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.
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):
CELLETS® 100
CELLETS® 200
CELLETS® 350
CELLETS® 500
CELLETS® 700
CELLETS® 1000
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!
Over the past few weeks, we have explored the fascinating world of patents related to controlled and modified drug release through our eight-part blog series. This journey has taken us from the extended release of pyridostigmine and atomoxetine to the innovative formulations of gamma-hydroxybutyrate. 🚀💊
Each entry provided valuable insights into the advancements in Cellets technology and its impact on drug administration. We examined how highly lipophilic physiologically active substances and pulsatile release mechanisms are poised to revolutionize therapeutic approaches. 🌟
The insights gained from this series underscore the importance of these technologies in enhancing patient outcomes. Not only do they improve compliance, but they also enable targeted therapies tailored to the unique needs of each patient.
Here’s a recap of the blog posts featured in the series:
We extend our heartfelt gratitude to everyone who has accompanied us on this enlightening journey. We look forward to sharing more insights and innovations in the field of drug development in the future. Stay tuned for our upcoming content and follow us on LinkedIn! 📅✨
https://cellets.com/wp-content/uploads/2024/10/Firefly-Firefly-create-a-picture-in-which-shows-a-pharmaceutical-laboratory.-There-are-people-of-dif-6.jpg512512Bastian Arlthttps://cellets.com/wp-content/uploads/2016/10/Logo_Cellets_2016_website.pngBastian Arlt2025-01-07 11:19:492025-01-07 11:21:57Conclusion of the Blog Series: Innovations in Controlled Drug Release
The patent application US20240350420A1 focuses on pharmaceutical formulations and methods for treating conditions such as hyperhidrosis, which involves excessive sweating. The document details the development of modified-release compositions, specifically utilizing Pilocarpine HCl, a muscarinic agonist. These formulations aim to optimize drug delivery by employing various release mechanisms, including immediate, delayed, or sustained release. The innovations include encapsulation techniques using polymer coatings to control dissolution rates under different conditions, ensuring stable and effective drug delivery over time.
Additionally, the application highlights formulations combining Pilocarpine with other agents like Oxybutynin to enhance therapeutic efficacy. The study of dissolution profiles under varying environmental conditions further underscores the emphasis on stability and performance consistency. This approach is designed to improve patient outcomes by tailoring release profiles to meet specific medical needs while minimizing side effects through controlled drug exposure.
Why CELLETS® are important in these methods for treating hyperhidrosis
CELLETS® are microcrystalline cellulose spheres, serving 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 the active compounds and functional polymers. Their consistent size and smooth surface allow precise and even distribution of coatings, which is critical for achieving predictable drug release kinetics.
Cellets are the crucial base for formulations relying on pellet technologies. These powerful formulations for oral drug uptake allow improving the pharmacokinetic profile of APIs, especially highly lipophilic drugs, by controlling their release rate. By coating excipients and API, multi-layer systems created on these cores allow gradual drug dissolution, reducing fluctuations in drug plasma levels and minimizing side effects. For example, in this patent of a Pilocarpine HCl formulation, coating CELLETS® with siutable excipients enable extended drug release, maintaining therapeutic concentrations for longer durations and improving patient compliance by reducing dosing frequency.
Their flexibility in application allows them to be used across various dosage forms, such as capsules or compressed tablets and even gel-like dosage forms. Additionally, the uniformity of these MCC starter beads ensures that each pellet provides a controlled dose of the active ingredient, making them integral to achieving consistent therapeutic outcomes in complex drug delivery systems.
