Fixed Dose Formulation Development of Bilastine and Montelukast Sodium as Tablets and Simultaneous Estimation of its Active Ingredients and Impurities With a Validated RP HPLC Method

Abstract

Asthma, and allergic rhinitis (AR), are the two commonest diseases that affect millions of newlinepeople around the world. Fixed dose combination formulations of Bilastine and newlineMontelukast Sodium are launched in 2020 to treat allergic rhinitis and allergic rhinoconjunctivitis newlineassociated with asthma. Uncoated tablets of Bilastine 20 mg and newlineMontelukast Sodium, equivalent to 10 mg Montelukast are prepared using pharmaceutical newlinegrade of Microcrystalline Cellulose, Colloidal Silicon Dioxide, Sodium Starch Glycolate newlineand Magnesium Stearate by direct compression method. Pre and post compression newlineevaluation of physical and chemical properties of drugs in combination with excipients newlinewere evaluated and manufacturing formula was finalized. A reverse phase high newlineperformance liquid chromatographic (RP-HPLC) methods were developed and validated newlinefor qualitative purpose as well as quantitative estimation of % Assay and % Release of newlineBilastine and Montelukast from bulk and tablet dosage forms. A HPLC was method was newlinealso developed and validated for profiling of related impurities from tablet formulation. newlineThe validated analytical methods for assay, dissolution and impurities were validated as newlineper ICH guidelines with respect to specificity, precision (system, method and intermediate), newlinelinearity, range, limit of detection, limit of quantitation, accuracy, stability in aqueous newlinesolution and robustness. Further, the developed formulation was also subjected to long term newlineand accelerated stressed conditions and stressed samples were examined in terms of assay, newlinedissolution and related substance estimation using the validated HPLC methods and results newlineshows stability of product in all stability conditions. A comparative dissolution study was newlinealso performed to compare the developed formulation with marketed formulation in respect newlineof assay, dissolution (% release) and related substance. Comparative results show no newlinesignificant differences and both formulations found comparable. On the basis of above newlinestudies, it is concluded that, the developed formulation wa