Functional Excipients
FORMULATION DEVELOPMENT - Overcoming Early Phase Development Challenges & Optimizing Formulations With a Minimal Amount of API
ABSTRACT Softgel is a proven and effective delivery technology for poorly soluble drugs and can incorporate a wide range of fill formulations to optimize the…
SPECIAL FEATURE - Excipients: Enhancing the New, Poorly Soluble APIs
Contributor Cindy H. Dubin interviews several excipient manufacturers who share their insights about the role excipients play in formulating and manufacturing drugs for improved bioavailability, solubility, and delivery.
EXECUTIVE INTERVIEW - Croda: Understanding & Addressing the Purity Needs of the Pharmaceutical Market
Dr. Andrew Kaziska, Health Care Applications Manager at Croda Inc, discusses his company’s Super Refining technology and the benefits of excipient purity in drug formulations.
EXCIPIENT UPDATE - Soluplus®: An Understanding of Supersaturation From Amorphous Solid Dispersions
Oksana Tsinman, Konstantin Tsinman, PhD, and Shaukat Ali, PhD, describe the application of a hydrophilic polymeric solubilizer in solid dispersions of a model drug carbamazepine. The scope of this study is limited to understanding of hydrophilic polymers and their behaviors on amorphous dispersions.
EXCIPIENT UPDATE - Elution of Dexamethasone Acetate Into Buffered Saline Solution Through a Silicone Elastomer Using Excipients
Brian Reilly, Mustafa Al-Azzam, and Robert Kivlin measure the elution rate of DMA from a cured silicone matrix into a physiological environment with the goal of understanding the influence of load level and the use of excipients in DMA delivery through a cured silicone matrix.
BIOAVAILABILITY ENHANCEMENT - Navigating a Broad Spectrum of Solubilization Technologies: Part III of III
Marshall Crew, PhD, President & CEO, Agere Pharmaceuticals, Inc., concludes his multiple-part series discussing today’s most challenging issues in solubility.
FORMULATING PEPTIDES - Novel Formulations for Non-Invasive Delivery & Stabilization of Peptides
Edward T. Maggio, PhD, examines how alkylsaccharides offer exciting prospects for novel formulations, providing non-invasive delivery, stabilization, and immunogenicity reduction for biotherapeutic products, resulting in broader patient acceptance and compliance and an increase in their acceptance as viable commercial pharmaceuticals.
BIOAVAILABILITY ENHANCEMENT - Navigating a Broad Spectrum of Solubilization Technologies: Part II of III
Marshall Crew, PhD, President & CEO, Agere Pharmaceuticals, Inc., continues his multiple-part series discussing today’s most challenging issues in solubility.
EXCIPIENT UPDATE - Maximizing the Stability of Therapeutic Proteins Using Recombinant Human Albumin
Mark Perkins, PhD, reviews some of the important factors involved, and highlights the advantages of including recombinant human albumin to stabilize protein therapeutics with reference to a recent case study.
BIOAVAILABILITY ENHANCEMENT - Navigating a Broad Spectrum of Solubilization Technologies: Part I of III
In the past two columns, The Second Quadrant focused on excipients and the roles they play in the quest to overcome bioavailability challenges of poorly…
EXCLUSIVE ONLINE CONTENT
Evonik Partners With University of Mainz to Commercialize New Class of PEG Lipids for Nucleic Acid Delivery
Evonik and the University of Mainz have signed a license agreement to commercialize randomized polyethylene glycols (rPEGs), a new class of PEGs. Evonik intends to use….
Novo Holdings to Acquire Catalent
Catalent, Inc., a leader in enabling the development and supply of better treatments for patients worldwide, and Novo Holdings, a holding and investment company that is responsible for managing the assets and wealth of the Novo Nordisk Foundation, recently announced they….
Colorcon Unveils Corelease - A Unified Brand for Novel Controlled-Release Formulated Systems
Ready formulated systems approach simplifies the development and manufacturing for controlled release…..
Roquette Completes Acquisition of Qualicaps & Reinforces Global Position in the Pharmaceutical Industry
This strategic investment creates a stronger leader, with an expanded global footprint, as well as an enriched offering of oral dosage solutions…..
Acquisition of Solus BioTech Expands Croda's Specialized Pharma Business in Asia
Croda International Plc recently announced it has acquired Solus BioTech, a global leader in premium, biotechnology-derived materials, from Solus Advanced Materials…..
MARKET NEWS & TRENDS
WEBINARS
WEBINAR - Beyond the Lab: Unleashing the Potential of In Silico Modeling in Drug Product Formulation
In this webinar you will learn how digital chemistry tools facilitate rapid screening of formulation parameters, aiding in the identification of optimal drug delivery systems, excipient selection, and dosage forms….
