Partition coefficients (n-octanol/water) of N-butyl-p-aminobenzoate and other local anesthetics measured by reversed-phase high-performance liquid chromatography |
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Authors: | RJE Grouls EW Ackerman HHM Korsten LJ Hellebrekers DD Breimer |
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Institution: | aDepartment of Pharmaceutical Services, Catharina Hospital, Michelangelolaan 2, P.O. Box 1350, 5602 ZA Eindhoven, Netherlands;bDepartment of Anesthesiology, Catharina Hospital, Eindhoven, Netherlands;cDepartment of Clinical Sciences of Companion Animals and Department of Anesthesiology, Faculty of Veterinary Medicine, University of Utrecht, Utrecht, Netherlands;dCenter for Bio-Pharmaceutical Sciences, Leiden, Netherlands |
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Abstract: | For the determination of the logarithmic partition coefficients between n-octanol and water (log Po/w) of local anesthetics, the pH of the aqueous phase needs to be adjusted to high values to ensure that the local anesthetics are in the unionized form. Using the shake-flask or the stir-flask method, this high pH may catalyze hydrolysis, leading to increasing amounts of impurities in time. These impurities exclude non-selective quantification methods like UV spectrometry and require repetitive quantitative analysis of both liquid phases resulting in a tedious and time-consuming method. A rapid reversed-phase HPLC method was developed to measure log Po/w of the local anesthetics N-butyl-p-aminobenzoate, methyl-p-aminobenzoate, benzocaine, procaine, mepivacaine, prilocaine, lidocaine, bupivacaine, etidocaine, tetracaine and oxubuprocaine. |
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Keywords: | Partition coefficient |
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