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Manufacture Small Molecules, Ingredients, Formulation

The Excipient of the Future

Oral administration remains the most convenient form of delivery for patients and healthcare providers, but the poor solubility and bioavailability of newer APIs have become major roadblocks for pharmaceutical development. It has been reported that up to 80 percent of new chemical entities under development today have poor solubility, resulting in limited oral bioavailability. Consequently, technologies that help companies overcome the inherent low solubility of many newly developed APIs have never been more important.

Although there are a number of approaches to improving solubility, bioavailability and dissolution rates, formulation technologies have, for the most part, remained unchanged for decades. The use of drug carriers (e.g., mesoporous silica), spray drying and hot-melt extrusion (HME), as well as improved production methods such as continuous manufacturing, can all have an impact, while personalized medicine, 3D printing, and amorphous solid dispersion look set to be the disruptive technologies of the future. However, new manufacturing techniques are not enough in isolation – we also need innovative formulations. A good example is mesoporous silica formulations, which have been shown to be excellent carriers for poorly water-soluble drugs. Though the concept was first introduced in the early 1970s by pharmacists Donald Monkhouse and John Lach, the technology and its applications are still relatively new to the pharma industry. I believe this is exactly the type of formulation innovation we as an industry need to embrace.

Right now, there is a huge demand for greater flexibility and efficiency. Continuous manufacturing is one solution, but one of the key drawbacks is the need for a relatively high amount of API in early development and increased sensitivity to changing API properties during the pharmaceutical development process, whereby changes in physical particle attributes may result in difficult and unreliable process development. 

One potential way to overcome this issue could be realized through a more intelligent approach to excipient design. The use of API-loaded mesoporous silica instead of the pure API results in homogenized particle properties throughout the pharmaceutical development cycle. Ultimately, the API loaded onto the mesoporous silica will retain the same particle properties at all stages in process development. This allows robust continuous processes to be developed early on in the project, minimizing API requirements. This is just one example of how incorporating smart excipient strategies can lead to more efficient drug development.

The pharmaceutical industry is in urgent need of faster, more efficient and flexible solutions to produce oral medications. Instead, taking a holistic view when it comes to pharmaceutical advances will be the key to the industry’s next and greatest successes. By combining advances in discovery, formulation, and manufacturing to produce the best and most robust products, true progress in drug development can be made.

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About the Author
Dieter Lubda

Director of R&D Operations, Merck KGaA, Darmstadt, Germany

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