title: Oseltamivir phosphate-amberlite(TM) IRP 64 ionic complex for taste masking: preparation and chemometric evaluation.
abstract: The objective of the present work was to evaluate and characterize a pediatric-friendly formulation of a bitter tasting drug, oseltamivir phosphate (drug). Amberlite IRP64 (resin) was used to make ionic complexes for masking its bitterness. Complexes of four drug-to-resin ratios, 1:1, 1:2, 1:4, and 1:6 (w/w), were prepared and characterized. At buccal pH of 6.8, drug-resin complexes of 1:1, 1:2, 1:4, and 1:6 ratios released 42.13%, 23.26%, 4.13%, and 14.94%, respectively, of loaded drug after 20 s. However, at stomach pH of 1.2 (0.1 N HCl), 61.96%, 70.18%, 85.88%, and 91.42% of drug was released from the same complexes in 6 min. Near-infrared (NIR) chemical imaging of the complexes showed homogeneous distribution of drug in the resin. Chemometric partial least squares model using NIR data of the drug showed a high correlation between calibration and predicted data (R(2) > 0.998). Overall, these results indicated the complex formation between drug and resin. The pH dependence of drug release from these complexes could minimize drug release in the mouth, whereas immediately releasing it in the stomach. Electronic tongue used to evaluate taste indicated that conductivity taste signals were different from control, suggesting taste masking of the drug.
authors.affiliation: Division of Product Quality Research, Office of Testing and Research, OPS, CDER, FDA, Silver Spring, Maryland.
authors.forename: Akhtar
authors.initials: A
authors.lastname: Siddiqui
authors.affiliation: Division of Product Quality Research, Office of Testing and Research, OPS, CDER, FDA, Silver Spring, Maryland.
authors.forename: Rakhi B
authors.initials: RB
authors.lastname: Shah
authors.affiliation: Division of Product Quality Research, Office of Testing and Research, OPS, CDER, FDA, Silver Spring, Maryland. Electronic address: Mansoor.Khan@fda.hhs.gov.
authors.forename: Mansoor A
authors.initials: MA
authors.lastname: Khan
mesh_terms: D000998:Antiviral Agents / Q000008:administration & dosage* / Q000737:chemistry; D002648:Child; D004337:Drug Carriers / Q000737:chemistry*; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007477:Ions / Q000737:chemistry; D053139:Oseltamivir / Q000008:administration & dosage* / Q000737:chemistry; D012117:Resins, Synthetic / Q000737:chemistry*; D017550:Spectroscopy, Fourier Transform Infrared; D019265:Spectroscopy, Near-Infrared; D013649:Taste; D014059:Tongue / Q000502:physiology
chemical_list: D000998:Antiviral Agents; D004337:Drug Carriers; D007477:Ions; D012117:Resins, Synthetic; D053139:Oseltamivir; C046797:amberlite