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Development and validation of high-performance liquid chromatographic method for quantification of Irinotecan and its active metabolite SN-38 in colon tumor bearing NOD/SCID mice plasma samples: application to pharmacokinetic study

Taneja Neetika, Gota Vikram, Gurjar Murari, Singh Kamalinder K.

Acta Chromatographica

2019

Vol. 31, no. 3

166--172

Irinotecan (IRT) is an antineoplastic agent widely used in the treatment of various cancers primarily in colorectal cancer. A new, simple and sensitive high-performance liquid chromatography (HPLC) method coupled with fluorescence detector was developed and validated to quantify IRT and its active metabolite SN38 in the plasma of non-obese diabetic/severe combined immune-deficient mice (NOD/SCID) mice bearing colon tumor. The plasma samples were extracted by precipitation method using acetonitrile with 0.1% formic acid. The chromatographic separation was achieved using mobile phase consisted of water and acetonitrile (57:43 v/v) pH 3 at the flow rate of 0.8 mL/min in C18 column (internal diameter, 250 × 4.6 mm; pore size, 5 μm). The method was validated according to the bioanalytical guidelines defined by Food and Drug Administration (FDA) and European Medicine Agency (EMA). A regression (R2) value of 0.999 and 0.997 for IRT and SN38 suggested the good linearity in the range of 0.1–10 μg/mL and 5–500 ng/mL, respectively. The calculated lower limit of quantification (LLOQ) and limit of detection (LOD) for IRT were 0.1 and 0.065 μg/mL, respectively. However, for SN38, LLOQ and LOD were 5 and 2 ng/mL, respectively. The intra-day and inter-day variations (coefficient of variance; % CV) observed during the validation were found to be within the set limit of 15%. Both accuracy and percentage recovery analyzed and calculated from the quality control samples were in the between the defined range of 85–115%. Plasma samples were found to be stable when stored at room temperature for 2 h, after 2 freeze–thaw cycles and at −80 °C for 2 months. The developed method was successfully applied to study the plasma elimination profile of IRT in NOD/SCID mice with tumor. The results from plasma concentration time profile and pharmacokinetic parameter analyzed suggested the rapid elimination of IRT and SN38 from the plasma of NOD/SCID mice.

Membranes affinity of hydroxycamptothecins, anticancer agents, determined by fluorescence spectra analysis

Cyrankiewicz M., Ziomkowska B., Kruszewski S.

Optica Applicata

2006

Vol. 36, nr 2-3

209-215

In this paper the method of determination of membranes affinity of hydroxycamptothecins is described. Under physiological conditions hydroxycamptothecins easily hydrolyze and convert into inactive carboxylate form. The process of deactivation is inhibited when the molecules of drug are bound to cell membranes so it is desirable that hydroxycamptothecins molecules bind easily to membranes. A quantitative measure of drugs affinity to membranes is the association constant. To determine this parameter the small unilamellar liposomes are used as model membranes. The affinities of 10-hydroxycamptothecin, SN-38 and DB-67 to membranes are determined. The association constants are calculated on the basis of changes of fluorescence spectra.