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Effect of pH on the Sublingual Absorption of Oxycodone (Al-Ghananeem et al, 2005)

Effect of pH on the Sublingual Absorption of Oxycodone (Al-Ghananeem et al, 2005)

  1. Jatelka
    AAPS PharmSciTech, 2006, Vol.7(1), pp.E163-E167

    Al-Ghananeem, Abeer ; Malkawi, Ahmad ; Crooks, Peter

    ABSTRACT
    The purpose of this study was to develop a sublingual spray drug delivery formulation of oxycodone and evaluate the effect of formulation pH on sublingual absorption of oxycodone for acute pain management using rabbit as the animal model. Using a new, sensitive, and specific liquid chromatography/mass spectrometry (LC/MS) with electro-spray ionization detector assay, the absorption bioavailabil-ity of sublingual oxycodone was determined in rabbits by comparing plasma concentration after sublingual spray delivery with equivalent intravenous dose. The effect of formulation pH on sublingual absorption of oxycodone was also tested on rabbits that had received oxycodone sub-lingually at a dose of 0.1 mg/0.1 mL (pH 4.0 and 9.0). Blood samples were collected at different time points, and plasma oxycodone concentrations were determined by LC/MS. Following administration of a 0.1 mg dose, the aver-age Cmax values were found to be 64.9 ± 12.1 and 95.2 ± 10.1 ng/mL, for pH 4.0 and 9.0, respectively. The area under the curve (AUC) values were found to be 5807.0, and 8965.3 ng.min/mL for formulation pH 4.0 and 9.0, respectively. The mean sublingual bioavailability of oxy-codone was 45.4% ± 20.1% and 70.1% ± 17.9%, for pH 4.0 and 9.0, respectively. The formulation pH had no significant influence on oxycodone bioavailability (P G .05). A sublin-gual spray dosage form of oxycodone hydrochloride would be a good alternative for fast onset pain management, espe-cially in children.