Controlled release of verapamil hydrochloride from waxy microparticles prepared by spray congealing.
In this work, the potential of waxes for preparing with the ultrasonic spray congealing technique microparticles for controlling the in vitro release of verapamil HCl was investigated. The first part of the study encompassed the optimisation of the formulation to achieve an efficient drug incorporation together with a satisfactory in vitro drug release rate. In particular, microcrystalline wax, stearyl alcohol and mixtures of the two were used. Also a surfactant (soya lecithin) was added to the formulations. After the particle size analysis, the characterisation of the microparticles involved the study of the solid state of drug and carriers in the systems (DSC, HSM and XRD) and the morphological and chemical analyses of the microparticle surface (SEM and XPS). Finally, the drug release mechanism from these devices was evaluated using the statistical moment analysis. The results of this study show that by selecting the type and the amount of the carriers, microparticles with a spherical shape and a good encapsulation efficiency were observed. These particles showed a zero-order release for 8 h, without modifying the solid state properties of the drug. Therefore, waxy microparticles prepared by the ultrasonic spray congealing technique are promising solvent-free devices for controlling the release of verapamil HCl.
Passerini
Nadia
N
Department of Pharmaceutical Sciences, University of Bologna, Via S. Donato 19/2, Italy. passerin@biocfarm.unibo.it
Perissutti
Beatrice
B
Albertini
Beatrice
B
Voinovich
Dario
D
Moneghini
Mariarosa
M
Rodriguez
Lorenzo
L
D000465:Algorithms; D002121:Calcium Channel Blockers / Q000008:administration & dosage*; D002152:Calorimetry, Differential Scanning; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D003692:Delayed-Action Preparations; D004339:Drug Compounding; D005079:Excipients; D007700:Kinetics; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D010316:Particle Size; D012995:Solubility; D013052:Spectrometry, X-Ray Emission; D014700:Verapamil / Q000008:administration & dosage*; D014885:Waxes; D014961:X-Ray Diffraction
D002121:Calcium Channel Blockers; D003692:Delayed-Action Preparations; D005079:Excipients; D014885:Waxes; D014700:Verapamil