the bioavailable plasma AUC 0-inf comprises from about 0.0 to about 50 ng·h/ml; and wherein after administering the polymorph Form γ to a patient, bioavailable plasma concentration of the rifaximin reaches a maximum value (C max ) from about 0.0 ng/ml to about 5000 ng/ml; the C max is reached within a time (t max ) from about 1.0 h to about 6.0 h; and the bioavailable plasma AUC 0-24h comprises between about 0.0 and about 22000 ng·h/ml and the bioavailable plasma AUC 0-inf comprises from about 0.0 to about 22000 ng·h/ml.
Claim 27
Dependent Claim
19 words
The method of claim 25 , wherein the rifaximin Form α has a water content of less than 4.5%.
Claim 28
Dependent Claim
22 words
The method of claim 25 , wherein the rifaximin Form β has a water content of greater than or equal to 4.5%.
Claim 29
Dependent Claim
21 words
The method of claim 25 , wherein the rifaximin Form γ has a water content from about 0% to about 2%.
Claim 30
Dependent Claim
25 words
The method of claim 25 , wherein the rifaximin Form β has a dissolution rate of from about 0.001 to about 0.016 mg/min/cm 2 .
Claim 31
Dependent Claim
25 words
The method of claim 25 , wherein the rifaximin Form γ has a dissolution rate of from about 0.1 to about 0.16 mg/min/cm 2 .
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