title: Formulation and evaluation of a montelukast sodium orally disintegrating tablet with a similar dissolution profile as the marketed product.
abstract: A major challenge of orally disintegrating tablet (ODT) development is predicting its bioequivalence to its corresponding marketed product. Therefore, comparing ODT dissolution profiles to those of the corresponding marketed product is very important. The objective of this study was to develop a 5.2-mg montelukast sodium (MS) ODT with a similar dissolution profile to that of the marketed chewable tablet. Dissolution profiles were examined in different media to screen each formulation. We found that MS dissolution from ODTs in acidic medium heavily depended on manufacturing methods. All MS ODTs prepared using direct compression rapidly disintegrated in acidic medium. However, dispersed MS powders aggregated into sticky masses, resulting in slow dissolution. In contrast, MS ODTs prepared using wet granulation had much faster dissolution rates in acidic medium with no obvious aggregation. Additionally, the optimized formulation, prepared using wet granulation, displayed similar dissolution profiles to the marketed reference in all four types of media examined (f2>50). The in vitro disintegration time of the optimized ODT was 9.5 ± 2.4 s, which meets FDA requirements. In conclusion, the wet granulation preparation method of MS ODTs resulted in a product with equivalent dissolution profiles as those of the marketed product.
authors.affiliation: a School of Pharmacy, East China University of Science and Technology , Shanghai , P.R. China.
authors.forename: Yong
authors.initials: Y
authors.lastname: Chen
authors.affiliation: a School of Pharmacy, East China University of Science and Technology , Shanghai , P.R. China.
authors.forename: Tingting
authors.initials: T
authors.lastname: Feng
authors.affiliation: a School of Pharmacy, East China University of Science and Technology , Shanghai , P.R. China.
authors.forename: Yong
authors.initials: Y
authors.lastname: Li
authors.affiliation: a School of Pharmacy, East China University of Science and Technology , Shanghai , P.R. China.
authors.forename: Bin
authors.initials: B
authors.lastname: Du
authors.affiliation: a School of Pharmacy, East China University of Science and Technology , Shanghai , P.R. China.
authors.forename: Weiyu
authors.initials: W
authors.lastname: Weng
mesh_terms: D000085:Acetates / Q000008:administration & dosage / Q000737:chemistry*; D000284:Administration, Oral; D018927:Anti-Asthmatic Agents / Q000008:administration & dosage / Q000737:chemistry*; D003521:Cyclopropanes; D004339:Drug Compounding; D065546:Drug Liberation; D006244:Hardness; D020024:Leukotriene Antagonists / Q000008:administration & dosage / Q000737:chemistry*; D011804:Quinolines / Q000008:administration & dosage / Q000737:chemistry*; D012995:Solubility; D013440:Sulfides; D013607:Tablets; D017155:Wettability
chemical_list: D000085:Acetates; D018927:Anti-Asthmatic Agents; D003521:Cyclopropanes; D020024:Leukotriene Antagonists; D011804:Quinolines; D013440:Sulfides; D013607:Tablets; C093875:montelukast
keywords: Dissolution profile comparison; evaluation; formulation; montelukast sodium; orally disintegrating tablets; wet granulation method