The function of Pilocarpine HCl
Pilocarpine HCl is a cholinergic agonist that stimulates muscarinic receptors to increase secretion production and smooth muscle contraction. It is primarily used in ophthalmology to treat glaucoma by reducing intraocular pressure through enhanced aqueous humor outflow. Additionally, it is used in managing xerostomia (dry mouth) caused by conditions like Sjögren’s syndrome or following radiation therapy for head and neck cancers. Its parasympathomimetic action helps stimulate saliva production and improve 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.
https://cellets.com/wp-content/uploads/2024/11/US20240350420A1-treating-hyperhidrosis.jpg512512Bastian Arlthttps://cellets.com/wp-content/uploads/2016/10/Logo_Cellets_2016_website.pngBastian Arlt2024-11-21 18:49:002024-11-21 19:03:13Patent on pharmaceutical compositions and methods for treating hyperhidrosis
Patents US20240350437A1 and US20240350438A1 – Gamma-hydroxybutyrate compositions having improved pharmacokinetics in the fed state – Google Patents relates to pharmaceutical compositions and systems designed to provide controlled and consistent drug release for oral administration. The invention addresses challenges associated with delayed or multi-stage drug delivery, particularly for active pharmaceutical ingredients (APIs) with complex absorption profiles or sensitivity to environmental factors like pH. More specifically, gamma-hydroxybutyrate (GHB) is employed as API. GHB is a drug from the group of sedatives that is approved for the treatment of narcolepsy with cataplexy in adults.
The core of the patent involves multiparticulate formulations, in which small spherical particles or granules are coated with APIs and polymers. These coatings are designed to modulate drug release rates, enabling gradual, sustained, or targeted delivery in the gastrointestinal tract. This technology is particularly useful for achieving precise therapeutic effects, minimizing dosing frequency, and reducing potential side effects caused by rapid drug release.
The document highlights advancements in coating techniques and the use of stabilizing agents to improve the integrity and functionality of the drug delivery system. It also discusses scalability and manufacturing efficiency, making these formulations suitable for large-scale production while maintaining consistency in dosage and performance.
Potential applications include treatments for chronic conditions or drugs that require precise dosing regimens. The invention provides flexibility in formulating for a range of APIs, allowing for customization to meet specific therapeutic needs. By enabling controlled drug release, the technology enhances 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 designed for oral administration. The patent introduces CELLETS® which are a key component of the drug delivery system. CELLETS® are small, uniform spherical particles made of inert microcrystalline cellulose (MCC), that act as carriers for active pharmaceutical ingredients (APIs). These particles provide an optimal surface for drug layering, facilitating precise drug release profiles. In this patent, these types of CELLETS® are applicable:
CELLETS® 90
CELLETS® 100
CELLETS® 127
The invention addresses challenges in achieving controlled drug release, particularly for APIs requiring multi-step or delayed absorption. By coating these MCC carriers with specific polymers and APIs, the system allows for tailored drug release at targeted points in the gastrointestinal tract. This is especially beneficial for drugs with narrow therapeutic windows or those sensitive to pH levels.
The patent emphasizes advancements in coating techniques and formulation stability, ensuring high reproducibility and efficient manufacturing processes. The resulting multiparticulate system supports dosage flexibility, reduced side effects, and improved patient adherence compared to conventional tablet or capsule forms.
The invention has implications for developing treatments for chronic conditions, where consistent and predictable drug release is critical. The application of CELLETS® in this context highlights their versatility and potential to enhance 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.
https://cellets.com/wp-content/uploads/2024/11/US20240350437A1.jpg512512Bastian Arlthttps://cellets.com/wp-content/uploads/2016/10/Logo_Cellets_2016_website.pngBastian Arlt2024-11-21 18:43:192024-11-21 19:02:57Patent on gamma-hydroxybutyrate compositions having improved pharmacokinetics in the fed state
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!
https://cellets.com/wp-content/uploads/2024/11/What-does-AI-say-about-Cellets.jpg10801920Bastian Arlthttps://cellets.com/wp-content/uploads/2016/10/Logo_Cellets_2016_website.pngBastian Arlt2024-11-13 13:56:572024-11-13 14:05:43What does AI say about CELLETS?
Please, find scientific literature on MCC pellets (CELLETS®), MCC spheres. This list is constantly updated and does not claim to be complete. If you are author, scientist or R&D specialist, please submit your present publication to us for improving the visibility.
