Patent on modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics

The patent US11896572B2, titled “Modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics,” outlines a pharmaceutical formulation aimed at optimizing the release and therapeutic effectiveness of gamma-hydroxybutyrate (GHB), a drug used for narcolepsy treatment. The patent focuses on improving GHB’s pharmacokinetics by creating a modified release system that extends its action, reducing the need for frequent dosing and improving patient compliance.

The formulation includes both immediate-release and delayed-release particles, allowing for a controlled release of GHB. This combination ensures that a portion of the drug is rapidly released for quick onset, while the remaining is gradually released, providing sustained therapeutic effects over time. The goal is to provide 6 to 8 hours of sleep with just one bedtime dose.

A key aspect of the patent is the use of CELLETS® which are spherical microcrystalline cellulose particles that serve as a core for both immediate and delayed-release systems (pellet technologies). These CELLETS® are critical because they provide a stable, uniform platform for the drug’s release. For the immediate-release component, CELLETS® are coated with sodium oxybate and a binder (povidone). For the delayed-release part, CELLETS® are coated with additional polymers, such as methacrylic acid copolymers and hydrogenated vegetable oil, which control the release based on pH levels in the gastrointestinal tract. This dual-layer system ensures precise drug release timing, optimizing the treatment’s effectiveness and minimizing side effects like abrupt peaks in drug concentration.

The CELLETS® play a crucial role in maintaining particle size consistency, which is important for ensuring predictable dissolution and absorption rates, thereby enhancing the overall pharmacokinetic profile of the drug. This innovation represents an advancement over traditional formulations by offering more reliable and patient-friendly narcolepsy management. In this specific patent, the following MCC Sphere types are recommended: CELLETS® 90, CELLETS® 100 or CELLETS® 127.

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.

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This text was generated by chatGPT engine version GPT‑4o, on Oct 21, 2024. Image was generated with Adobe Firefly.