title: The preparation of pellets containing a surfactant or a mixture of mono- and di-gylcerides by extrusion/spheronization.
abstract: The ability to incorporate either of the two components of a self-emulsifying system (polysorbate 80 (PSG80) and a mixture of mono- and di-glycerides (MDG)) separately into pellets prepared by extrusion/spheronization and the properties of any resulting pellets has been investigated. The results have established that it is possible to prepare satisfactory pellets thus adding to the range of ingredients that can be included in pellet formulations. For PS80, it was found possible to prepare pellets containing at least 92% of the surfactant/water mixture, but with a mixture of (MDG) and water, however, it was not possible to prepare pellets, which contained more than 46% of MDG. By analysis of variance significant relationships were established between the ratio of lactose to MCC and the ratio of the PS80 or MDG to water and the properties of the pellets. There were both similarities and differences of the two input factors, which provided relationships for the two materials. The quantity of liquid required, the fluid content of the pellets, the tensile strength and porosity of the pellets provided relationships for both systems, whereas the extrusion force and the median pellet size gave relationships for the PS80 systems, but they did not for the MDG systems. The opposite was true for interquartile range (IQR), the yield in the modal fraction and the shape factor. It was possible to identify global relationships for these systems and those reported previously, when the two components were combined as a self-emulsifying system, by the application of perceptual mapping. It was found that, there were relationships between the size range, expressed as the IQR and the fluid level required to make pellets; the quantity of the non-aqueous component of the fluid and the pellet shape factor; the extrusion force and the tensile strength of the pellets and the yield in the modal fraction and the ratio of the non-aqueous to aqueous content of the fluid used to prepare the pellets. The ability to use the materials independently offers further alternatives for the formulation of water insoluble drugs into pellet formulations.
authors.affiliation: The School of Pharmacy, University of London, Brunswick Square, London WC1N 1AX, UK. michael.newton@pharmacy.ac.uk
authors.forename: John Michael
authors.initials: JM
authors.lastname: Newton
authors.forename: Mariana Reis
authors.initials: MR
authors.lastname: Pinto
authors.forename: Fridrun
authors.initials: F
authors.lastname: Podczeck
mesh_terms: D001702:Biopharmaceutics; D055598:Chemical Phenomena; D002626:Chemistry, Pharmaceutical; D002627:Chemistry, Physical; D004075:Diglycerides / Q000737:chemistry*; D004304:Dosage Forms; D004339:Drug Compounding; D015195:Drug Design; D005079:Excipients / Q000737:chemistry* / Q000145:classification; D005989:Glycerides / Q000737:chemistry*; D006244:Hardness; D008855:Microscopy, Electron, Scanning; D015233:Models, Statistical; D008970:Molecular Weight; D010316:Particle Size; D011136:Polysorbates; D012044:Regression Analysis; D013501:Surface-Active Agents / Q000737:chemistry* / Q000145:classification; D013718:Tensile Strength
chemical_list: D004075:Diglycerides; D004304:Dosage Forms; D005079:Excipients; D005989:Glycerides; D011136:Polysorbates; D013501:Surface-Active Agents