title: Evaluation of Chlorpheniramine Maleate microparticles in orally disintegrating film and orally disintegrating tablet for pediatrics.
abstract: OBJECTIVE
  To mask the bitterness of Chlorpheniramine Maleate via encapsulating drug into Eudragit EPO microparticles, and then incorporate these microparticles into orally disintegrating films (ODF) and orally disintegrating tablets (ODT) for pediatric uses.
  
  
  METHODS
  Spray drying of water-in-oil emulsion was utilized to encapsulate Chlorpheniramine Maleate into Eudragit EPO microparticles. Based on an orthogonal experimental design L9 (3(3)), polynomial regression models were developed to evaluate correlation between microparticle properties (encapsulation efficiency and drug release) and variables (X1: weight ratio of polymer to drug, X2: volume ratio of oil to water and X3: Q-flow of spray dryer). ODF and ODT formulations were evaluated including weight variation, content uniformity, tensile strength, disintegration time, friability and dissolution profiles. The bitterness taste test was evaluated in 10 adult volunteers.
  
  
  CONCLUSIONS
  From polynomial regression analysis, the best values of variables leading to the optimized microparticles were X1 = 10, X2 = 3 and X3 = 45. The optimized microparticles were incorporated into ODF and ODT with satisfactory weight and drug content uniformity, and acceptable physical strength. Both dosage forms disintegrated immediately (less than 40 s) in simulated saliva solutions. The outcome of taste-masking test indicated that microparticles alleviated drug bitterness significantly; bitterness was not discernible with microparticles incorporated in ODT, whereas only slight bitterness was detected from microparticles incorporated into ODF.
  
  
  CONCLUSIONS
  Both ODF and ODT are shown to be suitable vehicles for taste masked Chlorpheniramine Maleate microparticles with potential for pediatric uses.
authors.affiliation: Department of Pharmaceutical Sciences, University of Tennessee Health Science Center , Memphis, TN , USA .
authors.forename: Hao
authors.initials: H
authors.lastname: Lou
authors.forename: Min
authors.initials: M
authors.lastname: Liu
authors.forename: Wen
authors.initials: W
authors.lastname: Qu
authors.forename: Zheyi
authors.initials: Z
authors.lastname: Hu
authors.forename: Ed
authors.initials: E
authors.lastname: Brunson
authors.forename: James
authors.initials: J
authors.lastname: Johnson
authors.forename: Hassan
authors.initials: H
authors.lastname: Almoazen
mesh_terms: D000284:Administration, Oral; D000328:Adult; D055598:Chemical Phenomena; D002626:Chemistry, Pharmaceutical; D002648:Child; D002744:Chlorpheniramine / Q000008:administration & dosage* / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding; D065546:Drug Liberation; D006801:Humans; D008954:Models, Biological; D010316:Particle Size; D011109:Polymethacrylic Acids / Q000737:chemistry*; D012044:Regression Analysis; D012463:Saliva / Q000737:chemistry; D012995:Solubility; D013607:Tablets; D013649:Taste; D013718:Tensile Strength; D014059:Tongue
chemical_list: D004337:Drug Carriers; D011109:Polymethacrylic Acids; D013607:Tablets; D002744:Chlorpheniramine; C518398:Eudragit E PO
keywords: Design of experiment; microparticle; orally disintegrating film; orally disintegrating tablet; taste masking