The objective of this work was to use a full factorial design and response surface methodology to optimize and prepare fast disintegrating tablets of Itopride hydrochloride (ITOHCl). Tablets were prepared by direct compression technique and evaluated for their drug content, weight variation, hardness, friability, wetting, disintegration time, and in-vitro release. In addition, the optimum formulation was evaluated for taste, mouth feel and in-vivo disintegration time in human volunteers. A 32 full factorial design was employed to evaluate different variables affecting ITOHCl tablets. Furthermore, The response surface methodology was used to analyze the effect of the total amounts of superdisintegrant (SD, X1) and the percentage of sodium starch glycolate (% SSG) in the total amounts of superdisintegrant (SSG, X2) on the % friability (Y1), Disintegration time (Y2) and ITOHCl released after 10 mins (Y3). The increase in the (SD, X1) led to an increase in the % friability while an increase in % SSG led to a decrease in the % friability. The (SD, X1) were found to have a positive influence on the disintegration time, whereas the % SSG had a non-significant effect on the disintegration time. In addition, the release of ITOHCl from different formulations was affected by both (SD, X1) and the percentage of SSG. The optimized formulation showed in-vivo disintegration time comes in accordance with the in-vitro data and has a good mouth feel and bitter taste masking character compared with commercial ITOHCl tablets.

The objective of this work was to use a full factorial design and response surface methodology to optimize and prepare fast disintegrating tablets of Itopride hydrochloride (ITOHCl). Tablets were prepared by direct compression technique and evaluated for their drug content, weight variation, hardness, friability, wetting, disintegration time, and in-vitro release. In addition, the optimum formulation was evaluated for taste, mouth feel and in-vivo disintegration time in human volunteers. A 32 full factorial design was employed to evaluate different variables affecting ITOHCl tablets. Furthermore, The response surface methodology was used to analyze the effect of the total amounts of superdisintegrant (SD, X1) and the percentage of sodium starch glycolate (% SSG) in the total amounts of superdisintegrant (SSG, X2) on the % friability (Y1), Disintegration time (Y2) and ITOHCl released after 10 mins (Y3). The increase in the (SD, X1) led to an increase in the % friability while an increase in % SSG led to a decrease in the % friability. The (SD, X1) were found to have a positive influence on the disintegration time, whereas the % SSG had a non-significant effect on the disintegration time. In addition, the release of ITOHCl from different formulations was affected by both (SD, X1) and the percentage of SSG. The optimized formulation showed in-vivo disintegration time comes in accordance with the in-vitro data and has a good mouth feel and bitter taste masking character compared with commercial ITOHCl tablets.

Itopride HCl is a novel prokinetic agent. It is used mainly in gastroesophageal reflux disease. The objective of this investigation was to formulate sustained release matrix tablets of Itopride HCl using different polymer and polymer combinations to prolong the drug release over 12 hours hence improve patient compliance and minimize side effects. The tablets of Itopride HCl were prepared using different cellulosic polymers and methacrylate copolymers (Eudragits) in various ratios. The in-vitro drug release was carried out using the pH shift method. Optimization of polymer concentration that controls the drug release was performed. Bioavailability study on rabbits was performed to investigate the rate and extent of Itopride HCl absorption from the optimum formulated tablet compared to that of commercial immediate release tablets (Ganaton®). The drug release was found to depend upon the polymer type and concentration. Sustained release tablets containing either hydroxypropyl methyl cellulose or Eudragit RSPM in 1:3 (drug: polymer, weight ratio) gave the most sustaining effect among the single polymers. The drug release rate from tablets prepared using polymer combinations is slower compared to that from matrices containing single polymers. Tablets containing drug, hydroxypropyl methylcellulose and Eudragit RSPM in weight ratio of 1:1:3 gave the slowest drug release rate. The time for reaching peak plasma concentration (Tmax) and the area under the curve from zero to 24 h AUC(0– 24) were higher following formulated tablet administration compared to the marketed tablets. The percentage relative bioavailability of Itopride HCl from the selected formula was found to be 129%.

