title: Emulsified systems based on glyceryl monostearate and potassium cetyl phosphate: scale-up and characterization of physical properties.
abstract: Introducing a pharmaceutical product on the market involves several stages of research. The scale-up stage comprises the integration of previous phases of development and their integration. This phase is extremely important since many process limitations which do not appear on the small scale become significant on the transposition to a large one. Since scientific literature presents only a few reports about the characterization of emulsified systems involving their scaling-up, this research work aimed at evaluating physical properties of non-ionic and anionic emulsions during their manufacturing phases: laboratory stage and scale-up. Prototype non-ionic (glyceryl monostearate) and anionic (potassium cetyl phosphate) emulsified systems had the physical properties by the determination of the droplet size (D[4,3], mum) and rheology profile. Transposition occurred from a batch of 500-50,000g. Semi-industrial manufacturing involved distinct conditions: intensity of agitation and homogenization. Comparing the non-ionic and anionic systems, it was observed that anionic emulsifiers generated systems with smaller droplet size and higher viscosity in laboratory scale. Besides that, for the concentrations tested, augmentation of the glyceryl monostearate emulsifier content provided formulations with better physical characteristics. For systems with potassium cetyl phosphate, droplet size increased with the elevation of the emulsifier concentration, suggesting inadequate stability. The scale-up provoked more significant alterations on the rheological profile and droplet size on the anionic systems than the non-ionic.
authors.affiliation: Department of Pharmacy, School of Pharmaceutical Sciences, University of São Paulo, 580 Prof. Lineu Prestes Av., Bl. 13/15, Conjunto das Químicas, Cidade Universitária, 05508-900 São Paulo, SP, Brazil.
authors.forename: André Rolim
authors.initials: AR
authors.lastname: Baby
authors.forename: Diego Monegatto
authors.initials: DM
authors.lastname: Santoro
authors.forename: Maria Valéria Robles
authors.initials: MV
authors.lastname: Velasco
authors.forename: Cristina Helena
authors.initials: CH
authors.lastname: Dos Reis Serra
mesh_terms: D000838:Anions / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D015195:Drug Design; D004355:Drug Stability; D045703:Emulsifying Agents / Q000737:chemistry*; D004655:Emulsions / Q000737:chemistry; D005079:Excipients / Q000737:chemistry; D005989:Glycerides / Q000737:chemistry*; D010755:Organophosphates / Q000737:chemistry*; D010316:Particle Size; D012212:Rheology; D013678:Technology, Pharmaceutical / Q000379:methods*; D014783:Viscosity
chemical_list: D000838:Anions; D045703:Emulsifying Agents; D004655:Emulsions; D005079:Excipients; D005989:Glycerides; D010755:Organophosphates; C532212:potassium cetyl phosphate; C048159:glyceryl monostearate