Research article Optimising the in vitro and in vivo performance of oral cocrystal formulations via spray coating European Journal of Pharmaceutics and Biopharmaceutics, Volume 124, March 2018, Pages 13-27
Dolores R. Serrano, David Walsh, Peter O’Connell, Naila A. Mugheirbi, Zelalem Ayenew Worku, Francisco Bolas-Fernandez, Carolina Galiana, Maria Auxiliadora Dea-Ayuela, Anne Marie Healy
Conference abstract Multiple-unit orodispersible mini-tablets International Journal of Pharmaceutics, Volume 511, Issue 2, 25 September 2016, Page 1128
Anna Kira Adam, Christian Zimmer, Stefan Rauscher, Jörg Breitkreutz
Research article Asymmetric distribution in twin screw granulation European Journal of Pharmaceutics and Biopharmaceutics, Volume 106, September 2016, Pages 50-58
Tim Chan Seem, Neil A. Rowson, Ian Gabbott, Marcelde Matas, Gavin K. Reynolds, AndyIngram
Research article Physical properties of pharmaceutical pellets Chemical Engineering Science, Volume 86, 4 February 2013, Pages 50-60
Rok Šibanc, Teja Kitak, Biljana Govedarica, StankoSrčič Rok Dreu
Research article Labscale fluidized bed granulator instrumented with non-invasive process monitoring devices Chemical Engineering Journal, Volume 164, Issues 2–3, 1 November 2010, Pages 268-274
Jari T. T. Leskinen, Matti-Antero H. Okkonen, Maunu M. Toiviainen, Sami Poutiainen, Mari Tenhunen, Pekka Teppola, Reijo Lappalainen, Jarkko Ketolainen, Kristiina Järvinen
Research article Granule size distribution of tablets Journal of Pharmaceutical Sciences, Volume 99, Issue 4, April 2010, Pages 2061-2069
Satu Virtanen, Osmo Antikainen, Heikki Räikkönen, Jouko Yliruusi
Research article New insights into segregation during tabletting International Journal of Pharmaceutics, Volume 397, Issues 1–2, 15 September 2010, Pages 19-26
S. Lakio, S. Siiriä, H. Räikkönen, S. Airaksinen, T. Närvänen, O. Antikainen, J.Yliruusi
Research article In vivo evaluation of the vaginal distribution and retention of a multi-particulate pellet formulation European Journal of Pharmaceutics and Biopharmaceutics, Volume 73, Issue 2, October 2009, Pages 280-284
Nele Poelvoorde, Hans Verstraelen, Rita Verhelst, Bart Saerens, Ellen De Backer, Guido Lopes dos Santos Santiago, Chris Vervaet, Mario Vaneechoutte, Fabienne De Boeck, Luc Van Borteld, Marleen Temmerman, Jean-Paul Remon
List – Publications with MCC spheres, 2008 and earlier
Research article Attrition strength of different coated agglomerates Chemical Engineering Science, Volume 63, Issue 5, March 2008, Pages 1361-1369
B. van Laarhoven, S.C.A. Wiers, S.H. Schaafsma, G.M.H. Meesters
https://cellets.com/wp-content/uploads/2021/03/books-2463779_1920-small.jpg601854Bastian Arlthttps://cellets.com/wp-content/uploads/2016/10/Logo_Cellets_2016_website.pngBastian Arlt2024-11-13 10:25:012024-11-28 11:50:22Scientific literature on MCC pellets (CELLETS®)
A nutritional table for CELLETS®, what is it about? CELLETS® are made of 100% microcrystalline cellulose (MCC), developed for state of the art oral dosage forms, such as MUPS, capsules, sachets, stick pack units. Anyway, some pharmaceutical applications move towards food products and vice versa. This field of nutraceutical applications are extending market share and we got more frequently asked about energy and nutritional levels of MCC. So, let’s shed some light on this.
