US20240350420A1 methods for treating hyperhidrosis
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Patent on pharmaceutical compositions and methods for treating hyperhidrosis

The patent application US20240350420A1 focuses on pharmaceutical formulations and methods for treating conditions such as hyperhidrosis, which causes excessive sweating. It details the development of modified-release compositions using Pilocarpine HCl, a muscarinic agonist. These formulations aim to optimize drug delivery by using various release mechanisms, including immediate, delayed, or sustained release. Notably, the innovations include encapsulation techniques with polymer coatings. These coatings control dissolution rates under different conditions, ensuring stable and effective drug delivery over time.

Moreover, the application highlights formulations that combine Pilocarpine with other agents, such as Oxybutynin, to boost therapeutic efficacy. It also examines dissolution profiles under varying environmental conditions, emphasizing stability and performance consistency. Consequently, this approach seeks to improve patient outcomes by tailoring release profiles to specific medical needs. Additionally, it minimizes side effects through controlled drug exposure.

Why CELLETS® are important in these methods for treating hyperhidrosis

CELLETS® are microcrystalline cellulose spheres. They serve as an essential component in drug delivery systems designed for controlled and extended release of active pharmaceutical ingredients (API). These spheres act as inert core substrates, providing a uniform and stable base for layering active compounds and functional polymers. In addition, their consistent size and smooth surface allow precise and even distribution of coatings, which is critical for predictable drug release kinetics.

Cellets form the crucial base for formulations that rely on pellet technologies. These formulations improve the pharmacokinetic profile of APIs, especially highly lipophilic drugs, by controlling their release rate. By coating excipients and API, multi-layer systems on these cores enable gradual drug dissolution. This process reduces fluctuations in plasma drug levels and minimizes side effects. For example, in a Pilocarpine HCl formulation, coating CELLETS® with suitable excipients allows extended drug release. This maintains therapeutic concentrations longer and improves patient compliance by reducing dosing frequency.

Moreover, their flexibility allows use across various dosage forms, such as capsules, compressed tablets, or even gel-like forms. Additionally, the uniformity of these MCC starter beads ensures each pellet delivers a controlled dose of the active ingredient. Therefore, they are integral to achieving consistent therapeutic outcomes in complex drug delivery systems.

The function of Pilocarpine HCl

Pilocarpine HCl is a cholinergic agonist. It stimulates muscarinic receptors, increasing secretion production and smooth muscle contraction. Primarily, it treats glaucoma in ophthalmology by reducing intraocular pressure. This effect occurs through enhanced aqueous humor outflow. Additionally, it manages xerostomia (dry mouth) caused by conditions like Sjögren’s syndrome or radiation therapy for head and neck cancers. Its parasympathomimetic action stimulates saliva production and improves symptoms.

Document information

Document Type and Number: (“Pharmaceutical compositions and methods for treating hyperhidrosis”).

Kind Code: A1

Inventors:

Stephen Wayne Andrews, Samuel Bruce Balik, John Edward Jett, Robert Michael LEMING

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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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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