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Publication Number
US-11129817-B2
Publication Date
2021-09-28
Expiration Date
Abstract
Provided herein are solid dispersions comprising rifaximin and pharmaceutical compositions and uses thereof.
Core Innovation
The invention describes a method of preventing complications of liver disease in a subject having liver cirrhosis by administering a pharmaceutical composition containing rifaximin and hydroxypropyl methylcellulose acetate succinate (HPMC-AS). The pharmaceutical composition further includes poloxamer 407, croscarmellose sodium, microcrystalline cellulose, colloidal silicon dioxide, and magnesium stearate in defined wt % ranges, and the total amount of rifaximin is 40 mg.
The disclosed formulations are rifaximin solid dispersion (SSD) formulations using HPMC-AS, with an option for poloxamer 407. The compositions are provided in defined dosing forms including 40 mg and 80 mg, including immediate release (IR) and sustained extended release (SER), and include film coating for tablet presentations.
The document describes a clinical study framework for preventing cirrhosis complications and reducing clinical outcomes, including time to hospitalization and all-cause mortality, and reducing time to medically refractory ascites. A Phase 2 randomized, double-blind placebo-controlled trial in subjects with early decompensated cirrhosis (ascites) is described with primary endpoints including time to all-cause mortality or hospitalization due to HE, EVB, SBP, or HRS.
Claims Coverage
The partial content includes one independent claim. It covers one overarching inventive concept: preventing selected liver disease complications in a cirrhosis subject by administering a specific pharmaceutical composition with defined wt % ranges of rifaximin, HPMC-AS, and optional poloxamer 407, plus other excipients, with the rifaximin amount fixed at 40 mg, and complication types limited to HE, EVB, SBP, and HRS.
Prevention of selected cirrhosis complications using a defined 40 mg rifaximin composition
A method of preventing complications of liver disease in a subject having liver cirrhosis by administering a pharmaceutical composition containing 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 8 wt % to about 10 wt % croscarmellose sodium, from about 49 wt % to about 51 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, wherein the total amount of rifaximin is 40 mg, and wherein the complications of liver disease are selected from HE, EVB, SBP, and HRS.
Immediate release prevention of selected cirrhosis complications
The pharmaceutical composition is an immediate release composition.
Tablet form prevention of selected cirrhosis complications
The pharmaceutical composition is formulated as a tablet.
Prevention targeting esophageal variceal bleeding
The complication of liver disease is esophageal variceal bleeding (EVB).
Prevention targeting spontaneous bacterial peritonitis
The complication of liver disease is spontaneous bacterial peritonitis (SBP).
Prevention targeting hepatorenal syndrome
The complication of liver disease is hepatorenal syndrome (HRS).
Overall, the claim set covers prevention of hepatic encephalopathy, esophageal variceal bleeding, spontaneous bacterial peritonitis, and hepatorenal syndrome in a liver cirrhosis subject using a specifically defined pharmaceutical composition in which rifaximin is fixed at 40 mg and formulated with HPMC-AS and specified excipients in defined wt % ranges, with further refinements for immediate release and tablet form.
Stated Advantages
Prevents complications of liver disease in a subject having liver cirrhosis.
Reduces time to hospitalization and all-cause mortality.
Reduces time to medically refractory ascites.
Documented Applications
Prevention of cirrhosis complications including hepatic encephalopathy, esophageal variceal bleeding, spontaneous bacterial peritonitis, and hepatorenal syndrome in subjects with early decompensated cirrhosis (ascites).
Assessment in a Phase 2 randomized, double-blind placebo-controlled trial for time to all-cause mortality or hospitalization due to HE, EVB, SBP, or HRS.
Assessment of secondary endpoint related to time to medically refractory ascites.
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