New and Novel Excipients 2022
The pharmaceutical industry needs innovative, new and novel excipients solutions to support the developments in next generation therapeutics, new manufacturing concepts (eg. continuous manufacturing, 3Dprinting, etc.), drug delivery and API challenges such as solubility and permeability just to mention some.
What is a novel excipient?
Novel excipients have different definitions. Here are some of the most important ones.
FDA Definition of novel excipients
In this guidance, the phrase new excipients means any inactive ingredients that are intentionally added to therapeutic and diagnostic products, but that: (1) we believe are not intended to exert therapeutic effects at the intended dosage, although they may act to improve product delivery (e.g., enhance absorption or control release of the drug substance); and (2) are not fully qualified by existing safety data with respect to the currently proposed level of exposure, duration of exposure, or route of administration.
Source: Guidance for Industry Nonclinical Studies for the Safety Evaluation of Pharmaceutical Excipients
EU definition of novel excipients
A novel excipient is an excipient which is being used for the first time in a drug product, or by a new route of administration (ICH). It may be a new chemical entity or a well established one which has not yet been used for human administration and /or for a particular human administration pathway in the EU and/or outside the EU.
Source: GUIDELINE ON EXCIPIENTS IN THE DOSSIER FOR APPLICATION FOR MARKETING AUTHORISATION OF A MEDICINAL PRODUCT
The summary of the “The Excipients Week – New and Novel Excipients” as published end of 2022
klucel™ xtend HPC – new hydrophilic matrix polymer addresses the limitations of traditional hypromellose polymers
Ashland introduces Klucel™ xtend hydroxypropyl cellulose (HPC) controlled release matrix former, designed to deliver unsurpassed process versatility and release profile efficiency.
Until now, there were limited options for managing the release profile of formulations, especially high dose, controlled release formulations. Ashland’s step change Klucel™ xtend HPC has been shown to match the release profile of widely used hypromellose controlled release formulations at half the polymer concentration.
The need for hot-melt extrusion (HME) polymers is expected to grow as the pharma industry moves to implement more continuous and sustainable processes. klucel™ xtend HPC is the only cellulosic excipient that provides a compendial extended-release polymer option for plasticizer-free HME. This oral matrix former is the new gold standard for extended-release tablets. klucel™ xtend HPC extending your options for
- highly soluble APIs
- high drug load formulations
- melt granulation or HME processing
- increased patient compliance
- complex formulations
More product information – click here
Eastman BioSustane™
A solution for poor solubility, extended release, depot formulation, and abuse deterrence
Eastman BioSustane™ SAIB NF is a novel, non-polymeric excipient derived from biobased material: sucrose. Highly hydrophobic, it has multiple potential applications. BioSustane can be used as:
- A carrier for amorphous solid dispersion for poorly water-soluble drugs
- A sustained-release excipient compatible with both water-soluble and poorly water-soluble drugs
- An abuse-deterrent excipient when formulating APIs that are subject to abuse
- A novel depot former for injectable drugs as shown in some U.S. Food and Drug Administration (FDA) approved drug formulations. Note: Eastman does not market an injectable grade of BioSustane. Customer is responsible for ensuring BioSustane meets injectable grade.
In addition, the mucoadhesive property of BioSustane is hypothesized to enhance the bioavailability of the APIs.
More product information – click here
Emulfree® Duo
Emulfree® Duo by GATTEFOSSÉ is a ready-to-use PEG-free system. It has been designed to stabilize the oil phase within the bi-gel, by ensuring fine and homogeneous dispersion in the aqueous phase. With Emulfree® Duo the whole process can be carried out at room temperature, which is ideal for thermo sensitive drugs. This excipient is compatible with a wide range of oils, solvents and penetration enhancers, and enables the formulation of a wide range of textures, from light lotions to rich creams, depending on the overall formulation
More information on Emulfree® Duo
Kollitab™ DC 87 L – BASF´s new all-in-one tableting solution
Kollitab™ DC 87 L is an all-in-one tableting solution that includes a filler, binder, disintegrant and lubricant.
- It provides superior flowability, achieves high tablet strength when applying a broad range of compression forces (both low and high), and ensures fast tablet disintegration.
- Its “all-in-one” nature enables fast tablet development, simplifies formulation processes, and reduces manufacturing complexity.
More information on Kollitab™ DC 87 L
EUDRACAP®
EUDRACAP® by Evonik are ready-to-fill coated capsules for fast drug development. EUDRACAP® pre-locked capsules are suitable for the filling of drug forms including powders, pellets and granules. They are easy to open and close on standard capsule filling systems.
