FORMULATION DEVELOPMENT AND EVALUATION OF CHRONOMODULATED DRUG DELIVERY SYSTEM BY ZAFIRLUKAST
Objective: The main objective of the present study was to formulate and evaluate a time-controlled single unit oral pulsatile drug delivery system containing Zafirlukast for the prevention of nocturnal asthma attacks. To provide time-scheduled drug release for Asthama disease. It is used for preventing the asthmatic attacks at early morning. Pulsatile release dosage form is increasing patient compliance by reducing the dosing frequency especially at early morning.
Methods: Core tablets were prepared by incorporating different concentration of natural and synthetic superdisintegrants. Drug containing core tablets (ZC1- ZC15) with different composition of natural superdisintegrants (Plantago ovata seed powder, Locust bean gum) synthetic superdisintegrants (Sodium starch glycolate (SSG), Cross carmellose sodium (CCS), Crospovidone (CP)) were prepared by direct compression technique. The core tablets were subjected to pre-formulation, physicochemical and In vitro drug release studies. The fast disintegrating core tablet formulation was selected and press-coated tablets (P1-P11) were prepared with different compositions of hydrophobic polymers Eudragit RS100, Eudragit RL 100, Ethyl cellulose and hydrophilic polymers Hydroxy propyl methyl cellulose K4M, K100M. The optimised formulation was selected and quantified based on in vitro drug release profile in simulated gastric and intestinal fluids.
Results: The pre and post-compressional parameters of tablets were also found to be within limits. Formulation ZC5 with 16 mg of Locust bean gum showed least disintegrating time, i.e., 22.13 sec and was selected as the best immediate release core tablet. The press-coated tablet formulation P8 having 62.5 mg Eudragit RS100 and 62.5 mg of HPMC K4M in ratio 1:1 over the core tablet ZC5 showed rapid and drug release nearly after 4 h lag time and 98.86 % up to 12 hours. Accelerated stability studies of the optimized formulation P8 indicated no significant difference in release profile after a period of 3 months.
Conclusion: The in vitro dissolution study showed that lag time before drug release was highly affected by the coating amount level and nature of coating polymer used. Time-controlled pulsatile release tablets can be prepared using press-coating techniques.
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