Formulation and Evaluation of Gastroretentive, Sustained Release Floating Beads of Aceclofenac by Non-Effervescent Method

Abstract

Introduction: Bioavailability enhancement for a drug with a short biological half-life and low water solubility is a great challenge for a researcher. Various drug molecules (like metformin HCl, baclofen, etc.), whose major site of intake is the part of the digestive system or the proximal part of the small intestine.

Objectives: The drug Aceclofenac has a relatively low dissolution rate, brief half-life and is readily bypassed by the stomach without effective absorption. To overcome this problem we prepare sustained release gastro-retentive floating non effervescent type multi-particulate system.

Methods: In the present study Gastro-retentive non effervescent type floating bead is prepared using Aceclofenac as a model drug and by using the oil emulsification and ionic gelation process to get better buoyancy of microsphere bead with short lag time for floating and good drug loading capacity.

Results: From the characterization study of optimum floating bead, it is observed that floating time almost 24 hr. with very short floating lag time within 15 seconds, more than 90% drug entrapment efficiency and 12 hours sustained release of drug is observed. The formulation F5 showed high entrapment efficiency (90.12%) as well as more sustained effects.

Conclusion: The present study demonstrated a successful preparation of floating beads of Aceclofenac by emulsion gelation method. These results suggest that developed gastro retentive floating beads can improve the bioavailability of Aceclofenac, reduce its dosing frequency, and enhance its patient compliance.