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D de Vos

Publications and source records attributed to D de Vos.

29 records · Page 2Linked to original sources

The bioavailability of Tamoplex (tamoxifen). Part 4. A parallel study comparing Tamoplex and four batches of Nolvadex in healthy male volunteers.

A randomized parallel design has been validated for the study of tamoxifen bioavailability. Strong evidence was presented for the bioequivalence of Tamoplex 10 mg and four Nolvadex 10 mg preparations. Interbatch differences were of the same magnitude as differences between Tamoplex 10 mg and Nolvadex 10 mg. No in vitro--in vivo relationship could be established. Distribution and metabolism are the dominating factors in tamoxifen pharmacokinetics.

Adult↗

The bioavailability of Tamoplex (tamoxifen). Part 2. A single dose cross-over study in healthy male volunteers.

Tamoxifen and N-desmethyltamoxifen plasma concentrations were determined in a single dose cross-over study with Tamoplex and Nolvadex at the dose height of 40 mg in 18 healthy male volunteers with a wash-out period of at least 140 days. ANOVA, power analysis and novel bioequivalence tests on AUC, Cmax and tcmax, including a non-parametric one, demonstrated bioequivalence of Tamoplex and Nolvadex 10 mg tablets. The mean AUC ( +/- SD) values of tamoxifen after administration of Tamoplex or Nolvadex tablets were 1076 +/- 265 and 1131 +/- 301 h ng ml-1, respectively. ANOVA on the AUC values gave a p value of 0.450 with a power of 0.85 and a 95% confidence interval of 81.8-108.5% was obtained. The 0.8 power test showed a determined difference of 18.9%, whereas the actual difference was 4.9%. Interindividual and intraindividual variation was assessed. The pharmacokinetic data, well established for 34 hr, constitute a basis for further studies on tamoxifen distribution, elimination and metabolism.

Adult↗

pH modulates cisplatin toxicity.

Cisplatin in normal saline of pH 2.5 caused haemolysis of rat erythrocytes, whereas cisplatin in normal saline of pH 3.5 did not. Even a difference of 0.2 pH units appeared to be of significant importance: haemolysis of rat erythrocytes was observed with cisplatin in saline of pH 3.0 but not with cisplatin in saline of pH 3.2. The LD in mice was 15.4 mg/kg for cisplatin in saline of pH 2.5 versus 24.0 mg/kg for cisplatin in saline of pH 3.5. Experiments with cisplatin should include careful control of pH.

Animals↗

The bioavailability of Tamoplex (tamoxifen). Part 1. A pilot study.

Tamoxifen and N-desmethyltamoxifen plasma concentrations were found to be similar after a first single dose and during two months therapy with Tamoplex or Nolvadex in groups of 6 and 8 patients, respectively. Single dose absorption results in 10 healthy male volunteers demonstrated bioequivalence of Tamoplex and Nolvadex 10 mg tablets. A large interindividual variation in tamoxifen absorption data was observed, probably related to the dominating metabolic clearance of tamoxifen.

Adult↗

Assay of HA-966 in rat plasma by capillary gas-liquid chromatography with nitrogen-selective detection.

A gas-liquid chromatographic method for the determination of the gamma-aminobutyric acid-like drug 1-hydroxy-3-aminopyrrolidone-2 (HA-966) in plasma is described. HA-966 was converted into its diacetyl derivative AC2HA-966 with acetic anhydride. This compound could be suitable eluted from a capillary OV-17 support-coated open tubular column. A sensitive detection method was achieved by making use of nitrogen-phosphorus-selective flame ionization.

Animals↗

Determination of plasma concentrations of underivatized cyclophosphamide by capillary gas chromatography.

A sensitive method for the clinical determination of cyclophosphamide in 0.2 ml plasma by capillary gas chromatography with nitrogen-phosphorus detection is described. A detection limit of 50 nl/ml is readily obtainable, which is sufficiently low to measure the cyclophosphamide concentrations occurring in clinical practice. The selection of internal standards and the use of the nitrogen-phosphorus detection system is discussed, as well as eventualities for determination of cyclophosphamide metabolites.

Biological Availability↗

The acute toxicity and in vivo antitumour activity against L1210 leukemia of triphenyltin 3,5-diisopropylsalicylate, bis (di-n-butyl-(s)-2-pyrrolidone-5-carboxylato)tin oxide and di-n-butyltin bis(3-amino-4-methylbenzoate).

Triphenyltin 3,5-di-isopropylsalicylate, compound 1, is characterized by a maximum tolerated dose (MTD) of 20 mg/kg. Bis[di-n-butyl(2-pyrrolidone-5-carboxylato)tin] oxide, compound 2, and (di-n-butyltin bis(3-amino-4-methyl-benzoate), compound 3, exhibit similar acute toxicities (MTD = 8 mg/kg) despite their lower in vitro activity, as compared to compound 1, against the two human tumor cell lines MCF-7 and WiDr. All three are inactive in vivo against L1210 leukemia in mice.

Aminobenzoates↗