Emisphere Technologies, Inc., a biopharmaceutical company, announced that six posters presenting the application of its unique eligen oral drug delivery technology were presented at the American Association of Pharmaceutical Scientists (AAPS) 2003 Annual Meeting this week.

"We continue to make advances using our proprietary technology," said Steven Dinh, Vice President of Research and Technology Development. "Our presentations at AAPS highlight how Emisphere delivery agents enable the delivery of a diverse group of macromolecules."

"The Utility of Emisphere's eligen Technology for the Oral Delivery of Heparin in Solid Dosage Forms," poster T3169, was presented on October 28. Previous studies have demonstrated that heparin administered with an Emisphere delivery agent is absorbed from the gastrointestinal tract. The current studies demonstrate that several different formulation approaches have improved the delivery of heparin in solid dosage forms in monkeys and healthy human volunteers. Heparin combined with an Emisphere delivery agent in tablet and capsule dosage forms were prepared and characterized prior to use. When administered to monkeys, the heparin tablet and capsule formulations produced substantial increases in antifactor Xa, an indicator for anti-coagulation, with the maximum effect observed at 1.5 hours post-dose. The tablet and capsule formulations delivered substantial levels of heparin in healthy humans.

"These data are critical to our heparin oral delivery program," said Shingai Majuru, Ph.D., Director of Pharmaceutics Research and Development at Emisphere Technologies. "We previously established that orally delivered heparin was active and well-tolerated in human subjects using our eligen technology. In the current study, we showed that the oral delivery of heparin was further enhanced with a solid dosage prototype formulation using an Emisphere delivery agent."

"Oral Delivery of Insulin: In Situ Portal Perfusion in A Rat Model," poster M1038, was presented on October 27. This study used an in situ single pass intestinal perfusion model in rats to evaluate insulin absorption into the portal vein and systemic circulation following administration with an Emisphere delivery agent. The delivery agent increased insulin absorption, but unlike other forms of insulin delivery, did not reverse the portal-to- systemic insulin concentration relationship. Hence, oral delivery of insulin mimics the physiological route of disposition of insulin, thereby maximizing hepatic (liver) utilization while minimizing circulating insulin.