FORMULATION DEVELOPMENT AND EVALUATION OF IMMEDIATE RELEASE FORMULATION CONTAINING AN ANTI-HYPERTENSIVE AGENTS

Abstract

The aim of the project is to prepare immediate release tablet of BCS Class II drug used in the treatment of hypertension for better patient compliance. Different methods like direct compression and wet granulation were discovered to manufacture IR tablets. Though, direct compression method shown higher weight variation and thus further trials were attended using wet granulation method. Excipient likes Lactose Monohydrate, Sucrose, MCC, Ferric Oxide Red, Maize Starch, Sodium starch glycolate, Crospovidone, Polysorbate-80, IPA, Maize Starch, Purified Water, Colloidal silicon dioxide, magnesium stearate were used. The Preformulation studies like bulk density, tapped density, Carr’s index, Hausner’s ratio, LOD, and compatibility study of all excipients with API were conceded out. Wet granulation was carried out in RMG (Rapid mixer granulator), Retsch dryer used as a drying, Octagonal blender used as blending, and compression. The formulation were evaluated that hardness, disintegration time, diameter, thickness, content uniformity and in-vitro drug release and compared it with the drug release of innovator product. The stability study of optimized formulation was carried out for 1 month, 2 month and 3 month at different condition as per ICH guidelines. Simultaneously, the minor project carried out at institute with the aim to formulation, evelopment and optimization of SEDDS of BCS class II drug of antihypertensive agent. Lercanidipine hydrochloride is poorly water soluble anti-hypertensive drug have highly lipophilic and exhibit variables bioavailability as low as 10% when given orally. To overcome the dissolution issue, self-emulsifying drug delivery systems were prepared. An extensive quantitative solubility studies and pseudo ternary phase diagrams were conducted. For the selection of optimized batch 23 factorial design applied by using design expertsoftware. The liquid SEDDS contained drug (lercanidipine HCL), cinnamon oil as an oil, ween-80 as a surfactant and PEG-400 as a Co-surfactant were used as a excipients. The SEDDS were developed and characterized for % transmission, globule size, zeta potential, transmission electron microscopy (TEM), and % drug release. The stability study of optimized formulation was carried out for 1 month, 2 month and 3 month at different condition like short term, intermediate and long term condition as per ICH guideline.