Floating system for enhancing dissolution rate of pioglitazone

Abstract

Introduction: Due to basic properties, piogitazone is slowly dissolved in the intestine lupr, and increased dissolution rate of this drug may leads to elevated bioavailability. Therefore, it is expected that by providing a floating form and increasing the residence time of the drug in the stomach, the dissolution rate and then sabsequently bioavailibility of pioglitazone may increased. Aim: Preparation of a floating system for pioglitazone for enhancing of dissolution rate in stomach. Materials and Methods: Polymers and suitable excipients such as (HPMC), carbopol and psyllium, lactose, tragacanth, calcium carbonate and magnesium stearate in defferent ratio were used for the preparation of floating tablets by direct compression method. Dissolution test and also evaluating of boutancy behavior were studied. Finally the DSC spectra were taken. Results: Formulations with equal amounts of the three polymers were not floated and tablets were not disintegrated during 24 hours. Formulations containing high amounts of psyllium were finally disintegrated after 30 minutes. Carbomer containing tablets also had 3 to 4 seconds lag-time and floated 1 to 3 hours. However, carbomer-only containing tablets were disintegrated during few minutes. HPMC-only containing formulations also showed a 20 minutes lag-time with a 90 minutes duration time. Psyllium-only containing formulations were also disintegrated faster; however, combination of HPMC and psyllium in the formulations caused an increased duration time and were not disintegrated during 24 hours. Suitable releas profile was obtained during the 3 hr. DSC results rouled out any interaction between the drug and applied excipients. Conclusion: Selected formulations are able to be floated for 3 hours and proper dissolution rate was ontained, which may increase the bioavailability of the drug.