SULODEXIDE (INN)
PRODUCT PROFILE
SYNTEX S.A.
Luis De Sarro 501 - (B1838DQK) – Luis Guillón – Buenos Aires – Argentina – Tel./Fax: (54 11) 4367-6100 syntex@syntexar.com –
www.syntexar.com
Brief Introduction
According to Martindale 34° Ed., Sulodexide is a heparinoid consisting of a
mixture of low molecular weight heparin (Fast Moving Heparin, FMH) and
Dermatan Sulfate (DS).
Review of the 14th Annunal Pharmacy Conference on Anticoagulation
Therapy (1999) (1) also defines Sulodexide as a mixture of 80 % low
molecular weight heparin and 20 % dermatan sulfate, total components of
sulodexide being from porcine origin.
Use
Sulodexide (INN) is well known for the treatment of vascular pathologies
with thrombotic risk, such as peripheral occlusive arterial disease,
cardiovascular pathologies, etc.
Due to its hypolipemiant activity (reducing triglycerides and cholesterol
values in plasma), it is used also in the prophylaxis of myocardial reinfarction.
Recently, novel application was found for Sulodexide, in the treatment of
diabetic nephropathy in patients with both insulin and non-insulin dependent
diabetes mellitus.
Strong reduction in albumin excretion was obtained by using Sulodexide in
such cases (2).
The precise mechanism is not known but it may include restoration of the
physiologic glomerular membrane anionic charge via enhanced synthesis
and sulfation of heparin in renal vascular membranes, direct replenishment
of renal heparin sulfate, inhibition of transforming growth factor β 1-mediated
mesangial matrix overproduction, inhibition of mesangial cell hyperplasia,
etc.
Production
Currently, Syntex S.A. is producing Sulodexide at kilo-lab scale.
SYNTEX S.A.
Luis De Sarro 501 - (B1838DQK) – Luis Guillón – Buenos Aires – Argentina – Tel./Fax: (54 11) 4367-6100 syntex@syntexar.com –
www.syntexar.com
Specifications
Appearance:
Solubility (5% soln.):
pH (5% soln.):
Loss on drying:
Organic Sulphur:
Sulphate / carboxylic ratio:
Electrophoresis:
(cellulose acetate,
barium acetate buffer)
OSCS:
Heavy metals:
Anti-clotting activity:
Anti-Xa activity:
Residual solvents:
Total plate count:
E. Coli:
Salmonella:
S. Aureus:
white or almost white powder
clear solution
5.5 - 8.0
not more than 8.0%
7.0 – 11.0% d.b.
≥ 1.5
CS: not more than 5%
DS: 15-25 %
FM: 75-85 %
SM: not more than 5%
absent (NMR-H)
not more than 30 ppm
not more than 70 IU/mg
not less than 50 IU/mg
methanol ≤ 500 ppm
ethanol ≤ 1.5 %
acetone ≤ 1000 ppm
not more than 1000 CFU/g
absent /g
absent / 10 g
absent /g
Note
Ideas and data previously mentioned must be understood just as guidelines in
applications development and not as a recommendation of use against any patent.
SYNTEX S.A.
Luis De Sarro 501 - (B1838DQK) – Luis Guillón – Buenos Aires – Argentina – Tel./Fax: (54 11) 4367-6100 syntex@syntexar.com –
www.syntexar.com
Bibliographic Reference
1. www.uspharmacist.com/ce/antico/lesson.html
2. Palazzini, E. et al, US Patent 7259152
3. Harenberg, J., Journal of Med. Res. Rev., 18, 1-20 (1998)
4. Gambaro, G. et al, J. Am. Soc. Nephr, 11, 359-368 (2000)
5. Skrha, J. et al, Diabetes Res. Clin. Pract., 38, 25-31 (1997)
6. Ofosu, F. et al, Sem. Thromb. Hemost., 24, N° 2, 127-138 (1998)
7. Bianchini, P. et al, US Patent 3936351
8. Edigio et al, US Patent 5236910
9. Marchi et al, US Patent 5496807
10. Baggio et al, US Patent 5686432
SYNTEX S.A.
Luis De Sarro 501 - (B1838DQK) – Luis Guillón – Buenos Aires – Argentina – Tel./Fax: (54 11) 4367-6100 syntex@syntexar.com –
www.syntexar.com