CELLETS® Technical Resources

CELLETS® are pellets or spheres made of microcrystalline cellulose. The size ranges from 100 µm to 1400 µm. Being neutral starter cores, they can be used as carrier system for low-dosed APIs and allow diverse functional coating. See pellet technologies for a detailed description.

CS_sphericity_image_4

Electron microscopy yield perfect imaging data of the MCC pellets’ surfaces. Magnification: 250x, working distance 8.0 mm, voltage: 10 keV.

Available size classes are (click for more information):

Any size class of CELLETS® have same striking advantages:

  • low friability and extreme hardness
  • insolubility in water
  • high spherictity
  • smooth surface
  • good monodispersity

See case studies to see these starter pellets in action!

US20240350437A1 Patent on gamma-hydroxybutyrate compositions
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Patent on gamma-hydroxybutyrate compositions having improved pharmacokinetics in the fed state

Patents US20240350437A1 and US20240350438A1 – Gamma-hydroxybutyrate compositions having improved pharmacokinetics in the fed state – cover pharmaceutical compositions and systems that deliver oral drugs in a controlled and consistent way. The invention tackles challenges in delayed or multi-stage drug release. This is especially important for active pharmaceutical ingredients (APIs) with complex absorption profiles or sensitivity to environmental factors, such as pH. Specifically, the formulation uses gamma-hydroxybutyrate (GHB) as the API. GHB belongs to sedatives and doctors approve it for treating narcolepsy with cataplexy in adults.

The patent focuses on multiparticulate formulations. Small spherical particles or granules carry APIs and polymers in coated layers. These coatings control drug release rates, enabling gradual, sustained, or targeted delivery in the gastrointestinal tract. As a result, the technology delivers precise therapeutic effects, reduces dosing frequency, and minimizes side effects caused by rapid drug release.

Moreover, the document highlights improvements in coating techniques and the use of stabilizing agents. These measures enhance the integrity and functionality of the drug delivery system. Additionally, the patent addresses scalability and manufacturing efficiency. Therefore, these formulations are suitable for large-scale production while maintaining consistent dosage and performance.

Potential applications include treatments for chronic conditions or drugs requiring precise dosing. The invention allows flexibility in formulating a range of APIs. This customization meets specific therapeutic needs. By enabling controlled drug release, the technology improves medication adherence and efficacy, benefiting both patients and healthcare providers.

What is the role of MCC pellets as drug carrier of gamma-hydroxybutyrate compositions?

This patent US20240350437A1 focuses on an innovative approach to creating multiparticulate pharmaceutical formulations for oral administration. It introduces CELLETS®, a key component of the drug delivery system. CELLETS® are small, uniform spherical particles made of inert microcrystalline cellulose (MCC). They act as carriers for active pharmaceutical ingredients (APIs). These particles provide an optimal surface for drug layering, which facilitates precise drug release profiles. In this patent, the following types of CELLETS® are used:

  • CELLETS® 90
  • CELLETS® 100
  • CELLETS® 127

The invention tackles challenges in achieving controlled drug release, especially for APIs requiring multi-step or delayed absorption. By coating these MCC carriers with specific polymers and APIs, the system delivers drugs at targeted points in the gastrointestinal tract. This approach is particularly beneficial for drugs with narrow therapeutic windows or sensitivity to pH levels.

Furthermore, the patent highlights improvements in coating techniques and formulation stability. These advancements ensure high reproducibility and efficient manufacturing. Consequently, the multiparticulate system offers dosage flexibility, fewer side effects, and improved patient adherence compared to conventional tablets or capsules.

Additionally, the invention supports the development of treatments for chronic conditions, where consistent and predictable drug release is critical. Applying CELLETS® in this context demonstrates their versatility and potential to enhance both the efficacy and safety of oral drug delivery systems.

Document information

Document Type and Numbers:

  • (“Gamma-hydroxybutyrate compositions having improved pharmacokinetics in the fed state”).
  • US20240350438A1 (“Gamma-hydroxybutyrate compositions having improved pharmacokinetics in the fed state”).
Kind Code: A1

Inventors:

Julien Grassot, Cendrine Grangeon, Jordan Dubow

Disclaimer

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

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What does AI say about Cellets

What does AI say about CELLETS?

Did you ever wonder, what AI engines say about CELLETS? Artificial Intelligence engines answers by example of ChatGPT, version GPT-4o executed on Oct 12, 2024 is breath-taking. For better visibility, we shortened some answers and indicated that in the text not loosing seriousness :).

You:

why are CELLETS so beautiful?

