Oral liquid formulations of lipid-lowering and blood pressure-lowering drugs
Inventors
Ugwu, Sydney • Fu, Zengli • He, James
Assignees
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Publication Number
US-12377045-B2
Publication Date
2025-08-05
Expiration Date
Abstract
This application discloses oral liquid formulations of lipid/cholesterol-lowering drugs and blood pressure-lowering drugs, and combinations thereof, comprising surfactant(s) as stabilizer(s), which forms micelles with the drug molecules to enhance their solubility and stability.
Core Innovation
The invention relates to an oral liquid formulation comprising a combination of drugs selected from ezetimibe, statins, fenofibrate, amlodipine, and specified antihypertensive agents including valsartan, candesartan, telmisartan, losartan and salts thereof. The formulation further includes about 20% to about 90% w/w of one or more non-ionic surfactants that are liquids at ambient conditions, about 0.05% to about 7.5% w/w of a co-solvent selected from an oil, glycerin, propylene glycol, polyethylene glycols that are liquids at ambient conditions, C1-C6 straight and branch monoalcohols, and combinations thereof, and water and a buffering agent.
In embodiments described in the document, ezetimibe is combined with lipid-lowering drugs such as statins and fenofibrate, and the formulation is also described with combinations that include blood pressure-lowering drugs such as amlodipine and agents selected from ACE inhibitors, ARBs, and CCBs. The use of non-aqueous solubilizing excipients is described as forming micelles or microemulsions to enhance solubility and absorption, while also supporting stability.
The document further describes illustrative examples of oral liquid formulations with maintained physical and analytical performance, including stability at ambient conditions. An ambient stability study is reported as maintaining assay and pH, and an example formulation is described with dispersibility and droplet/zeta potential characterization.
Claims Coverage
The independent claim covers an oral liquid formulation containing a specified combination of lipid-lowering and blood-pressure-lowering drugs, together with defined amounts of non-ionic surfactants, a liquid co-solvent, buffering agent, and water, with drug-specific concentration limits. The independent claim includes five main inventive features.
Drug combination selected from listed lipid and cardiovascular agents
The formulation comprises a combination of drugs selected from ezetimibe, statins, fenofibrate, amlodipine, valsartan, candesartan, telmisartan, losartan and salts thereof, with amounts defined such that if present ezetimibe is present in an amount of 0.05% to 10% w/w and if present the statins, fenofibrate, amlodipine, valsartan, candesartan, telmisartan, losartan and salts thereof are present in an amount of 0.05% to 20% w/w.
Non-ionic surfactants that are liquids at ambient conditions in a defined w/w range
The formulation comprises about 20% to about 90% w/w of one or more non-ionic surfactants that are liquids at ambient conditions.
Liquid co-solvent selected from specified classes in a defined w/w range
The formulation comprises about 0.05% to about 7.5% w/w of a co-solvent selected from the group consisting of an oil, glycerin, propylene glycol, polyethylene glycols that are liquids at ambient conditions, C1-C6 straight and branch monoalcohols and combinations thereof.
Buffering agent in a defined w/w range
The formulation comprises about 0.1% to about 5% w/w of a buffering agent.
Water as the formulation base component
The formulation further comprises water in the oral liquid formulation, with the drug concentration rules applied for ezetimibe and the statins/fenofibrate/amlodipine/ARB drugs and salts thereof.
Overall, the claims focus on an oral liquid formulation defined by a combination of specified lipid- and cardiovascular drugs with defined drug concentration limits, a high fraction of non-ionic surfactants that are liquids at ambient conditions, a defined level of a specified liquid co-solvent class, a buffering agent in a defined amount range, and water.
Stated Advantages
Enhanced solubility and absorption through micelles/microemulsion formation as described in the document.
Improved stability at ambient conditions, including maintained assay and pH in an ambient stability study as described in the document.
Documented Applications
Oral liquid formulations for lipid-lowering drugs and blood-pressure-lowering drugs using the specified drug combinations and excipients as described in the document.
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