Aim: Dosing frequency is a major hurdle in geriatrics with frequent drug administration. In such cases, oral controlled release floating formulations are helpful which causes reduction in dosing frequency and fluctuation of drug levels in plasma. The main aim of the current research was to prepare Captopril floating controlled release formulations in order to achieve extended gastric retention in the upper GIT. Methodology: Captopril tablets were prepared using different concentrations of poly ethylene oxide water soluble resin (PEO WSR) 303 (5% to 30%) by direct compression technique. Captopril formulations CSP1 and CSP6 were formulated using PEO WSR 303. Pre and post compression parameters were evaluated. Dissolution studies were performed for the prepared tablets using 0.1N hydrochloric acid as dissolution medium. Results: The dissolution studies showed controlled drug release up to 12h. The formulation CSP5 prepared using 25% w/w of PEO WSR 303 showed maximum drug release of 97.97% at 12h. Almost similar drug release profile was also observed for CSP6 which was prepared using 30%w/w PEO WSR 303. These two formulations were further added with various concentrations of sodium bicarbonate (5% to 15%) and citric acid (2.5% to 10%) which enhanced floating of drug in Gastro intestinal tract (GIT). Formulation CSP8 containing 10% of sodium bicarbonate with 25% PEO WSR 303 showed less buoyancy lag time and prolonged drug release. Formulation CSP15 showed very less buoyancy lag time of 5sec. Characterization studies like Fourier Transform Infra Red spectroscopy (FTIR) and Scanning Electron Microscopy (SEM) were also carried out. Conclusion: The prepared Captopril floating tablets could be an alternative formulation for prolonged drug release.

Drug solubility plays an important role in the improvement of bioavailability. Biopharmaceutical Classification System (BCS) Class-II drugs have less solubility and more permeability. Most of the drugs available in the market belong to BCS class-II. The objective of the present study is to improve the solubility of BCS Class-II drug, Cilnidipine by formulating them as solid dispersions and to make controlled release formulations. Solid dispersions of Cilnidipine were prepared by solvent evaporation technique using plasdone K-29/32. Various physical parameters were evaluated for the prepared solid dispersions. The in vitro drug release studies were performed for the solid dispersions using phosphate buffer pH 6.8. The solid dispersions which showed maximum drug release were selected for the preparation of oral controlled release formulations. Tablets were prepared using Cilnidipine solid dispersions and varying concentrations of polyethylene oxide (PEO) WSR 303 by direct compression technique. Pre and post-compression parameters were evaluated along with in vitro drug release studies. In vitro dissolution studies revealed that solid dispersion CP3 containing Cilnidipine and plasdone K-29/32 in 1:3 ratios showed faster drug release in a short time. The pre and post compression parameters of the solid dispersions and tablets were within specified limits. Formulation CPP5 containing CP3 solid dispersion with 25% w/w of PEO WSR 303 showed prolonged drug release up to 12h. Similar drug release was also obtained with CPP6 formulation having 30%w/w of PEO WSR 303. The present study prepared a novel Cilnidipine pharmaceutical product having increased solubility and prolonged drug release which is not available in the market. The solubility of Cilnidipine was enhanced using plasdone K-29/32 and the drug release was delayed using PEO WSR 303 as polymer. This could be advantageous to many of the patients with cardiovascular disorders.

Aim: The main perspective of the present research work was to prepare Metoprolol floating controlled release formulations. Methodology: After performing the characterization studies, Metoprolol tablets were prepared using various concentrations of poly ethylene oxide (PEO) WSR 303 (5% to 30%) by direct compression method. Formulations MP1 and MP6 were formulated using PEO WSR 303. Various pre and post compression parameters were evaluated. Dissolution studies were performed for the prepared tablets using dissolution medium of 0.1N hydrochloric acid. Results: Characterization studies like Fourier Transform Infra Red (FTIR) and Scanning Electron Microscopy (SEM) for Metoprolol, Polyethylene oxide WSR 303 and their combination were carried out, which revealed that there is no interaction between drug and polymer. The dissolution studies showed the controlled release pattern of Metoprolol up to 24h. The formulation MP5 prepared using 25% w/w of PEO WSR 303 showed maximum drug release of 98.22% at 24h. Similar drug release profile was observed for MP6 which was formulated using 30%w/w PEO WSR 303. These two formulations were further added with various concentrations of sodium bicarbonate (5% to 15%) and citric acid (2.5% to 10%) which enhanced floating of drug. Formulation MP8 containing 10% of sodium bicarbonate with 25% PEO WSR 303 showed less buoyancy lag time and prolonged drug release. Formulation MP15 showed very less buoyancy lag time of 4sec. Conclusion: Thus the prepared Metoprolol floating tablets showed prolonged drug release which could be a promising formulation for anti-hypertensive patients.