Perindopril L-Arginine
目录号 : GC25723Perindopril L-Argininel is a prodrug that is metabolized in the liver to its active diacid metabolite perindoprilat, which is rapidly and extensively absorbed, and become one of the highest tissue angiotensin-converting enzyme (ACE) affinities among the ACE inhibitors.
Cas No.:612548-45-5
Sample solution is provided at 25 µL, 10mM.
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Perindopril L-Argininel is a prodrug that is metabolized in the liver to its active diacid metabolite perindoprilat, which is rapidly and extensively absorbed, and become one of the highest tissue angiotensin-converting enzyme (ACE) affinities among the ACE inhibitors.
[1] Telejko E. et al. Curr Med Res Opin. 2007 May;23(5):953-60.
Cas No. | 612548-45-5 | SDF | Download SDF |
分子式 | C19H32N2O5.C6H14N4O2 | 分子量 | 542.67 |
溶解度 | DMSO: Insoluble;Water: 100 mg/mL (184.27 mM);Ethanol: 25 mg/mL (46.07 mM) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 1.8427 mL | 9.2137 mL | 18.4274 mL |
5 mM | 0.3685 mL | 1.8427 mL | 3.6855 mL |
10 mM | 0.1843 mL | 0.9214 mL | 1.8427 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,
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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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Molecular structure and stability of perindopril erbumine and Perindopril L-Arginine complexes
Eur J Med Chem 2009 Jan;44(1):101-8.PMID:18436349DOI:10.1016/j.ejmech.2008.03.012.
The methods of theoretical chemistry have been used to elucidate molecular properties of the antihypertensive, cardiovascular protective and antithrombotic perindopril ((2S,3aS,7aS)-1-[(2S)-2-[[(2S)-1-ethoxy-1-oxopentan-2-yl]amino]propanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carboxylic acid). The geometries and energies of various neutral and ionized complexes of perindopril erbumine and Perindopril L-Arginine have been computed using HF/6-31G(d) and Becke3LYP/6-31G(d) methods. The calculations showed that in both, the isolated state and water solution perindopril erbumine exists as a neutral complex. In the gas-phase Perindopril L-Arginine both neutral and ionic complexes are, at the HF level of theory, almost equally stable. The B3LYP level of theory slightly favors single proton transfer complex Perindopril L-Arginine (by about 14 kJ mol(-1)). In polar solvents like water, the ionized form of Perindopril L-Arginine becomes much more favored. According to our calculations l-arginine is bound to perindopril more strongly (by about 25 kJ mol(-1)) than erbumine.
The Development and Validation of a Stability-Indicating UHPLC-DAD Method for Determination of Perindopril L-Arginine in Bulk Substance and Pharmaceutical Dosage Form
Chromatographia 2014;77(21-22):1497-1501.PMID:25400289DOI:10.1007/s10337-014-2724-7.
A stability-indicating ultra-high-performance liquid chromatography (UHPLC) method with a diode array detector was developed and validated for the determination of cis/trans isomers of Perindopril L-Arginine in bulk substance and pharmaceutical dosage form. The separation was achieved on a Poroshell 120 Hilic (4.6 × 150 mm, 2.7 µm) column using a mobile phase composed of acetonitrile-0.1 % formic acid (20:80 v/v) at a flow rate of 1 mL min-1. The injection volume was 5.0 µL and the wavelength of detection was controlled at 230 nm. The selectivity of the UHPLC-DAD method was confirmed by determining Perindopril L-Arginine in the presence of degradation products formed during acid-base hydrolysis and oxidation as well as degradation in the solid state, at an increased relative air humidity and in dry air. The method's linearity was investigated in the ranges 0.40-1.40 µg mL-1 for isomer I and 0.40-2.40 µg mL-1 for isomer II of Perindopril L-Arginine. The UHPLC-DAD method met the precision and accuracy criteria for the determination of the isomers of Perindopril L-Arginine. The limits of detection and quantitation were 0.1503 and 0.4555 µg mL-1 for isomer I and 0.0356 and 0.1078 µg mL-1 for isomer II, respectively.