Lipid soluble thiamin derivatives

The transport system is saturated at relatively low concentrations of thiamin (about 2 /xmol per L), thus limiting the amount of thiamin that can be absorbed. As a result, increasing test doses of thiamin from 2.5 to 20 mg have only a negligible effect on the plasma concentration of thiamin or on urinary excretion. By contrast, the absorption of lipid-soluble aUithiamin derivatives is not apparendy saturable, and they can be used to achieve high blood concentrations of thiamin. 

Volvert, M.L., Seyen, S., Piette, M., et al. (2008) Benfotiamine, a synthetic S-acyl thiamine derivative, has different mechanisms of action and a different pharmacological profile than lipid-soluble thiamine disulfide derivatives. BMC Pharmacol. 8, 10. 

Benfotiamine, a lipid-soluble thiamine (vitamin Bl) derivative, prevents the increase in the intracellular hexosamine pathway and polyol pathway activation during hyperglycaemia [53]. It decreases hyperglycaemia-induced intracellular AGE formation... 

Synthetic allithiamin derivatives, such as thiamin propyl and tetrahydro-furfuryl disulfides, have been used for the prevention and treatment of thiamin deficiency. Because they are lipid soluble, and are not subject to the normal control of thiamin absorption by saturation of the intestinal transport system, they have potential benefits in the treatment of thiamin-deficient alcoholics, whose absorption of thiamin is impaired. 

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