DESIGN AND IN VIVO EVALUATION OF METOPROLOL TARTRATE BILAYER FLOATING TABLETS IN HEALTHY HUMAN VOLUNTEERS

Prasanna kumari Jambarapu, Ramarao T, Jayaveera K N, Bhikshapathi DVRN, Madhusudan Rao Yamsani

Abstract


The aim of the present investigation was to prepare bilayer floating tablets of metoprolol tartrate using the combination of superdisintigrants, HPMC K grade polymers and natural polymers like xanthan gum and guar gum by direct compression method. Bilayer floating tablets were prepared using optimized immediate release layer and floating layer as sustained release layer. The physico-chemical characteristics of the prepared tablets were evaluated and found to be satisfactory. All the prepared batches showed in vitro buoyancy. It was observed that the tablets remained buoyant for more than 12 h.  Formulation F7 was selected as best formulation based on the in vitro characteristics and used in vivo radiographic studies by adding barium sulphate. These studies revealed that the tablets remained in the stomach for 210±5.4 min (n=3) in fasting human volunteers. Based on the in vivo performance in healthy subjects, the developed bilayer floating tablets showed superior bioavailability than the marketed tablets, the drug release was up to 12 h in controlled manner. The systemic availability of the best formulation was high after administration to obtain immediate action due to the immediate release layer, from sustained release layer the drug was released in controlled manner. It can be concluded that the best formulation F7 by choosing biphasic drug release pattern in a single dosage form could improve patient compliance and ensure better disease management.


Keywords


Metoprolol tartrate, superdisintigrants, HPMC, bilayer floating tablets, bioavailability

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