Controlled-Release Behavior of Diphenhydramine Hydrochloride Loaded Neutral Microgranules and Coated Using Ethylcellulose Water Dispersion

• Published in: Drug development and industrial pharmacy 1999, Vol.25 (1), p.81-87
• Main Authors: Opota, D. O., Joachim, G., Kalantzis, G., Piccerelle, P., Reynier, J. P., Joachim, J.
• Format: Article
• Language: English
• Subjects: Biological and medical sciences; Cellulose - analogs & derivatives; Chemistry, Pharmaceutical; Delayed-Action Preparations; Dicarboxylic Acids; Diffusion; Diphenhydramine - chemistry; Drug Carriers; General pharmacology; Histamine and antagonists. Allergy; Kinetics; Medical sciences; Microscopy, Electron, Scanning; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Plasticizers; Povidone; Solubility; Suspensions; Water
• ISSN: 0363-9045; 1520-5762
• DOI: 10.1081/DDC-100102145

The development of a loading method of a water-soluble drug using aqueous binding solution to produce microgranules that were then coated with an aqueous ethylcellulose dispersion to sustain drug release is described. The results, in terms of drug used, showed that besides the fluidized bed parameters, the amount of drug dissolved in the binder solution plays an important role in obtaining a satisfying result during the spraying process. Thus, it seems necessary to determine the critical concentration above which the material started to adhere to the interior of the fluidization column, and the possibility of drug layering onto carrier material is aggravated. ANOVA of the time parameter for release of 63.2% of total drug (td) value showed significant influence of ethylcellulose (Aquacoat ECD-30) and dibutyl sebacate concentration on diphenhydramine hydrochloride (DPH) release. The dissolution rate decreased with an increase in polymer concentration. The diffusional exponent n of the Peppas equation indicated that the DPH release kinetic was non-Fickian but approached Fickian diffusion, particularly at higher coating levels.