cardiovascular-agents and ethyl-cellulose

The objective of this study was to prepare and evaluate ivabradine HCl-loaded microspheres consisting of Eudragit LIOO-55 and ethyl cellulose prepared by oil-in-oil solvent evaporation method. Ivabradine HCl was encapsulated into microspheres by in situ method. The resultant microspheres were characterized with respect to drug loading, flow properties, Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), X-ray diffractometry (XRD), thermal analysis and release behavior. Chemical stability of IBH after being encapsulated into microspheres was confirmed by FTR, DSC and XRD. FTIR spectra reflect- ed no interaction between drug and excipients. TGA indicates that prepared microspheres showed much better thermal stability than pure drug ivabradine. SEM images showed formulation of microspheres in spherical shape. The maximum perceniage entrapment efficiency was found to be 81 ± 2.15 and percentage yield was 88 ± 2.65. The maximum in vito drug release was 94.5% for the pH 7.4 and demonstrated that all drug-loaded formulations had a pH-dependent drug release. The cumulative drug release data were analyzed by applying different kinetic models. Korsmeyer-Peppas equation was used to determine value of n which follows non-Fickian diffusion.

Topics: Acrylic Resins; Benzazepines; Calorimetry, Differential Scanning; Cardiovascular Agents; Cellulose; Chemistry, Pharmaceutical; Crystallography, X-Ray; Delayed-Action Preparations; Diffusion; Drug Carriers; Drug Compounding; Drug Liberation; Drug Stability; Hydrogen-Ion Concentration; Ivabradine; Kinetics; Microscopy, Electron, Scanning; Microspheres; Models, Chemical; Particle Size; Solubility; Spectroscopy, Fourier Transform Infrared; Surface Properties; Technology, Pharmaceutical; Thermogravimetry

This study aimed to develop and evaluate a novel multi-unit tablet that combined a pellet with a sustained-release coating and a tablet with a pulsatile coating for the treatment of circadian rhythm diseases. The model drug, isosorbide-5-mononitrate, was sprayed on microcrystalline cellulose (MCC)-based pellets and coated with Eudragit(®) NE30D, which served as a sustained-release layer. The coated pellets were compressed with cushion agents (a mixture of MCC PH-200/ MCC KG-802/PC-10 at a ratio of 40:40:20) at a ratio of 4:6 using a single-punch tablet machine. An isolation layer of OpadryII, swellable layer of HPMC E5, and rupturable layer of Surelease(®) were applied using a conventional pan-coating process. Central-composite design-response surface methodology was used to investigate the influence of these coatings on the square of the difference between release times over a 4 h time period. Drug release studies were carried out on formulated pellets and tablets to investigate the release behaviors, and scanning electron microscopy (SEM) was used to monitor the pellets and tablets and their cross-sectional morphology. The experimental results indicated that this system had a pulsatile dissolution profile that included a lag period of 4 h and a sustained-release time of 4 h. Compared to currently marketed preparations, this tablet may provide better treatment options for circadian rhythm diseases.

Topics: Administration, Oral; Angina Pectoris; Cardiovascular Agents; Cellulose; Chemistry, Pharmaceutical; Chronobiology Disorders; Delayed-Action Preparations; Drug Carriers; Excipients; Hypromellose Derivatives; Isosorbide Dinitrate; Kinetics; Methacrylates; Methylcellulose; Microscopy, Electron, Scanning; Polymers; Solubility; Tablets; Technology, Pharmaceutical