MCC is a modified form of cellulose that is often used as a filler and stabilizer in the food and pharmaceutical industries. It consists of plant fibers and serves primarily as a dietary fiber, but contains practically no usable nutrients such as vitamins, minerals, proteins or fats. It is calorie-free as it is not digested in the human body.
As microcrystalline cellulose is not metabolized, it does not provide any usable macro- or micronutrients. A nutritional table for 100 g of microcrystalline cellulose would therefore 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 and is not broken down or absorbed in the human digestive tract [1]. It therefore has no calories and provides no nutrients to the body. This nutritional table also holds for CELLETS® but has rare importance in pharmaceutical formulations.
This article “In vitro validation of colon delivery of vitamin B2 through a food grade multi-unit particle system” discusses a novel method for delivering active ingredients, particularly riboflavin, to the colon in a food-grade, environmentally friendly form using a double-layer coated multi-unit particle system (MUPS). The MUPS uses a shellac outer layer, alginate inner layer, and cellulose core, maintaining integrity through upper digestive processes. Tests showed it releases about 90% of riboflavin in the colon, enhancing gut health by promoting beneficial short-chain fatty acids. This sustainable approach addresses rising demand for effective colon-targeted health products and aligns with EU regulations limiting microplastic use in consumable goods.
The MUPS containing riboflavin, branded as Humiome® B2 by DSM-Firmenich, utilizes cellulose pellets known as CELLETS® as the core material. The manufacturing process involves a fluid bed layering method, where riboflavin and pectin are applied as a binder onto the Cellets. The MUPS is then coated with layers of sodium alginate and hardened with calcium chloride, followed by a shellac outer layer. This design ensures a controlled, colonic release, offering an efficient, food-grade delivery system for active nutrients.
The study demonstrates the efficacy of a shellac-alginate MUPS for targeted delivery of riboflavin to the colon, using food-grade materials that align with environmental standards. In vitro models validated its effectiveness, with around 90% of riboflavin reaching the colonic region. Results show promise for health benefits linked to microbiome modulation and short-chain fatty acid production. Future clinical studies will focus on the impact of this delivery system on microbiome and host health, supporting its potential in functional foods, supplements, and medical nutrition.
Abstract
Colon target delivery of active ingredients is frequently applied in pharmaceutical products. However, in functional food and beverage applications, dietary supplements, and medical nutrition, formats targeting colonic delivery to improve human health are rare. Nevertheless, there is emerging evidence for beneficial effects of colonic delivered nutrients on gut microbiota and host health which increases the demand for sustainable food grade materials that are regulatory approved for application. In this paper, we describe a double layer coated multi-unit particle system (MUPS) with a diameter of approximately 730 microns consisting of food grade materials: shellac as outer layer, alginate as inner layer, cellulose as a core and riboflavin as active ingredient. The suitability of the MUPS for colonic delivery was tested in three well-established in vitro digestion and fermentation models: the USP Apparatus 3 and the TNO Intestinal Models 1 and 2 (TIM-1 and TIM-2). All systems confirmed the integrity of the MUPS under simulated upper gastrointestinal tract conditions with approximately 90% of the active ingredient being released under simulated ileal-colonic conditions. The TIM-2 model also showed the effects of riboflavin loaded MUPS on the microbiome composition with an increase in the production of short-chain fatty acids, acetate and butyrate. The results of these experiments provide a reliable basis for validation of this vitamin-loaded food grade MUPS in future human clinical trials. In addition, following the recent announcement of the European Commission to restrict intentionally added microplastics to products, the materials used in the described formulation offer an environmentally friendly alternative to often applied methyl acrylate based coatings.
https://cellets.com/wp-content/uploads/2024/11/18762891_bja00045_i0001_part.jpg285477Bastian Arlthttps://cellets.com/wp-content/uploads/2016/10/Logo_Cellets_2016_website.pngBastian Arlt2024-11-12 14:54:572024-11-12 15:10:56In vitro validation of colon delivery of vitamin B2 through a food grade multi-unit particle system
This article on homogeneity and mechanical properties of orodispersible films loaded with pellets was published on Oct 20 2024 on ScienceDirect.
