Dr Maj-Britt Cepok, Head of Business Development Pharma at BENEO, talks to Dr Kevin Robinson about trends in excipients and explains why the right filler-binder can make all the difference
KSR: How is the excipient market developing and what does the future hold?
MBC: The global pharmaceutical excipients market is expected to reach more than $9.5 billion by 2025.1,2 Growth drivers include the rising number of elderly populations, advances in functional excipients and increasing generic drugs sales.
We are also seeing growing interest in excipients that can enhance drug solubility and bioavailability, as well as a desire to prolong the shelf-lives of medicines and improve manufacturing efficiency, such as using continuous processing, for example. Increased R&D spending and growing competition are further driving demand and putting drug formulators under pressure to develop innovative dosage forms.
KSR: What are they looking for?
MBC: Pharmaceutical manufacturers are seeking out multifunctional excipients that address several technical challenges at once while enhancing formulation at the same time. There is a desire to fulfil specific needs for paediatrics and geriatrics, such as taste masking and easy swallowing.
This goes hand in hand with the requirement for improved compliance and better ease of use. For example, controlled release applications can reduce the frequency of administration and extend the duration of effect.
Some manufacturers are looking for medications that do not need to be taken with food or water, whereas others want to offer a choice of different product options and alternative delivery forms. All the while, however, solutions have to be realised with more efficient production processes.
Multifunctional excipients such as galenIQ can help manufacturers to overcome multiple challenges. They play an important role in innovating delivery technologies and can accelerate the development of new products as they involve significantly lower development costs and fewer regulatory hurdles than creating completely new excipients.
Dr Maj-Britt Cepok
KSR: What makes BENEO’s excipient so special?
MBC: galenIQ is the pharmaceutical grade of isomalt, our disaccharide alcohol derived from beet sugar, which is the main reason why it has a taste profile that’s very close to sucrose. It therefore reduces the bitterness of APIs and contributes to a pleasant taste and mouthfeel in the final product.
In addition, galenIQ offers multiple technological benefits, such as excellent flowability and high compressibility. It also enables high content uniformity in both low and high dosage forms. Furthermore, its oil-binding capacity makes it suitable as a carrier for liquisolid formulations.
KSR: Can you give an example of how the excipient facilitates pharmaceutical production?
MBC: A good example is that it helps to overcome compression challenges when using oily plant extracts in tablets. Plant extracts have become increasingly important ingredients in pharmaceutical and nutraceutical dosage forms. However, they are often sticky or oily and can be difficult to formulate into solid formats such as tablets.
Using galenIQ 721 as a filler-binder solves this problem. It acts like a sponge by absorbing the oily plant extracts but remains as a dry, flowable powder. The excipient’s morphology helps to retain the homogeneity of the mixture and makes the production of robust tablets with high content uniformity much easier.
As galenIQ is water-soluble, plant extract tablets disintegrate rapidly without the need for a superdisintegrant or additional binders. As a further bonus, only very low compression forces are required during the tableting process.
KSR: Do these benefits only apply to tablets?
MBC: Not at all! The galenIQ range is available in a wide array of particle size distributions, morphologies and levels of solubility for wet granulation, roller compaction, other agglomeration processes and pan-coating. This makes it a highly flexible filler-binder. And because it is sweet tasting, it is ideal for chewables, effervescents, syrups, powdered formulas such as sachets and many others.
Current trends show that consumers want to take their medicines and nutritional supplements in a way that is effective yet also convenient and pleasant.
Here, galenIQ is ideal for handy sachets and stickpacks that taste good and can be taken “on the go” with or without water. In addition, in medicated hard-boiled lozenges, galenIQ 900 provides low hygroscopicity, which promotes long shelf-life stability.
Isomalt is known to form an amorphous glass that is extremely stable against degradation by heat, humidity or acids. Worldwide, it’s the most frequently used sugar replacer in hard candies — and galenIQ offers the same benefits in pharmaceutical quality.
Compared with sugars and other polyalcohols, it ensures that the lozenge does not become sticky or difficult to handle, even under high temperature and humidity storage conditions and therefore helps to reduce the need for costly protective packaging.
At 25 °C and up to 65% RH, it adsorbs virtually no additional water. This characteristic enables it to provide optimal protection, even for moisture-sensitive APIs, which is a decisive advantage compared with other bulk excipients. Furthermore, its low hygroscopic nature and anticaking properties make production processes such as mixing or agglomeration much easier.
KSR: Why is the right choice of excipient so important?
MBC: Let me give you an example: when developing powder mixtures for oral applications such as stickpacks, it is important that bulk excipients fulfil the necessary requirements, such as excellent flowability, low hygroscopicity, high physical stability during mixing, content uniformity and chemical stability, to name just a few.
There is a broad range of excipients on the market, but it can be difficult to find a multifunctional platform that combines all of these properties.
In addition, compliance is key; medicines that taste good can considerably increase acceptance by certain patient groups, such as children, the elderly and people with chronic conditions. Choosing the right filler-binder can enhance the overall taste and mouthfeel of pharmaceutical as well as nutraceutical products … and thus improve compliance.
KSR: Talking of patient compliance, consumers in the nutraceuticals space are increasingly turning to tooth-friendly and low-glycaemic formulations. Does BENEO’s excipient meet these needs?
MBC: With its low glycaemic index (GI) and only half the calories of sucrose, galenIQ has almost no effect on blood sugar or insulin levels, and is thus suitable for everyone, including those with diabetes. It is also kind to teeth. Dental cavities develop when bacteria convert fermentable carbohydrates into acids, which then attack tooth enamel.
As most micro-organisms in the oral cavity are unable to feed on isomalt, the pH in the mouth remains above the critical level of 5.7, as has been shown in numerous clinical trials. Furthermore, isomalt reduces plaque formation as it cannot serve as a structural component of plaque.
By stimulating saliva production, it even has a remineralising effect, which promotes the repair of incipient cavities. Research also suggests that isomalt enhances the positive effects of fluoride. So, all in all, our excipient more than satisfies consumer demand for medicines and nutraceutical supplements that are both tooth-friendly and low GI.