Investigation on recombinant hirudin via oral route

Peptides. 2006 Apr;27(4):836-40. doi: 10.1016/j.peptides.2005.08.015. Epub 2006 Feb 13.

Abstract

The possibility for oral administration of peptide recombinant hirudin variant (rHV2-K47) as an anticoagulant agent was evaluated in several aspects. The proteolytic properties of rHV2-K47 and its stability during storage were examined by in vitro experiments. Radiolabeled rHV2-K47 was infused into the duodenum of rats and rHV2-K47 absorbed into serum was shown to be intact by electrophoresis pattern. The in vivo coagulation time of blood from mouse was prolonged significantly after oral administration of rHV2-K47. The bioavailability (F) of rHV2-K47 via oral route reached 10.11% in comparison with intravenous administration as gold standard. All the results suggested that rHV2-K47 could be delivered successfully via the oral route.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Animals
  • Anticoagulants / administration & dosage*
  • Anticoagulants / pharmacology*
  • Blood Coagulation / drug effects
  • Drug Stability
  • Duodenum
  • Hirudins / administration & dosage*
  • Hirudins / pharmacology*
  • Intestinal Absorption
  • Intestinal Mucosa / drug effects
  • Male
  • Mice
  • Rats
  • Recombinant Proteins / administration & dosage
  • Recombinant Proteins / pharmacology

Substances

  • Anticoagulants
  • Hirudins
  • Recombinant Proteins