Patent on extended release compositions comprising pyridostigmine

The following patent on “Extended release compositions comprising pyridostigmine” employs CELLETS® as starter spheres made of Microcrystalline Cellulose. Please, read a summary below.

CELLETS

Microcrystalline cellulose pellets (Cellets) are highly spherical starter pellets consisting of 100 % microcrystalline cellulose in sizes between 100 µm and 1,400 µm.

They act as neutral starter cores and as multiparticulate carriers in extended release formulations of highly active or low concentrated API.

Chemical inertness, high friability, high sphericity and smooth surface properties are key advantages for easy and reliable drug delivery formulations.

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.

Product Information

Product, standard sizes	Size
Cellets 100	100-200 µm
Cellets 200	200-355 µm
Cellets 350	350-500 µm
Cellets 500	500-710 µm
Cellets 700	700-1000 µm
Cellets 1000	1000-1400 µm

Source: ingredientpharm, Patent on extended release compositions comprising pyridostigmine, https://cellets.com/portfolio-item/cellets/

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