Mechanism of disintegration by superdisintegrants
There are five major mechanisms for tablet disintegration as follows:-
1) Swelling
2) Porosity and Capillary Action (Wicking)
3) Deformation
4) Due to disintegrating particle/particle repulsive forces
5) Enzymatic reaction
Swelling: Swelling is believed to be a mechanism in which certain
disintegrating agents (such as starch) impart the disintegrating effect. By
swelling in contact with water, the adhesiveness of other ingredients in a
tablet is overcome causing the tablet to fall apart. E.g Sodium starch
Glycolate.
Porosity and Capillary Action (Wicking):
Effective disintegrants that do not swell are believed to impart
their disintegrating action through porosity and capillary action. Tablet
porosity provides pathways for the penetration of fluid into tablets. The
disintegrant particles (with low cohesiveness & compressibility) themselves
act to enhance porosity and provide these pathways into the tablet. Liquid is drawn
up or “wicked” into these pathways through capillary action and rupture the
interparticulate bonds causing the tablet to break apart. E.g. Crospovidone,
Crosscarmillose.
Deformation: Starch grains are generally thought to be “elastic” in nature
meaning that grains that are deformed under pressure will return to their
original shape when that pressure is removed. But, with the compression forces involved
in tableting, these grains are believed to be deformed more permanently and are
said to be “energy rich” with this energy being released upon exposure to
water. In other words, the ability for starch to swell is higher in “energy
rich” starch grains than it is for starch grains that have not been deformed
under pressure.
Due to disintegrating particle/particle repulsive forces:
Another mechanism of disintegration attempts to explain the swelling
of tablet made with “nonswellable” disintegrants. Guyot-Hermann has proposed a particle repulsion theory based on
the observation that nonswelling particle also cause disintegration of tablets.
The electric repulsive forces between particles are the mechanism of
disintegration and water is required for it. Researchers found that repulsion
is secondary to wicking. It is believed that no single mechanism is responsible
for the action of most disintegrants. But rather, it is more likely the result
of inter-relationships between these major mechanisms.
By Enzymatic Reaction: Enzymes present in the body also act as disintegrants. These
enzymes enhance the binding action of binder and helps in disintegration. Due
to swelling, pressure is exerted in the outer direction that causes the tablet to
burst or the accelerated absorption of water leads to an enormous increase in
the volume of granules to promote disintegration.
No comments:
Post a Comment