Pharmaceutical formulations for treating endometriosis, uterine fibroids, polycystic ovary syndrome or adenomyosis
Inventors
Jayanth, Jayanthy • Spence, Kevin C. • McClelland, Gregory A. • Stepanenko, Anna V. • Ju, Tzuchi R. • SHAO, XI
Assignees
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Publication Number
US-12102637-B2
Publication Date
2024-10-01
Expiration Date
Abstract
The present disclosure relates to pharmaceutical compositions comprising a gonadotropin-releasing hormone (GnRH) antagonist and methods of preparing and using such compositions. The disclosure also relates to methods of facilitating release of a GnRH antagonist from a pharmaceutical composition.
Core Innovation
The invention relates to a pharmaceutical composition comprising elagolix sodium in specified weight-percent ranges together with sodium carbonate, where the composition is in the form of a stable immediate release tablet. The tablet includes a first filler and a second filler in defined weight-percent amounts, where the first filler is mannitol and the second filler is pregelatinized starch, and each weight percentage is based on the total tablet weight.
The disclosure addresses maintaining a stable immediate release tablet pharmaceutical composition when formulating elagolix sodium with sodium carbonate and defined fillers. In one aspect, the composition further specifies a binder in an amount from about 2% to about 5% by weight and a lubricant in an amount from about 1% to about 5% by weight.
The formulation framework remains defined by elagolix sodium at about 20% to about 60% by weight, sodium carbonate at about 10% to about 30% by weight, mannitol as the first filler at about 20% to about 50% by weight, and pregelatinized starch as the second filler at about 1% to about 20% by weight. The disclosed material further reports stability-focused composition language and formulation and stability characterization context.
Claims Coverage
The independent claims provide formulation coverage for a stable immediate release tablet pharmaceutical composition. Across the two independent claims, the main inventive features are the defined excipient system and, for the second independent claim, defined binder and lubricant ranges.
Stable immediate release tablet with defined elagolix sodium, sodium carbonate, and filler system
A pharmaceutical composition comprising from about 20 to about 60% by weight of elagolix sodium, from about 10 to about 30% by weight of sodium carbonate, a first filler in an amount from about 20% to about 50% by weight and a second filler in an amount from about 1% to about 20% by weight, wherein the first filler is mannitol and the second filler is pregelatinized starch, wherein each weight percentage is on the basis of the total weight of the pharmaceutical composition, and wherein said composition is in the form of a stable immediate release tablet.
Stable immediate release tablet with defined elagolix sodium, sodium carbonate, fillers, binder, and lubricant
A pharmaceutical composition comprising from about 20 to about 60% by weight of elagolix sodium, from about 10 to about 30% by weight of sodium carbonate, a first filler in an amount from about 20% to about 50% by weight and a second filler in an amount from about 1% to about 20% by weight, wherein the first filler is mannitol and the second filler is pregelatinized starch, a binder in an amount from about 2 to about 5% by weight, and a lubricant in an amount from about 1 to about 5% by weight, wherein each weight percentage is on the basis of the total weight of the pharmaceutical composition, and wherein said composition is in the form of a stable immediate release tablet.
Claim coverage centers on stable immediate release tablet formulations that combine elagolix sodium with sodium carbonate and a specific two-filler system of mannitol and pregelatinized starch. Additional coverage in the second independent claim includes defined ranges for a binder and lubricant while keeping the same core immediate release tablet excipient framework.
Stated Advantages
Stability of the immediate release tablet pharmaceutical composition.
Reduces gel formation of the elagolix sodium monosodium salt.
Suppresses formation of the lactam degradation product, Compound B.
Provides dissolution advantages, including faster release.
Maintains dissolution similarity after storage up to about 24 months.
Reduces Compound B to below specified weight percentages under defined storage conditions.
Achieves hormone suppression outcomes, including rapid LH/FSH and estradiol suppression.
Documented Applications
Dose-dependent suppression of estradiol in premenopausal women with endometriosis-associated pain following treatment with elagolix tablets.
Treating endometriosis.
Treating uterine fibroids (leiomyomas).
Treating PCOS.
Treating adenomyosis.
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