Abstract
Objective: The present study was undertaken with an objective to design, develop and evaluate gastro retentive floating tablets of an antihypertensive drug, quinapril HCl, which release the drug in a sustained manner over a period of 12 h.Methods: In this research work, we used hydrophilic polymer hydroxypropyl methylcellulose (HPMC K4M), the gas generating agent sodium bicarbonate and citric acid at different ratios for the preparation of tablets. A 32 factorial design was applied systematically; the amount of HPMC K4M (X1) and the amount of citric acid (X2) were selected as independent variables. The dependent variables chosen were percentage drug release at 6 h (Q6), percentage drug release at 12 h (Q12) and floating lag time. The high concentration of HPMC K4M and citric acid gives a sustained release for quinapril HCl floating tablets. The tablets were prepared by direct compression technique and evaluated for tablet thickness, hardness, weight variation, friability, floating lag time and In vitro drug release.Results: The In vitro drug release indicated the floating dosage forms showed slower release when the concentration of HPMC K4M increases. Formulation F4 having ratio 25:8 (HPMC K4M: citric acid) was considered as an optimised formulation which shows satisfactory sustained drug release and remained buoyant on the surface of the medium for more than 12 h. It can also conclude that floating drug delivery system of quinapril HCl can be successfully formulated as an approach to increase gastric residence time and thereby improving its bioavailability.Conclusion: The developed effervescent based floating tablets are a promising floating drug delivery system for oral sustained administration of quinapril HCl.
Highlights
The oral drug delivery is most widely used routes of administration in all different routes that have been utilized for systemic delivery of drugs from the different dosage form
floating drug delivery systems (FDDS) of quinapril HCl were prepared by using polymer hydroxypropyl methylcellulose (HPMC K4M), and using sodium bicarbonate and citric acid as the gas generating agent
It was concluded that quinapril HCl floating drug delivery systems prepared by direct compression method using HPMC K4M as a polymer and citric acid and sodium bicarbonate as the gas generating agent
Summary
The oral drug delivery is most widely used routes of administration in all different routes that have been utilized for systemic delivery of drugs from the different dosage form. To prolong the residence time of dosage forms within gastrointestinal tract until all drug is released at desired rate is one of the real challenges for oral controlled-release drug delivery system. In the present research work, gastro-retentive dosage forms gives more attention due to they can improve the performance of floating controlled release drug delivery systems. Several technical approaches are currently utilized in the prolongation of gastric residence time, including high density, swelling and expanding, polymeric mucoadhesive, ion-exchange, raft forming, magnetic and floating drug delivery systems (FDDS), as well as other delayed gastric emptying devices [1, 2]
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