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Publication Number
US-11672781-B2
Publication Date
2023-06-13
Expiration Date
Abstract
The invention provides a pharmaceutical composition comprising sodium lauryl sulfate, hydroxypropyl methylcellulose (HPMC), a copolymer of vinylpyrrolidone and vinyl acetate, and a therapeutically effective amount of metaxalone or a pharmaceutically acceptable salt thereof. Related processes and methods are also disclosed.
Core Innovation
Metaxalone is described as having poor solubility and a food effect. The disclosed approach provides a pharmaceutical composition comprising metaxalone, or a pharmaceutically acceptable salt thereof, together with sodium lauryl sulfate, hydroxypropyl methylcellulose (HPMC), and a copolymer of vinylpyrrolidone and vinyl acetate.
The composition is defined by specific weight percentage ranges for metaxalone, sodium lauryl sulfate, HPMC, and the copolymer of vinylpyrrolidone and vinyl acetate. The copolymer can be defined by formula (I) including repeating-unit parameters (n and m).
Embodiments are described as oral solid dosage forms, including spray-dried amorphous dispersion compositions, such as tablets and capsules. Solid-state stability is assessed by XRPD after accelerated storage, dissolution performance is evaluated in 0.1 N HCl and FaSSGF, and in-vivo dog and human studies use pharmacokinetic parameters including Cmax, Tmax, and AUC.
Claims Coverage
The document contains one independent claim directed to a specific pharmaceutical composition defined by quantitative weight-percent ranges for metaxalone, sodium lauryl sulfate, HPMC, and a vinylpyrrolidone/vinyl acetate copolymer, with dependent claims refining formulation parameters and dosage-form or performance aspects.
Specific pharmaceutical composition wt% formulation
A pharmaceutical composition comprising metaxalone or a pharmaceutically acceptable salt thereof, sodium lauryl sulfate, hydroxypropyl methylcellulose (HPMC), and copolymer of vinylpyrrolidone and vinyl acetate, each in specified weight-percent ranges.
Copolymer defined by formula parameter bounds
The copolymer of vinylpyrrolidone and vinyl acetate is defined by formula (I) with repeating-unit parameters n and m.
Spray-dried amorphous dispersion composition form
A pharmaceutical composition is provided in the form of a spray-dried amorphous dispersion.
Improved solubility, bioavailability, and pharmacokinetic parameters
A pharmaceutical composition improves solubility, bioavailability, and Cmax and/or Tmax compared to metaxalone compositions not formulated with sodium lauryl sulfate, HPMC, and a copolymer of vinylpyrrolidone and vinyl acetate.
Method of treating musculoskeletal pain or condition
A method for treating musculoskeletal pain or a musculoskeletal condition by administering the pharmaceutical composition to a patient in need thereof.
Overall, the claim coverage centers on a metaxalone formulation combining sodium lauryl sulfate, HPMC, and a vinylpyrrolidone/vinyl acetate copolymer at specified weight-percent ranges, with refinements that define copolymer parameters and narrow to spray-dried amorphous dispersion dosage forms, and with comparative performance language tied to solubility, bioavailability, and Cmax/Tmax improvements, as well as a related patient-treatment method.
Stated Advantages
Improves solubility.
Improves bioavailability.
Improves pharmacokinetic exposure as indicated by Cmax and/or Tmax.
Documented Applications
Treating musculoskeletal pain or a musculoskeletal condition by administering the claimed pharmaceutical composition to a patient in need thereof.
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