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Selected Publication:
Egginger, G; Lindner, W; Brunner, G; Stoschitzky, K.
Direct enantioselective determination of (R)- and (S)-propranolol in human plasma. Application to pharmacokinetic studies.
J Pharm Biomed Anal. 1994; 12(12):1537-1545
Doi: 10.1016%2F0731-7085%2894%2900129-4
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PubMed
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- Co-authors Med Uni Graz
- Brunner Gernot
- Stoschitzky Kurt
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- Abstract:
- In order to examine possible drug interactions of (R)- and (S)-propranolol a randomized, double blind, crossover study has been performed, administering orally single doses of 40 mg (R,S)- and of 20 mg (S)-propranolol. HCl three times daily over a week to reach steady state conditions. After the first single dose of 40 mg (R,S)-propranolol. HCl, the AUC0-infinity and Cmax values of the (S)-isomer were greater than those of the (R)-isomer: the ratio of AUC(S) over AUC(R) was 1.77 (P < 0.05) and that of Cmax 1.57 (P < 0.01). When (S)-propranolol.HCl was given as a single 20 mg dose, the AUC(S) value was a factor of 0.55 lower than that administration of 40 mg (R,S)-propranolol.HCl. At steady state, the AUC of (S)-propranolol was 1.52 times higher (P < 0.01) than that of the (R)-isomer after administration of 40 mg racemate, and comparing the (S)-isomer, the ratio was 1.21. Following administration of the first single dose of 40 mg of the racemate, the mean (SD) clearance of the (R)- and (S)-isomers was 110 (84) and 61 (37) ml min-1 kg-1, respectively; at steady state these values were 89 (55) and 57 (37) ml min-1 kg-1, respectively. Respective values for (S)-propranolol after single isomer administration (20 mg) were 86 (36) and 57 (25) ml min-1 kg-1 in single dose and steady state situations. The data are based on the quantitative analysis of (R)- and (S)-propranolol in plasma.(ABSTRACT TRUNCATED AT 250 WORDS)
- Find related publications in this database (using NLM MeSH Indexing)
- Chromatography, High Pressure Liquid - methods
- Cross-Over Studies - methods
- Double-Blind Method - methods
- Half-Life - methods
- Humans - methods
- Metabolic Clearance Rate - methods
- Propranolol - blood
- Stereoisomerism - blood
- Find related publications in this database (Keywords)
- Propranolol Enantiomers
- Stereoselective Pharmacokinetics
- Enantioselective LC-Bioassay
- Oxazolidine-2-One-Derivative
- Fluorometric Detection