An in vitro study with an ussing chamber showing that unfractionated heparin crosses rat gastric mucosa

Journal of Pharmacology and Experimental Therapeutics

Volumn 322, Issue 1, 2007, Pages 299-305

  Moazed, Bita ^a   Hiebert, Linda M ^a,b  

^a UNIVERSITY OF SASKATCHEWAN   (Canada)

^b UNIVERSITY OF SASKATCHEWAN   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

BUFFER; HEPARIN;

ANIMAL TISSUE; ANTICOAGULATION; APPARATUS; ARTICLE; CONTROLLED STUDY; DRUG ABSORPTION; DRUG DIFFUSION; IN VITRO STUDY; MALE; NONHUMAN; PH; POTENTIAL DIFFERENCE; PRIORITY JOURNAL; RAT; SEROSA; SHORT CIRCUIT CURRENT; STOMACH MUCOSA;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL TRANSPORT; GASTRIC MUCOSA; HEPARIN; HYDROGEN-ION CONCENTRATION; MALE; RATS; RATS, WISTAR;

EID: 34250711342     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.106.116939     Document Type: Article

References (26)

1. Bârzu T, Molho P, Tobelem G, Petitou M, and Caen J (1985) Binding and endocytosis of heparin by human endothelial cells in culture. Biochim Biophys Acta 845:196-203.
2. Boneu B (2000) Low molecular weight heparins: are they superior to unfractionated heparins to prevent and to treat deep vein thrombosis? Thromb Res 100:V113-V120.
3. Canadian Pharmaceutical Association (2005) Compendium of Pharmaceuticals and Specialities, Canadian Pharmaceutical Association Ottawa, ON, Canada.
4. Casu B and Gennaro U (1975) A conductimetric method for the determination of sulphate and carboxyl groups in heparin and other mucopolysaccharides. Carbohydr Res 39:168-176.
5. Cooke HJ and Dawson DC (1978) Transport characteristics of isolated newborn rabbit ileum. Am J Physiol 234:E257-E261.
6. Costantini V, Deveglia R, Stabile A, and Nenci GG (2000) Absorption and antithrombotic activity of unfractioned heparin after intraduodenal administration in rats. Blood Coagul Fibrinolysis 11:7-13.
7. Dal Pozzo A, Acquasaliente M, Geron MR, and Andriuoli G (1989) New heparin complexes active by intestinal absorption: I-multiple ion pairs with basic organic compounds. Thromb Res 56:119-124.
8. Eastman IM and Miller EG (1935) Gastrointestinal pH in rats as determined by the glass electrode. J Biol Chem 110:255-262.
9. Engelberg H (1995) Orally ingested heparin is absorbed in humans. Clin Appl Thromb Hemost 1:283-285.
10. Glimelius B, Busch C, and Hook M (1978) Binding of heparin on the surface of cultured human endothelial cells. Thromb Res 12:773-782.
11. Hiebert LM and Jaques LB (1976a) The observation of heparin on endothelium after injection. Thromb Res 8:195-204.
12. Hiebert LM and Jaques LB (1976b) Heparin uptake on endothelium. Artery 2:26-37.
13. Hiebert LM, Wice SM, and Jaques B (1996) Antithrombotic activity of oral unfractionated heparin. J Cardiovasc Pharmacol 28:26-29.
14. Hiebert LM, Wice SM, and Ping T (2005) Increased plasma anti-Xa activity and recovery of heparin from urine suggest absorption of orally administered unfractionated heparin in human subjects. J Lab Clin Med 145:151-155.
15. Hiebert LM, Wice SM, Mcduffie NM, and Jaques LB (1993) The heparin target organ-the endothelium: studies in a rat model. Q J Med 86:341-348.
16. Hiebert LM, Wice SM, Ping T, Herr D, and Laux V (2001) Antithrombotic efficacy in a rat model of the low molecular weight heparin, reviparin sodium, administered by the oral route. Thromb Haemost 85:114-118.
17. 14C-labeled porcine intestinal mucosal heparin following administration to rats by the oral route. Can J Physiol Pharmacol 78:307-320.
18. Hiebert LM, Wice SM, and Abdelhameed T (2007) Evidence for the absorption of heparin by rat stomach. Biomed Pharmacother 61:68-74.
19. Ichikawa T, Ishihara K, Kusakabe T, Hiruma H, Kawakami T, and Hotta K (2000) CGRP modulates mucin synthesis in surface mucus cells of rat gastric oxyntic mucosa. Am J Physiol 79:G82-G89.
20. Jaques LB (1977) Determination of heparin and related sulfated mucopolysaccharides. Methods Biochem Anal 24:203-312.
21. Jaques LB, Hiebert LM, and Wice SM (1991) Evidence from endothelium of gastric absorption of heparin and of dextran sulfates 8000. J Lab Clin Med 117:122-130.
22. Leone-Bay A, Paton DR, Variano B, Leipold H, Rivera T, Miura-Fiura-Fraboni J, Baughman RA, and Santiago N (1998) Acylated non-"-amino acids as novel agents for the oral delivery of heparin sodium, USP. J Control Release 50:41-49.
23. Loomis TA (1959) Absorption of heparin from the intestine. Proc Soc Exp Biol Med 101:447-449.
24. Money SR and York JW (2001) Development of oral heparin therapy for prophylaxis and treatment of deep venous thrombosis. Cardiovasc Surg 9:211-218.
25. Pinel C, Wice SM, and Hiebert LM (2004) Orally administered heparins prevent arterial thrombosis in a rat model. Thromb Haemost 91:919-926.
26. Sue TK, Jaques LB, and Yuen E (1976) Effects of acidity, cations and alcoholic fractionation on absorption of heparin from gastrointestinal tract. Can J Physiol Pharmacol 54:613-617.