Composition and method for treating metabolic disorders

Inventors

Cincotta, Anthony H.

Assignees

Veroscience LLC

Abstract

Bromocriptine citrate administered to a vertebrate, animal or human, can be used for any purpose including, e.g., the long-term modification and regulation of metabolic disorders, including prediabetes, obesity, insulin resistance, hyperinsulinemia, hyperglycemia and type 2 diabetes mellitus (T2DM) and/or, e.g., the treatment of other medical disorder(s) including immune or endocrine disorders or diseases. Bromocriptine citrate is administered over a limited or extended period at a time of day dependent on re-establishing the normal circadian rhythm of central dopaminergic activity of healthy members of a similar species and sex. Insulin resistance, hyperinsulinemia and hyperglycemia, T2DM, prediabetes, MS or all, can be controlled in humans on a long term basis by such treatment inasmuch as the daily administration of bromocriptine citrate resets neuronal activity timing in the neural centers of the brain to produce long term effects.

Core Innovation

The disclosed invention provides pharmaceutical dosage forms comprising bromocriptine citrate, wherein the bromocriptine citrate has greater water solubility and improved stability compared to bromocriptine mesylate. The document emphasizes that this solubility and stability improvement supports better dissolution and increased water-related performance of the bromocriptine citrate formulation relative to bromocriptine mesylate.

The invention further includes dosage forms with timed dosing regimens for treating metabolic disorders by resetting central circadian rhythm of dopaminergic activity. The described metabolic disorders include type 2 diabetes mellitus (T2DM), prediabetes, obesity, insulin resistance, hyperinsulinemia, hyperglycemia, and metabolic syndrome (MS).

The disclosed dosage forms encompass oral/sublingual and parenteral options and include pharmaceutically acceptable excipients such as low moisture filler (anhydrous corn starch), water-scavenging agent (silicon dioxide), and excipients that influence release, including release-controlling agent (hydroxypropylmethyl cellulose), disintegrating agent, and other excipients such as citric acid, permeation enhancers, and bioadhesives. The document also describes comparative solubility and stability testing of bromocriptine citrate versus bromocriptine mesylate and reports accelerated storage evaluation under specified pH and aqueous conditions.

Claims Coverage

The partial content identifies four independent claims that collectively cover bromocriptine citrate-based pharmaceutical dosage forms with greater water solubility and/or improved stability compared to bromocriptine mesylate, including parenteral embodiments and pharmaceutically acceptable excipients.

Across the independent claims, the core claimed scope is centered on bromocriptine citrate-based pharmaceutical dosage forms that exhibit greater water solubility and/or improved stability compared to bromocriptine mesylate, with additional coverage of parenteral embodiments and inclusion of pharmaceutically acceptable excipients.

Stated Advantages

Documented Applications