Preparation and characterization of Eudragit L30 D-55, L100 and S100 coated Montelukast sodium pellets for chronotherapy: A possible relevance to therapeutic targets

Abstract

Author(s): Ponnaganti SS Prasanna Kumar and Lankalapalli Srinivas*

Objective: The initial research investigation on the current research work was to design, develop oral formulation of Pulsatile Drug Delivery Systems (PDDS) for Montelukast sodium with aim of treatment for asthma and designed as Pellets type of system with immediate and extended release of drug occurs after the lag time period. In chronic asthma condition patients suffered during the early morning hours (04.00 am to 06.00 am) so immediate release dosage forms are not suitable but the modified release formulation that is given at bed time and releases the drug as pulsed manner despite to wake up the patient.

Methods: In this present investigation, Montelukast sodium pellets were prepared using Fluidized Bed Processor (FBP), seal coating with HPMC E5 and enteric coatings with Eudragit L30 D-55, Eudragit L100 and Eudragit S100 polymers for extending lag period prior the drug release.

Results: The drug-excipient compatibility for the formulation was assessed using FTIR and DSC; the results obtained shown that no chemical interactions. The optimised formulations of IR Pellets MEF-6 showed release of drug 99% at 6 h with 4.5 h lag time and ER Pellets MXR-8 showed 99% of drug release at 12 h with 05 h lag time. SEM Studies showed uniform surface morphology on the prepared coated pellets. As per ICH standards for optimized formulations, stability experiments were also conducted for 6 months at 40ºC at 75% RH and it was concluded to be stable.

Conclusion: The designed pellets of both IR and ER release with enteric coatings beneficial to patients with night time dosing that can prevent the asthma episodes at early morning and development of exacerbations serving as effective therapy for various diseases.

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