Simultaneous determination of the camptothecin analogue CPT-11 and its active metabolite SN-38 by high-performance liquid chromatography: application to plasma pharmacokinetic studies in cancer patients

Barilero, Iman; Gandía, Daniel; Armand, Jean‐Pierre; Mathieu-Boué, Anne; Ré, Micheline; Gouyette, Alain; Chabot, Guy G.

doi:10.1016/0378-4347(92)80156-k

Cited by 71 publications

(25 citation statements)

References 4 publications

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“…These methods involve the simultaneous quantification of the lactone and carboxylate forms (27,29,32,37 ) or quantification of the total forms, i.e., lactone plus carboxylate (26,28,30,31,(33)(34)(35)(36). In most of these methods, both CPT-11 and SN-38 were quantified and the related compound camptothecin was used as the internal standard.…”

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confidence: 99%

Sensitive HPLC-Fluorescence Method for Irinotecan and Four Major Metabolites in Human Plasma and Saliva: Application to Pharmacokinetic Studies

Poujol¹,

Pinguet²,

Malosse³

et al. 2003

Clinical Chemistry

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Methods:The sample pretreatment involved protein precipitation with methanol-acetonitrile (50:50 by volume) followed by acidification with hydrochloric acid to convert the lactone ring-opened form into its lactone form, quantitatively. HPLC separation was performed on a Xterra RP18 column. The excitation wavelength was 370 nm, and the emission wavelength was set at 470 nm for the first 24 min and then at 534 nm for the next 4 min. The stabilities of irinotecan and its four metabolites in plasma, saliva, and acidic extracts were also investigated under various conditions. Results: Assays were linear in the tested range of 0.5-1000 g/L. For the five analytes, limits of quantification were 0.5 g/L in both matrices. The interassay imprecision (as relative standard deviation) was 3.2-14% in plasma and 2.6 -5.6% in saliva. Assay recoveries ranged from 92.8% to 111.2% for plasma and 100.1% to 104.1% for saliva. Mean extraction recovery from plasma or saliva was 90%.

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confidence: 99%

Sensitive HPLC-Fluorescence Method for Irinotecan and Four Major Metabolites in Human Plasma and Saliva: Application to Pharmacokinetic Studies

Poujol¹,

Pinguet²,

Malosse³

et al. 2003

Clinical Chemistry

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“…Methods for quantitative determination of CPT-11 and SN-38 in plasma could be classified in two categories: quantification of total concentration (Barilero et al, 1992;de Bruijn et al, 1997de Bruijn et al, , 1999Rivory et al, 1998;Sparreboom et al, 1998;Sumiyoshi et al, 1995) and ORIGINAL RESEARCH measurement of lactone and carboxylate forms (Chollet et al, 1998;de Bruijn et al, 1997;Kaneda et al, 1997;Rivory and Robert, 1994;Warner and Burke, 1997). Clinical applicability of the assay that determines lactone form was compromised by stability problem associated with lactone-carboxylate inter conversion (de Bruijn et al, 1997).…”

Section: Discussionmentioning

confidence: 98%

“…In recent years, several HPLC methods with fluorescence detection have been developed to quantify SN-38 generated from CPT-11 in human plasma (Barilero et al, 1992;de Bruijn et al, 1997de Bruijn et al, , 1999Escoriaza et al, …”

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confidence: 99%

A sensitive and rapid liquid chromatography tandem mass spectrometry method for quantitative determination of 7‐ethyl‐10‐hydroxycamptothecin (SN‐38) in human plasma containing liposome‐based SN‐38 (LE‐SN38)

