Development of immediate release Rupatadine fumarate 10 mg tablets: A Quality by Design (QbD) approach
Fecha
2019
Tipo
artículo original
Autores
Castillo Henríquez, Luis
Vargas Zúñiga, Rolando
Carazo Berrocal, Gustavo
Madrigal Redondo, German
Calvo Guzmán, Briner
Baltodano Viales, Eleaneth
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ISSN de la revista
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Editor
Resumen
The main objective of this research is to develop an immediate release Rupatadine fumarate 10
mg tablets formulation by direct compression, through a Quality by Design approach in Costa
Rica.
Methods: According to a Quality by Design approach; Target Product Profile, Quality Target
Product Profile and the Critical Quality Attributes were defined. In the preformulation study,
compatibility tests were carried out between the raw materials. The Critical Material Attributes
were established using Quality Risk Management. Three formulation prototypes were prepared
by direct compression and its Critical Process Parameters were defined. The analysis of the
prototypes was realized in terms of organoleptic properties, identification, potency, content
uniformity, dissolution, disintegration, friability and loss by drying.
Results: All the prototypes showed a white or slightly pink surface, potency between 90.0 –
110.0% of the labeling, an acceptance value for the content uniformity lower than the
specification (AV < 15), the dissolved amount of active pharmaceutical ingredient was greater
than 85.0 % at 30 minutes, friability less than 1.0 %, a disintegration time less than 15 minutes
and moisture content less than 2.0%.
Conclusions: The approaching of a Quality by Design model to the current development allowed
to obtain satisfactory results in the three formulation prototypes. The excipients to be used can be
lactose monohydrate, microcrystalline cellulose, sodium croscarmellose, pregelatinized starch,
magnesium stearate, stearic acid and PVP K-30.
Descripción
Palabras clave
Antihistaminic, Direct compression, Formulation, Immediate release, Pharmaceutical Research and Development, Quality by Design, Rupatadine fumarate, Tablets