A RESEARCH ON FORMULATION AND EVALUATION OF FLOATING MICROSPHERES OF TOLPERISONE HYDROCHLORIDE
Manisha Kumari*, Prasanjit Paul and Dr. Nitin Kumar
ABSTRACT
Tolperisone HCl, a centrally acting muscle relaxant. Tolperisone HCl
with its shorter half life, of 1.5- 2.5 hours, high first pass metabolism
with frequent dosing characteristics makes it suitable candidate for
development of oral controlled release dosage form. Nine formulations
of drug loaded microspheres using three different polymeric
combinations and ratio were prepared by emulsion solvent evaporation
technique. The various polymer used in the formulations were Ethyl
cellulose, Eudragit RS100 & Eudragit S100 (all hydrophobic). Average
particle size ranged from 56.68 μm to 87.50 μm. Percentage yield
ranged from 77.28 to 90.22% and drug entrapment efficiency ranges
from 69.12 to 82.64%. Percentage drug loading was found to be
satisfactory. Kinetics study showed that drug release follows first order kinetics. Batch F4
shows best dissolution profile because of highest similarity factor f2 (f2=75.62) among all the
batches (which ranged from 51.74 to 75.62). FTIR study confirmed the stable character of
Tolperisone HCl in formulations. Scanning electron microscopy revealed that the
microspheres were spherical. Nine different formulations (F1 to F9) of Tolperisone HCl
loaded microspheres were prepared using various polymeric combinations with a view for the
sustained delivery of the drug over a time period of 12 hours.
Keywords: Floating microspheres, Gastro retentive drug delivery system, Emulsion solvent evaporation technique, Muscle relaxant.
[Full Text Article]