Development of sustained release matrix tablets of didanosine containing methacrylic and ethylcellulose polymers

• Published in: International journal of pharmaceutics Vol. 234; no. 1; pp. 213 - 221
• Main Authors: Sánchez-Lafuente, Carla, Teresa Faucci, M., Fernández-Arévalo, Mercedes, Álvarez-Fuentes, Josefa, Rabasco, Antonio M., Mura, Paola
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier B.V 02.03.2002; Elsevier
• Subjects: Anti-HIV Agents - administration & dosage; Anti-HIV Agents - chemistry; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antiviral agents; Biological and medical sciences; Cellulose - analogs & derivatives; Chromatography, High Pressure Liquid; Delayed-Action Preparations; Didanosine; Didanosine - administration & dosage; Didanosine - chemistry; Ethocel; Eudragit; General pharmacology; Hardness; Hydrogen-Ion Concentration; Image Processing, Computer-Assisted; Matrix tablets; Medical sciences; Methacrylates; Microscopy, Electron, Scanning; Particle Size; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Polymers; Sustained release; Ethocel; Sustained release; Didanosine; Matrix tablets; Eudragit; Methacrylate polymer; Purine nucleoside; Pharmaceutical technology; Controlled release form; Control release polymer; Mechanical properties; Cellulose(ethyl); Slow release form; Drug carrier; Hardness; In vitro; Matrix tablet; Property formulation relationship; Thickness; Dideoxynucleoside; Dosage form; Antiviral; Active ingredient; Release; Physicochemical properties
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/S0378-5173(01)00962-0

Didanosine, a nucleoside analog used in the treatment of acquired immuno deficiency syndrome (AIDS), has been incorporated into directly compressed monolythic matrices whose excipients were mixtures at different ratios of a methacrylic resin (Eudragit RSPM) and an ethylcellulose (Ethocel 100), both water-insoluble and pH-independent polymers. Technological characterization (drug particle morphology, mean weight, diameter, thickness and hardness of tablets) was carried out and in vitro drug release behaviour was measured using the USP basket apparatus. The effect of varying the Eudragit–Ethocel ratio, as well as the drug–polymeric matrix ratio, was evaluated. The results showed the suitability of Eudragit–Ethocel mixtures as matrix-forming material for didanosine sustained release formulations. Combination of the moderate swelling properties of Eudragit RSPM with the plastic properties of the more hydrophobic Ethocel 100 allowed suitable modulation of didanosine release.