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THE PHARMA REVIEW (SEPTEMBER 2009)

Development and Optimization of the of Hydrodyamically Balanced Tablets of Itopride Hydrochloride

R.Margret chandira, Debjit.B. , B.S.Venkataeswarlu, Chiranjib.B, M.V..Kumudhavalli, B.Jayakar

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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