Development of oral heparin therapy for prophylaxis and treatment of deep venous thrombosis

Cardiovasc Surg. 2001 Jun;9(3):211-8. doi: 10.1016/s0967-2109(00)00144-7.

Abstract

Objective: To review the current research and published literature regarding the development of oral heparin therapy for the prophylaxis and treatment of deep venous thrombosis.

Background: Currently, the accepted practice of prophylaxis and/or treatment of acute deep venous thrombosis (DVT) is intravenous or subcutaneous (SQ) heparin followed by oral warfarin or SC low molecular weight heparin (LMWH) therapy followed by warfarin. Both of which are less than ideal. More recently, advances have been made towards an effective oral heparin preparation that would resolve many of the drawbacks to the current therapies.

Methods: A review of the current and relevant English literature identified via a search of the Medline database from January 1990 to present.

Results: Initial oral heparin therapy for DVT was unsuccessful due to presumed inadequate intestinal absorption as a result of heparin's molecular and structural characteristics. The development of oral heparin therapy, based on combining heparin with the carrier molecule Sodium N-(8[2-hydroxybenzoyl]amino) caprylate (SNAC) to enhance its intestinal absorption and bioavailability for the prophylaxis and treatment of DVT has been demonstrated to be effective in animal models. More recent efforts have been aimed at human trials.

Conclusion: Recent advances in prophylaxis and treatment of DVT have stimulated great interest among researchers to develop an effective, convenient, and well tolerated oral therapy. An effective oral heparin therapy may represent an ideal method of prophylaxis and treatment of DVT.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Anticoagulants / administration & dosage*
  • Anticoagulants / chemistry
  • Anticoagulants / pharmacology
  • Antithrombin III / metabolism
  • Biological Availability
  • Caprylates
  • Chemistry, Pharmaceutical
  • Decanoates
  • Disease Models, Animal
  • Drug Carriers
  • Drug Evaluation, Preclinical
  • Heparin / administration & dosage*
  • Heparin / chemistry
  • Heparin / pharmacology
  • Humans
  • Hydroxybenzoates
  • Intestinal Absorption
  • Treatment Outcome
  • Venous Thrombosis / drug therapy*
  • Venous Thrombosis / prevention & control*

Substances

  • Anticoagulants
  • Caprylates
  • Decanoates
  • Drug Carriers
  • Hydroxybenzoates
  • sodium N-(10-(2-hydroxybenzoyl)amino)decanoate
  • Antithrombin III
  • Heparin
  • octanoic acid