Poor efficacy inside the gastrointestinal tract - various drugs exert their therapeutic effect within the gastrointestinal tract. These drugs mediate their effect through receptors that are expressed in a limited segment of the digestive system i.e., the upper gastrointestinal tract. However, due to natural peristalsis these drugs are not concentrated near their target for sufficient time, and therefore suffer from similar drawbacks as drugs with a narrow absorption window.
The Challenge - prolonging the retention of drugs beyond their absorption window. The development of a dosage form that would withstand the hostile environment of the stomach and overcome natural emptying of its contents into the intestine has eluded drug developers for decades.
The benefit -
drugs with poor absorption or low local efficacy in the intestine could be enhanced by a dosage form that releases the drug gradually and continuously into the upper intestine, thus "upstream" from the relevant site of action. By releasing drugs with short absorption and short half-life slowly and steadily into their absorption sites, more stable blood levels and better dosing regimens can be attained. |