Tablets and minitablets prepared from spray-dried SMEDDS containing naproxen.
The purpose of this study was to compare different solidification techniques (i.e., adsorption technique, spray-drying process, high-shear granulation, fluid-bed granulation) for preparing solid SMEDDS powders by using solid carriers identified as appropriate and to produce a single (tablets) or multiunit (minitablets) solid dosage form based on prepared solid SMEDDS loaded with naproxen in a dissolved (6% w/w) or supersaturated (18% w/w) state. Among the solidification techniques and carriers tested, the powders produced using the spray-drying process and maltodextrin (MD) as a carrier exhibited the best self-microemulsifying properties, comparable with liquid SMEDDS. Furthermore, DoE (Design of Experiments) showed that pressure at the nozzle and pump speed (regulating feed flow rate) applied during spray drying had a major and significant influence on self-microemulsifying properties (mean droplet size and PDI) of the solid SMEDDS prepared. Furthermore, it was shown that compression of solid SMEDDS into (mini) tablets influences its self-microemulsifying properties in a negative direction. This resulted in lowering the dissolution profile of naproxen from tablets and minitablets in comparison with liquid and solid SMEDDS. However, all compressed SMEDDS formulations still had considerable influence on the dissolution profile and solubility enhancement of naproxen.
Krka, d.d., Novo mesto, Šmarješka cesta 6, 8000 Novo mesto, Slovenia; Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, 1000 Ljubljana, Slovenia.
Katja
K
Čerpnjak
Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, 1000 Ljubljana, Slovenia.
Alenka Zvonar
AZ
Pobirk
Krka, d.d., Novo mesto, Šmarješka cesta 6, 8000 Novo mesto, Slovenia; Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, 1000 Ljubljana, Slovenia.
Franc
F
Vrečer
Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, 1000 Ljubljana, Slovenia. Electronic address: Mirjana.Gasperlin@ffa.uni-lj.si.
Mirjana
M
Gašperlin
D002152:Calorimetry, Differential Scanning; D002482:Cellulose / Q000737:chemistry; D016503:Drug Delivery Systems; D065546:Drug Liberation; D006244:Hardness; D009288:Naproxen / Q000008:administration & dosage*; D011208:Powders; D012822:Silicon Dioxide / Q000737:chemistry; D012995:Solubility; D013607:Tablets / Q000737:chemistry*; D013678:Technology, Pharmaceutical / Q000379:methods*
D011208:Powders; D013607:Tablets; D009288:Naproxen; D012822:Silicon Dioxide; D002482:Cellulose
DSC; Dissolution profile improvement; DoE; SEM; Self-(micro) emulsifying properties; Solidification