Formulation, Optimization and Evaluation of Rimegepant Pulsatile Tablets for Chronotherapeutic Management of Migraine
Abstract
Background: Migraine attacks frequently show circadian variation, and conventional immediate-release oral dosage forms may not provide drug exposure at the most therapeutically relevant time. Rimegepant, a calcitonin gene-related peptide (CGRP) receptor antagonist, is an effective agent for acute and preventive migraine therapy; however, a programmed oral delivery system may improve chronotherapeutic targeting. Objective: This study aimed to formulate, optimize and evaluate rimegepant pulsatile tablets designed to provide a defined lag phase followed by rapid drug release. Methods: Tablets were prepared by direct compression using microcrystalline cellulose, lactose, crospovidone, hydroxypropyl methylcellulose (HPMC), ethyl cellulose, magnesium stearate and talc. A two-factor, three-level experimental design was applied to evaluate the influence of crospovidone and HPMC concentrations on disintegration/lag time and percent drug release. Preformulation studies, UV spectrophotometric analysis, FTIR, DSC, precompression evaluation, post-compression testing, in vitro dissolution and accelerated stability studies were performed. Results: Rimegepant showed acceptable organoleptic properties, a melting range of 150-153 °C and maximum absorbance at 260 nm. FTIR and DSC results indicated the absence of major drug-excipient incompatibility. The prepared batches exhibited disintegration/lag times ranging from 49 to 80 min and drug release from 70% to 91%. The optimized formulation F9,…
Read the paper
Related studies
- Calcium Ions in the Physiology and Pathology of the Central Nervous System
- AI-powered in silico twins: redefining precision medicine through simulation, personalization, and predictive healthcare
- In silico functional, structural and pathogenicity analysis of missense single nucleotide polymorphisms in human MCM6 gene
- In Silico drug repurposing pipeline using deep learning and structure based approaches in epilepsy
- Targeting serotonin receptors with phytochemicals – an in-silico study
- In silico exploration of anti-prostate cancer compounds from differential expressed genes
Go deeper in Evidence Hub
Evidence Hub adds a study data sheet (design, sample size, evidence level, key numbers), an AI summary and a chat grounded in the paper's text.