New Method Increases Dissolvability of Drugs

Scientists discovered an excipient that improved absorption of a prostate cancer drug 3-fold.

Scientists recently discovered a novel technique to customize ingredients that will help oral medications be dissolved and absorbed by the body more easily.

This method could potentially allow life-saving drugs to take effect more quickly, and lower the cost of creating new drugs, according to the study published by ACS Central Science.

A challenge to creating new oral medications is to ensure that the body will absorb the drug molecules. Currently, many drug structures are difficult for the body to absorb, and do not easily dissolve on the molecular level, making them less effective.

If the drug is not able to be fully dissolved, the dose must be increased. Increasing the dosage may also increase the likelihood of side effects.

Certain medications that treat conditions such as cancer already have numerous side effects. By decreasing the dose, it is likely that side effects can be lessened, and the medication will be more tolerable.

“A way to explain the differences in solubility of medicines is to think of how sugar easily dissolves in water and is rapidly absorbed by your digestive system, whereas sand doesn't dissolve in water and if swallowed, would pass right through the digestive system,” said lead researcher Theresa Reineke, PhD.

Drug manufacturers currently add excipients to assist the medications with dissolving in the stomach and intestinal fluid. Before this recent discovery, there have been little improvements to this technique.

Scientists examined phenytoin, a seizure medication, and nilutamide, a prostate cancer drug, under automated equipment to synthesize long-chain molecules, according to the study.

They tested each drug’s efficiency as an excipient, and discovered that 1 excipient allowed the insoluble drugs to completely dissolve in intestinal fluid. When testing phenytoid with this excipient in animal models, they discovered drug absorption that was 3 times faster compared with the previous formulation.

“While we were pleased with the results with these specific drugs, the most important thing is that we have developed a high throughput methodology for excipient development that could be used by many companies to create other life-saving medicines,” Dr Reineke said.

These findings could have the potential to lower drug costs, which has been a highly publicized topic. Other scientists have created new methods to manufacture important chemical compounds used in pharmaceuticals called amines.

Together with the current findings, new drug creation methods could save the pharmaceutical industry billions.

“It takes about $1 billion dollars and 10 to 15 years for a pharmaceutical company to develop a new drug, but then they sometimes find marketable formulations are limited by solubility,” said co-author of the study Steven Guillaudeu. “The methodology our team has created could help drug companies advance their pipeline compounds by using a better method to improve solubility and therefore bioavailability. The approach could have a major impact on the multibillion-dollar industry.”