Controlled release pharmaceutical formulations of nitazoxanide
Inventors
Rossignol, Jean-Francois • Ayers, Marc
Assignees
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Publication Number
US-11426388-B2
Publication Date
2022-08-30
Expiration Date
Abstract
Solid dosage formulations of nitazoxanide or a nitazoxanide analogue are provided that comprise a controlled release portion and an immediate release portion. The pharmaceutical composition is typically in the form of a bilayer solid oral dosage form comprising (a) a first layer comprising a first quantity of nitazoxanide or analogue thereof in a controlled release formulation; and (b) a second layer comprising a second quantity of nitazoxanide or analogue thereof in an immediate release formulation. Method of using the formulations in the treatment of hepatitis C are also provided.
Core Innovation
The invention relates to controlled-release solid oral dosage formulations comprising nitazoxanide and/or tizoxanide, where the solid oral dosage form includes a first portion in a controlled release formulation and a second portion in an immediate release formulation for hepatitis C treatment. The disclosed approach aims to improve bioavailability and tolerability by combining controlled release and immediate release portions within the same solid oral dosage form.
The described dosage form is exemplified as a bilayer tablet having a first controlled-release layer or portion and a second immediate-release layer or portion. The disclosure further defines controlled release versus immediate release and provides exemplar tablet compositions using release-controlling and excipient materials. Controlled release portion examples include low-viscosity polymer materials such as low viscosity hydroxypropyl methylcellulose (Methocel), together with named filler, binder, disintegrant, glidant, and lubricant components.
Claims Coverage
Independent claim 1 covers a two-portion solid oral pharmaceutical composition using nitazoxanide and/or tizoxanide with the first portion in a controlled release formulation and the second portion in an immediate release formulation, yielding two inventive features: the controlled-release first portion and the immediate-release second portion.
Two-portion solid oral dosage form with controlled-release first portion and immediate-release second portion
A pharmaceutical composition in the form of a solid oral dosage form comprising a first portion comprising a first quantity of nitazoxanide, tizoxanide or a combination thereof in a controlled release formulation, and a second portion comprising a second quantity of nitazoxanide, tizoxanide or a combination thereof in an immediate release formulation.
The core claim coverage is the solid oral, two-portion formulation architecture: controlled release of nitazoxanide/tizoxanide in a first portion combined with immediate release of nitazoxanide/tizoxanide in a second portion.
Stated Advantages
Improved bioavailability.
Improved tolerability.
Higher exposure (AUC/Cmin) with controlled-release dosing compared to immediate release.
Improved virologic responses in hepatitis C clinical evaluation (including reported virologic response measures).
Documented Applications
Treatment of hepatitis C, including chronic hepatitis C, with controlled-release solid oral dosage forms of nitazoxanide or analogues combining controlled-release and immediate-release portions; a clinical viral kinetics study is described for HCV genotype 4.
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