Deep Vein Thrombosis Research Today is a free monthly online journal that collates and summarizes the latest research about Deep Vein Thrombosis, including details on dvt, prevention, effects, causes, air travel, blood clots.

A newly developed oral heparin derivative for deep vein thrombosis: non-human primate study.

Kim SK, Lee DY, Kim CY, Nam JH, Moon HT, Byun Y

Department of Materials Science and Engineering, Gwangju Institute of Science and Technology, Gwangju 500-712, Republic of Korea.

The development of orally active heparin will have tremendous clinical importance since it can be used to effectively prevent deep vein thrombosis (DVT) in a long-term chronic treatment. We developed in this study a new orally active heparin derivative (Db-LHD), which has heparin chemically conjugated with deoxycholic acid and DMSO molecules by secondary interactions. Db-LHD was prepared in the powder form in soft capsules. When we administered Db-LHD capsules to monkeys, its oral physiological availability was increased up to 16.6%. The maximum anti-FXa activity at 5 mg/kg of Db-LHD was more than twice the minimum effective anti-FXa activity (MEC, 0.1 IU/mL) for preventing DVT, and the anti-FXa activity in plasma was maintained for 10 h above the MEC in monkeys. Also, we evaluated anti-thrombogenic effect of Db-LHD in a rat thrombosis model. A subcutaneous administration of enoxaparin (100 IU/kg), which was the highest recommended dose for the prevention of venous thromboembolism, reduced thrombus formation by 38.9+/-14.2%. On the other hand, 5 mg/kg (425 IU/kg) of orally administered Db-LHD reduced thrombus formation by 51.0+/-2.0. We propose a new orally active heparin, Db-LHD, in a solid dosage form to effectively prevent DVT and PE.

Published 19 October 2007 in J Control Release, 123(2): 155-63.
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