Poor solubility used to be one of the main showstoppers during the development of oral drug products. Advances in excipients, process technologies, equipment and predictive tools have fortunately all helped to substantially de-risk the process. However, while the risk of running into a dead-end may have reduced, market demand for solutions that can address the solubility challenges of complex drug products has skyrocketed in recent years.
Today, poor solubility affects around 40% of currently marketed drugs and the majority of actives in clinical development. One key factor behind this trend is a shift towards actives with a higher molecular weight and increased lipophilicity, which can result in a decrease in aqueous solubility.
In this interview, Dr. Jessica Müller-Albers, Director of Strategic Marketing for Oral Drug Delivery Solutions at Evonik, shares some of the Company’s top recommendations to enhance the solubility of poorly soluble drugs.
“A vast range of factors can affect drug solubility, as well as overall bioavailability, based upon the product’s inherent permeability,” said Dr. Müller-Albers. “In addition to drug concentration and disintegration time of the dosage form, it is also critical to understand the inter-relationships that can occur between properties including molecular weight, lipophilicity, solid state, particle size and surface area. To ensure reliable process development and scale-up, it’s also important to review how these physical properties can be utilized with the right equipment and process technologies”.
So how can pharma companies minimize project risk and development costs, select the right excipients, equipment and process technologies to complement their API and dosage form, and hopefully also enable higher drug loadings and improve stability? Dr. Müller-Albers listed five key factors that companies should keep in mind to help ensure their path to solubility enhancement is as seamless and as low risk as possible.