Gas and liquid chromatographic analyses of nimodipine calcium antagonist in blood plasma and cerebrospinal fluid

Krol, G.J.; Noe, Anson; Yeh, S. C.; Raemsch, K D

doi:10.1016/s0378-4347(00)83318-6

Cited by 62 publications

(18 citation statements)

References 10 publications

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“…Our results demonstrated, however, that the mean half-life of nimodipine for the two formulations tested was 27.83 h (test formulation) and 32.78 h (reference formulation). Such a discrepancy could be due to the greater sensitivity of our method, with a limit of quantification of 100 pg/mL, while values found in previous studies were in the range 0.24 to 5 ng/mL (Krol et al, 1984;Jackobsen et al, 1986;Rosseel et al, 1990;Qian, Gallo, 1992;Fischer et al, 1993;Yan et al, 1993;Mück, 1995;Aymard et al, 1998;Gualano et al, 1999;López et al, 2000;Blardi et al, 2002;Qiu et al, 2004;Zhonggui et al, 2004;Nirogi et al, 2006). This improved sensitivity enabled the determination of plasma drug concentrations up to 48 h after drug administration, which was not possible in other studies that allowed the measurement of plasma drug levels only up to 10 h after drug administration.…”

Section: Pharmacokinetic Studycontrasting

confidence: 58%

“…The present LC-MS-MS method offered an LLOQ of 100 pg/mL with a mean accuracy of 7.0% and a mean precision of 103.0% (n=5), which is more sensitive than or comparable to reported methods (Krol et al, 1984;Jackobsen et al, 1986;Rosseel Bogaert, Huyghens, 1990;Qian, Gallo, 1992;Aymard et al, 1998;López et al, 2000;Blardi et al, 2002;Mück, 1995;Qiu et al, 2004;Nirogi et al, 2006;Qin et al, 2008). Data for LLOQ are presented in Table II.…”

Section: Linearity and Lower Limit Of Quantificationmentioning

confidence: 71%

“…Gas chromatography (GC) methods with electron-capture (Krol et al, 1984;Jackobsen, et al, 1986) and nitrogenphosphorus detection (Rosseel, Bogaert, Huyghens, 1990) were used to determine nimodipine in plasma, which can provide a lower limit of quantification (LLOQ) of 5 ng/mL, using 1 mL of plasma. The method described by Krol et al (1984) is sensitive and selective; however, it requires a large amount of plasma and elaborate and lengthy sample preparation.…”

Section: Introductionmentioning

confidence: 99%

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Determination of nimodipine in plasma by HPLC-MS/MS and pharmacokinetic application

Nascimento

Moraes

Bezerra

et al. 2010

Braz. J. Pharm. Sci.

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To develop and validate a rapid, specific and highly sensitive method to quantify nimodipine in human plasma using dibucaine as the internal standard (IS). The analyte and IS were extracted from plasma samples by liquid-liquid extraction using hexane-ethyl acetate (1:1 v/v). The chromatographic separation was performed on a Varian ® Polaris C18 analytical column (3 mm, 50 x 2.0 mm) and pre-column Securityguard TM C18 (4.0 x 3.0 mm) with a mobile phase of Acetonitrile-Ammonium acetate 0.02 ml/L (80:20v/v). The method had a chromatographic run time of 4.5 min and linear calibration curve over the range of 0.1-40 ng/mL (r > 0.9938). The limit of quantification was 100 pg/mL. Acceptable precision and accuracy were obtained for concentrations over the standard curve ranges. This validated method was successfully applied in determining the pharmacokinetic profile of nimodipine tablets of 30 mg administered to 24 healthy volunteers. The proposed method of analysis provided a sensitive and specific assay for nimodipine determination in human plasma. The time for the determination of one plasma sample was 4.5 min. This method is suitable for the analysis of nimodipine in human plasma samples collected for pharmacokinetic, bioavailability or bioequivalence studies in humans.Uniterms: Nimodipine/determination in plasma. Nimodipine/pharmacokinetic profile. Nimodipine/ quantitative analysis. Pharmacokinetics/method validation.Um método rápido, específico e sensível para quantificar nimodipino em plasma humano usando dibucaína como padrão interno (IS) é descrito. O analito e o IS foram extraídos das amostras de plasma por extração líquido-líquido usando hexano-acetato de etila (1:1 v/v). A separação cromatográfica foi realizada utilizando-se uma coluna analítica C18 Varian ® Polaris (3 mm, 50 x 2,0 mm) e uma pré-coluna Securityguard TM C18 (4,0 x 3,0 mm) e acetonitrila-acetato de amônia 0,02 mol/L (80:20 v/v) como fase móvel. O método apresentou tempo total de corrida de 4,5 min e curva de calibração linear com concentrações entre 0,1-40 ng/mL (r > 0,9938). O limite de quantificação foi de 100 pg/mL. Os valores de precisão e exatidão foram obtidos por meio da análise das amostras de controle de qualidade. A análise de uma única amostra de plasma foi realizada em 4,5 minutos. A metodologia validada foi aplicada na determinação do perfil farmacocinético do nimodipino, comprimido de 30 mg administrado em 24 voluntários saudáveis. O método para quantificar nimodipino em plasma é adequado para aplicação em estudos farmacocinéticos, biodisponibilidade e bioequivalência em humanos.