Khan¹,

Ahmad²,

Ahmad³

2003

Biomedical Chromatography

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7-Ethyl-10-hydroxycamptothecin (SN-38) is an active metabolite of Irinotecan (CPT-11), an anticancer pro-drug. To support clinical pharmacokinetic studies for liposome based formulation of SN-38 (LE-SN38) in cancer patients, a rapid, simple and sensitive liquid chromatography tandem mass spectrometry (LC-MS/MS) method has been developed and validated for the quantification of total SN-38 in human plasma. Sample preparation was carried out by one-step protein precipitation using cold acetonitrile with 0.5% acetic acid (v/v). Camptothecin was used as an internal standard (IS). Chromatographic separation of SN-38 and IS was achieved using a Synergi Hydro-RP column (C(18), 50 x 2 mm, 4 micro m), with a gradient elution of acetonitrile and 0.1% acetic acid. After ionization in electrospray source (positive ions), the acquisition was performed in the multiple reactions monitoring mode. Quantitation was accomplished using the precursor-->product ion combinations of m/z 393.1-->349.2 for SN-38 and 349.1-->305.1 for IS. The quantification limit of 0.05 ng/mL was achieved by using much lower volume (0.2 mL) of plasma and in the presence of LE-SN38. The method was validated over the concentration range of 0.05-400 ng/mL. Accuracy was within +/-12% of nominal at all concentration levels. Inter-day and intra-day precisions expressed as percentage coefficient of variation (%CVs) for quality control (QC) samples were less than 14 and 5%, respectively.

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“…There are several liquid-liquid extraction approaches available for simultaneous measurement of the δ-lactone and δ-hydroxy acid forms of various CPTs in human plasma (Beijnen et al, 1993;Li and Zhang, 1996;Warner and Burke, 1997;Loos et al, 1997;Sparreboom et al, 1998a;Sai et al, 2002). Solid phase extraction (Barilero et al, 1992;Takimoto et al, 1994;Oguma et al, 2000Oguma et al, , 2001 and restricted access media methodologies have been recently reported (Ma et al, 2002) for simultaneous determination of these CPT forms in human plasma. All of these methods require immediate sample processing in order to avoid inter-conversion between the two forms.…”

Section: Introductionmentioning

confidence: 98%

Quantitative determination of DRF‐1042 in human plasma by HPLC: validation and application in clinical pharmacokinetics

Upreti

Mamidi

Katneni

et al. 2003

Biomedical Chromatography

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A simple and sensitive high-performance liquid chromatography (HPLC) method has been developed and validated for the determination of DRF-1042, a novel orally active camptothecin (CPT) analog, in human plasma. The sample preparation was a simple deproteinization with acidified methanol yielding almost 100% recovery of DRF-1042. An isocratic reverse-phase HPLC separation was developed on a Supelcosil-LC318 column (250 x 4.6 mm, 5 microm) with mobile phase consisting of 1% v/v triethylamine acetate, pH 5.5 and acetonitrile (80:20, v/v) at a fl ow rate of 1.0 mL/min. The eluate was monitored with a fluorescence detector set at excitation and emission wavelengths of 370 and 430 nm, respectively. The standard curves were linear (r(2) > 0.999) in the concentration ranges 5.0-2004 ng/mL. The lower limit of quantification (LLQ) of the assay was 5 ng/mL. The mean measured quality control (QC) concentrations (range 5 ng/mL to 40 microg/mL) deviated from the nominal concentrations in the range of -10.5-0.08 and -14.5-7.97%, inter- and intra-day, respectively. The inter- and intra-day precisions in the measurement of QC samples at four tested concentrations, were in the range 0.64-5.89% relative standard deviation (RSD) and 0.33-14.7% RSD, respectively. The method was found to be suitable for measurement of plasma concentrations above the calibration curve after serial dilutions. Stability of DRF-1042 was confirmed in a battery of studies, viz., on bench-top, in the auto-sampler, in the stock solutions, after four quick freeze-thaw cycles, up to one month at -20 degree C in human plasma and up to 2 months in the ex vivo samples. The method is simple, sensitive and reliable and has been successfully implemented to investigate the clinical pharmacokinetics of DRF-1042 in cancer patients in a phase I clinical trial.

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Simultaneous determination of the camptothecin analogue CPT-11 and its active metabolite SN-38 by high-performance liquid chromatography: application to plasma pharmacokinetic studies in cancer patients

Cited by 71 publications

References 4 publications

Sensitive HPLC-Fluorescence Method for Irinotecan and Four Major Metabolites in Human Plasma and Saliva: Application to Pharmacokinetic Studies

Sensitive HPLC-Fluorescence Method for Irinotecan and Four Major Metabolites in Human Plasma and Saliva: Application to Pharmacokinetic Studies

A sensitive and rapid liquid chromatography tandem mass spectrometry method for quantitative determination of 7‐ethyl‐10‐hydroxycamptothecin (SN‐38) in human plasma containing liposome‐based SN‐38 (LE‐SN38)

Quantitative determination of DRF‐1042 in human plasma by HPLC: validation and application in clinical pharmacokinetics

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