4.7 Article

Evaluation of Pentravan®, Pentravan® Plus, Phytobase®, Lipovan® and Pluronic Lecithin Organogel for the transdermal administration of antiemetic drugs to treat chemotherapy-induced nausea and vomiting at the hospital

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INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 515, 期 1-2, 页码 774-787

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ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2016.11.014

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Ondansetron; Dexamethasone; Aprepitant; Transdermal vehicle; Franz-type diffusion cell; Kinetic

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The objective of this study was to evaluate five commercial ready-to-use transdermal vehicles (Phytobase (R), Lipovan (R), Pentravan (R), Pentravan (R) Plus and Pluronic Lecithin Organogel (PLO)), for the compounding of three antiemetic drugs (ondansetron, dexamethasone and aprepitant) and their administration in combination to treat chemotherapy-induced nausea and vomiting (CINV) at the hospital. Drugs were individually formulated in these vehicles and in mixture in Pentravan (R) Plus using different penetration enhancers. Quality control of the forms has demonstrated that formulation process was mastered and convenient for the hospital (time required: 20 min). Diffusion experiments through synthetic membranes and pig ear epidermis performed using Franz-type diffusion cells, have shown that the release and permeation process were greater for ondansetron than for dexamethasone and aprepitant, with a release step not limiting. As permeation of aprepitant was too low, it was discarded of the study. When ondansetron and dexamethasone were compounded in combination in Pentravan (R) Plus, the most efficient vehicle, a permeation decrease was observed. Finally, the use of tween 20 instead of EtOH as chemical enhancer has led to 2-fold factor increase in the flux of dexamethasone, resulting in fluxes convenient for transdermal administration of ondansetron to a child, but insufficient for an adult and for dexamethasone. (C) 2016 Elsevier B.V. All rights reserved.

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