WEBINAR - Understanding Patch Composition for Effective Transdermal Delivery
As the advantages of transdermal drug delivery grow, the global market for transdermal patches also is growing. Join DuPont™ Liveo™ Healthcare Solutions and Gattefossé Pharmaceuticals for a complimentary one-hour webinar to explore the current….
Where Do We Stand on Poorly Soluble Drugs and Peptides in Oral Delivery?
The Rule of 5 suggests that, for oral bioavailability, a better chance for oral absorption is obtained when the molecules are within the parameters of the Rule of 5’. However, the pharmaceutical industry is achieving oral efficacy with drugs that exceed….
Oral Delivery of Hydrophilic Macromolecules: Lipid-Based Nanocarriers as Key to Success
This LIVE event has already taken place CLICK HERE to access the recorded version of this event and receive a copy of the presentation. Join…
WHITE PAPERS
WHITEPAPER - Copolymer Microstructures: Connecting Monomer Sequence Distribution With Biomedical End-Application Performance
To gain insights into advanced copolymer characterization techniques and their impact on drug release in biomedical products, we invite you to explore the latest Corbion white paper…..
WHITEPAPER - Monitoring Low Dose API Blend Uniformity With Parteck® M Mannitol Using Near-Infrared (NIR) Spectroscopy
Direct compression is often used for tablet manufacturing because it is the shortest, most effective, and least complex method. The physical properties of active pharmaceutical…
WHITEPAPER - The Viscosity Reduction Platform: Viscosity-Reducing Excipients for Protein Formulation
This white paper evaluates the viscosity-reducing capacities of excipients and excipient combinations…..
WHITEPAPER - Improving API Solubility by Salt & Cocrystal Formation
Ensuring sufficient solubility is critical to the success of small molecule drugs. An active pharmaceutical ingredient (API) must be absorbed by the body and enter the systemic circulation to deliver the desired therapeutic effect. Many APIs,….
WHITEPAPER - Overcoming the Knowledge Gap: Long-Acting Injectables & Implantables
This whitepaper delves into the numerous benefits of long-acting drug delivery systems, including their ability to harness highly potent APIs, streamline development and intellectual property protection, and provide consistent drug release over extended periods.
What are functional excipients?
The global pharmaceutical excipients market was valued at $7.7 billion in 2020 and is expected to reach $11.2 billion by 2026. Functional excipients are witnessing a strong demand as companies supply a wide range of functional excipients that help manufacturers produce cost-effective, high-quality, finished pharmaceutical product. Many industry experts point to a widening demand and use of organic pharmaceutical excipients. These organic excipients include oleochemicals, petrochemicals, proteins, carbohydrates, and others. Additionally, binders and functional excipients are witnessing a strong demand. Regarding delivery route, it is the topical segment that is witnessing fast growth in the global pharmaceutical excipients market, as topical drug delivery is witnessing a significantly stronger progression because of its ability to surpass the metabolism pathways of the stomach and liver.
However, the high cost associated with the drug development process will impede the growth rate of the pharmaceutical excipients market. Additionally, strict government regulations have hindered the pharmaceutical excipients market growth. Safety, quality concerns, and lack of awareness will further challenge the market in the forecast period mentioned above.
This is particularly true for novel excipients, which do have technical, therapeutic, and commercial benefits in oral drug delivery. Despite their formulation-enhancing benefits, novel excipients are sacrificed early in development because of a lack of precedence of use.
Without an independent pathway to allow new excipients or new uses for existing excipients into drug products, except when associated with a drug filing, there are limited tools available for pharmaceutical companies to formulate better performing, and in many cases, life-saving drugs. Meanwhile, drug manufacturers are reluctant to use new excipients and take on the additional layer of scrutiny from regulatory agencies to demonstrate full excipient characterization, safety, quality, function, and appropriateness of use.
Functional Excipients and the FDA
The Food & Drug Administration (FDA) has acknowledged that the lack of novel excipients is indeed a problem. In September 2021, the Agency announced the Novel Excipient Review Pilot Program, which will select and review four novel excipients in the next two years using a new pathway. This will allow manufacturers to obtain an FDA review prior to the use of the novel excipient in a drug formulation.
The FDA’s recent stance and acceptance that the novel excipients are critical in development of new drug candidates, the perceptions around the novel excipients are being changed as the Agency continues to embrace the facts that the pharma industry is in dire need of new excipients for bringing the innovative drugs to the market faster. This is the first time in history that the agency is opening doors for novel excipients to be freely evaluated and used in the innovative formulations for NCEs.
Note, though, that this is not an excipient approval process; the novel excipient would still be evaluated as part of the overall drug product approval. In the next 3 to 5 years, we can expect to see an acceleration in the examination of the composition and purity of excipients.