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Publication Number
US-10953018-B2
Publication Date
2021-03-23
Expiration Date
Abstract
Disclosed herein are novel pharmaceutical formulations of aprepitant suitable for parenteral administration including intravenous administration. Also included are formulations including both aprepitant and dexamethasone sodium phosphate. The pharmaceutical formulations are stable oil-in-water emulsions for non-oral treatment of emesis and are particularly useful for treatment of subjects undergoing highly emetogenic cancer chemotherapy.
Core Innovation
The invention relates to physically stable oil-in-water emulsion formulations comprising aprepitant for intravenous and/or parenteral administration. The compositions include aprepitant together with an emulsifier, an oil, and water, and are described as stable emulsions suitable for use as pharmaceutical compositions.
The formulations emphasize physical stability criteria including submicron droplet size and a limited amount of large fat globules, with stability assessed using USP <729> aligned criteria. Physical stability is described together with chemical stability maintained by controlling the composition pH using pH adjustment and/or buffering agents.
The patent content further describes embodiments that optionally include dexamethasone or dexamethasone sodium phosphate in addition to aprepitant. Representative formulation examples and results are provided, including measured droplet size and pH values and stability outcomes, including freeze-thaw stability results.
Claims Coverage
The partial content provides one independent claim directed to a method of treating nausea and vomiting using a physically stable aprepitant emulsion with specified wt/wt weight ratios. The dependent claims refine this independent claim by specifying routes, quantitative composition constraints, and optional/formulation details.
Physically stable aprepitant oil-in-water emulsion for nausea and vomiting treatment
A method for treating nausea and vomiting comprising administering a physically stable pharmaceutical composition that is an emulsion comprising aprepitant, an emulsifier, an oil, and water.
Specified emulsifier-to-aprepitant weight ratio
The ratio of the emulsifier to aprepitant (wt %:wt %) ranges from about 18:1 to 22:1.
Specified oil-to-aprepitant weight ratio
The ratio of the oil to aprepitant (wt %:wt %) ranges from about 11:1 to 15:1.
Formulation constrained by pH range
The composition has a pH that ranges from 7.5 to 9.0.
Intravenous administration
Administering the composition intravenously.
Overall, the claim coverage centers on administering a physically stable aprepitant emulsion with defined emulsifier-to-aprepitant and oil-to-aprepitant weight ratios, together with dependent refinements including a specified pH range and intravenous administration.
Stated Advantages
Prolonged shelf life.
Reduced toxicity (non-detergent).
Documented Applications
Treating nausea and vomiting in a subject in need thereof using a physically stable pharmaceutical composition comprising aprepitant as an emulsion.
Intravenous and/or parenteral use of physically stable aprepitant oil-in-water emulsion formulations.
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