title: Development and in vitro/in vivo evaluation of etodolac controlled porosity osmotic pump tablets.
abstract: The aim of the current work was the design and evaluation of etodolac controlled porosity osmotic pump (CPOP) tablets exhibiting zero-order release kinetics. Variables influencing the design of (1) core tablets viz., (a) osmogent type (sodium chloride, potassium chloride, mannitol, and fructose) and (b) drug/osmogent ratio (1:0.25, 1:0.50, and 1:0.75), and (2) CPOP tablets viz., (a) coating solution composition, (b) weight gain percentage (1-5%, w/w), and (c) pore former concentration (5%, 10%, and 20%, v/v), were investigated. Statistical analysis and kinetic modeling of drug release data were estimated. Fructose-containing core tablets showed significantly (P < 0.05) more retarded drug release rates. An inverse correlation was observed between drug/fructose ratio and drug release rate. Coating of the optimum core tablets (F4) with a mixture of cellulose acetate solution (3%, w/v), diethyl phthalate, and polyethylene glycol 400 (85:10:5, v/v, respectively) till a 4% w/w weight gain enabled zero-order sustained drug delivery over 24 h. Scanning electron microscopy micrographs of coating membrane confirmed pore formation upon contact with dissolution medium. When compared to the commercial immediate-release Napilac® capsules, the optimum CPOP tablets (F4-34) provided enhanced bioavailability and extended duration of effective etodolac plasma concentration with minimum expected potential for side effects in healthy volunteers.
authors.affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El-Aini, Egypt.
authors.forename: Ahmed
authors.initials: A
authors.lastname: Abd-Elbary
authors.forename: Mina Ibrahim
authors.initials: MI
authors.lastname: Tadros
authors.forename: Ahmed Adel
authors.initials: AA
authors.lastname: Alaa-Eldin
mesh_terms: D000328:Adult; D002626:Chemistry, Pharmaceutical / Q000379:methods* / Q000592:standards; D018592:Cross-Over Studies; D004353:Drug Evaluation, Preclinical / Q000379:methods / Q000592:standards; D017308:Etodolac / Q000737:chemistry* / Q000493:pharmacokinetics* / Q000592:standards; D006801:Humans; D007408:Intestinal Absorption / Q000187:drug effects / Q000502:physiology; D008297:Male; D009995:Osmosis / Q000187:drug effects* / Q000502:physiology; D010865:Pilot Projects; D016062:Porosity; D013608:Tablets, Enteric-Coated / Q000592:standards
chemical_list: D013608:Tablets, Enteric-Coated; D017308:Etodolac