Polymorphic forms α, β and γ of rifaximin
DC CAFC
First Claim
Patent Images
1. Rifaximin in polymorphic form α
- free from other polymorphic forms of rifaximin not derived from Form α
by water absorption or release, 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
.
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Abstract
Crystalline polymorphous forms of rifaximin (INN) antibiotic named rifaximin α and rifaximin β, and a poorly crystalline form named rifaximin γ, useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.
29 Citations
57 Claims
-
1. Rifaximin in polymorphic form α
- free from other polymorphic forms of rifaximin not derived from Form α
by water absorption or release, 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
. - View Dependent Claims (2, 3, 9)
- free from other polymorphic forms of rifaximin not derived from Form α
-
4. Rifaximin in polymorphic form β
- free from other polymorphic forms of rifaximin not derived from Form β
by water absorption or release, wherein the rifaximin Form β
has x-ray powder diffraction pattern peaks at about 5.4°
, 9.0° and
20.9°
2-θ
. - View Dependent Claims (5, 10)
- free from other polymorphic forms of rifaximin not derived from Form β
-
6. Rifaximin in polymorphic form γ
- free from other polymorphic forms of rifaximin not derived from Form γ
by water absorption or release, wherein the rifaximin Form γ
has x-ray powder diffraction pattern peaks at about 5.0°
, 7.1°
, and 8.4°
2-θ
. - View Dependent Claims (7, 8, 11)
- free from other polymorphic forms of rifaximin not derived from Form γ
-
12. Rifaximin in polymorphic Form α
- , β
or γ
, wherein the polypmorphic form of rifaximin is obtained by a process comprising crystallizing rifaximin from a solvent to obtain the Form α
, β
or γ
by controlling the water content of the polymorph, temperature of crystallization and length of time of crystallization to choose a rifaximin product in Form α
, β
or γ
, wherein said Form α
has x-ray powder diffraction pattern peaks at about 7.4°
;
19.7°
;
21.0° and
22.1°
2-θ
, said Form β
has x-ray powder diffraction pattern peaks at about 5.4°
;
9.0°
; and
20.9°
2-θ
, and said Form γ
has x-ray powder diffraction pattern peaks at about 5.0°
, 7.1°
, and 8.4°
2-θ
. - View Dependent Claims (13, 14, 15, 16, 17)
- , β
-
18. Rifaximin Form α
- prepared by a process wherein rifaximin Form β
having x-ray powder diffraction pattern peaks at about 5.4°
;
9.0°
; and
20.9°
2-θ
is transformed to rifaximin Form α
by reducing the water content of the rifaximin Form β
in amount sufficient to obtain rifaximin Form α
having x-ray powder diffraction pattern peaks at about 7.4°
;
19.7°
;
21.0° and
22.1°
2-θ
.
- prepared by a process wherein rifaximin Form β
-
19. Rifaximin Form β
- prepared by a process wherein rifaximin Form α
having x-ray powder diffraction pattern peaks at about 7.4°
;
19.7°
;
21.0° and
22.1°
2-θ
is transformed to rifaximin Form β
by increasing the water content of the rifaximin Form α
in amount sufficient to obtain rifaximin Form β
having x-ray powder diffraction pattern peaks at about 5.4°
;
9.0°
; and
20.9°
2-θ
.
- prepared by a process wherein rifaximin Form α
-
20. A solid pharmaceutical composition comprising rifaximin in polymorphic Form α
- and a pharmaceutically acceptable excipient or carrier, 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
. - View Dependent Claims (21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33)
- and a pharmaceutically acceptable excipient or carrier, wherein the rifaximin Form α
-
34. A solid pharmaceutical composition comprising rifaximin in polymorphic Form β
- and a pharmaceutically acceptable excipient or carrier, wherein the rifaximin Form β
has x-ray powder diffraction pattern peaks at about 5.4°
;
9.0°
; and
20.9°
2-θ
. - View Dependent Claims (35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46)
- and a pharmaceutically acceptable excipient or carrier, wherein the rifaximin Form β
-
47. A solid pharmaceutical composition comprising rifaximin in polymorphic Form γ
- and a pharmaceutically acceptable excipient or carrier, wherein the rifaximin Form γ
has x-ray powder diffraction pattern peaks at about 5.0°
, 7.1°
, and 8.4°
2-θ
. - View Dependent Claims (48, 49, 50, 51, 52, 53, 54, 55, 56, 57)
- and a pharmaceutically acceptable excipient or carrier, wherein the rifaximin Form γ
Specification
-
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Litigation Data
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Current AssigneeAlfasigma S.p.A.
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Original AssigneeALFA Wassermann BV (Alfasigma S.p.A.)
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InventorsRighi, Paolo, Braga, Dario, Confortini, Donatella, Viscomi, Giuseppe Claudio, Rosini, Goffredo, Cannata, Vincenzo, Campana, Manuela
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Primary Examiner(s)Kifle; Bruck
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Application NumberUS12/119,600Publication NumberTime in Patent Office1,029 DaysField of Search540/456, 514/279US Class Current514/279CPC Class CodesC07B 2200/13 Crystalline forms, e.g. pol...C07D 491/22 in which the condensed syst...C07D 498/22 in which the condensed syst...
