Mebeverine acid
(Synonyms: 美贝维林盐酸盐,Mebeverine metabolite Mebeverine acid) 目录号 : GC61037A metabolite of mebeverine
Cas No.:475203-77-1
Sample solution is provided at 25 µL, 10mM.
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Mebeverine acid is a metabolite of the antispasmodic agent mebeverine.1
1.Moskaleva, N.E., Baranov, P.A., Mesonzhnik, N.V., et al.HPLC-MS/MS method for the simultaneous quantification of desmethylmebeverine acid, mebeverine acid and mebeverine alcohol in human plasma along with its application to a pharmacokinetics studyJ. Pharm. Biomed. Anal.138118-125(2017)
Cas No. | 475203-77-1 | SDF | |
别名 | 美贝维林盐酸盐,Mebeverine metabolite Mebeverine acid | ||
Canonical SMILES | O=C(O)CCCN(CC)C(C)CC1=CC=C(OC)C=C1 | ||
分子式 | C16H25NO3 | 分子量 | 279.37 |
溶解度 | DMSO : 13.33 mg/mL (47.71 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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1 mg | 5 mg | 10 mg | |
1 mM | 3.5795 mL | 17.8974 mL | 35.7948 mL |
5 mM | 0.7159 mL | 3.5795 mL | 7.159 mL |
10 mM | 0.3579 mL | 1.7897 mL | 3.5795 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Identification of Mebeverine acid as the main circulating metabolite of mebeverine in man
J Pharm Biomed Anal 2002 Jun 20;29(1-2):335-40.PMID:12062694DOI:10.1016/s0731-7085(02)00023-7.
The intestinal spasmolytic drug mebeverine is known to undergo fast in vivo enzymatic hydrolysis into mebeverine alcohol and veratric acid. A reversed-phase HPLC method with coulometric detection was developed in order to assay the hitherto unidentified secondary metabolite Mebeverine acid. After intake of a single oral dose of 405 mg mebeverine hydrochloride in four healthy human volunteers, peak plasma concentrations of Mebeverine acid were found to be 1000-fold higher than those of mebeverine alcohol, i.e. approximately 3 microg/ml versus 3 ng/ml. The appearance of Mebeverine acid in plasma (median T(max)=1.25 h) as well as its disappearance (median apparent t(1/2)=1.1 h) were rapid. The urinary excretion of Mebeverine acid within the first 4 h after dosing amounted to 67% of the mebeverine dose (median range: 23-107%). Mebeverine acid appears to be a valuable marker of oral exposure to mebeverine.
HPLC-MS/MS method for the simultaneous quantification of desmethylmebeverine acid, Mebeverine acid and mebeverine alcohol in human plasma along with its application to a pharmacokinetics study
J Pharm Biomed Anal 2017 May 10;138:118-125.PMID:28192719DOI:10.1016/j.jpba.2017.02.006.
A new simple, rapid and sensitive high pressure liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method was developed and validated for simultaneous analysis of mebeverine metabolites as: mebeverine alcohol (MAL), Mebeverine acid (MAC) and desmethylmebeverine acid (DMAC) in human plasma. Sample preparation was performed by protein precipitation following the separation of analytes using an Acquity UPLC BEN C8 column 1.7 mm 2.1×50mm (Waters, USA). 2H5-desmethylmebeverine acid (2H5-DMAC) was used as the internal standard (IS). The proposed method was validated with linear ranges of 0.1-10ng/mL; 1-100ng/mL and 5-1000ng/mL for MAL, MAC and DMAC, respectively. Accuracy for all analytes (%RE), given as deviation between nominal and measured concentration and assay variability (CV) ranged from -4.04% to 4.60% and from 0.31% to 6.43% respectively both for within- and between-run. The overall recoveries for all metabolites were above 85%. The proposed method was used successfully for analysis of real samples from a pharmacokinetics study.
Use of polarity switching for the simultaneous bioanalysis of analytes with three orders of magnitude difference in concentration by LC-MS/MS
Bioanalysis 2013 Aug;5(15):1911-8.PMID:23905864DOI:10.4155/bio.13.142.
Background: The challenge of quantifying two compounds in a single assay with drastic dynamic ranges is to obtain linearity without source or detector saturation at the mass spectrometer. Results: In positive-ionization mode, the nonlinear relationships for Desmethyl Mebeverine acid (DMAC) were demonstrated using three common strategies to overcome this issue: using offset voltage parameters, less-sensitive product ion or 13C mass SRM transitions. On the contrary, nonlinear relationships for DMAC were overcome if negative-ionization mode was used. Due to Mebeverine analytical LLOQ, dilution was not suitable for a single assay of Mebeverine and DMAC. However, polarity switching in negative mode for DMAC was successfully found to compensate for the nonlinearity at the mass spectrometer while preserving Mebeverine linear regression model in positive mode. Conclusion: The polarity switching strategy has demonstrated the advantage of improving linearity for analytes having different ionization polarities and three orders of magnitude difference in concentration.