FORMULATION, IN VITRO, AND IN VIVO EVALUATION OF TASTE-MASKED ORAL DISINTEGRATING TABLETS OF FEXOFENADINE HYDROCHLORIDE USING SEMISYNTHETIC AND NATURAL SUPERDISINTEGRANTS

Objective: The aim of the present research work was to prepare and evaluate taste-masked oral disintegrating tablets (ODT) of Fexofenadine hydrochloride. Methods: In the present work, Eudragit EPO, a taste masking agent and Karaya gum (GK) (natural), Sodium starch glycolate, and Croscarmellose sodium (CCS) (semi-synthetic) super disintegrants in three ratios (3, 6,9%) were used. Taste masked granules were prepared by different ratios of the drug: Eudragit EPO (1:1, 1:1.5, 1:2) by wet granulation method. The optimized taste-masked granules (1:2) were selected by sensory evaluation test to prepare 9 Fexofenadine ODT (FH1-FH9) formulations. These were evaluated for different parameters. Then desirability function (DF) was calculated for all formulations using disintegration time (DT), time taken for the tablet to release 90% of the drug (t 90%), and % drug dissolved in 10 min (Q10) as significant parameters. Results: The best formulation (FH6) showed the highest DF value due to less DT and 100% in vitro drug release within 15 min. Thus, FH6 formulation containing 9% CCS was selected as the best among the prepared formulations to which in vivo studies were performed on rabbits to find maximum plasma concentration (Cmax), time taken to reach maximum concentration (tmax), area under the curve (AUC), rate of elimination (Kel), absorption rate (Ka) and half-life(t1/2) and compared with Fexofenadine (Allegra) marketed tablets. Total bioavailability was increased for the test formulation compared to the reference formulation. Conclusion: Fexofenadine was successfully prepared as ODT with increased AUC and decreased tmax to which stability studies were conducted which were found to be stable

Design, Characterization and Evaluation of Metallic Nano Biocomposites of Neomycin

Neomycin is formulated into nanoparticles in order to increase the therapeutic efficacy, decrease the dose of drug and to decrease the topical dose related toxic effects. The present study was aimed at the preparation of zinc nanoparticles (ZN), chitosan nanoparticles (CN), zinc neomycin nanoparticles (ZNN) and zinc chitosan neomycin nanoparticles (ZCNN) in order to compare their antibacterial activity. Nanoparticles were prepared by subjecting the nano suspension containing the specified ingredients to stirring at 40oC for 4-5 h. The prepared nanoparticles were evaluated for particle size and surface morphology by Transmission Electron Microscopy (TEM), mean particle size and particle size distribution by DLS, percentage yield, loading efficiency, in vitro drug release by diffusion technique and agar cup plate method. TEM microphotographs and zeta sizer analysis revealed that the prepared nanoparticles were in the nanometric range, the particle size and particle size range of ZCNN was less compared to ZNN indicated more surface area of ZCNN. Among all the nanoparticles prepared, percentage yield, loading efficiency, in vitro drug release and zone of inhibition was found to be more for ZCNN. Thus, the results suggested that ZCNN act as promising drug delivery systems with better in vitro characteristics compared to other nanoparticles with increased therapeutic activity of neomycin

FORMULATION, IN VITRO, AND IN VIVO EVALUATION OF TASTE-MASKED ORAL DISINTEGRATING TABLETS OF FEXOFENADINE HYDROCHLORIDE USING SEMISYNTHETIC AND NATURAL SUPERDISINTEGRANTS

Objective: The aim of the present research work was to prepare and evaluate taste-masked oral disintegrating tablets (ODT) of Fexofenadine hydrochloride. Methods: In the present work, Eudragit EPO, a taste masking agent and Karaya gum (GK) (natural), Sodium starch glycolate, and Croscarmellose sodium (CCS) (semi-synthetic) super disintegrants in three ratios (3, 6,9%) were used. Taste masked granules were prepared by different ratios of the drug: Eudragit EPO (1:1, 1:1.5, 1:2) by wet granulation method. The optimized taste-masked granules (1:2) were selected by sensory evaluation test to prepare 9 Fexofenadine ODT (FH1-FH9) formulations. These were evaluated for different parameters. Then desirability function (DF) was calculated for all formulations using disintegration time (DT), time taken for the tablet to release 90% of the drug (t 90%), and % drug dissolved in 10 min (Q10) as significant parameters. Results: The best formulation (FH6) showed the highest DF value due to less DT and 100% in vitro drug release within 15 min. Thus, FH6 formulation containing 9% CCS was selected as the best among the prepared formulations to which in vivo studies were performed on rabbits to find maximum plasma concentration (Cmax), time taken to reach maximum concentration (tmax), area under the curve (AUC), rate of elimination (Kel), absorption rate (Ka) and half-life(t1/2) and compared with Fexofenadine (Allegra) marketed tablets. Total bioavailability was increased for the test formulation compared to the reference formulation. Conclusion: Fexofenadine was successfully prepared as ODT with increased AUC and decreased tmax to which stability studies were conducted which were found to be stable.</jats:p

