PMID- 33030036 OWN - NLM STAT- MEDLINE DCOM- 20201019 LR - 20240329 IS - 1938-2723 (Electronic) IS - 1076-0296 (Print) IS - 1076-0296 (Linking) VI - 26 DP - 2020 Jan-Dec TI - Comparative Anticoagulant and Thrombin Generation Inhibitory Profile of Heparin, Sulodexide and Its Components. PG - 1076029620954913 LID - 10.1177/1076029620954913 [doi] LID - 1076029620954913 AB - INTRODUCTION: Sulodexide represents a mixture of fast-moving heparin (FMH) and dermatan sulfate (DS) and has been used for the management of venous diseases such as DVT and related disorders. The purpose of this study is to compare sulodexide and its components with unfractionated heparin (UFH) to determine its suitability for the indications in which UFH is used. MATERIALS AND METHOD: Active pharmaceutical ingredients (API) versions of sulodexide, FMH and DS were obtained from Alfasigma. API versions of UFH were obtained from Medefil Inc. Normal human citrated plasma was obtained from blood bank of the Loyola University Medical Center. Each of the individual agents were supplemented in plasma at a graded concentration of 0.0-10 microg/mL. Clotting assays (PiCT, aPTT, PT and TT), anti-Xa and anti-IIa and thrombin generation studies were carried out. Results were compiled as mean +/- SD of 3 individual determination. RESULT: In the clot based (PiCT, aPTT and TT), anti-Xa and IIa assays, both the UFH and FMH produced stronger activities in these assays followed by sulodexide. DS did not show any anticoagulant activity. In the thrombin generation assay, FMH and UFH produced comparable inhibition of thrombin generation as measured by various parameters. Sulodexide was slightly weaker in this assay, whereas DS produced relatively weaker effects. CONCLUSION: In comparison to sulodexide, both UFH and FMH exhibit comparable anticoagulant activity despite differences in their molecular weight. These results suggest that sulodexide can be developed as a parenteral anticoagulant for indications in which UFH is used. FAU - Siddiqui, Fakiha AU - Siddiqui F AUID- ORCID: 0000-0002-2219-7049 AD - Department of Pathology and Laboratory Medicine, Cardiovascular Research Institute, Loyola University Chicago, Health Sciences Division, Maywood, IL, USA. FAU - Hoppensteadt, Debra AU - Hoppensteadt D AUID- ORCID: 0000-0001-9342-4213 AD - Department of Pathology and Laboratory Medicine, Cardiovascular Research Institute, Loyola University Chicago, Health Sciences Division, Maywood, IL, USA. AD - Department of Pharmacology and Neuroscience, Cardiovascular Research Institute, Loyola University Chicago, Health Sciences Division, Maywood, IL, USA. FAU - Bontekoe, Emily AU - Bontekoe E AD - Department of Pathology and Laboratory Medicine, Cardiovascular Research Institute, Loyola University Chicago, Health Sciences Division, Maywood, IL, USA. FAU - Farooqui, Ambar AU - Farooqui A AD - Department of Pathology and Laboratory Medicine, Cardiovascular Research Institute, Loyola University Chicago, Health Sciences Division, Maywood, IL, USA. FAU - Jeske, Walter AU - Jeske W AD - Department of Pathology and Laboratory Medicine, Cardiovascular Research Institute, Loyola University Chicago, Health Sciences Division, Maywood, IL, USA. AD - Department of Thoracic and Cardiovascular Surgery, Cardiovascular Research Institute, Loyola University Chicago, Health Sciences Division, Maywood, IL, USA. FAU - Fareed, Jawed AU - Fareed J AUID- ORCID: 0000-0003-3465-2499 AD - Department of Pharmacology and Neuroscience, Cardiovascular Research Institute, Loyola University Chicago, Health Sciences Division, Maywood, IL, USA. LA - eng PT - Comparative Study PT - Journal Article PL - United States TA - Clin Appl Thromb Hemost JT - Clinical and applied thrombosis/hemostasis : official journal of the International Academy of Clinical and Applied Thrombosis/Hemostasis JID - 9508125 RN - 0 (Anticoagulants) RN - 0 (Antithrombins) RN - 0 (Glycosaminoglycans) RN - 75HGV0062C (glucuronyl glucosamine glycan sulfate) RN - 9005-49-6 (Heparin) RN - EC 3.4.21.5 (Thrombin) SB - IM MH - Anticoagulants/administration & dosage/*pharmacology MH - Antithrombins/administration & dosage/pharmacology MH - Blood Coagulation/*drug effects MH - Glycosaminoglycans/administration & dosage/*pharmacology MH - Heparin/administration & dosage/pharmacology MH - Humans MH - Italy MH - Sensitivity and Specificity MH - Thrombin/administration & dosage/*pharmacology PMC - PMC7549168 OTO - NOTNLM OT - COVID-19 OT - dermatan sulfate OT - fast moving heparin OT - sulodexide OT - thrombin generation inhibition OT - unfractionated heparin COIS- Declaration of Conflicting Interests: The author(s) declared no potential conflicts of interest with respect to the research, authorship, and/or publication of this article. EDAT- 2020/10/09 06:00 MHDA- 2020/10/21 06:00 PMCR- 2020/10/08 CRDT- 2020/10/08 08:44 PHST- 2020/10/08 08:44 [entrez] PHST- 2020/10/09 06:00 [pubmed] PHST- 2020/10/21 06:00 [medline] PHST- 2020/10/08 00:00 [pmc-release] AID - 10.1177_1076029620954913 [pii] AID - 10.1177/1076029620954913 [doi] PST - ppublish SO - Clin Appl Thromb Hemost. 2020 Jan-Dec;26:1076029620954913. doi: 10.1177/1076029620954913.