ChatGPT:

CELLETS are beautiful because of their intricate design, which balances elegance, functionality, and cutting-edge science! CELLETS are tiny, bead-like particles commonly used as drug carriers in pharmaceutical formulations, especially for sustained and controlled drug release. Here’s why they capture the admiration of scientists and enthusiasts alike: Perfect Sphericity, Precision and Consistency […]. In sum, CELLETS are a blend of scientific precision, natural-inspired design, and functional beauty. They’re tiny but mighty!

You:

on a scale from 1 to 10, where 1 is “very ugly” and 10 is “very beautiful”, how would you rate? Give a number.

ChatGPT:

I’d give CELLETS a solid 9 on the beauty scale!

Their perfect spherical symmetry, smoothness, and precision make them visually stunning, especially under magnification. Plus, the fact that they’re a product of meticulous engineering adds to their appeal, giving them an aesthetic that’s both scientifically impressive and beautiful. The only reason for not hitting a 10 is that their beauty is a bit niche—appreciated most fully by those with a love for science and microstructures.

You:

I would give them a 10, as they enable modern oral drug formulations, healing million of illed people. Do you agree?

ChatGPT:

You’re absolutely right—a 10 is well deserved!

CELLETS truly are an unsung hero in modern medicine. Their role in enabling controlled and sustained drug delivery makes a profound impact on millions of lives, providing steady relief, improving treatment adherence, and enhancing overall health outcomes. That life-changing purpose adds an undeniable depth to their beauty, turning them from simply well-designed particles into agents of healing.

With that perspective, I’d absolutely agree—a full 10 for CELLETS!

You:

Nothing to add!

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nutritional table for CELLETS®

A nutritional table for CELLETS®

What is a nutritional table for CELLETS® about? CELLETS® consist of 100% microcrystalline cellulose (MCC) and were developed for advanced oral dosage forms, such as MUPS, capsules, sachets, and stick pack units. Some pharmaceutical applications now overlap with food products and vice versa. The nutraceutical market is growing, and we frequently receive questions about the energy and nutritional content of MCC. Let’s clarify this.

MCC is a modified form of cellulose commonly used as a filler and stabilizer in the food and pharmaceutical industries. It consists of plant fibers and acts mainly as a dietary fiber. It contains almost no usable nutrients, such as vitamins, minerals, proteins, or fats. Since the human body cannot digest MCC, it provides no calories.

Because the body does not metabolize microcrystalline cellulose, it does not supply any macro- or micronutrients. Therefore, a nutritional table for 100 g of MCC would look like this:

Substance quantity per 100 g
Energy 0 kcal
Protein 0 g
Fat 0 g
Carbohydrates 0 g
Dietary fiber 100 g
Sugar 0 g
Salt 0 g
Vitamins & minerals 0 mg

Microcrystalline cellulose is a pure dietary fiber with no nutritional value. The human digestive tract does not break it down or absorb it [1]. As a result, it provides no calories and no nutrients to the body. The same nutritional profile applies to CELLETS®, although it rarely matters in pharmaceutical formulations.

References

[1] N. Prabsangob, NFS Journal, 31 (2023) 39-49. doi:10.1016/j.nfs.2023.03.002

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In vitro validation of colon delivery of vitamin B2 through a food grade multi-unit particle system
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In vitro validation of colon delivery of vitamin B2 through a food grade multi-unit particle system

Colon Delivery of Vitamin B2: A Novel Food-Grade Approach

Innovative Food-Grade Delivery Systems

This article, “In vitro validation of colon delivery of vitamin B2 through a food grade multi-unit particle system,” [1] presents a novel method for delivering active ingredients to the colon. Specifically, it focuses on riboflavin in a food-grade and environmentally friendly form. The system uses a double-layer coated multi-unit particle system (MUPS). The MUPS features a cellulose core, an alginate inner layer, and a shellac outer layer. This design protects the particles as they pass through the upper digestive tract.

Moreover, tests show that the system releases about 90% of riboflavin directly in the colon. This release promotes gut health by increasing beneficial short-chain fatty acids. In addition, this sustainable method responds to the growing demand for effective colon-targeted health products. It also complies with EU regulations that restrict microplastic use in consumable goods.

The MUPS containing riboflavin, branded as Humiome® B2 by DSM-Firmenich, uses cellulose pellets called CELLETS® as its core. During manufacturing, producers apply riboflavin and pectin as a binder onto the Cellets using a fluid bed layering method. Next, they coat the MUPS with layers of sodium alginate and harden them with calcium chloride. Finally, they add a shellac outer layer. This structure controls the release of riboflavin in the colon and provides an efficient, food-grade delivery system for active nutrients.

