FORMULATION AND EVALUATION OF SUSTAINED-RELEASE PELLETS OF LORNOXICAM

Objective: The aim of the study was to develop sustained release pellets of lornoxicam using Eudragit RLPO and Eudragit RSPO to reduce the dosing frequency. Methods: The sustained release pellets of lornoxicam were prepared by extrusion–spheronization technique using Eudragit RLPO and Eudragit RSPO as release retardant polymers and microcrystalline cellulose as spheronizing agent. A 32 Full factorial design was applied to investigate the combined effect of the two independent variables i.e. concentration of Eudragit RLPO (X1) and concentration of Eudragit RSPO (X2) on the dependent variables, In vitro drug release at 1h (Y1), In vitro drug release at 4 h (Y2) and In vitro drug release at 12 h. (Y3). Results: The optimized formulation (F0) show in vitro drug release 11.24±1.21 %, 43.69±1.28 %, 82.69±1.74 % and 100.24±1.56 % at 1 h, 4 h, 12 h and 24 h respectively. Drug excipients compatibility study by FTIR showed no interaction between drug and excipients. Eudragit RLPO and Eudragit RSPO had a significant effect on in vitro drug release. Conclusion: From all parameters and experimental design evaluation, it was concluded that the drug release rate decreased with an increase the concentration of Eudragit RLPO and Eudragit RSPO. SEM Photomicrograph of pellets revealed that the surface was rough and the pellets were spherical shaped in nature. The in vitro release kinetics revealed higuchi model is followed and drug release is by anamolous diffusion.

Formulation and In vitro Evaluation of Unfolding Type Expandable Gastroretentive Film of Enalapril Maleate

The present work was based on the development and characterization of unfolding type gastroretentive dosage form appropriate for controlled release of enalapril maleate. Drug loaded films were prepared by solid dispersion technique using methocel K15 and eudragit RSPO and eudragit RLPO as polymers and polyethylene glycol 400 (PEG 400) as the plasticizer. The film folded in a capsule shell was shown to unfold in the gastric juice and provide drug release up to 12 h in the acidic medium. Formulations provided satisfactory unfolding characteristics allowing expansion to remain in the stomach. Formulation containing above 60% content of eudragit RSPO and eudgrait RLPO combination of total polymer content provided satisfactory film integrity over 12 hours. The result revealed that formulation F1 showed a minimum percentage of drug release of 63.41% followed by formulation F2, F3, F4 and F5 with 66.76%, 80.21%, 83.26% and 86.92% release in 8 hour respectively. Formulation with high proportion of eudragit RLPO and RSPO combination in total polymer content was found to be slow in drug release and lower the release from the polymeric film over time. As the concentration of HPMC K 15 in total polymer content increased the release rate of enalapril maleate as well as % release from the polymeric film also increased over time. Most of the formulation followed Higuchi release kinetics followed by Korsmeyer release kinetics. The drug release mechanism from the film follows Fickian and Non Fickian release kinetics. The films were evaluated for mechanical properties, in vitro drug release and unfolding behavior based on the mechanical shape memory of polymers. Absence of drug polymer interaction and uniform drug dispersion in the polymeric layers was revealed by DSC, FT-IR and SEM studies.Bangladesh Pharmaceutical Journal 20(2): 148-154, 2017

Preparation and In vitro Evaluation of Mucoadhesive Tablets of Montelukast Sodium

Mucoadhesive tablets of montelukast sodium were prepared in order to release the drug for a prolonged period of time so as to reduce the frequency of administration. Direct compression technique was applied using the mucoadhesive polymers which were Methocel K4M CR, Methocel K15M CR, Methocel K100M CR and Eudragit RLPO. Highest percent release of drug after 8 hours was 76% for Methocel K4M CR, 72.13% for Methocel K15M CR, 65.68% for Methocel K100M CR, 65.53% for the combination of Methocel K15M CR and Eudragit RLPO. Higuchi, Krosmeyer-Peppas was the best fitted model for drug release. The Methocel K15M CR containing drug showed good mucoadhesive strength. The highest ex-vivo mucoadhesive strength and ex-vivo residence time were observed with Methocel K15M CR and Eudragit RLPO combination. Fourier transform infrared (FT-IR) spectroscopy revealed the compatibility of drug with the polymers.Bangladesh Pharmaceutical Journal 20(2): 123-131, 2017