An increasing number of active ingredients are also sensitive to heat, moisture, gastric acids or certain processing conditions. Here, EUDRACAP® can help protect the active ingredient to optimize rates of absorption and avoid premature dissolution. Together with the regulatory excellence of EUDRAGIT® and Evonik’s local market knowhow, these USP and EP compliant EUDRACAP® capsules can help you to reduce clinical risk and accelerate time to market.
THE BENEFITS OF EUDRACAP®
- Precise pH targeting
- Effective acid resistance for up to 4 hours
- Optimized absorption rates
- Reduce clinical risk
- Accelerate time to market
Apisolex™
Apisolex™ by Lubrizol Life Science – Health is a Solubility-enhancing Excipient for Injectable Drug Formulations.
Approximately 60% of potential active pharmaceutical ingredients (APIs) under development, and more than 40% of those in reformulation, are poorly water soluble. Excipients offer the most versatile approach to solving these solubility challenges and have long played a key role in allowing poorly soluble APIs to be formulated into products with improved bioavailability and therapeutic effects. However, as the number of poorly soluble APIs grows, existing excipients are still not able to solve all of the complex formulation challenges.
Rescue Your Parenteral Drug Formulation with Apisolex™ Polymer
- Safe, poly-amino acid based amphiphilic polymer which is a non-toxic, non-immunogenic, biocompatible, and biodegradable alternative to PEG.
- Increases solubility of hydrophobic APIs by up to 50,000-fold.
- High drug loading (up to 40:100 API:solubilizer ratio).
- Forms stable, lyophilized drug product that reconstitutes in less than 30 seconds in saline.
- Enables IP protection and 505(b)(2) formulations/lifecycle management.
Apinovex™
Apinovex™ by Lubrizol Life Science – Health is a Solubility-Enhancing Excipients for Amorphous Solid Dispersions.
Lubrizol’s Apinovex™ polymers are high molecular weight polyacrylic acid excipients designed to provide both processing and formulation benefits for spray-dried amorphous solid dispersions (ASDs). Apinovex polymers enable formulators to enhance the solubility of BCS Class II and IV APIs and develop more efficient oral dosage forms with high, stable drug loading.
Enhance Oral Solubility with Apinovex™ Polymers
- High, stable drug loading (up to 80%) via spray drying.
- Significantly improved drug release profile compared to crystalline APIs.
- Enables IP protection and 505(b)(2) formulations/lifecycle management.
Parteck® COAT
Parteck® COAT by Merck is a polyvinyl alcohol (PVA) with a unique structure specifically designed for immediate-release film coating applications. Due to its optimized particle size, it helps to reduce dissolving times when preparing the coating solution, thus increasing process efficiency. Its low viscosity and high stability against moisture and oxidation makes it very well-suited for use as a film-forming polymer in coatings.
Benefits of Parteck® COAT:
- Excellent surface finishing – increase the value of your formulation
- Rapid preparation of coating liquids even at room temperature
- Low viscosity at high polymer concentration – enables reduced process times and enhanced efficiency
- Stable moisture and oxygen barrier – effective protection of moisture-sensitive APIs
- Multi-compendial material, a GRAS polymer and compliant with Ph Eur, ChP, JPE and USP
More information on Parteck® COAT
Roquette Launches Next-Generation Direct Compression Solutions at CPHI 2022: New PEARLITOL® CR-H mannitol and PEARLITOL® 200 GT mannitol.
PEARLITOL® CR-H is a patented blend of mannitol and hydroxypropyl methylcellulose (HPMC) that allows for the sustained release of active pharmaceutical ingredients in direct compression formulations. The first mannitol-based excipient of its kind to support this functionality, it creates new opportunities to enter the controlled release drug delivery space – an application which typically requires wet granulation processes. As well as removing the extra drying step necessary with wet granulation, the co-processed mannitol and HPMC brings superior functional properties, like flowability, that help optimize tablet processibility.
PEARLITOL® 200 GT is a one-of-a-kind granulated mannitol excipient designed to enhance tableting performance. In addition to addressing the capping and sticking issues commonly observed with other excipient solutions, it offers high-speed, high-volume continuous manufacturing – enabling the production of up to 250,000 tablets per hour without compromising on tablet quality. Meanwhile, it supports patient-friendly innovation by facilitating the development of harder, smaller tablets and can be used in novel pharmaceutical applications, such as fast-dissolving medications.
Lonza Launches New Capsule to Deliver Acid-Sensitive Active Pharmaceutical Ingredients to the Intestine
The Capsugel® Enprotect™ capsule does not disintegrate during stomach transit and only releases its contents in the intestine. Capsugel® Enprotect™ capsules significantly simplify the drug product manufacturing process by mitigating the need for additional capsule coating or sealing.
Learn more here and watch the video – click here to watch