US8569326B2
Active / In Force
US
⏱️ 5.8 years remaining
Forms of rifaximin and uses thereof
Assignee: Aptuit Inc
•
Filing: 2012-08-16
•
Granted: 2013-10-29
•
Expires: 2032-08-16
Abstract
Abstract The present invention relates to Rifaximin polymorphic forms, to their use in medicinal preparations and to therapeutic methods using them.
Inventors
- 👤 Karen S. Gushurst
- 👤 Donglai Yang
- 👤 Petinka Vlahova
- 👤 Jeffrey S. Stults
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 10:22
CPC Classifications
C; C07; C07D; C07D498/00; C07D498/22; A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/4353; A61K31/437; A61P; A61P1/00; A61P31/00; A61P31/04; C07D498/12; C07B; C07B2200/00; C07B2200/13
Claims Analysis
Total Claims: 25
Claim 1
Independent Claim
49 words
A rifaximin polymorph Form ζ, wherein the polymorphic Form ζ exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ (+/−0.20 degree θ) comprising: 4.69, 7.63, 12.52, and 13.87; 4.69, 7.63 and 12.52; 4.69, 7.63 and 13.87; 4.69, 12.52 and 13.87; or 7.63, 12.52 and 13.87.
Claim 2
Dependent Claim
49 words
A rifaximin polymorph Form ζ, wherein the polymorphic Form ζ exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ (+/−0.20 degree θ) comprising: 4.69, 7.63, 12.52, and 13.87; 4.69, 7.63 and 12.52; 4.69, 7.63 and 13.87; 4.69, 12.52 and 13.87; or 7.63, 12.52 and 13.87.
Claim 3
Dependent Claim
87 words
A rifaximin polymorph Form η, wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ (+/−0.20 degree θ) comprising: 6.1, 7.3, and 7.5; 6.1, 7.3, and 7.9; 6.1, 7.3 and 8.8; 6.1, 7.3 and 12.7; 6.1, 7.5 and 7.9; 6.1, 7.5 and 8.8; 5.3, 6.1 and 7.3; 5.3, 6.1 and 7.5; 6.1, 7.3, 7.5, 7.9, 8.8 and 12.7; 5.3, 6.1, 7.3, 7.9, 8.8 and 12.7; 5.3, 6.1, 7.3, 7.5, 8.8, and 12.7; or 5.3, 6.1, 7.3, 7.5, 7.9, 8.8 and 12.7.
Claim 4
Dependent Claim
87 words
A rifaximin polymorph Form η, wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ (+/−0.20 degree θ) comprising: 6.1, 7.3, and 7.5; 6.1, 7.3, and 7.9; 6.1, 7.3 and 8.8; 6.1, 7.3 and 12.7; 6.1, 7.5 and 7.9; 6.1, 7.5 and 8.8; 5.3, 6.1 and 7.3; 5.3, 6.1 and 7.5; 6.1, 7.3, 7.5, 7.9, 8.8 and 12.7; 5.3, 6.1, 7.3, 7.9, 8.8 and 12.7; 5.3, 6.1, 7.3, 7.5, 8.8, and 12.7; or 5.3, 6.1, 7.3, 7.5, 7.9, 8.8 and 12.7.
Claim 5
Dependent Claim
154 words
A rifaximin polymorph Form ι, wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ (+/−0.20 degree θ) comprising: 5.49, 5.88, 7.86, 9.03, 12.66, and 13.89; 5.49, 5.88, 7.86, 9.03, and 12.66; 5.49, 5.88, 9.03, 12.66 and 13.89; 5.49, 7.86, 9.03, 12.66 and 13.89; 5.49, 5.88, 7.86, 9.03 and 13.89; 5.88, 7.86, 9.03, 12.66 and 13.89; 5.9, 7.9, and 9.0; 12.7, 13.9, and 14.9; 5.9, 7.9, and 12.7; 5.9, 9.0, and 12.7; 5.9, 13.9, and 14.9; 5.9, 7.9, and 14.9; 7.4, 20.0 and 20.9; 9.0, 12.7, and 14.9; 20.0, 20.9 and 23.4; 5.9, 7.9, 9.0, and 14.9; 5.9, 7.9, 9.0, and 12.7; 5.9, 7.4, 7.9 and 9.4; 7.4, 12.7, 13.9 and 23.4; 5.9, 13.9, 14.9, 20.0 and 20.9; 5.9, 7.9, 9.0, 12.7, 13.9, and 14.9; 5.9, 7.4, 7.9, 12.7, 13.9, 14.9, 20.0, 20.9 and 23.4; or 5.9, 7.4, 7.9, 9.0, 9.4, 12.7, 13.9, 14.9, 20.0, 20.9 and 23.4.
