Acrylic co-polymer and organic acid-based press coated pulsatile tablet of nifedipine using 32 factorial design: use of novel solubilizer for solubility enhancement

Many diseases exhibit circadian fluctuation, including diabetes, asthma, rheumatoid arthritis, and hypertension. These disorders cannot be effectively treated with conventional dosage forms and instead require time-scheduled drug release for pharmacological effectiveness. The objective of this work was to use simple process to overcome the solubility problem by employing a novel solubilizer and to generate peristaltic release based on the physical and chemical interactions between acrylic copolymer and organic acid. To address the solubility issue of nifedipine, sepitrap 4000 is being used as a solubilizer inside the core tablet. The resulting physical mixture underwent various analyzes including saturated solubility, in-vitro dissolution, FTIR, DSC, and PXRD. A saturation solubility analysis confirmed 368% improvement as significant impact of sepitrap 4000 on nifedipine solubility and bioavailability. The 3² complete factorial design was used to optimize press-coated pulsatile formulation, with lag time and time required to release 50% of drug, as responses and concentrations of eudragit RSPO and tartaric acid as independent variables. According to stability study, developed pulsatile product was found to be suitably stable under rapid and regulated settings. As a result, produced pulsatile tablet is suitable formulation for alleviation of early morning blood pressure spikes and other cardiac problems that follow a circadian rhythm.