| Autor: |
Kraft, Walter K., Barneschi, Irene, Bocchi, Maria, Santoro, Debora, Cella, Massimo |
| Předmět: |
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| Zdroj: |
Journal of Pediatric Pharmacology & Therapeutics; 2024, Vol. 29 Issue 1, p49-52, 4p |
| Abstrakt: |
OBJECTIVE: Sublingual buprenorphine has demonstrated efficacy for treatment of the neonatal opioid withdrawal syndrome (NOWS), but the current formulation used in clinical practice contains 30% ethanol. Ethanol as a pharmacologically active excipient ideally should be removed from neonatal formulations. The objective of this study was to determine the relative bioavailability of a novel ethanol-free formulation (CHF6563) compared with the commonly used ethanolic solution in a phase I, open-label, 2-period, single-dose, crossover study in healthy adults. METHODS: Eighteen adult opioid-naïve volunteers were administered one of the formulations in a randomized crossover treatment. After a 10-day washout period, subjects received the other formulation. Serial blood samples were drawn for pharmacokinetic analysis over 48 hours. RESULTS: The geometric mean ratio (90% CIs) of the ethanol-free buprenorphine solution AUC0-last was 0.80 (0.65-0.99) and Cmax was 0.81 (0.66-0.99) compared with reference ethanolic formulation. The ethanol-free formulation had a greater degree of intersubject variability than the ethanol-containing reference formulation (coefficient of variation of 59% vs 31.5%, respectively, for AUC0-last). CONCLUSIONS: In an adult population, a novel ethanol-free formulation of buprenorphine containing widely used excipients demonstrated a slight decrease in bioavailability when compared with an ethanolic solution. These RESULTS: will inform those seeking to develop ethanol-free pediatric drug formulations. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
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