Abstract
The objective was to control the release of diltiazem HCl. Emulsion solvent evaporation technique was applied to encapsulate diltiazem HCl using ethyl cellulose or Eudragit RS100. The prepared microspheres were characterized concerning entrapment efficiency;micromeritics properties and surface morphology using SEM and mixed with carbopol, hydroxypropyl methyl cellulose, or chitosan in different ratios. The in-vitro dissolution and kinetic analysis were carried out using various models. In-vivo studies for selected formulae were carried out compared with a marketed product to evaluate their pharmacokinetic parameters. The prepared microspheres showed entrapment efficiency of 67.45 and 76.82% for ethyl cellulose and Eudragit microspheres, respectively. Moreover, Eudragit microspheres mixed with hydroxypropyl methyl cellulose at a ratio of 1:3 showed a sustained release of diltiazem HCl over 12 h, with t½ 14.8 hr. The formulated diltiazem HCl capsule can be successfully used for twice daily dosing. Key words: Microencapsulation, chitosan, Eudragit RS 100, microspheres, bioavailability.
Highlights
Coronary heart disease (CHD), one of the major causes of death and disability, attracts much attention from biomedical research community
Differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR) spectroscopic analysis were used for the evaluation of physicochemical compatibility and interactions
They helped in the prediction of possible interaction of DLZ with the polymers used in microsphere formulations
Summary
Coronary heart disease (CHD), one of the major causes of death and disability, attracts much attention from biomedical research community. During the past few decades, various types of oral controlled-release formulations have been developed to improve the clinical efficacy of drugs that have short half lives as well as to increase patient compliance. These formulations are designed to deliver drugs at a predetermined rate over a wide range of conditions and durations of therapeutic treatments (Löbenberg et al., El-Say et al.2005; Li et al, 2007; Aamir and Ahmad, 2009; Sabitha et al, 2010; Lekshmi et al, 2012)
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