Claim 6
Dependent Claim
154 words
A rifaximin polymorph Form ι, wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ (+/−0.20 degree θ) comprising: 5.49, 5.88, 7.86, 9.03, 12.66, and 13.89; 5.49, 5.88, 7.86, 9.03, and 12.66; 5.49, 5.88, 9.03, 12.66 and 13.89; 5.49, 7.86, 9.03, 12.66 and 13.89; 5.49, 5.88, 7.86, 9.03 and 13.89; 5.88, 7.86, 9.03, 12.66 and 13.89; 5.9, 7.9, and 9.0; 12.7, 13.9, and 14.9; 5.9, 7.9, and 12.7; 5.9, 9.0, and 12.7; 5.9, 13.9, and 14.9; 5.9, 7.9, and 14.9; 7.4, 20.0 and 20.9; 9.0, 12.7, and 14.9; 20.0, 20.9 and 23.4; 5.9, 7.9, 9.0, and 14.9; 5.9, 7.9, 9.0, and 12.7; 5.9, 7.4, 7.9 and 9.4; 7.4, 12.7, 13.9 and 23.4; 5.9, 13.9, 14.9, 20.0 and 20.9; 5.9, 7.9, 9.0, 12.7, 13.9, and 14.9; 5.9, 7.4, 7.9, 12.7, 13.9, 14.9, 20.0, 20.9 and 23.4; or 5.9, 7.4, 7.9, 9.0, 9.4, 12.7, 13.9, 14.9, 20.0, 20.9 and 23.4.
Claim 7
Dependent Claim
69 words
A rifaximin polymorph Form ι-dry, wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ (+/−0.20 degree θ) comprising: 6.04, 7.90, 8.92, 9.49, 12.76, and 14.14; 6.04, 8.92, 9.49, 12.76 and 14.14; 6.04, 7.90, 9.49, 12.76 and 14.14; 6.04, 7.90, 8.92, 9.49 and 14.14; 6.04, 7.90, 8.92, 9.49 and 12.76; 6.04, 7.90, 8.92, 12.76 and 14.14; or 7.90, 8.92, 9.49, 12.76, and 14.14.
Claim 8
Dependent Claim
69 words
A rifaximin polymorph Form ι-dry, wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ (+/−0.20 degree θ) comprising: 6.04, 7.90, 8.92, 9.49, 12.76, and 14.14; 6.04, 8.92, 9.49, 12.76 and 14.14; 6.04, 7.90, 9.49, 12.76 and 14.14; 6.04, 7.90, 8.92, 9.49 and 14.14; 6.04, 7.90, 8.92, 9.49 and 12.76; 6.04, 7.90, 8.92, 12.76 and 14.14; or 7.90, 8.92, 9.49, 12.76, and 14.14.
Claim 9
Dependent Claim
69 words
A rifaximin polymorph Form ι-dry′, wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ (+/−0.20 degree θ) comprising: 6.16, 7.92, 8.89, 9.55, 12.80, and 14.25; 6.16, 8.89, 9.55, 12.80 and 14.25; 6.16, 7.92, 9.55, 12.80 and 14.25; 6.16, 7.92, 8.89, 12.80 and 14.25; 6.16, 7.92, 8.89, 9.55 and 14.25; 6.16, 7.92, 8.89, 9.55 and 12.80; or 7.92, 8.89, 9.55, 12.80 and 14.25.
Claim 10
Dependent Claim
69 words
A rifaximin polymorph Form ι-dry′, wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ (+/−0.20 degree θ) comprising: 6.16, 7.92, 8.89, 9.55, 12.80, and 14.25; 6.16, 8.89, 9.55, 12.80 and 14.25; 6.16, 7.92, 9.55, 12.80 and 14.25; 6.16, 7.92, 8.89, 12.80 and 14.25; 6.16, 7.92, 8.89, 9.55 and 14.25; 6.16, 7.92, 8.89, 9.55 and 12.80; or 7.92, 8.89, 9.55, 12.80 and 14.25.
