Enmascaramiento de sabores en formas farmacéuticas sólidas orales / Taste masking in oral solid dosage forms

Aunque tradicionalmente ligado a formas farmacéuticas líquidas orales, el enmascaramiento del sabor como parámetro crítico en la formulación de medicamentos ha cobrado recientemente un nuevo auge en respuesta al desarrollo de formas farmacéuticas sólidas orales que persiguen una disgregación, bien ex vivo, bien en la cavidad bucal. El enmascaramiento no sólo comprende la neutralización del potencial sabor desagradable inherente al principio activo, sino también la obtención de un sabor agradable en la formulación final, con repercusión tanto a nivel sanitario, puesto que cuanto mayor sea la aceptación por parte del paciente, mayor será su adherencia al tratamiento; como a nivel económico, ya que el sabor del producto puede marcar la diferencia entre el éxito y el fracaso comercial. Mediante esta revisión se ponen de relieve las estrategias aplicables en el enmascaramiento de sabores de formas farmacéuticas sólidas orales, se clasifican y describen los principales excipientes correctores del sabor, así como se efectúa una compilación exhaustiva de las técnicas de evaluación de la eficacia de los distintos recursos empleados en el enmascaramiento del sabor desagradable. De esta forma, se amplía el ámbito de aplicación del concepto enmascaramiento del sabor, demostrándose que es un área del cual aún hay mucho por decir

Despite being traditionally associated with oral liquid dosage forms, taste masking as critical attribute in the formulation of drug products has recently experienced a renaissance, mostly due to the development of oral solid dosage forms aimed at achieving disintegration either under ex vivo conditions or even more relevantly into the oral cavity. Not only does taste masking involve the neutralization of the potential unpleasant flavour inherent to the drug substance, but also seeks to achieve tasty flavour in the final drug product, since it has influence both to a sanitary extent (the higher the patient acceptance, the better the patient compliance) and to an economical extent (since the flavour of a marketed product can make the difference between commercial success or commercial failure). The purpose of this review is to outline the strategies likely to be applied in taste masking of oral solid dosage forms, to sort out and describe the major flavour-modifying agents in the pharmaceutical field, as well as to compile comprehensively testing techniques of the efficacy of the various taste masking strategies. Consequently, this review adds to the scope of taste masking a further dimension, serving thus as a proof-of-concept that much remains still to be said in this area

Validation protocol of analytical procedures for quantification of drugs in polymeric systems for parenteral administration: dexamethasone phosphate disodium microparticles.

In this work a protocol to validate analytical procedures for the quantification of drug substances formulated in polymeric systems that comprise both drug entrapped into the polymeric matrix (assay:content test) and drug released from the systems (assay:dissolution test) is developed. This protocol is applied to the validation two isocratic HPLC analytical procedures for the analysis of dexamethasone phosphate disodium microparticles for parenteral administration. Preparation of authentic samples and artificially "spiked" and "unspiked" samples is described. Specificity (ability to quantify dexamethasone phosphate disodium in presence of constituents of the dissolution medium and other microparticle constituents), linearity, accuracy and precision are evaluated, in the range from 10 to 50 µg mL(-1) in the assay:content test procedure and from 0.25 to 10 µg mL(-1) in the assay:dissolution test procedure. The robustness of the analytical method to extract drug from microparticles is also assessed. The validation protocol developed allows us to conclude that both analytical methods are suitable for their intended purpose, but the lack of proportionality of the assay:dissolution analytical method should be taken into account. The validation protocol designed in this work could be applied to the validation of any analytical procedure for the quantification of drugs formulated in controlled release polymeric microparticles.