Methods and compositions for preventing and relieving muscle cramps and for recovery from neuromuscular irritability and fatigue following exercise

Inventors

Bean, Bruce P.MacKinnon, DonaldMacKinnon, Roderick

Assignees

Cliff-Cartwright CorpSalarius Pharmaceuticals Inc

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Publication Number

US-9937135-B2

Patent

Publication Date

2018-04-10

Expiration Date


Abstract

Described herein are compositions comprising capsaicin and methods of treating muscle cramping in a subject, comprising orally administering to the subject a composition comprising capsaicin and an excipient.

Core Innovation

The invention relates to oral comestible compositions, including beverages, that include channel-activating agents for use in preventing and relieving muscle cramps and accelerating nerve-muscle recovery after exercise. The compositions are described with mechanistic rationale involving gastroesophageal sensory neurons and TRP/ASIC channels associated with neuromuscular irritability and exercise fatigue.

The channel-activating agents include TRPV1 activators and TRPA1 activators, including capsaicin and capsaicinoids, cinnamaldehyde and cinnamon oil, and gingerols. The compositions optionally further include ASIC activators implemented via low pH using acidulants such as acetic acid, phosphoric acid, citric acid, and related acids, together with excipients.

The disclosure includes formulations with excipients such as sweeteners, electrolytes, and viscosity modifiers like gums and starches, and it specifies concentration ranges for the active agents. Human and in vitro findings are described, including electromyography outcomes showing rapid and sustained cramp reduction after ingestion of a TRP-Stim beverage and in vitro rat trigeminal neuron activation with synergistic effects from capsicum and ginger extracts.

Claims Coverage

The independent claim defines a specific beverage composition containing capsaicin, cinnamaldehyde, and a gingerol, with required w/w or mg/mL concentration ranges, plus an excipient. The independent claim set covers inventive features focused on the combination of three channel-activating agents and their defined concentration constraints, with dependent claims further narrowing the excipient and optional formulation aspects.

Combination beverage with capsaicin, cinnamaldehyde, and a gingerol

A beverage comprising capsaicin, cinnamaldehyde, a gingerol, and an excipient.

Capsaicinoid concentration constraints

The beverage comprises 0.001% to 1% weight/weight (w/w) capsaicinoids per weight of beverage or 0.0001-0.01 mgs of total capsaicinoids/mL of beverage.

Gingerol concentration constraints

The beverage comprises a total of 0.001% to 1% weight/weight (w/w) of a gingerol per weight of the beverage.

Packaging volume for the unit container

The beverage is bottled or packaged in a unit containing between 10 mL and 1000 mL of the beverage.

Electrolyte excipient

The beverage further comprises an electrolyte.

Excipient selected from specified gums and starches and gum arabic

An excipient is selected from gums and starches including gellan gum, carob bean gum, carrageenan, alginates, agar, guar gum, xanthan gum, carboxymethyl cellulose, clear starch, pectin, gelatin, and specified starches, and gum arabic.

Overall claim coverage centers on a beverage that combines capsaicin, cinnamaldehyde, and a gingerol in specified concentration ranges, together with an excipient. Dependent coverage further specifies optional formulation elements such as electrolyte inclusion and defined excipient classes, and adds a unit packaging volume constraint.

Stated Advantages

Rapid and sustained cramp reduction after ingestion of a TRP-Stim beverage.

Prevention and relief of muscle cramps.

Accelerating nerve-muscle recovery after exercise.

Documented Applications

Preventing and relieving muscle cramps and accelerating nerve-muscle recovery after exercise using an oral comestible composition, including a beverage, containing TRP/ASIC channel-activating agents.

Use of a TRP-Stim beverage evaluated with electromyography outcomes for rapid and sustained cramp reduction.

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