About ProThelial
Difference Between ProThelial and Ordinary Sucralfate
Difference between ProThelial and Ordinary Sucralfate
Why polymerized cross-linked sucralfate is associated with 2-3 day reversal
of mucositis while ordinary sucralfate is not, can be explained by understanding the
chemistry of the two and a review of literature.
The Chemistry
Polymerized cross-linked sucralfate achieves and maintains a surface concentration of
sucralfate, three hours following administration, that is 800% greater on normal
mucosal lining and 2,400% greater on ulcerated mucosal lining [ Kashimura K, Ozawa K
(1999) Sucralfate Preparations. US Patent 5,968,906. Oct 19, 1999. ]. Chemically,
standard potency sucralfate (such as Carafate, or generic sucralfate) is more easily
hydrated by water. Hydrated sucralfate remains in solution, making less of it available
for adherence to the lining.
Polymerization with multi-dentate chelators convert singular sucralfate into
energetically stable sheets of sucralfate preferred over hydration by water. Polymerized
sheets of sucralfate are cross-linked by chelatable multivalent cations which lead to
energetically preferred pi-stacking (or pancaking) on to itself thereby achieving and
maintaining high surface concentrations of sucralfate. Pi-stacking is a phenomenon
common to electro-dense compounds [ McGaughey GB, Gagnes M, Rappe AK (1998)
Pi-stacking interactions. J Biol Chem 273(25): 15458-15463; Ma JC, Dougherty DA.
The Cation-Pi interaction (1997) Chem Rev 97:1303-1324. ] which sucralfate is, and
which sucralfate sheets exaggerate.
Standard Sucralfate Is Not Polymerized Cross-Linked Sucralfate [PCLS]