PubMed Health⌕ Search

Biomedical subjects

D De Vos

Publications and source records attributed to D De Vos.

27 records · Page 2Linked to original sources

The bioavailability of Tamoplex (tamoxifen). Part 3. A steady-state study in breast cancer patients.

The bioavailability of two tamoxifen preparations (Tamoplex and Nolvadex) was compared in a multiple dose two-way cross-over design in twelve breast cancer patients. The formulations were found to be bioequivalent. Mean steady-state serum levels of tamoxifen and N-desmethyltamoxifen were 133 ng/ml and 242 ng/ml, respectively, at a single daily dose of three tablets of Tamoplex 10 mg and 128 ng/ml and 248 ng/ml, respectively, at a single daily dose of three tablets of Nolvadex 10 mg. While there was a large interpatient as well as intrapatient variability in steady-state levels of tamoxifen and N-desmethyltamoxifen, their ratio appeared to be constant in the individual patient.

Adult↗

The bioavailability of two new preparations of spironolactone tablets.

Two new preparations of spironolactone tablets containing 25 and 100 mg of spironolactone have been characterized by their disintegration time, tablet spironolactone content, dissolution profile and bioavailability in comparison with two known spironolactone preparations as reference material. The preparations were found to possess almost identical characteristics, assuring a proper clinical use of the new tablet preparations. For spironolactone, a positive outcome of the in vitro dissolution test coincides with an excellent bioavailability.

Adult↗

Bioavailability of methotrexate tablets.

The bioavailability of methotrexate 10 mg tablets has been determined to be 62 +/- 16%. After administration of a dose of 30 mg/m2 a maximum plasma concentration of ca. 20.10(-7) mole/l was found after ca. 1.7 h. The methotrexate plasma half-life was 2.4 h. It was concluded that the 10 mg tablet formulation at the dosage investigated is a suitable clinical methotrexate preparation.

Administration, Oral↗

Cytotoxic activity of di-n-butyltin(IV)(X-A-B-Y) compounds related to salicylic acid against human tumour cells.

A series of di-n-butyltin(IV) compounds of the type di-n-butyltin(IV)(X-A-B-Y) with the (X-A-B-Y) being related to salicylic acid was tested in vitro for cytotoxic activity against tumour cells of the human A 204, MCF-7, T24, WiDr and IgR-37 cell lines using the PIT method. In each cell line the di-n-butyltin(IV) compounds displayed similar activity. As compared to cisplatin, the compounds were 4- to 10-fold more effective against A 204, MCF-7 and T24 tumour cells and slightly more effective against WiDr cells. The effectiveness against IgR-37 cells was similar for cisplatin and di-n-butyltin (IV) compounds.

Cell Survival↗

In vitro antiproliferative effects, toxicity profiles in vivo in mice and antitumour activity in tumour-bearing mice of five organotin compounds.

The in vitro antiproliferative effects, the toxicity profiles in vivo in mice and the antitumour activity in tumour-bearing mice were screened for five recently synthesized organotin compounds: triphenyltin 5-sulfosalicylate (1), triphenyltin 5-aminosalicylate (2), triphenyltin 4-fluorobenzoate (3), tri-n-butyltin 2,6-difluorobenzoate (4) and di-n-butyltin bis (2,5-dihydroxybenzoate) (5). The in vitro chemosensitivity tests showed that compound 1 has the lowest antiproliferative effect in C26-10. In WiDr, compounds 1 and 5 were less active than the other compounds tested. The IC50 for cisplatin in C26-10 was in the same range as for 1. For compound 3 a steep dose response curve in C26-10 turned out to be remarkably different from the curves of the other compounds. In vivo, compound 1 was most toxic, mainly through paralysis. At their maximum tolerated dose (MTD) for single administration compounds 1, 2, 3 and 4 are inactive against murine colon carcinoma Colon 26. At a single administration, compound 5 was the most active compound with Test/Control ratio (T/C) below 0.6 and Growth Delay Factor (GDF) above 1.0, their respective cut-off levels for sensitivity.

Adenocarcinoma, Mucinous↗