Abstract

FORMULATION AND IN-VITRO EVALUATION OF FLOATING PULSATILE TABLET OF LISINOPRIL

Durga Bhavani K.* and Poornima N. B.

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Abstract

This study focuses on formulating and evaluating Lisinopril Floating Pulsatile Release Tablets (FPRTs) for enhanced chronomodulated therapy in hypertension treatment. The methodology involves the preparation of rapid-release core tablets (RRCTs) through direct compression, incorporating various superdisintegrants. These cores are subsequently compression-coated with hydrophilic polymers, including HPMC E5, HPMC K4M, HPMC K15M, and Xanthan gum, to achieve desired floating and pulsatile release characteristics. Objectives encompass optimizing drug release timing, minimizing dose-related side effects, and improving bioavailability. The comprehensive plan includes preformulation studies, Lisinopril standard curve preparation, pre-formulation studies of the drug and formulations, and the formulation and development of RRCTs and FPRTs. Evaluation parameters comprise physical characteristics, friability, drug content, disintegration, in-vitro release, buoyancy, swelling index, release kinetics, and stability studies following ICH guidelines. Lisinopril, an ACE inhibitor, is chosen for its relevance in treating hypertension, heart failure, nephropathy, and myocardial infarction. The selection of a floating pulsatile release tablet aligns with the need for chronopharmacotherapy, avoiding first-pass metabolism, targeting specific sites like the stomach, accommodating drugs with short halflives, improving bioavailability, and enhancing patient compliance. Future directions involve scale-up, in-vivo studies, in vitro-in vivo correlation, and bioequivalence assessments with market products. In conclusion, Formulation FP8 demonstrates promising drug release kinetics and stability, offering a potential solution for addressing circadian variability in hypertension, thereby contributing to the progression of chronomodulated drug delivery systems.

Keywords: Lisinopril, Floating Pulsatile Release Tablets, Chronomodulated Therapy, Hypertension, Drug Delivery.