The stability of miconazole in various diluents and polyvinyl chloride (PVC) containers was determined and the release of diethylhexyl phthalate (DEHP) from PVC bags into intravenous infusions of miconazole was measured. An injection formulation (80 ml) containing a 1% solution of miconazole with 11.5% of Cremophor EL was added to 250-ml PVC infusion bags containing 5% glucose injection or 0.
View Article and Find Full Text PDFA rapid isocratic technique was developed for the analysis of three cephalosporins: cefaloridine, cefuroxime and ceftazidime in parenteral solutions using high-performance liquid chromatography (HPLC) with UV detection and C18 column. The availability and compatibility of drugs from solutions infused via plastic infusion bags through plastic administration sets have been examined. No significant drugs loss was observed during the simulated infusions (n = 4) for 1 h using PVC infusion bags and administration sets.
View Article and Find Full Text PDFJ Clin Pharm Ther
April 1994
The availability and compatibility of drugs from solutions infused via PVC infusion bags through PVC administration sets have been examined. No significant drug loss was observed during simulated infusions using PVC infusion bags and administration sets over time periods used in hospitals (cisplatin, 2 h; carboplatin, 1 h). The stability of carboplatin was studied in 5% dextrose.
View Article and Find Full Text PDFJ Pharm Biomed Anal
January 1994
A rapid isocratic technique was developed for the analysis of cephamandole nafate and cephamandole in parenteral solutions using high-performance liquid chromatography (HPLC) with UV detection and C18 column. The availability and compatibility of drugs from solutions infused via plastic infusion bags through plastic administration sets have been examined. No significant drugs loss was observed during simulated infusions (n = 4) for 1 h using PVC infusion bags and administration sets.
View Article and Find Full Text PDFA rapid isocratic technique was developed for the analysis of four anthracyclines (doxorubicin, epirubicin, daunorubicin and pirarubicin) in parenteral solutions using high pressure liquid chromatography (HPLC) with fluorescence detection and a C18 Hypersil ODS column. The availability and compatibility of these drugs from solutions infused via PVC infusion bags through PVC administration sets have been examined. No significant drug loss was observed during simulated infusions (n = 4) for 24 h using PVC infusion bags and administration sets.
View Article and Find Full Text PDF2-(4-Methyl-1-piperazinylmethyl) acrylophenone dihydrochloride (MPMAP) is a novel inhibitor of microtubule assembly in vitro and in vivo whose molecular mechanism of action has not been investigated (M. L. Mallevais, A.
View Article and Find Full Text PDFArzneimittelforschung
April 1986
The structure-activity relationships of nine products of the acrylophenone family have been studied. In a previous report 2-(4-methyl-1-piperazinylmethyl)acrylophenone was shown to be an antimicrotubular drug. The effects of these drugs on the bovine brain tubulin polymerization were determined by a turbidimetric assay.
View Article and Find Full Text PDFNine (amino-methyl)-2 acrylophenone derivatives having in vitro antimicrotubular activities very similar to those of colchicine are tested on Triton WR 1339-induced hyperlipidemia in rats. By producing a disorganization of the microtubular system, these drugs reduce the lipoprotein secretory process from hepatocytes, and more particularly the triglyceride-rich VLDL secretory process, such that the serum triglyceride, cholesterol and phospholipid levels are decreased. On the other hand, HDL-cholesterol and HDL-phospholipids are increased in a significant manner.
View Article and Find Full Text PDFEthacrynic acid is a well known diuretic drug. We present here evidence that this compound is also an antimicrotubular agent which inhibits the brain tubulin polymerization and can displace 3H colchicine from its binding site. Since 2-mercaptoethanol reversibly inhibits the anti-microtubular properties, we conclude that ethacrynic acid binds covalently to brain tubulin through a cysteine near the colchicine site.
View Article and Find Full Text PDFWith the relation between chemical structure and pharmacological activity as a guide, we have been for some time synthetizing a wide range of beta-amino-ketone derivatives. One of them, 2-(4-methyl-1-piperazinylmethyl) acrylophenone, MPMAP, possesses antimicrotubular activities. This product inhibits 50% of the microtubule polymerization at a 3.
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