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Abstract: As Itopride hydrochloride is
gastroprokinetic drug, the site of action is stomach;
and as the drug pH ranges from 3.5 to 5.5, the present
work was aimed to formulate floating tablets of Itopride
hydrochloride using an effervescent approach for
gastroretentive drug delivery system. The present
investigation concerns the development of floating
tablets of Itopride hydrochloride, a novel prokinetic
drug, which after oral administration are designed to
prolong the gastric residence time and thereby increase
drug bioavailability, and drug release rate. Floating
tablets were fabricated; using direct compression
method; containing Itopride hydrochloride, polymers HPMC
K100M, HPMC K15M and Carbopol 934 P, along with gas
generating agent sodium bicarbonate and citric acid. The
addition of Carbopol aided in the reduction of the drug
dissolution due to their hydrophobic nature. The
concentration of these agents was also optimized to get
desired controlled release of drug. The floating tablet
formulations were evaluated for physical
characterization, assay, swelling index, in-vitro drug
release, hardness, friability and weight variation. The
results indicated that gas powered floating tablets of
Itopride hydrochloride containing 125 mg HPMC K100M, 40
mg HPMC K15M, and 40 mg Carbopol provides a better
option for 24 hours release action and improved
bioavailability.
Introduction
Itopride hydrochloride improves GI motility by a dual
mode of action, dopamine D2 receptor blockade and acetyl
cholinesterase inhibitory action. Moreover, it is 5HT4
antagonist unlike cisapride, which is agonist and is
responsible for adverse cardiac effect.
Itopride, by virtue of its dopamine D2 receptor
antagonism, removes the inhibitory effects on
acetylcholine release. It also inhibits the enzyme
acetylcholine esterase that prevents the degradation of
acetylcholine. The net effect is an increase in
acetylcholine concentration, which in turn, promotes
gastric motility, increases the lower esophageal
sphincter pressure, accelerates gastric emptying and
improves gastro-duodenal co-ordination. Itopride
hydrochloride is the drug of first choice in the therapy
of upper dyspepsia. It is a prokinetic drug that
activates the gastrointestinal motility through
synergism of its dopamine D2 - receptor antagonistic
action and its acetylcholine esterase inhibitory action.
In addition to these actions it has an anti-emetic
action that is based on its dopamine D2 receptor
antagonistic action. As Itopride Hydrochloride is a
prokinetic drug and its primary site of action is
stomach and also the drug pH range is 3.5 to 5.5 it
would be beneficial to formulate a floating drug
delivery system of itopride hydrochloride, which would
be once a day formulation. Hence, my objective was to
design and develop floating tablets of Itopride
hydrochloride.
Materials and Methods
Materials
Itopride HCl was received as a gift sample from Micro
Labs Ltd., Hosur (TN). HPMC K15M, HPMC K100M, Carbopol
934P was procured by signets drug pvt.ltd,Mumbai. Sodium
bicarbonate, Citric acid,PVP-K30, Magnesium stearate,
Talc, Aesosil were procured from Nice chem., Cochin. All
other reagents used were of analytical grade and
procedure from commercial sources.
1.Formulation of Hydrodyamically Balanced Tablets
Itopride HCl
Floating tablets containing Itopride HCl were prepared
by direct compression technique using varying
concentrations of different grades of polymers with
sodium bicarbonate and citric acid. All the ingredients
were accurately weighed and sifted through different
mesh sieves accordingly. Then, except magnesium stearate,
all other ingredients were blended in glass mortar
uniformly. After sufficient mixing of drug as well as
other components, magnesium stearate was added, as post
lubricant, and further mixed for additional 2-3 minutes.
The tablets were compressed with 11mm punch using rotary
tablet machine. The weights of the tablets were kept
constant for all formulation.Hydro-dynamically balanced
tablets of Itopride HCl were prepared and evaluated for
their use as gastroretentive drug delivery systems to
increase its local action and bioavailability.
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