Microbial Metabolism and Inhibition Studies of Phenobarbital

Purpose: Screening scale studies were performed with eight cultures for their ability to metabolize phenobarbital, an antiepileptic, sedative, hypnotic and substrate for CYP 2C9 and 2C19. Methods: The transformation of phenobarbital was confirmed and characterized by fermentation techniques, high performance liquid chromatography (HPLC), mass spectrometry (MS) and metabolism inhibition studies. Results: Among the different cultures screened, a fungus, Rhizopus stolonifer NCIM 880, transformed phenobarbital to its metabolite, the N-glucuronide of p- hydroxy phenobarbital. HPLC data show a solvent peak at 2.4 min, culture components peaks at 4.0 and 5.4 min, respectively, and phenobarbital peak at 10.3 min, for both controls and test samples, but only the sample of Rhizopus stolonifer showed an additional peak at 3.1 min, indicating formation of a metabolite. Conclusion: Microbial metabolism of phenobarbital was similar to the metabolism of the drug in mammals. Therefore, Rhizopus stolonifer can be used as a suitable in vitro model to mimic CYP 2C9 metabolism and to synthesize metabolites required for further pharmacological and toxicological studies

Microbial Metabolism and Inhibition Studies of Phenobarbital

Purpose: Screening scale studies were performed with eight cultures for their ability to metabolize phenobarbital, an antiepileptic, sedative, hypnotic and substrate for CYP 2C9 and 2C19. Methods: The transformation of phenobarbital was confirmed and characterized by fermentation techniques, high performance liquid chromatography (HPLC), mass spectrometry (MS) and metabolism inhibition studies. Results: Among the different cultures screened, a fungus, Rhizopus stolonifer NCIM 880, transformed phenobarbital to its metabolite, the N-glucuronide of p- hydroxy phenobarbital. HPLC data show a solvent peak at 2.4 min, culture components peaks at 4.0 and 5.4 min, respectively, and phenobarbital peak at 10.3 min, for both controls and test samples, but only the sample of Rhizopus stolonifer showed an additional peak at 3.1 min, indicating formation of a metabolite. Conclusion: Microbial metabolism of phenobarbital was similar to the metabolism of the drug in mammals. Therefore, Rhizopus stolonifer can be used as a suitable in vitro model to mimic CYP 2C9 metabolism and to synthesize metabolites required for further pharmacological and toxicological studies

Microbial Metabolism and Inhibition Studies of Phenobarbital

Purpose: Screening scale studies were performed with eight cultures for their ability to metabolize phenobarbital, an antiepileptic, sedative, hypnotic and substrate for CYP 2C9 and 2C19. Methods: The transformation of phenobarbital was confirmed and characterized by fermentation techniques, high performance liquid chromatography (HPLC), mass spectrometry (MS) and metabolism inhibition studies. Results: Among the different cultures screened, a fungus, Rhizopus stolonifer NCIM 880, transformed phenobarbital to its metabolite, the N-glucuronide of p- hydroxy phenobarbital. HPLC data show a solvent peak at 2.4 min, culture components peaks at 4.0 and 5.4 min, respectively, and phenobarbital peak at 10.3 min, for both controls and test samples, but only the sample of Rhizopus stolonifer showed an additional peak at 3.1 min, indicating formation of a metabolite. Conclusion: Microbial metabolism of phenobarbital was similar to the metabolism of the drug in mammals. Therefore, Rhizopus stolonifer can be used as a suitable in vitro model to mimic CYP 2C9 metabolism and to synthesize metabolites required for further pharmacological and toxicological studies