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About Orafate™ 

Pharmacology of Orafate™ 

The clinical efficacy of any topical agent is limited to the concentration achieved in its 
surface application. The surface concentration achieved by standard potency sucralfate does 
not allow for accelerated healing, pain relief and reduction of infection as does Orafate™.  

Orafate™ achieves surface concentrations of sucralfate that contribute directly to its 
ability to treat oral mucosal wounds.  As discussed below, 3 hours post administration, 
Orafate™ maintains sucralfate concentrations that are 800-2400% greater than that of generic 
sucralfate of identical formulary strength (1gram/10ml). 

This is due to the unique polymerization of sucralfate within Orafate™  that transpires 
between sucralfate and calcium-chelated malate. Instead of singular sucralfate molecules 
suspended in a liquid or gel, sucralfate polymerizes into sheets in Orafate™ and gives 
rise to a stackable egg-crate configuration of sucralfate.

PHARMACOLOGY OF ENHANCED MUCO-ADHERENCE
Orafate™ differs substantially from other oral hydrogel oral devices. Its proprietary system 
of polymerization converts generic sucralfate molecules into sucralfate sheets. This conversion 
from singular suspended sucralfate to “sheets” of sucralfate enhances the surface concentration 
or potency of sucralfate in Orafate™. Sucralfate ‘sheets’ are termed high potency sucralfate.

Muco-Adherence Study: Rabbits with acetic acid-induced erosion of the pharyngeal, esophageal, 
gastric and colonic mucosa, received a single 14mg per kg dose of either 10% generic potency 
sucralfate suspension (n=4) or 10% high potency sucralfate  (HPS) suspension (n =4) then 
euthanized 3 hours later. One centimeter square samples of ulcerated and non-ulcerated mucosa 
were evaluated for the surface concentration of sucralfate by atomic absorption of adherent 
aluminum. The sucralfate surface concentration of 10% high potency sucralfate exceeded that of 
10% standard potency sucralfate by several fold, achieving surface concentrations 23 times (2400%) 
higher on acid injured mucosa and 7 times (800%) higher on normal 
un-injured mucosa as shown in Table 1.

Table 1


BI-MODAL ACTION: Mechanical and Mucosa-Mediated
The entirety of the clinical efficacy of sucralfate in Orafate™ resides in its physical contact 
with the mucosa. The clinical effects of this physical contact are conveyed through two modes of 
action – one is physiochemical, while the other is mucosally mediated. The latter is secondary to 
effects of Orafate™  on mucosa-based receptors that are responsible for pain and on growth 
factors that mediate the balance between pro-inflammatory and anti-inflammatory cytokines. 

The physiochemical interaction of sucralfate involves its engagement of saliva, mucus and the 
epithelium – the traditional “band-aid” effect. The second mode of action involves 
micro-environmental changes immediate to nociceptor membranes and the incidental contact of 
sucralfate with growth factors, the latter of which is believed to contribute to accelerated 
wound healing.

Sucralfate ‘sheets’ physically cover the immediate micro-environment of surrounding nociceptors 
in the mucosal lining. Stimulated receptors switched on by ion-fluxes across their surface 
membrane lead to pain and continued inflammation. The electro-negative micro-environ created by
high potency sucralfate switches off ion-fluxes across nociceptor membranes returning them to normal 
neutral state. The presumed subsidence of ion-fluxes across receptor membranes due to sucralfate 
sheets is believed to be the basis for symptom relief upon contact with Orafate™.

The coating action of ‘sucralfate sheets’ in Orafate™ affect the movement and activation of growth 
factors by spatially limiting their movement on the mucosal lining. Injured and ulcerated mucosal 
cells both increase their secretion of growth factors and their expression of growth factor receptors 
on membranes of damaged and nearby cells. This combination of events – enhanced secretion of 
growth factors and increased expression of growth factor receptors – result from the a cytokine 
imbalance favoring pro-inflammatory over anti-inflammatory cytokines.  The macromolecular bulk of 
‘sucralfate  sheets’ facilitate the engagement of growth factor with their nearby receptors thereby 
restoring cytokine balance in the mucosa, and accelerating healing. 

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