Pharmaceutical composition containing brexanolone, ganaxolone, or zuranolone, and use thereof
Inventors
Strickley, Robert G. • Xu, Lianhong • Hong, Zhi
Assignees
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Publication Number
US-12370200-B2
Publication Date
2025-07-29
Expiration Date
Abstract
Disclosed herein is a pharmaceutical composition comprising a pharmaceutically effective amount of a neuroactive steroid that is a positive modulator of γ aminobutyric acid type A (GABAA) receptors. Also disclosed are methods of treating diseases using the pharmaceutical composition and processes of producing the pharmaceutical composition.
Core Innovation
The invention relates to pharmaceutical compositions of neuroactive steroids comprising brexanolone for treating central nervous system (CNS) disorders. The compositions include brexanolone characterized as brexanolone polymorph Form A, with XRPD diffractogram peaks as specified, and the compositions define performance after administration by intramuscular or subcutaneous injection using pharmacokinetic criteria.
A problem addressed by the invention is the provision of a brexanolone pharmaceutical composition that delivers a desired pharmacokinetic profile after a single intramuscular or subcutaneous dose. In particular, the composition provides a maximum plasma concentration (Cmax) in about 30 minutes to about 6 hours and maintains a plasma concentration of brexanolone of more than about 5% of Cmax for at least about 5 days after injection.
The disclosure further describes controlled-release behavior using particle-based formulation, with particle populations formed as large particles and small particles. The particle populations are characterized by bimodal particle sizes and a defined ratio of small to large particles by weight, and the formulation includes excipient options and exclusions, including compositions substantially free of cyclodextrins and exclusions of sulfobutyl ether β-cyclodextrin.
Claims Coverage
The provided independent claim content identifies two inventive feature groups.
Brexanolone polymorph Form A XRPD peak characterization
A pharmaceutical composition comprising brexanolone wherein brexanolone is brexanolone polymorph Form A characterized by having at least three peaks selected from the specified XRPD 2θ values.
Single-dose IM/SC pharmacokinetics with prolonged plasma concentration
A pharmaceutical composition wherein a single dose by intramuscular or subcutaneous injection provides a Cmax in about 30 minutes to about 6 hours and maintains plasma concentration of brexanolone of more than about 5% of Cmax for at least about 5 days after injection.
The claimed invention is defined by brexanolone polymorph Form A XRPD peak characteristics and by a specific pharmacokinetic profile after a single intramuscular or subcutaneous injection.
Stated Advantages
Provides a maximum plasma concentration (Cmax) in about 30 minutes to about 6 hours after a single intramuscular or subcutaneous injection.
Maintains plasma concentration of brexanolone of more than about 5% of Cmax for at least about 5 days after the injection.
Documented Applications
Treatment of central nervous system (CNS) disorders using brexanolone pharmaceutical compositions, including postpartum depression and epilepsy-related disorders.
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