title: Preparation and Evaluation of Hot-Melt Extruded Patient-Centric Ketoprofen Mini-Tablets.
abstract: BACKGROUND
  Bitter tasting drugs represent a large portion of active pharmaceutical ingredients. Mini-tablets are specifically designed for patients with difficulty in swallowing particular in young children up to 10 years of age, geriatric patients and patients with esophagitis.
  
  
  OBJECTIVE
  The present study was aimed to prepare, taste-masked mini-tablets, which are easily swallowed dosage forms, primarily to be used by pediatric and geriatric patients.
  
  
  METHODS
  Ketoprofen (10%-50% w/w) and Eudragit® EPO were blended and extruded with a 5-mm strand die and cut into consistent mini-tablets by using an adapted downstream pelletizer.
  
  
  RESULTS
  Differential scanning calorimetry and polarized light microscopy-hot stage microscopy studies confirmed that the binary mixtures were miscible under the employed extrusion temperatures. In-vitro release studies showed that drug release was less than 0.5% within the first 2 min in simulated salivary fluid (pH 6.8) and more than 90% in the first 20 min in gastric media (pH 1.0). The results of the electronic tongue analysis were well correlated with the drug release profile of the mini-tablets in the artificial saliva. Scanning electron microscopy revealed no cracks on the surface of the minitablets, confirming that the mini-tablets were compact solids. Chemical imaging confirmed the uniform distribution of ketoprofen inside the polymer matrices.
  
  
  CONCLUSIONS
  Eudragit® EPO containing ketoprofen at various drug loads were successfully melt extruded into tastedmasked mini-tablets. The reduced drug release at salivary pH correlated well with Astree e-Tongue studies for taste masking efficiency.
authors.forename: Abdullah S
authors.initials: AS
authors.lastname: Alshetaili
authors.forename: Bjad K
authors.initials: BK
authors.lastname: Almutairy
authors.forename: Roshan V
authors.initials: RV
authors.lastname: Tiwari
authors.forename: Joseph T
authors.initials: JT
authors.lastname: Morott
authors.forename: Sultan M
authors.initials: SM
authors.lastname: Alshehri
authors.forename: Xin
authors.initials: X
authors.lastname: Feng
authors.forename: Bader B
authors.initials: BB
authors.lastname: Alsulays
authors.forename: Jun-Bom
authors.initials: JB
authors.lastname: Park
authors.forename: Feng
authors.initials: F
authors.lastname: Zhang
authors.affiliation: Department of Pharmaceutics and Drug Delivery, Director, Pii Center for Pharmaceutical Technology, School of Pharmacy, The University of Mississippi, University, MS 38677, USA. marepka@olemiss.edu.
authors.forename: Michael A
authors.initials: MA
authors.lastname: Repka
mesh_terms: D000284:Administration, Oral; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry*; D015374:Biosensing Techniques / Q000295:instrumentation; D002152:Calorimetry, Differential Scanning; D018360:Crystallography, X-Ray; D003692:Delayed-Action Preparations; D004339:Drug Compounding; D062609:Electronic Nose; D005079:Excipients / Q000737:chemistry*; D005750:Gastric Juice / Q000737:chemistry; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007660:Ketoprofen / Q000008:administration & dosage / Q000737:chemistry*; D007700:Kinetics; D008855:Microscopy, Electron, Scanning; D008859:Microscopy, Polarization; D011109:Polymethacrylic Acids / Q000737:chemistry*; D033362:Powder Diffraction; D012463:Saliva / Q000737:chemistry; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013499:Surface Properties; D013607:Tablets; D013649:Taste; D013678:Technology, Pharmaceutical / Q000295:instrumentation / Q000379:methods*; D013696:Temperature
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D003692:Delayed-Action Preparations; D005079:Excipients; D011109:Polymethacrylic Acids; D013607:Tablets; C518398:Eudragit E PO; D007660:Ketoprofen