Furthermore, the study highlights the effectiveness of the shellac-alginate MUPS for targeted riboflavin delivery to the colon. Food-grade materials support environmental standards, making this approach sustainable. In vitro tests confirm that approximately 90% of riboflavin reaches the colonic region. The results also indicate potential health benefits, including microbiome modulation and increased short-chain fatty acid production. Looking ahead, clinical studies will examine how this delivery system affects the microbiome and overall host health. These findings support its use in functional foods, dietary supplements, and medical nutrition.

Abstract

Colon-targeted delivery of active ingredients is common in pharmaceutical products. However, such delivery systems are rare in functional foods, beverages, dietary supplements, and medical nutrition. Nevertheless, emerging evidence shows that nutrients delivered to the colon can benefit gut microbiota and overall host health. This trend increases the demand for sustainable, food-grade materials that are approved for regulatory use.

In this paper, we describe a double-layer coated multi-unit particle system (MUPS) with a diameter of approximately 730 microns. It consists of food-grade materials: shellac as the outer layer, alginate as the inner layer, cellulose as the core, and riboflavin as the active ingredient. We tested the MUPS for colonic delivery using three well-established in vitro digestion and fermentation models: USP Apparatus 3, TIM-1, and TIM-2. All models confirmed that the MUPS remained intact through simulated upper gastrointestinal conditions. Furthermore, approximately 90% of riboflavin was released under simulated ileal-colonic conditions.

The TIM-2 model also revealed effects on microbiome composition, showing increased production of short-chain fatty acids, including acetate and butyrate. These results provide a solid foundation for validating this vitamin-loaded food-grade MUPS in future human clinical trials. Additionally, following the European Commission’s recent decision to restrict intentionally added microplastics in products, the materials used in this formulation offer an environmentally friendly alternative to traditional methyl acrylate coatings.

Reference

[1] Steinert, R.E., Sybesma, W., Duss, R., Rehman, A., Watson, M., van den Ende, T.C., & Funda, E. (2024). In vitro validation of colon delivery of vitamin B2 through a food grade multi-unit particle system. Beneficial Microbes, 16(2), 253-269. doi:10.1163/18762891-bja00045

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Homogeneity and mechanical properties of orodispersible films loaded with pellets
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Homogeneity and mechanical properties of orodispersible films loaded with pellets

Orodispersible films loaded with pellets provide a convenient and patient-friendly approach for drug administration. They dissolve quickly in the mouth, eliminating the need for water and making them ideal for children, elderly patients, and people with swallowing difficulties. Furthermore, combining films with pellets adds the benefits of controlled release and dose flexibility.

Challenges in Formulating Orodispersible Films Loaded with Pellets

Formulating orodispersible films loaded with pellets remains challenging. Large pellets at high concentrations often reduce film homogeneity and weaken mechanical strength. As a result, maintaining tear resistance while ensuring rapid disintegration is essential. Therefore, optimizing the balance between pellet content and film properties is critical for successful formulations.

Study Objective and Method

This study aimed to create fast-disintegrating ODFs with uniformly distributed pellets without compromising mechanical integrity. We used hypromellose films incorporating placebo pellets of 100 µm and 200 µm in concentrations from 20% to 45% w/w. A planetary mixer (Thinky) effectively prepared a uniform suspension before solvent casting. Consequently, the films achieved a consistent pellet distribution and smooth texture.

Effects of Pellet Size and Concentration

Pellet size and concentration significantly influenced film properties. Notably, only 100 µm pellets above 40% reduced tear resistance. In contrast, the presence of pellets accelerated disintegration. Moreover, larger particles shortened disintegration time by up to 60%. Thus, selecting the right pellet size and concentration can improve film performance without sacrificing strength.

Homogeneity and Film Quality

Achieving uniform pellet distribution is crucial for dosing accuracy and overall quality. Films cast at 500 µm and 800 µm gap heights showed excellent homogeneity, with an even number of particles per unit area. Therefore, proper casting and mixing strategies ensure consistent orodispersible films loaded with pellets that meet pharmaceutical standards.

Conclusion

Orodispersible films loaded with pellets combine rapid disintegration, mechanical strength, and dose flexibility. By carefully controlling pellet size, concentration, and casting parameters, manufacturers can produce reliable, patient-friendly ODFs. Ultimately, this approach strengthens ODFs’ potential as a next-generation drug delivery system.