Claim 11
Dependent Claim
73 words
A rifaximin polymorph Form B, wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ (+/−0.20 degree θ) comprising: 5.24, 6.84, 7.74, 8.71, 10.16, and 12.21; 5.24, 7.74, 8.71, 10.16 and 12.21; 5.24, 6.84, 8.71, 10.16 and 12.21; 5.24, 6.84, 7.74, 10.16 and 12.21; 5.24, 6.84, 7.74, 8.71 and 12.21; 5.24, 6.84, 7.74, 8.71 and 10.16; 6.84, 7.74, 8.71, 10.16 and 12.21; or 5.24, 6.84 and 7.74.
Claim 12
Dependent Claim
73 words
A rifaximin polymorph Form B, wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2θ (+/−0.20 degree θ) comprising: 5.24, 6.84, 7.74, 8.71, 10.16, and 12.21; 5.24, 7.74, 8.71, 10.16 and 12.21; 5.24, 6.84, 8.71, 10.16 and 12.21; 5.24, 6.84, 7.74, 10.16 and 12.21; 5.24, 6.84, 7.74, 8.71 and 12.21; 5.24, 6.84, 7.74, 8.71 and 10.16; 6.84, 7.74, 8.71, 10.16 and 12.21; or 5.24, 6.84 and 7.74.
Claim 13
Dependent Claim
62 words
A pharmaceutical composition comprising the rifaximin polymorph Form ζ of claim 1 , rifaximin polymorph Form η of claim 2 , rifaximin polymorph Form ι of claim 3 , rifaximin polymorph Form ι-dry of claim 4 , rifaximin polymorph Form ι-dry′ of claim 5 , or rifaximin polymorph Form B of claim 6 , or mixtures thereof; and a pharmaceutically acceptable carrier.
Claim 14
Dependent Claim
17 words
The rifaximin polymorph Form ζ of claim 1 , containing less than 5% by weight total impurities.
Claim 15
Dependent Claim
17 words
The rifaximin polymorph Form η of claim 2 , containing less than 5% by weight total impurities.
Claim 16
Dependent Claim
17 words
The rifaximin polymorph Form ι of claim 3 , containing less than 5% by weight total impurities.
Claim 17
Dependent Claim
17 words
The rifaximin polymorph Form ι-dry of claim 4 , containing less than 5% by weight total impurities.
Claim 18
Dependent Claim
17 words
The rifaximin polymorph Form ι-dry′ of claim 5 , containing less than 5% by weight total impurities.
Claim 19
Dependent Claim
16 words
The rifaximin Form B of claim 6 , containing less than 5% by weight total impurities.
Claim 20
Dependent Claim
42 words
The rifaximin polymorph Form ζ of claim 1 , wherein the compound is at least 50% pure, or at least 75% pure, or at least 80% pure, or at least 90% pure, or at least 95% pure, or at least 98% pure.
Claim 21
Dependent Claim
42 words
The rifaximin polymorph Form η of claim 2 , wherein the compound is at least 50% pure, or at least 75% pure, or at least 80% pure, or at least 90% pure, or at least 95% pure, or at least 98% pure.
Claim 22
Dependent Claim
41 words
The rifaximin polymorph Form ζ claim 3 , wherein the compound is at least 50% pure, or at least 75% pure, or at least 80% pure, or at least 90% pure, or at least 95% pure, or at least 98% pure.
Claim 23
Dependent Claim
42 words
The rifaximin polymorph Form ι-dry of claim 4 , wherein the compound is at least 50% pure, or at least 75% pure, or at least 80% pure, or at least 90% pure, or at least 95% pure, or at least 98% pure.
Claim 24
Dependent Claim
42 words
The rifaximin polymorph Form ι-dry′ of claim 5 , wherein the compound is at least 50% pure, or at least 75% pure, or at least 80% pure, or at least 90% pure, or at least 95% pure, or at least 98% pure.
Claim 25
Dependent Claim
42 words
The rifaximin polymorph Form B, of claim 6 , wherein the compound is at least 50% pure, or at least 75% pure, or at least 80% pure, or at least 90% pure, or at least 95% pure, or at least 98% pure.
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