1. Quinine sulphate pellets for flexible pediatric drug dosing: formulation development and evaluation of taste-masking efficiency using the electronic tongue
- Author
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Jean Paul Remon, Nathalie Huyghebaert, Pierre Claver Kayumba, Jd Ntawukuliryayo, Christophe B.Y. Cordella, Chris Vervaet, National University of Rwanda, Partenaires INRAE, Laboratory of Pharmaceutical Technology, Universiteit Gent = Ghent University [Belgium] (UGENT), and Alpha MOS France
- Subjects
pediatric formulation ,Chemistry, Pharmaceutical ,Pellets ,Pharmaceutical Science ,02 engineering and technology ,Biosensing Techniques ,electronic tongue ,Pharmacology ,030226 pharmacology & pharmacy ,Dosage form ,Dibutyl sebacate ,taste-masking ,Pellet Dosage Form ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,Polymethacrylic Acids ,Tongue ,quinine sulphate ,medicine ,Humans ,Technology, Pharmaceutical ,Dissolution testing ,Particle Size ,Child ,Quinine ,Chromatography ,Chemistry ,Plasticizer ,General Medicine ,Eudragit EPO ,021001 nanoscience & nanotechnology ,pellets ,[SDV.MP]Life Sciences [q-bio]/Microbiology and Parasitology ,Taste ,extrusion-spheronisation ,[SDV.SPEE]Life Sciences [q-bio]/Santé publique et épidémiologie ,Stearic acid ,[SDV.IMM.VAC]Life Sciences [q-bio]/Immunology/Vaccinology ,0210 nano-technology ,Biotechnology ,medicine.drug - Abstract
International audience; The purpose of this study was to develop a taste-masked quinine sulphate dosage form as a flexible pediatric formulation tool. Pellets were produced as they offer more flexibility to body weight dose adaptation and therefore represent an alternative to tablet breaking in pediatrics. Quinine sulphate pellets were produced via extrusion-spheronisation. Next pellets were coated using Eudragit E PO to obtain a taste-masked formulation. Using 15% dibutyl sebacate (based on polymer weight) as a plasticizer in the formulation caused rapid pellet agglomeration during storage at 40 degrees C and 75% relative humidity. Using stearic acid (15% based on polymer weight) as plasticizer yielded pellets which were less sensitive to sticking. Quinine sulphate release in water within the first 5 min of dissolution testing: 9.2%, 5.9% and 2.1% of the drug dose was released from pellets coated with 10%, 20% and 30% (w/w) Eudragit E PO, respectively. These observations correlated well with the bitterness score of the formulations determined via the Astree electronic tongue and its Bitterness Prediction Module, showing that 20% (w/w) Eudragit E PO was required to obtain a homogeneous film and to delay quinine sulphate release sufficiently to mask the bitterness after drug administration. In acid medium immediate quinine sulphate release was obtained.
- Published
- 2007
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