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Section: Pharmacokinetic Studycontrasting

confidence: 58%

Section: Linearity and Lower Limit Of Quantificationmentioning

confidence: 71%

Section: Introductionmentioning

confidence: 99%

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Determination of nimodipine in plasma by HPLC-MS/MS and pharmacokinetic application

Nascimento

Moraes

Bezerra

et al. 2010

Braz. J. Pharm. Sci.

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“…Therapeutic concentrations of nimodipine are about 1 nm. (Plasma levels in clinical trials are 10-60 ng ml-' and approximately 2 % of this amount is free (Krol, Noe, Yeh & Raemsch, 1984;Scriabine et al 1985). Since the molecular weight of nimodipine is 418-5, the free concentration is 0 5-3 nm.…”

Section: Discussionmentioning

confidence: 99%

Nimodipine block of calcium channels in rat anterior pituitary cells.

Cohen

McCarthy

1987

The Journal of Physiology

158

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SUMMARY1. Ca channels were studied in the GH4C1 clonal cell line derived from rat anterior pituitary cells. The whole-cell variation of the patch-electrode voltage-clamp technique was used.2. Two types of Ca channels were found. One type ('slowly inactivating' channels) is insensitive to changes in holding potential, does not inactivate during test pulses lasting several seconds, and deactivates very quickly upon repolarization. For holding potentials <-40 mV, a second type of Ca channel is available for opening. This population ('transient' channels) differs from the first type in that it activates at more negative potentials, inactivates rapidly with either Ca or Ba as the charge carrier, deactivates about 10 times more slowly upon repolarization, and is less selective for Ba over Cs.3. Nimodipine preferentially blocks the slowly inactivating channels. Block of these channels is time-and voltage-dependent, such that block is maximized by long depolarizations.4

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“…Exceptions were the constant infusion with NT where gas chromatographic-mass spectromctric detection [5] was used. The corresponding NM study was determined by high-perfor mance liquid chromatography [6 Extraction. Volumes of 0.5 ml plasma arc shaken with 1 ml toluene containing 50 ng/ntl of the internal standard and 50 pi 0.5 M NaOH in 2-ml autosamplcr bottles for 5 min.…”

Section: Subjectsmentioning

confidence: 99%

Pharmacokinetics and Metabolism of Calcium-Blocking Agents Nifedipine, Nitrendipine, and Nimodipine

et al. 1986

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Gas and liquid chromatographic analyses of nimodipine calcium antagonist in blood plasma and cerebrospinal fluid

Cited by 62 publications

References 10 publications

Determination of nimodipine in plasma by HPLC-MS/MS and pharmacokinetic application

Determination of nimodipine in plasma by HPLC-MS/MS and pharmacokinetic application

Nimodipine block of calcium channels in rat anterior pituitary cells.

Pharmacokinetics and Metabolism of Calcium-Blocking Agents Nifedipine, Nitrendipine, and Nimodipine

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