Patent on extended release compositions comprising pyridostigmine

US Patent 20240299305 addresses an extended-release formulation of pyridostigmine, a drug primarily used to treat myasthenia gravis (MG). The goal of the patent is to create a dosage form that prolongs the drug’s therapeutic effects while minimizing side effects like dose dumping (a rapid release of the drug that can cause adverse effects). The patent describes a gastroretentive drug delivery system, designed to float and remain in the stomach for a longer time, thereby ensuring gradual release and absorption.

A key aspect of this patent is the use of CELLETS®, which are small, inert core particles used as carriers in pharmaceutical formulations. These CELLETS® serve as a starter sphere for the extended-release composition, being coated with layers of active ingredients like pyridostigmine and other substances that control the drug’s release rate. The formulation is intended to provide a controlled, steady release of pyridostigmine, improving patient outcomes by maintaining a stable plasma concentration of the drug for up to 24 hours.

The dosage form also incorporates components like a gas-generating agent, which enables the tablet to float in the stomach, and a water-soluble hydrophilic polymer that swells upon contact with gastric fluids, preventing the tablet from passing through the digestive system too quickly. This gastroretentive property is vital to ensure that the drug stays in the stomach long enough to achieve the desired extended release.

By utilizing CELLETS® and other advanced components, the patent aims to reduce the frequency of administration (allowing for once-daily dosing) and improve patient compliance, which is especially important for MG patients who need consistent, long-term management of their symptoms.