Itopride HCl is a novel prokinetic agent. It is used mainly in gastroesophageal reflux disease. The objective of this investigation was to formulate sustained release matrix tablets of Itopride HCl using different polymer and polymer combinations to prolong the drug release over 12 hours hence improve patient compliance and minimize side effects. The tablets of Itopride HCl were prepared using different cellulosic polymers and methacrylate copolymers (Eudragits) in various ratios. The in-vitro drug release was carried out using the pH shift method. Optimization of polymer concentration that controls the drug release was performed. Bioavailability study on rabbits was performed to investigate the rate and extent of Itopride HCl absorption from the optimum formulated tablet compared to that of commercial immediate release tablets (Ganaton®). The drug release was found to depend upon the polymer type and concentration. Sustained release tablets containing either hydroxypropyl methyl cellulose or Eudragit RSPM in 1:3 (drug: polymer, weight ratio) gave the most sustaining effect among the single polymers. The drug release rate from tablets prepared using polymer combinations is slower compared to that from matrices containing single polymers. Tablets containing drug, hydroxypropyl methylcellulose and Eudragit RSPM in weight ratio of 1:1:3 gave the slowest drug release rate. The time for reaching peak plasma concentration (Tmax) and the area under the curve from zero to 24 h AUC(0– 24) were higher following formulated tablet administration compared to the marketed tablets. The percentage relative bioavailability of Itopride HCl from the selected formula was found to be 129%.

Itopride HCl is a novel prokinetic agent. It is used mainly in gastroesophageal reflux disease. The objective of this investigation was to formulate sustained release matrix tablets of Itopride HCl using different polymer and polymer combinations to prolong the drug release over 12 hours hence improve patient compliance and minimize side effects. The tablets of Itopride HCl were prepared using different cellulosic polymers and methacrylate copolymers (Eudragits) in various ratios. The in-vitro drug release was carried out using the pH shift method. Optimization of polymer concentration that controls the drug release was performed. Bioavailability study on rabbits was performed to investigate the rate and extent of Itopride HCl absorption from the optimum formulated tablet compared to that of commercial immediate release tablets (Ganaton®). The drug release was found to depend upon the polymer type and concentration. Sustained release tablets containing either hydroxypropyl methyl cellulose or Eudragit RSPM in 1:3 (drug: polymer, weight ratio) gave the most sustaining effect among the single polymers. The drug release rate from tablets prepared using polymer combinations is slower compared to that from matrices containing single polymers. Tablets containing drug, hydroxypropyl methylcellulose and Eudragit RSPM in weight ratio of 1:1:3 gave the slowest drug release rate. The time for reaching peak plasma concentration (Tmax) and the area under the curve from zero to 24 h AUC(0– 24) were higher following formulated tablet administration compared to the marketed tablets. The percentage relative bioavailability of Itopride HCl from the selected formula was found to be 129%.

Itopride HCl is a novel prokinetic agent. It is used mainly in gastroesophageal reflux disease. The objective of this investigation was to formulate sustained release matrix tablets of Itopride HCl using different polymer and polymer combinations to prolong the drug release over 12 hours hence improve patient compliance and minimize side effects. The tablets of Itopride HCl were prepared using different cellulosic polymers and methacrylate copolymers (Eudragits) in various ratios. The in-vitro drug release was carried out using the pH shift method. Optimization of polymer concentration that controls the drug release was performed. Bioavailability study on rabbits was performed to investigate the rate and extent of Itopride HCl absorption from the optimum formulated tablet compared to that of commercial immediate release tablets (Ganaton®). The drug release was found to depend upon the polymer type and concentration. Sustained release tablets containing either hydroxypropyl methyl cellulose or Eudragit RSPM in 1:3 (drug: polymer, weight ratio) gave the most sustaining effect among the single polymers. The drug release rate from tablets prepared using polymer combinations is slower compared to that from matrices containing single polymers. Tablets containing drug, hydroxypropyl methylcellulose and Eudragit RSPM in weight ratio of 1:1:3 gave the slowest drug release rate. The time for reaching peak plasma concentration (Tmax) and the area under the curve from zero to 24 h AUC(0– 24) were higher following formulated tablet administration compared to the marketed tablets. The percentage relative bioavailability of Itopride HCl from the selected formula was found to be 129%.