PREPARATION AND IN-VITRO EVALUATION OF APREMILAST EFFERVESCENT FLOATING TABLETSAbstract
Apremilast, the new PDE4 inhibitor drug, exhibits low solubility and low permeability; therefore, shows variable bioavailability. Effervescent floating tablets of apremilast were developed to sustain the drug release rate by increasing gastric retention time. These tablets were prepared by wet granulation technique, using different polymers like carbopol 934P, hydroxypropyl methylcellulose K4M, tragacanth and sodium alginate, either alone or in combination. Prepared tablets were characterized for physical parameters like floating capacity, hardness, % weight variation, friability, and content uniformity. Additionally, tablets were evaluated for in vitro release characteristics for 24 h. Results of this study exhibited good physical properties within the limit of acceptance. Batches prepared by carbo-pol 934P did not show any initial burst release as compared to other polymers. When polymer concentrations were increased drug release rate was decreased. Drug release from the tablets was followed by zero-order controlled release. Sodium alginate/ tragacanth and HPMC K4 in 1:3 ratio exhibited best drug release for 24 h. Carbopol batches (1:3 ratio ) showed very first floating lag time (52 S) but less total floating time (only 8 hrs). However, formulations F5 and F6 (1:7) ratio showed total floating time more than 22 h. From this study we conclude that floating tablets enhance and sustained apremilast release time and would be considered for further in-vivo study.
R. Deshmukh, G. Jeswani and S. D. Paul *
Shri Shankaracharya Technical Campus, Shri Shankaracharya Group of Institutions, Faculty of Pharmaceutical Sciences, Bhilai, Chhattisgarh, India.
17 June 2020
23 October 2020
04 May 2021
01 June 2021