Pharmacokinetics of the enantiomers of indoprofen in man.

Indoprofen, a non-steroidal analgesic and antiinflammatory drug whose activity and safety in man have been established in a large number of studies, has an asymmetric carbon atom and can therefore occur as either the (+) or the (-) enantiomer. As it has been shown that its pharmacological effects are almost entirely due to the (+) isomer (d-indoprofen), some pharmacokinetic properties of the latter have been studied in man in comparison with the racemic mixture given by oral administration, d-indoprofen is cleared from plasma and excreted in urine (as unchanged plus conjugated drug) at a slower rate than l-indoprofen. Moreover, no stereospecific inversion of d-indoprofen to the inactive enantiomer occurs after either single or repeated (one week) administration. The pharmacokinetic behaviour of d-indoprofen in the human organism appears to be the same after administration of the racemic form or of the dextro-enantiomer, when the latter is given at half the dose.

High-performance liquid chromatographic method for pharmacokinetic studies on the new anthracycline 4-demethoxydaunorubicin and its 13-dihydro derivative.

The anthracyclines are a group of antitumoral antibiotics with significant clinical efficacy. Among the new anthracycline derivatives, 4-demethoxydaunorubicin showed interesting biological properties in terms of both spectrum of activity and therapeutic index and was recently introduced in clinical trials. The present paper describes the analytical method developed to investigate the pharmacokinetics of this derivative. The method consists of the extraction of 4-demethoxydaunorubicin and its 13-dihydro metabolite from plasma with chloroform--1-heptanol (9:1) and re-extraction with 0.3 M phosphoric acid, separation by high-performance liquid chromatography and quantification by sensitive fluorescence detection. Plasma level curves obtained from cancer patients treated with the drug are shown.