Effect of pH on sublingual absorption of oxycodone hydrochloride |
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Authors: | Abeer M Al-Ghananeem Ahmad H Malkawi Peter A Crooks |
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Institution: | (1) Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 40536-0082 Lexington, KY |
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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 electrospray ionization detector assay,
the absorption bioavailability 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 sublingually 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 average 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 oxycodone 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<.05). A sublingual spray dosage form of oxycodone hydrochloride would be a good alternative for fast onset pain management,
especially in children.
Published: March 10, 2006 |
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Keywords: | oxycodone sublingual spray acute pain rabbit |
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