title: Self-emulsifying pellets prepared by wet granulation in high-shear mixer: influence of formulation variables and preliminary study on the in vitro absorption.
abstract: A method of producing self-emulsifying pellets by wet granulation of powder mixture composed of microcrystalline cellulose, lactose and nimesulide as model drug with a mixture containing mono- and di-glycerides, polisorbate 80 and water, in a 10-l high shear mixer has been investigated. The effects of the formulation variables on pellets characteristics were evaluated by mixtures experimental design and by a polynomial model, in order to describe the phenomenon, to verify eventual interactions among components of the mixture and to investigate the feasibility of scaling-up. After determination of size distribution, the pellets were characterised by scanning electron microscopy, dissolution and disintegration tests, and by in vitro absorption test Such an approach, applied to the development of a self-emulsifying system for nimesulide as poorly water-soluble model drug, resulted in different formulations with improved drug solubility and permeability characteristics. The data demonstrate that pellets composed of oil to surfactant ratio of 1:4 (w/w) presented improvement in performance in permeation experiments.
authors.affiliation: Department of Pharmaceutical Sciences, University of Trieste, Piazzale Europa 1, 34127 Trieste, Italy.
authors.forename: Erica
authors.initials: E
authors.lastname: Franceschinis
authors.forename: Dario
authors.initials: D
authors.lastname: Voinovich
authors.forename: Mario
authors.initials: M
authors.lastname: Grassi
authors.forename: Beatrice
authors.initials: B
authors.lastname: Perissutti
authors.forename: Jelena
authors.initials: J
authors.lastname: Filipovic-Grcic
authors.forename: Anita
authors.initials: A
authors.lastname: Martinac
authors.forename: Francesco
authors.initials: F
authors.lastname: Meriani-Merlo
mesh_terms: D000042:Absorption; D000704:Analysis of Variance; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000493:pharmacokinetics; D002482:Cellulose / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D004337:Drug Carriers / Q000737:chemistry; D004339:Drug Compounding / Q000379:methods; D004655:Emulsions / Q000737:chemistry*; D005989:Glycerides / Q000737:chemistry; D007421:Intestine, Small / Q000378:metabolism; D008297:Male; D008855:Microscopy, Electron, Scanning / Q000379:methods; D010316:Particle Size; D011208:Powders / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D013449:Sulfonamides / Q000737:chemistry / Q000493:pharmacokinetics; D013499:Surface Properties; D013678:Technology, Pharmaceutical / Q000379:methods*; D017155:Wettability
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D004655:Emulsions; D005989:Glycerides; D011208:Powders; D013449:Sulfonamides; D002482:Cellulose; C109691:microcrystalline cellulose; C012655:nimesulide