gouthami polaki
Nansri Saha
Abstract
Oil entrapped floating calcium alginate beads of Telmisartan were successfully prepared using sodium
alginate as polymer and two different oil phases of mineral oil and olive oil by emulsion gelation method.
The FT-IR spectra of final optimized formulation confirms no drug- polymer incompatibility. The
floating time of beads was found to be more than 12 hrs suggesting that the method used for prepration
was effective. The floating time of optimized formulation was within 6 minutes and floating time
significantly increased as the amount of oil was increased in each formulation. The mean particle size
of beads was in range from (1.204 mm to 2.0072 mm) depending upon the type of polymer used. The
particle size increased significantly as the amount of polymer was increased in each preparation.
The %Entrapment efficiency of beads ranging from41.14%–85.79% increased in concentration of
polymer leads to increase in entrapment efficiency. The best formulation of oil entrapped floating
calcium alginate beads of Telmisartan for mineral oil was found to be F5 98.03% and for Olive oil oil
was found to be F7 96.7%, drug release in 12 hrs. The release kinetics of the optimized Telmisartan
loaded oil entrapped beads showed that it follows Higuchi release kinetics. The release of the drug from
the dosage form is carried out by diffusion and follows Korsmeyer peppas kinetics and the n value is
greater than 0.5 indicating non-Fickian release. The floating beads have been employed to make a
sustained release of the drug in the stomach to enhance bioavailability and to decrease dose dumping
and hence overcome its side effects. The developed formulation shows an alternative to the conventional
dosage form for the treatment of Telmisartan, a nonsedating antihistamine H1 blocker used for seasonal
allergic rhinitis and chronic idiopathic urticaria has limited absorption in the upper small intestine
with poor oral bioavailability. Hence finally it was concluded that the prepared oil entrapped floating
sodium alginate beads of Telmisartan may prove to
be potential candidate for safe and effective
sustained drug delivery over an extended period of
time which can reduce dosing frequency and
improved oral bioavailability.
Keywords: Gastroretentive Delivery System, Floating Alginate Beads Bioavailability, Telimisartan
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