AbstractA procedure for the differential pulse voltammetric determination of three local anesthetics (Heptacaine, Carbisocaine and Pentacaine) at a screen‐printed electrode surface modified with the dsDNA layer is described. The detection limits obtained after 120 s drug accumulation from 0.01 M phosphate buffer solution pH 6.96 are 0.02 μM (Pentacaine) and 0.03 μM (Carbisocaine and Heptacaine). The method was applied to the determination of Carbisocaine in spiked serum.

01 Nov 2003·European Journal of Medicinal ChemistryQ1 · MEDICINE

Quantitative relationship between rat intestinal absorption and Abraham descriptors

Q1 · MEDICINE

Article

Author: Michael H Abraham ; Chris N Luscombe ; Yuan H Zhao ; Anne Hersey

Literature data on the intestinal absorption of 158 drug and drug-like compounds in rats have been collected, and Abraham descriptors for the set of drugs have been calculated using the method of Platts and Abraham et al. Results show that there is a significant relationship between rat intestinal absorption and the Abraham descriptors. In agreement with the human intestinal absorption model, the dominant descriptors in the rat model are the drug hydrogen bond acidity and basicity. In order to compare the absorption models in humans and rats, the absorption model developed from rats was used to predict the absorption in humans. The rat intestinal absorption model is similar to the human absorption model, and data on rats can effectively be used to predict human intestinal absorption.

01 Sep 2003·Die Pharmazie

Differences between gastric antiulcer effects of trapencaine enantiomers.

Article

Author: Ricicová, V ; Babul'ová, A ; Benes, L ; Kupková, Z ; Nosál'ová, V

The spatial arrangement of single stereoisomers may influence pharmacodynamic, pharmacokinetic and toxicological properties of a drug. Trapencaine (I. N. N.), (+/-)-trans-2-(pyrrolidin-1-yl)cyclohexylester of 3-(n)-pentyloxycarbanilic acid, was developed as an antiulcer drug with gastroprotective, local anaesthetic and spasmolytic effects. Limited information is available about the potential pharmacodynamic differences of the enantiomers of trapencaine. Therefore, the enantiomers of (+/-)-trans- or cis-2-(pyrrolidin-1-yl)cyclohexylester of 3-(n)-pentyloxy carbanilic acid were synthesised and tested on models of acute gastric damage induced by indomethacin and/or ethanol. A difference was found between their antiulcer effect, with the (+)-trans-enantiomer being the most effective and the (-)-cis-enantiomer the least effective in the models used.

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Indication	Highest Phase	Country/Location	Organization	Date
Anesthesia	Phase 1	-	Slovak Academy of Sciences	-
Helicobacter pylori infection	Phase 1	-	Slovak Academy of Sciences	-

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