Abstract
Orodispersible films (ODFs) have served as an emerging platform for the delivery of drugs in a convenient way. The production of ODFs with incorporated pellets may still be a challenging process due to problems to obtain proper homogeneity and deteriorating mechanical properties of the films with incorporated relatively big particles in high concentration. The goal of this work was to evaluate the possibility to achieve fast disintegrating ODFs with homogenously incorporated spherical granules without loss of required mechanical properties. Hypromellose films with incorporated placebo pellets (size 200 µm or 100 µm) in a content range of 20–45 % w/w were prepared by a solvent casting method. Planetary mixer (Thinky) was successfully applied for preparation of a homogeneous mass for casting. The suspended spherical solid particles caused dose and size dependent changes in the mechanical properties and disintegration behaviour of ODFs films, but only 100 µm pellets in concentration higher than 40 % reduced significantly the tear resistance. The films with the pellets disintegrated faster and the larger particles reduced the disintegration time by 60 %. Good homogeneity of pellets distribution, expressed as a number of the particles per unit area, was confirmed for films obtained with a gap height 500 or 800 µm.
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.
https://cellets.com/wp-content/uploads/2024/10/1-s2.0-S0939641124003631-ga1_lrg.jpg8861546Bastian Arlthttps://cellets.com/wp-content/uploads/2016/10/Logo_Cellets_2016_website.pngBastian Arlt2024-10-24 09:25:532024-10-24 09:25:53Homogeneity and mechanical properties of orodispersible films loaded with pellets
The patent WO2019123269A1, titled “Packaged modified release gamma-hydroxybutyrate formulations having improved stability“ presents innovative formulations and packaging methods designed to enhance the dissolution and chemical stability of gamma-hydroxybutyrate (GHB), a treatment for narcolepsy. Current GHB treatments, like XYREM®, require patients to wake up mid-sleep for a second dose, making this method cumbersome. This patent aims to develop a once-nightly, modified-release GHB form that maintains stability through advanced packaging, which controls relative humidity to ensure long-term effectiveness and prevent chemical degradation of GHB into gamma-butyrolactone (GBL).
Key Innovations:
Modified Release Formulation: The patent includes an immediate and modified release component, both containing GHB or a pharmaceutically acceptable salt. The modified release form is designed to control the release of GHB over time, providing sustained therapeutic effects throughout the night without the need for a second dose. This formulation helps improve patient convenience and adherence to treatment.
Stability Issues with GHB: GHB is highly hygroscopic and chemically unstable, which leads to degradation, especially in high humidity environments. Its instability results in the formation of GBL, a degradation product that reduces the drug’s effectiveness. The patent addresses these challenges by creating a formulation with stable dissolution profiles and chemical stability, even under stressful storage conditions (e.g., high temperature and humidity).
Packaging Innovation: To further enhance the stability, the GHB formulations are packaged in a way that maintains a specific relative humidity range (29% to 54%) within the package. This careful control of humidity is crucial to prevent GHB from degrading into GBL. The packaging material has a low water vapor transmission rate, reducing moisture exposure and ensuring the drug remains stable over time.
Hydrophobic Coating: The patent uses a hydrophobic coating (e.g., glyceryl tristearate, hydrogenated vegetable oil) and methacrylic acid copolymers for the modified release component. These coatings help control the release rate of GHB and protect it from moisture, ensuring a steady release and preventing premature degradation.
Pharmaceutical Composition: The GHB composition in the patent includes varying ratios of immediate and modified release components. These compositions are tailored to provide a sufficient therapeutic dose while maintaining stability. The sizes of the particles and the specific formulation ratios (e.g., 40/60 to 60/40) are key factors in achieving the desired pharmacokinetics and release profiles.
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.
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.
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