Evaluation of Chlorpheniramine Maleate microparticles in orally disintegrating film and orally disintegrating tablet for pediatrics

Hao Lou, Min Liu, Wen Qu, Zheyi Hu, Ed Brunson, James Johnson, Hassan Almoazen

Research output: Contribution to journalArticle

12 Citations (Scopus)

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, X 2: 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. Results and discussion: From polynomial regression analysis, the best values of variables leading to the optimized microparticles were X 1=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. Conclusion: Both ODF and ODT are shown to be suitable vehicles for taste masked Chlorpheniramine Maleate microparticles with potential for pediatric uses.

Original languageEnglish (US)
Pages (from-to)910-918
Number of pages9
JournalDrug Development and Industrial Pharmacy
Volume40
Issue number7
DOIs
StatePublished - Jan 1 2014

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Chlorpheniramine
Pediatrics
Tablets
Pharmaceutical Preparations
Weights and Measures
Oils
Polynomials
Spray drying
Driers (materials)
Water
Tensile Strength
Disintegration
Dosage Forms
Statistical Models
Masks
Emulsions
Encapsulation
Saliva
Regression analysis
Design of experiments

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry

Cite this

Evaluation of Chlorpheniramine Maleate microparticles in orally disintegrating film and orally disintegrating tablet for pediatrics. / Lou, Hao; Liu, Min; Qu, Wen; Hu, Zheyi; Brunson, Ed; Johnson, James; Almoazen, Hassan.

In: Drug Development and Industrial Pharmacy, Vol. 40, No. 7, 01.01.2014, p. 910-918.

Research output: Contribution to journalArticle

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