Add time:07/28/2019         Source:sciencedirect.com

The aim was to study the pharmacokinetic equivalence of the local anaesthetic ropivacaine and its stable isotope analogue [2H3]-ropivacaine. Ropivacaine (40.0–53.0 mg) and [2H3]-ropivacaine (41.9–52.4 mg) were given simultaneously to eight healthy subjects as a single i.v. infusion. Blood and urine samples were collected and the concentrations of ropivacaine and [2H3]-ropivacaine were determined by gas chromatography–mass spectrometry (GC–MS) combined with an isotope dilution technique. The between-days accuracy was about 100% for both compounds and the between-days precisions were 3–13% and 5–11% for ropivacaine and [2H3]-ropivacaine, respectively. The plasma concentrations at the end of the infusion were similar for both forms (about 1 mg l−1), as were clearance (about 475 ml min−1), volume of distribution at steady state (about 54 l) and terminal half-life (about 1.8 h). The 95% confidence intervals for the ratios (ropivacaine/[2H3]-ropivacaine) of the individual parameters were in the range 0.90–1.10. It was concluded that ropivacaine and [2H3]-ropivacaine are pharmacokinetically equivalent.

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