ABSTRACT

Selexipag is a selective prostacyclin (IP, also called PGI2) receptor agonist. It is used in treatment of Pulmonary Arterial Hypertension. Selexipag Bioavailability is approximately 49%. After oral administration, maximum concentrations of Selexipag and its metabolite were observed to be reached at 1-3 and 3-4 hours, respectively. Absorption was impaired in the presence of food, resulting in delayed time to maximum concentration. In the present study, an attempt was made to improve bioavailability of Selexipag and formulate Selexipag sublingual tablets hence avoid first-pass metabolism and increase Bioavailability. To Improve Bioavailability of Selexipag, sublingual tablets were prepared. Various Superdisintegrants like Croscarmellose Sodium and Crospovidone were used. The tablet with mentioned excipients were evaluated for different parameter amongst them Mannitol and Microcrystalline Cellulose (MCC) in 60:40, 70:30 and 80:20 (Mannitol: MCC) three ratios were optimized for further formulation of sublingual tablets. The prepared tablets were evaluated for various parameters like Thickness, Hardness, Friability, Weight variation, Disintegration time, wetting time, % In vitro Drug Release. The stability study was carried out as per ICH guideline to meet the desirable characteristics. In a nut shell, Selexipag sublingual tablets were successfully formulated. Keywords: Selexipag, Sublingual tablet, Croscarmellose Sodium, Crospovidone, Mannitol and Microcrystalline Cellulose
Publication date: 01/11/2023

https://ijbpas.com/pdf/2023/November/MS_IJBPAS_2023_7413.pdf

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https://doi.org/10.31032/IJBPAS/2023/12.11.7413