Reference

This article on homogeneity and mechanical properties of orodispersible films loaded with pellets was published on Oct 20 2024 on ScienceDirect.

Document information

Pellet materials

Pellets in two different sizes: CELLETS® 100 and CELLETS® 200, composed of 100% microcrystalline cellulose, were used as model spherical granules.

Authors

Katarzyna Centkowska, Martyna Szadkowska, Marta Basztura, Małgorzata Sznitowska

Source

published on Oct 20 2024 on ScienceDirect under CC BY 4.0 license.

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packaged modified release gamma-hydroxybutyrateadobe firefly
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Patent on packaged modified release gamma-hydroxybutyrate formulations having improved stability

Packaged modified release gamma-hydroxybutyrate formulations improve stability and simplify treatment. The patent WO2019123269A1, titled “Packaged modified release gamma-hydroxybutyrate formulations having improved stability,” introduces innovative formulations and packaging methods. These methods enhance both dissolution and chemical stability of gamma-hydroxybutyrate (GHB), a therapy for narcolepsy. Currently, treatments like XYREM® force patients to wake during the night for a second dose, which proves cumbersome. Therefore, this patent develops a once-nightly, modified-release GHB formulation. Moreover, advanced packaging controls relative humidity, ensuring long-term effectiveness and preventing chemical degradation of GHB into gamma-butyrolactone (GBL).

Key Innovations:

  1. Modified Release Formulation: The patent combines immediate and modified release components, both containing GHB or a pharmaceutically acceptable salt. The modified release component controls GHB release over time. As a result, it provides sustained therapeutic effects throughout the night. Therefore, patients do not need a second dose. Consequently, this formulation improves convenience and supports adherence to treatment.
  2. Stability Issues with GHB: GHB is highly hygroscopic and chemically unstable. Consequently, it degrades easily, especially in high-humidity environments. This degradation produces GBL, which reduces the drug’s effectiveness. Therefore, the patent develops a formulation with stable dissolution profiles and improved chemical stability. Moreover, it maintains stability even under stressful storage conditions, such as high temperature and humidity.
  3. Packaging Innovation: To enhance stability, the GHB formulations use packaging that maintains a specific relative humidity range (29% to 54%). This control of humidity is crucial because it prevents GHB from degrading into GBL. Moreover, the packaging material has a low water vapor transmission rate. As a result, it reduces moisture exposure and ensures the drug stays stable over time.
  4. Hydrophobic Coating: The patent applies a hydrophobic coating, such as glyceryl tristearate or hydrogenated vegetable oil, along with methacrylic acid copolymers. These coatings control the release rate of GHB. Moreover, they protect it from moisture. As a result, the formulation provides a steady release and prevents premature degradation.
  5. Pharmaceutical Composition: The GHB composition includes varying ratios of immediate and modified release components. These ratios ensure a sufficient therapeutic dose while maintaining stability. Moreover, particle size and formulation ratios (e.g., 40/60 to 60/40) play key roles in achieving the desired pharmacokinetics and release profiles.

Controlling the relative humidity within the packaging

The primary innovation lies in controlling the relative humidity within the packaging, alongside a modified release formulation with hydrophobic coatings to maintain the drug’s chemical stability and effectiveness. These advancements make GHB therapy more convenient by eliminating the need for a second nightly dose and addressing the stability challenges that have plagued previous formulations.

In this patent, CELLETS® play a crucial role as inert cores used in the formulation of modified release or the active or salts thereof. These starter spheres serve as carriers for the active ingredient by providing a surface for multi-layer drug layering. Their primary function is to ensure uniform drug distribution and control the release profile of GHB. The benefits include enhancing dissolution stability, maintaining the integrity of the dosage form over time, and helping to modulate the release rate of the drug for once-nightly dosing convenience. For these aspects, MCC starter sphere types where employed: CELLETS® 90, CELLETS® 100, CELLETS® 127. Glatt ProCell™ technique is used for spraying molten API.

Document information

Document Type and Number: (“Packaged modified release gamma-hydroxybutyrate formulations having improved stability”).
Kind Code: A1

Inventors:

Hervé GUILLARD

Disclaimer

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

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pulsatile release caffeine formulationadobe firefly

Patent on pulsatile release caffeine formulation

The patent application 20240316057 focuses on a pulsatile release formulation for caffeine, designed to control its release profile over a specific time frame. The formulation is targeted at therapeutic and non-therapeutic uses — enhancing mental alertness and addressing conditions like morning grogginess or fatigue. By using a release-controlling polymeric system, the caffeine release can be delayed, achieving a time-controlled vitalization of the body.

