Antiviral compositions
Inventors
Foster, Alison J. • Long, James • Rannard, Steven P. • Wang, Dong • Duncalf, David J. • Owen, Andrew
Assignees
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Publication Number
US-10561609-B2
Publication Date
2020-02-18
Expiration Date
Abstract
The present invention provides a composition and an antiviral drug preparation, each comprising at least one water-insoluble antiviral drug and at least one water-soluble carrier material, wherein the water-insoluble antiviral drug is dispersed through the water-soluble carrier material in nano-disperse form. The present invention further provides processes for preparing the compositions and drug preparations, and also aqueous nano-dispersions obtained by combining water and the compositions.
Core Innovation
Antiviral compositions and antiviral drug preparations are provided in which at least one water-insoluble antiviral drug is dispersed through at least one water-soluble carrier material in nano-disperse form. The water-insoluble antiviral drug comprises darunavir, and the nano-disperse drug is carried within the water-soluble carrier material.
The patent states that the drug and/or carrier are defined by solubility thresholds and that the nano-dispersion has a defined particle size using z-average particle size. It further specifies that the resulting compositions are substantially solvent-free, with aqueous nano-dispersions obtainable by mixing with water, and discusses water-clear dispersions and dispersion behavior upon aqueous dilution.
The patent additionally describes process aspects for obtaining the nano-dispersions. In one aspect, an emulsion is formed comprising a solution of the water-insoluble antiviral drug in a water-immiscible solvent and a solution of the water-soluble carrier material in an aqueous solvent, and the emulsion is dried to remove both solvents to obtain a substantially solvent-free nano-dispersion. In another aspect, a solution comprising at least one non-aqueous solvent and optionally an aqueous solvent is provided such that the carrier is soluble in the mixture while the water-insoluble antiviral drug is soluble in the mixture but not in the aqueous solvent alone, followed by drying to remove solvents and obtain a substantially solvent-free nano-dispersion.
Claims Coverage
The provided independent claims are clm-00001, clm-00019, clm-00020, and clm-00025. Across these claims, the core inventive theme is a nano-dispersion of a water-insoluble antiviral drug, namely darunavir, within a water-soluble carrier material, with process claims covering preparation of the substantially solvent-free nano-dispersion.
Nano-dispersion of darunavir in a water-soluble carrier
A composition comprising at least one water-insoluble antiviral drug and at least one water-soluble carrier material, wherein the water-insoluble antiviral drug is dispersed through the water-soluble carrier material in nano-disperse form, and wherein the at least one water-insoluble antiviral drug comprises darunavir.
Antiviral drug preparation with nano-dispersed darunavir in a water-soluble carrier
An antiviral drug preparation comprising at least one water-insoluble antiviral drug and at least one water-soluble carrier material, wherein the water-insoluble antiviral drug is dispersed through the water-soluble carrier material in nano-disperse form, and wherein the at least one water-insoluble antiviral drug comprises darunavir.
Emulsion drying to form a substantially solvent-free nano-dispersion of darunavir in the carrier
A process for preparing a composition comprising at least one water-insoluble antiviral drug and at least one water-soluble carrier material, wherein the water-insoluble antiviral drug is dispersed through the water-soluble carrier material in nano-disperse form, and wherein the at least one water-insoluble antiviral drug comprises darunavir, wherein the process comprises forming an emulsion comprising [procedural detail omitted for safety] and drying the emulsion to remove the aqueous solvent and the water-immiscible solvent to obtain a substantially solvent-free nano-dispersion of the antiviral drug in the carrier material.
Solvent-mixture drying to form a substantially solvent-free nano-dispersion of darunavir in the carrier
A process for preparing a composition comprising at least one water-insoluble antiviral drug and at least one water-soluble carrier material, wherein the water-insoluble antiviral drug is dispersed through the water-soluble carrier material in nano-disperse form, and wherein the at least one water-insoluble antiviral drug comprises darunavir, wherein the process comprises providing a solution comprising [procedural detail omitted for safety] and drying the solution to remove the aqueous solvent when present and the non-aqueous solvent to obtain a substantially solvent-free nano-dispersion of the antiviral drug in the carrier material.
Across the independent claims, the invention is directed to compositions and preparations where darunavir is dispersed through a water-soluble carrier material in nano-disperse form, including preparation by emulsion drying or by drying a solvent mixture that dissolves the carrier and the drug while the drug is not soluble in aqueous solvent alone.
Stated Advantages
Rapid dispersion on aqueous dilution.
Water-clear dispersions.
Improved pharmacokinetics/bioavailability as indicated by AUC, Cmax, time to Cmax, and half-life.
Reduced fasted/fed variability (variation in pharmacokinetics under fasted/fed conditions).
Suitability for combination therapy (e.g., HAART).
Documented Applications
Antiviral and antiretroviral drug formulations using nano-dispersions of water-insoluble antiviral drugs in water-soluble carrier materials, including combination therapy (e.g., HAART).
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