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Modified release Gamma-Hydroxybutyrateadobe firefly
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Patent on modified-release Gamma-Hydroxybutyrate formulations having improved pharmacokinetics

The patent application titled “Modified Release Gamma-Hydroxybutyrate (GHB) Formulations Having Improved Pharmacokinetics” (US20240148685) focuses on improving the delivery of GHB, a substance used for treating sleep disorders like narcolepsy, through modified-release formulations. The goal is to optimize GHB’s absorption, enhancing patient convenience and compliance by reducing the need for multiple nightly doses.

The key innovation in the patent is the use of CELLETS®, microcrystalline spheres often employed as a neutral core for drug layering. In this application, CELLETS® act as carriers for the active ingredient, allowing precise control over the release profile of GHB. These small spherical particles, made from microcrystalline cellulose, offer uniform size and high mechanical strength, ensuring consistent drug loading and a controlled release rate.

In this patent, the CELLETS® are coated with various layers of GHB and release-modifying agents, enabling a predictable and sustained release of the active substance. This modified release profile allows GHB to be administered in a once-nightly dose rather than requiring the patient to wake up for a second dose, which was a limitation with previous immediate-release formulations. This extended-release mechanism helps maintain stable plasma concentrations of GHB over an 8-hour period, improving both the efficacy of the treatment and patient compliance.

The innovation emphasizes addressing the shortcomings of existing GHB formulations by ensuring a better pharmacokinetic profile—particularly regarding absorption, bioavailability, and minimizing drug levels in the bloodstream after the therapeutic effect has been achieved. In this specific patent, the following MCC Sphere types are recommended: CELLETS® 90, CELLETS® 100, CELLETS® 127.

Document information

Document Type and Number: (“Modified release Gamma-Hydroxybutyrate formulations having improved pharmacokinetics”)
Kind Code: A1

Inventors:

Dubow, Jordan (Lyon, FR)
Guillard, Hervé (Villeurbanne, FR)
Mégret, Claire (Lyon, FR)
Dubuisson, Jean-françois (Lyon, FR)

Disclaimer

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

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Patent on methods of administering gamma-hydroxybutyrate compositions with divalproex sodium

The United States Patent Application US20240024263 focuses on methods of administering gamma-hydroxybutyrate (GHB) in combination with divalproex sodium (DVP), particularly for treating conditions like narcolepsy. The aim is to co-administer these drugs without altering their dosage or efficacy. The patent emphasizes how DVP affects GHB’s pharmacokinetics, allowing adjustments to minimize side effects while ensuring therapeutic benefits.

The role of CELLETS® in this patent is critical. CELLETS® are microcrystalline cellulose spheres used in drug formulations. They provide a stable, controlled-release matrix for GHB, ensuring consistent drug delivery over time. This controlled release minimizes fluctuations in drug concentrations, improving safety and efficacy. These MCC starter beads also help prevent interaction between GHB and DVP, ensuring that neither drug’s therapeutic effects are compromised.

By using CELLETS®, the formulation enhances the pharmacokinetic profile of GHB, ensuring a smoother and more predictable drug release. This innovation is crucial when GHB is administered alongside DVP, as it allows for better management of conditions like excessive daytime sleepiness or cataplexy, without significantly altering either drug’s profile.

In summary, this patent introduces an optimized co-administration strategy for GHB and DVP, with Cellets playing a pivotal role in achieving steady, controlled drug release and mitigating adverse drug interactions. This approach aims to improve the overall effectiveness and safety of treatment for sleep-related disorders. In this specific patent, the following MCC Sphere types are recommended: CELLETS® 90, CELLETS® 100 or CELLETS® 127. United States Patent Application US20240024263 seems as well to be a patent following the patent US11896572B2 wherein modified-release formulations are described.

Document information

Document Type and Number: (“Methods of administering gamma-hydroxybutyrate compositions with divalproex sodium”)
Kind Code: A1

Inventors:

Baek, Bong-Sook, Flamel Ireland Limited (Dublin, IE)

Disclaimer

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

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Modified release gamma-hydroxybutyrateadobe firefly
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Patent on modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics

The development of modified release gamma-hydroxybutyrate represents a major advancement in narcolepsy therapy, aiming to improve both patient compliance and treatment effectiveness. Traditional formulations of gamma-hydroxybutyrate (GHB) require multiple nightly doses, which can disrupt sleep and reduce overall quality of life. The patented formulation described in US11896572B2 introduces a novel modified release system that extends the duration of action, making it possible to achieve 6 to 8 hours of therapeutic benefit with a single bedtime dose.

How Modified Release Gamma-Hydroxybutyrate Works

This formulation combines immediate-release and delayed-release mechanisms to provide both rapid onset and sustained therapeutic effects. The immediate-release portion allows GHB to take effect quickly, while the delayed-release portion maintains drug levels over time, reducing abrupt concentration peaks and minimizing side effects. This dual-action delivery is designed to improve pharmacokinetics and ensure more consistent symptom control.

The Role of CELLETS® in Modified Release Gamma-Hydroxybutyrate Drug Release

A central innovation in this patent involves the use of CELLETS®, spherical microcrystalline cellulose particles that provide a stable foundation for modified release drug delivery. In the immediate-release portion, CELLETS® carry a coating of sodium oxybate combined with a binder such as povidone. Meanwhile, the delayed-release portion relies on specialized polymers and hydrogenated vegetable oil, which work together to control pH-dependent release in the gastrointestinal tract. Furthermore, CELLETS® maintain consistent particle size and predictable dissolution rates, which in turn improve absorption and strengthen the overall pharmacokinetic profile of modified release gamma-hydroxybutyrate.

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. This specific patent, recommend the following MCC Sphere types: CELLETS® 90, CELLETS® 100 or CELLETS® 127.

Advantages for Narcolepsy Patients

The patented system combines immediate and delayed release. This design allows for a once-nightly dose, which improves adherence and convenience for patients. The innovation also ensures more restorative sleep. At the same time, it reduces the burden of frequent dosing. As a result, narcolepsy management becomes more reliable and patient-friendly.

By refining the pharmacokinetics of GHB, modified release gamma-hydroxybutyrate offers a significant improvement over traditional formulations.

Document information

Document Type and Number: (“modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics”)
Kind Code: B2

Inventors:

Jordan Dubow
Hervé Guillard
Claire Mégret
Jean-François DUBUISSON

Disclaimer

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

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