Determination of Simvastatin in human plasma by liquid chromatography–mass spectrometry

Yang, Haitao; Feng, Yan; Luan, Yiwen

doi:10.1016/s1570-0232(02)00800-0

Cited by 59 publications

(37 citation statements)

References 9 publications

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“…Simvastatin and simvastatin acid levels in the biological samples were determined using LC-MS as previously described with minor modification [29] . The diclofenac sodium solution (internal standard, final concentration, 1 mg/mL) of 10 mL and ether acetate of 1 mL were added to 100 mL of the biological sample.…”

Section: Drug Assaysmentioning

confidence: 99%

Decreased exposure of simvastatin and simvastatin acid in a rat model of type 2 diabetes

Zhang

et al. 2014

Acta Pharmacol Sin

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Aim: Simvastatin is frequently administered to diabetic patients with hypercholesterolemia. The aim of the study was to investigate the pharmacokinetics of simvastatin and its hydrolysate simvastatin acid in a rat model of type 2 diabetes. Methods: Diabetes was induced in 4-week-old rats by a treatment of high-fat diet combined with streptozotocin. After the rats received a single dose of simvastatin (20 mg/kg, po, or 2 mg/kg, iv), the plasma concentrations of simvastatin and simvastatin acid were determined. Simvastatin metabolism and cytochrome P4503A (Cyp3a) activity were assessed in hepatic microsomes, and its uptake was studied in freshly isolated hepatocytes. The expression of Cyp3a1, organic anion transporting polypeptide 2 (Oatp2), multidrug resistance-associated protein 2 (Mrp2) and breast cancer resistance protein (Bcrp) in livers was measured using qRT-PCR. Results: After oral or intravenous administration, the plasma concentrations and areas under concentrations of simvastatin and simvastatin acid were markedly decreased in diabetic rats. Both simvastatin metabolism and Cyp3a activity were markedly increased in hepatocytes of diabetic rats, accompanied by increased expression of hepatic Cyp3a1 mRNA. Furthermore, the uptake of simvastatin by hepatocytes of diabetic rats was markedly increased, which was associated with increased expression of the influx transporter Oatp2, and decreased expression of the efflux transporters Mrp2 and Bcrp. Conclusion: Diabetes enhances the metabolism of simvastatin and simvastatin acid in rats via up-regulating hepatic Cyp3a activity and expression and increasing hepatic uptake.

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Section: Drug Assaysmentioning

confidence: 99%

Decreased exposure of simvastatin and simvastatin acid in a rat model of type 2 diabetes

Zhang

et al. 2014

Acta Pharmacol Sin

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“…Simvastatin is orally administered as inactive prodrug in the lactone form which is converted in the liver into its active metabolite β-hydroxy acid [3]. Recently, numerous methods for analysis of simvastatin and its metabolites determination in human plasma by HPLC methods with difference detectors (ultraviolet, fluorescence and mass spectrometry) have been published [4][5][6][7][8][9]. In addition, some methods of gas chromatography with mass spectrometry for determination of simvastatin and its metabolites have also been published [10][11].…”

Section: Introductionmentioning

confidence: 99%

Method Validation for Analysis of Simvastatin in Human Plasma Using Liquid Chromatography Tandem Mass Spectrometry (LC-MS-MS)

Alakhali¹

2013

JCDR

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Introduction: The Liquid Chromatography Tandem Mass Spectrometry (LC-MS-MS) for determination simvastatin in human plasma has been developed after extraction by by ethyl acetate and hexane (90/10%, v/v) using lovastatin as internal standard. Material and Methods:The mobile phase consisting of mixture of acetonitrile and water (75/25%, v/v) 500μL/min by separated the solutes on a C18 column. discussion:The lower limit of quantitation of 0.25 ng/mL was achieved when the calibration curve was linear from 0.25-50 ng/mL. The entire run time for analysis was only 6 min. The quantitation in the selective reaction monitoring (SRM) in positive ion mode, the daughter ions m/z 325 for simvastatin and m/z 285 for lovastatin were used. The Parent ions in positive ion mode were m/z 441.3 for simvastatin and m/z 405.1 for lovastatin. The intra-day coefficients of variation were less than 14% while the inter-day coefficients of variation were less than 10%. conclusion:The LC-MS-MS detection is sensitive due to its capability to eliminate interferences from endogenous components.

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“…HPLC/UV detection at 238 nm was recommended for its determination in raw material and in tablets. The most widely used techniques for the assay of SIM in dosage forms or biological fluids were high performance liquid chromatography [3][4][5], liquid chromatography-mass spectrometry [6,7], gas chromatography-mass spectrometry [8], spectrophotometry [9], colorimetry [10] and voltammetry [11].…”

Section: Plastic Membrane Electrodementioning

confidence: 99%

Electrochemical Sensors for Direct Determination of Simvastatin in Pharmaceutical Formulations and Biological Fluids

Alarfaj

Aly

El‐Tohamy

2012

J. Chil. Chem. Soc.

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The construction and performance characteristics of simvastatin (SIM) selective electrodes were developed. Three types of electrodes: plastic membrane I, coated wire II, and coated graphite rod III were constructed based on the incorporation of simvastatin with phosphotungstic (PTA) or phosphomolybdic (PMA) acids and mixed ion pair (PTA/PMA) for the three electrodes, respectively. The influence of membrane composition, kind of plasticizer, type of ion-pair, pH of the test solution, soaking time, and foreign ions on the electrodes was investigated. The electrodes showed a Nernstain response with a mean calibration graph slope of 56.24±0.43, 55.44±0.14 and 58.93±0.34 mV decade -1 at 25ºC over simvastatin concentration range from 1.0 x 10 -6 -5.0 x 10 -2 , 9.0 x 10 -6 -5.0 x 10 -3 and 9.0 x 10 -7 -1.0 x 10 -2 mol L -1 , with detection limit of 5.0 x 10 -7 , 3.9 x 10 -6 and 3.2 x 10 -7 mol L -1 for electrode I, II and III, respectively. The pH range for the proposed electrodes was 4-7. The influence of possible interfering species such as common inorganic cations, many sugars, amino acids and a pharmacologically related drug 'ezetimibe' was studied. Statistical student's t-test and F test showed insignificant systematic error between proposed and official methods.

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Determination of Simvastatin in human plasma by liquid chromatography–mass spectrometry

Cited by 59 publications

References 9 publications

Decreased exposure of simvastatin and simvastatin acid in a rat model of type 2 diabetes

Decreased exposure of simvastatin and simvastatin acid in a rat model of type 2 diabetes

Method Validation for Analysis of Simvastatin in Human Plasma Using Liquid Chromatography Tandem Mass Spectrometry (LC-MS-MS)

Electrochemical Sensors for Direct Determination of Simvastatin in Pharmaceutical Formulations and Biological Fluids

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