Formulation and Evaluation of Pulsatile Drug Delivery System of Montelukast Sodium

[摘要] The present work was to formulate and evaluate an oral pulsatile drug delivery system of Montelukast sodium for nocturnal asthma. Pulsatile delivery system is capable of delivering drug when and where it required most with having a predetermined lag time. The basic design of pulsatile drug delivery system is core tablet prepared by direct compression method and then further coating the selected core tablet formulation. The nine core tablet formulations (F1 -F9 ) were prepared which consist of MCC, different concentrations of superdisintegrants like Sodium starch glycolate, crospovidone and croscarmellose sodium. The prepared core tablets were evaluated for pre and post compression parameters. The two best core tablet (F6 & F9) formulations were selected and coated with Eudragit S100 and ethyl cellulose with different concentrations (14% and 24%) by dip coating method. The coated tablets were evaluated for weight variation, hardness, drug content, disintegration time and in vitro dissolution studies. The C2 and C8 showed best release after specific lagtime i.e. with coat of Eudragit S100 24% and ethyl cellulose 24% respectively. Stability studies of the optimized formulations were carried out at 40 ± 2 °C / 75 ±5% RH for one months and it was found to be stable. Drug is released as a burst after lag time (during peak morning hours), hence pulsatile drug delivery of Montelukast sodium can be helpful for the asthma patients in giving relief from morning attacks. The present work was to formulate and evaluate an oral pulsatile drug delivery system of Montelukast sodium for nocturnal asthma. Pulsatile delivery system is capable of delivering drug when and where it required most with having a predetermined lag time. The basic design of pulsatile drug delivery system is core tablet prepared by direct compression method and then further coating the selected core tablet formulation. The nine core tablet formulations (F1 -F9 ) were prepared which consist of MCC, different concentrations of superdisintegrants like Sodium starch glycolate, crospovidone and croscarmellose sodium. The prepared core tablets were evaluated for pre and post compression parameters. The two best core tablet (F6 & F9) formulations were selected and coated with Eudragit S100 and ethyl cellulose with different concentrations (14% and 24%) by dip coating method. The coated tablets were evaluated for weight variation, hardness, drug content, disintegration time and in vitro dissolution studies. The C2 and C8 showed best release after specific lagtime i.e. with coat of Eudragit S100 24% and ethyl cellulose 24% respectively. Stability studies of the optimized formulations were carried out at 40 ± 2 °C / 75 ±5% RH for one months and it was found to be stable. Drug is released as a burst after lag time (during peak morning hours), hence pulsatile drug delivery of Montelukast sodium can be helpful for the asthma patients in giving relief from morning attacks.

[学科分类] 药学、药理学、毒理学（综合）

[关键词] Pulastile drug delivery system;Nocturnal asthma;Eudragit S100;Ethyl cellulose.