Pharmacy and Pharmaceutical Sciences Commons^™

Sequential Group Trial To Determine Gastrointestinal Site Of Absorption And Systemic Exposure Of Azathioprine, Jane M. Gervasio, Rex O. Brown, John Lima, M. G. Tabbaa, Thomas Abell, Robert Werkman, Lynda J. Haberer, Lawrence J. Hak

Scholarship and Professional Work – COPHS

Azathioprine (AZA) is used in the treatment of patients with refractory inflammatory bowel disease; however, its use is limited because of systemic toxicity associated with long-term use. Ileocecal delivery of AZA might be advantageous if local intestinal therapeutic effects could be provided with decreased systemic side effects. Decreased cecal systemic absorption would allow higher dosages of AZA to be administered. A two-phase study was performed to compare the systemic exposure of AZA and 6-mercaptopurine (6-MP) following administration of AZA into the stomach, jejunum, and cecum and to compare the systemic exposure to AZA and 6-MP following administration of three different …