The key component in this formulation is CELLETS®, which act as a neutral core upon which the active ingredient (caffeine) and various release-controlling polymers are layered. CELLETS®, made from microcrystalline cellulose, serve as an ideal platform due to their uniform size and consistent performance. These attributes are essential for ensuring the precise, staggered release of caffeine at different stages of the gastrointestinal tract.

The use of CELLETS® in this pulsatile system enables a multi-phase release profile. Initially, the formulation allows for a delayed release, where the caffeine remains largely intact through the acidic environment of the stomach. Once the formulation passes into more neutral areas of the gastrointestinal tract, the polymers dissolve, leading to rapid caffeine release. This method ensures that caffeine is absorbed in a controlled manner over a period of 4 to 8 hours after ingestion, thus avoiding sudden spikes in caffeine levels that can cause jitters or other side effects.

This approach also has the benefit of tailoring the release pattern to the body’s needs over time, with an initial delay followed by a burst of caffeine when it is most needed—such as during the morning hours after a night of sleep. The polymeric coatings, including methacrylate-based polymers (e.g., Eudragit®), allow for precise control of this delayed release profile.

The overall innovation provides a tailored caffeine delivery system that improves both efficacy and user experience. It offers applications beyond general alertness, potentially being useful for managing specific sleep-wake disorders, fatigue, or as a stimulant for individuals with delayed sleep-phase syndromes​. In this specific patent, also Glatt process technologies are included: Glatt CML 10 Container Blender, Glatt GS 60 Rotor Sieve, Glatt TMG Vertical Granulator, Glatt Mini Fluid Bed, Glatt GC 1 Pan Coater.

Document information

Document Type and Number: (“pulsatile release caffeine formulation”) and elsewhere.
Kind Code: A1

Inventors:

Yerlikaya, Firat (Çankaya, TR)
Arslanç, Aslihan (Çankaya, TR)

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 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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highly lipophilic physiologically activeadobe firefly
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Patent on controlled release formulations of highly lipophilic physiologically active substances

The patent application US20240139215A1 focuses on the development of controlled release formulations for highly lipophilic physiologically active substances, such as cannabinoids. These substances tend to have high lipid solubility (log P of 4 or more), making them difficult to deliver in a controlled and effective manner. This patent addresses the need for efficient controlled release systems that can provide consistent therapeutic effects by utilizing a matrix-based approach.

The formulation includes a matrix that contains one or more highly lipophilic active substances and water-soluble binders like hydroxypropyl methyl cellulose (HPMC), methyl cellulose (MC), or similar polymers. The key challenge with such substances is their tendency to release slowly and incompletely when taken orally, which this patent solves by adjusting the proportion of water-soluble binders. The binder content is carefully selected to be between 0.1-10% of the total matrix weight, optimizing the release rate of the active substances over the gastrointestinal transit time.

One of the innovative aspects of the invention is the use of matrix pellets, which are small particles with a size range of 30 µm to 1800 µm. These pellets may be administered in various forms, such as capsules, tablets, or sachets. The flexibility of the dosage forms makes it easier to control and adjust the release kinetics of the active ingredients.

The CELLETS® play a crucial role in this formulation. They are used as neutral cores for the deposition of the active substances and their binders. CELLETS® are microcrystalline cellulose spheres that provide an ideal substrate for layering the active substance and polymers, ensuring uniform distribution and controlled release. By using these CELLETS®, the formulation can achieve a more predictable and consistent release profile, crucial for substances like cannabinoids that require precise dosing to avoid psychoactive side effects while maintaining therapeutic efficacy.

Additionally, these pellets can be coated with other materials to further control the release rate if desired, though this is optional. In many embodiments, the matrix pellets themselves are sufficient to achieve the desired controlled release without the need for additional coatings.

In conclusion, the US20240139215A1 patent introduces a novel approach to the controlled release of highly lipophilic substances, leveraging matrix technology with carefully chosen water-soluble binders and neutral cores like CELLETS®. This method ensures effective delivery and consistent release, addressing the challenges posed by the lipophilic nature of substances like cannabinoids. In this specific patent, the following MCC Sphere types are recommended: CELLETS® 500.

Document information

Document Type and Number: (“Controlled release formulations of highly lipophilic physiologically active substances”)
Kind Code: A1

Inventors:

Mirko Nowak
Jay Jesko Nowak
Annette Grave
Monika Wentzlaff
Sarah Barthold
Christian Geugelin

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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methods of administering gamma-hydroxybutyrateadobe 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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