Design, development, and in vitro evaluation of sustained release tablet formulations of olmesartan medoxomil

Abstract

Enteral route is the most comfortable, extensively used route of administration for both prompt delivery systems and new drug delivery systems. Tablets are the most famous solid formulations available in the market and are preferred by patients and physicians alike. In case of treatment of chronic disease conditions, conventional release formulations are required to be administered in frequent manner and therefore shows patient non‒adherence to prescription.1 However, ingestion of majority of drugs shows first pass effect and/or first pass hepatic metabolism presystemic elimination by gastrointestinal degradation as a result of which low systemic bioavailability and shorter duration of action and development of non‒active or toxic transformed products.2 The objective of a sustained release (SR) dosage form is to maintain CSS levels for prolonged period. Systems that are designated as modified release/timed release can also be considered as attempts at achieving prolonged drug delivery.3‒6 SR formulations offers greater reduction in dosing frequency in comparison with immediate release formulations.7 SR formulations afford advantage over prompt release formulations by optimising biopharmaceutical, pharmacokinetic and pharmacodynamic properties of drug. The utilization of macromolecules like polymers in modulating the rate of drug release has turn to an essential tool in the product development of pharmaceutical formulations. Numerous reports over many years reveals that they play key role in the release of drugs from dosage form for various drugs.8 Natural polymers preferred primarily because they were economic, high drug holding capacity, high thermal stability, non‒carcinogenicity, mucoadhesivity, biodegradable, biocompatible, broad regulatory acceptance and ease of compression. Various gums and mucilages were used for the development of sustained release formulations in such as gums (xanthan, tragacanth, guar), pectin, alginates etc. cellulose derivatives such as HPC, HPMC, CMC, SCMC have been widely used as release retardants in the formulation of prolonged release dosage forms. The future of novel drug delivery systems (SR) is promising in arena like chronopharmacotherapeutic delivery system, mucoadhesive system, chronopharmacokinetic approach, targeted drug delivery approach, particulate system that provide high assurance and adoptability. Sustained release oral formulations by Direct Compression (DC) method was a simple approach due to its rapid production, Easer, No degradative effects occurred during manufacturing, compliance.7 The suitability of drug candidates for sustained release system based on biopharmaceutical, pharmacokinetic and pharmacodynamic properties of it. numerous studies have been reported in the literature regarding the utilisation