Development and optimization of dexketoprofen trometamol multiparticulates dosage forms

Abstract

The aim was to prepare extended release multi-particulates dosage form of Dexketoprofen trometamol which is the pharmacologically active isomer of ketoprofen. Utilization of active enantiomer with minimal dose and administration frequency, extended release multi-particulates dosage form were explored. Drug loaded pellets were prepared by two techniques i) Extrusion spheronization technique and ii) Wurster coating, while extended release coating of these two different drug pellets were done by wurster coating process. newlineFor drug loaded pellets prepared by extrusion spheronization process, lactose and microcrystalline cellulose as diluents, glycerin as plasticizer and povidone as binder were selected while for wurster process microcrystalline cellulose spheres as inert core, povidone as binder and Talc as anti-adherent were used. Kollicoat SR 30D as sustained release polymer, triethyl citrate as plasticizer and Talc as anti-tacking agent were used common for both drug loaded pellets coating for better comparison. newline newlineResults of various drug pellets formulation by extrusion spheronization process indicated that binder concentration, plasticizer concentration and lactose to MCC ratio at level of 1.49 to 1.95, 0.99 to 1.37 and 0.95 to 1.85 respectively yield good drug loaded pellets with targeted particle size fractions, assay and friability. Extruder and spheronizer speed were required 50 and 100 rpm respectively as optimum processing condition. Trial results of extended release coating of extrusion spheronised drug pellets were dictate that 28 %w/w extended release coating level with 10 %w/w talc concentration of total solid material and 10.0% w/w tri-ethyl citrate with respect to dry polymer amount yielded desired drug product quality attributes. Extended release coating process parameters optimization study indicated that atomisation air pressure 1.0 to 1.2 bar, product bed temperature 29 to 34°C and 7.8 to 10.0 gm/min yield good quality of extended release coated pellets in terms of desired quality attributes i.e. wit