title: The effects of screw configuration and polymeric carriers on hot-melt extruded taste-masked formulations incorporated into orally disintegrating tablets.
abstract: The primary aim of this research was to produce successfully taste masked formulations of Sildenafil Citrate (SC) using hot-melt extrusion (HME) technology. Multiple screw configurations and polymeric carriers were evaluated for their effects on taste masking efficiency, which was assessed by both E-tongue analysis and in vitro dissolution in simulated salivary fluid (SSF, pH 6.8 artificial saliva). The screw configurations were further assessed for their effects on the morphology of the API using PXRD, FT-IR and mid-infrared chemical imaging. It was determined that the screw configuration had a profound effect on the taste masking efficiency of the formulations as a result of altering the physical state of the API. Selected extruded formulations using ethylcellulose (EC) with a pore former were further formulated into orally disintegrating tablets (ODTs), which were optimized by varying the grade and percentage of the superdisintegrant used. An optimized disintegration time of approximately 8 seconds was achieved. The final ODT formulation exhibited excellent taste masking properties with over 85% drug release in gastric media as well as physical tablet properties. Interestingly, friability, which tends to be a common concern when formulating ODTs, was well within the acceptable limits (<1%) for common tablets.
authors.affiliation: Department of Pharmaceutics & Drug Delivery, University of Mississippi, University, MS, USA.
authors.forename: Joseph T
authors.initials: JT
authors.lastname: Morott
authors.forename: Manjeet
authors.initials: M
authors.lastname: Pimparade
authors.forename: Jun-Bom
authors.initials: JB
authors.lastname: Park
authors.forename: Chelsea P
authors.initials: CP
authors.lastname: Worley
authors.forename: Soumyajit
authors.initials: S
authors.lastname: Majumdar
authors.forename: Zhuoyang
authors.initials: Z
authors.lastname: Lian
authors.forename: Elanor
authors.initials: E
authors.lastname: Pinto
authors.forename: Yunxia
authors.initials: Y
authors.lastname: Bi
authors.forename: Thomas
authors.initials: T
authors.lastname: Durig
authors.forename: Michael A
authors.initials: MA
authors.lastname: Repka
mesh_terms: D000085:Acetates / Q000737:chemistry; D002482:Cellulose / Q000031:analogs & derivatives / Q000737:chemistry; D004337:Drug Carriers / Q000008:administration & dosage / Q000009:adverse effects / Q000737:chemistry*; D004339:Drug Compounding / Q000295:instrumentation*; D004867:Equipment Design; D005079:Excipients / Q000737:chemistry*; D005750:Gastric Juice / Q000737:chemistry; D006358:Hot Temperature; D006801:Humans; D008954:Models, Biological; D058986:Phosphodiesterase 5 Inhibitors / Q000008:administration & dosage / Q000009:adverse effects / Q000737:chemistry; D010879:Piperazines / Q000008:administration & dosage / Q000009:adverse effects / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry*; D011205:Povidone / Q000031:analogs & derivatives / Q000737:chemistry; D011687:Purines / Q000008:administration & dosage / Q000009:adverse effects / Q000737:chemistry; D012463:Saliva / Q000737:chemistry*; D000068677:Sildenafil Citrate; D012995:Solubility; D013449:Sulfonamides / Q000008:administration & dosage / Q000009:adverse effects / Q000737:chemistry*; D013499:Surface Properties; D013607:Tablets; D013649:Taste; D014665:Vasodilator Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000737:chemistry
chemical_list: D000085:Acetates; D004337:Drug Carriers; D005079:Excipients; D058986:Phosphodiesterase 5 Inhibitors; D010879:Piperazines; D011108:Polymers; D011687:Purines; D013449:Sulfonamides; D013607:Tablets; D014665:Vasodilator Agents; C525248:copolyvidonum Plasdone S-630; C013517:ethyl cellulose; D002482:Cellulose; C008079:hydroxypropylcellulose; D000068677:Sildenafil Citrate; D011205:Povidone
keywords: Bitter API; Chemical Imaging; Crystalline Solid Dispersion; Disintegrating Tablets; Hot Melt Extrusion; Screw Configuration; Taste Masking