Once-bitter tasting medicines are now easier to swallow with these new innovations in drug design.

By Get Science Staff – This article originally published on Get Science

Most kids don’t like taking medicine, and often for good reason. Children’s taste buds are more sensitive to bitter-tasting medicines, and swallowing tablets can be difficult. But what if a child with a life-threatening illness is refusing or unable to take a drug that could potentially save his or her life?

Dr. Jeremy Bartlett, associate research fellow with Pfizer Drug Product Design in Groton, Connecticut, was presented with such a challenge some three years ago, when a group of pediatric cancer patients reacted negatively to taking a drug that was tested in oral solution form. The young patients thought that the medicine tasted “spicy like Tabasco.” As critically ill cancer patients, these children were missing out on an experimental cancer drug that could potentially help keep them alive, due to the medicine’s taste.

“This drives me with a passion. We have potential medicines, but need to mask their taste profiles so that pediatric patients may be more willing to take them” said Bartlett, who for the past four years has led a Pfizer initiative working with a broad multidisciplinary team to design better tasting medicines for children.  His mission is critical: More than 90 percent of pediatricians report that a drug’s taste and palatability (or acceptability, which is influenced by taste, texture and smell) are the biggest barriers to completing treatment, according to a 2013 study in Clinical Therapeutics.

From Molecules to Medicines

Researchers devote years to discovering new molecules that can treat and cure illnesses, but how will those molecules be delivered as a potential medicine to the patient? That’s where drug product design plays an integral role. From formulating controlled-release tablets to testing transdermal patches, scientists like Bartlett specialize in ensuring that a drug is safely and effectively delivered to patients.

When it comes to designing medicines for children, it’s not as simple as making a smaller dose of an adult medicine and masking it in cherry flavoring. “Children are not little adults,” said Bartlett. “You can’t treat kids like little versions of adults. They have, among other things, different metabolisms, stomach sizes, medicine transit times and responses to medicines. All these components have to be factored in when designing medicines for children.”

Like a Glass of Water

Drug product designers also face the difficult task of striking the right balance of flavor. Children are generally more sensitive to sweet and bitter flavors than adults, and an additional 10 percent of kids have elevated taste receptors, which could make a drug that tastes acceptable to the majority of kids taste terrible to a minority of kids.

Creating drugs for global consumers also presents its challenges. A banana-flavored medicine might be popular among kids in the U.S., but may not appeal to those in Russia or China.

For the past few years, Bartlett and his team have been hard at work trying to solve the issue of taste in pediatric drugs. And they think they’ve found the answer: The best flavor may be no flavor at all.

“If we don’t have to worry about a child swallowing a medicine – if we can remove that battle for parents – and make taking medicines like drinking a glass of water, that would be a huge step forward,” Bartlett said.

Eliminating Poor Taste and Irritation

He and his colleagues might just be taking that step with a new innovation in drug product design. A fraction of the size of typical children’s tablets, these new taste-neutral drug products are tiny spheres known as oral multiparticulates. Each is coated in a tasteless barrier membrane that prevents the drug from being released in the mouth which inhibits the drug from interacting with the taste receptors, ideally eliminating issues of poor taste and irritation.

A single dose of this drug product can include thousands of these multiparticulates, packed in a sprinkle capsule, stick pack or sachets. And unlike powders or granules that can create a gritty, unpleasant “mouthfeel,” the multiparticulates travel smoothly through the mouth, resulting in a non-gritty, more pleasant experience. When the medicine reaches the stomach, it’s released.

It took a significant amount of time and effort, but Bartlett and his team recently produced a new experimental, pediatric drug product that is based on the multiparticulates technology that is in clinical testing.

“It’s a long process that takes time and resources, but our whole team is focused on getting medicines to the kids who need them,” he said. And while the final results have yet to come in, their very discerning taste-testers seem to be giving an early thumbs-up, according to Bartlett, who noted: “A potentially significant improvement over where we were, and so far no complaints.”