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1.
Ângelo M.L. Denadai André M. de Oliveira Izabela M.P. Daniel Luan A. Carneiro Kherolayne C. Ribeiro Heloísa de O. Beraldo 《Supramolecular chemistry》2013,25(3):204-212
Chlorhexidine is a widely used, di-cationic, broad-spectrum antimicrobial agent and losartan is a well-known, anionic-specific antagonist of AT1 renin–angiotensin receptor that acts as an anti-hypertensive agent. The combination of these molecules gives a chlorhexidine di-losartanate (ClxLos2) hydrophobic ion pair that spontaneously aggregates into nanoparticles (NPs). This work investigated the formation of ClxLos2 NPs using the analysis of the solid state by fourier transform infrared spectroscopy, thermogravimetric analysis, differential scanning calorimetry and scanning electron microscopy and in aqueous environment by calorimetric, zeta potential and dynamic light scattering titrations. Furthermore, to demonstrate the potential antimicrobial activity of ClxLos2, in vitro antibacterial tests were conducted against Staphylococcus aureus (ATCC 27664), Streptococcus viridans (ATCC 11563) and Enterococcus faecalis (ATCC 14508). Based on these studies, it is proposed that ClxLos2 could be used for controlled drug release based on ionic dissociation during dilution, thereby avoiding the use of any solid matrix. 相似文献
2.
《Biomedical chromatography : BMC》2017,31(7)
Two simple, selective, precise and highly sensitive high‐performance thin‐layer chromatography (HPTLC) methods have been developed and validated for analysis of five angiotensin II receptor antagonists, namely losartan, irbesartan valsartan, candesartan and olmesartan, which are widely used in clinical practice. HPTLC of the drugs was performed on pre‐coated silica gel HPTLC plates 60 F254 by development using a mobile phase composed of chloroform–acetone–glacial acetic acid (7.8:1.5:0.7m v/v/v), which was suitable for all of the studied drugs. The first method depended on utilizing reflectance/fluorescence mode for detection while the second method depended on using 2,3,5,6‐tetrachloro‐1,4‐benzoquinone as spraying reagent for the first time to form orange spots scanned at 460 nm. A good linear relationship was obtained over the concentration ranges of 1.2–60 and 360–3000 ng/band while detection and quantification limits were in the ranges of 0.07–0.43, 45.2–140.49 and 0.21–1.29, 137.05–425.74 ng/band for reflectance/fluorescence and reflectance/absorbance methods respectively. The developed methods were applied successfully for their determination in tablets and spiked human plasma for reflectance/fluorescence method with good accuracy and precision, and so can be applied in the pharmacokinetic and bioavailability studies. 相似文献
3.
Jian Wu WANG* Jiong JIA Hong Mei LI Cong WANG School of Chemistry Environmental Science Shandong University Jinan 《中国化学快报》2000,11(11)
Losartan 1 (Dup-753) is a nonpeptide angiotensin II receptor (type AT1) antagonist discovered by Duncia, J.V. et al. 1 in 1990 and its potassium salt (cozaar) has been marketed as an antihypertensive since 1995 2. 1 2 Starting from Dup-753, a great number of structural related compounds have been prepared by several laboratories and several antihypertensive drugs have been developed3. In order to find new and more active compounds, a novel type of Losartan analogues 2 was designed and syn… 相似文献
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Weina Ma Sen Sun Benwei Wang Liang Zhao Guoqing Zhang Yifeng Chai 《Biomedical chromatography : BMC》2013,27(9):1219-1224
Losartan is an effective anti‐hypotension drug frequently used in clinic. Compound danshen tablet (CDST) is an important traditional Chinese multiherbal formula composed of Danshen, Sanqi and Bingpian, which is widely used for the treatment of cardiovascular and cerebrovascular diseases in China. More often, losartan and CDST are simultaneously used for the treatment of anti‐hypertension in the clinic. The aim of this study was to compare the pharmacokinetics of losartan and EXP3174 after oral administration of single losartan and both losartan and CDST, and to investigate the influence of CDST on the pharmacokinetics of losartan and its metabolite EXP3174. Male Sprague–Dawley rats were randomly assigned to two groups: a losartan‐only group and a losartan and CDST group. Plasma concentrations of losartan and EXP3174 were determined by LC‐MS at designated points after drug administration, and the main pharmacokinetic parameters were estimated. It was found that there were significant differences (p < 0.05) between the pharmacokinetic parameters of losartan and EXP3174, which showed that CDST influenced the metabolism and excretion of losartan in vivo. The result could be used for clinical medication guidance of losartan and CDST to avoid the occurrence of adverse reactions. Copyright © 2013 John Wiley & Sons, Ltd. 相似文献
6.
选用科素亚和硝苯地平控释片拜新同治疗高血压合并糖尿病患者30例。结果表明,联合应用科素亚和拜新同的患者较单剂科素亚的患者降压效果更明显且能相对较快降低血压,增加患者依从性,患者能做到长期服药,从而使科素亚的靶器官保护作用得以发挥。 相似文献
7.
Hala E. Zaazaa Rasha Abdel-Ghany Mahmoud Sayed M. Abdelkawy Shimaa A. Atty 《液相色谱法及相关技术杂志》2020,43(13-14):474-481
AbstractTwo precise and selective stability-indicating RP-LC methods have been developed and validated for simultaneous determination of metolazone in its binary mixture with losartan potassium (method 1) and spironolactone (method 2) in the presence of their degradation products. For method 1, the chromatographic separation was achieved on Kromasil C18 column, the mobile phase consisted of a mixture of 0.1% ortho-phosphoric acid in acetonitrile and 0.1% ortho-phosphoric acid in water (28:72, v/v) pumped at flow rate 2?mL/min and UV detection at 235?nm. Linearity was determined over the concentration range of 2–16µg/mL for metolazone and 40–320µg/mL for losartan potassium. For method 2, chromatographic separation of metolazone and spironolactone was achieved on a Symmetry C8 column using a mobile phase that consisted of acetonitrile, methanol, and 0.1% ortho-phosphoric in water in gradient mode pumped at a flow rate 1.5?mL/min with programed wavelength detection. Linearity was determined over the concentration range of 2–16µg/mL for metolazone and 20–160µg/mL for spironolactone. The suggested methods were proved to be highly selective, precise and accurate for simultaneous determination of the cited drugs in their combined pharmaceutical dosage form in the presence of their degradation products. The proposed methods were validated in compliance with ICH guidelines.
- Highlights
Synchronized determination of metolazone and co-formulated drugs in presence of their degradation products.
Act as a method for screening of metolazone and co-formulated drugs in quality control laboratories.
Validation of suggested methods according to ICH guidelines.
The pathway of degradation of metolazone under different stress conditions was proposed.
8.
《Biomedical chromatography : BMC》2017,31(10)
Losartan and tripterygium glucoside tablet (TGT) are often simultaneously used for reducing urine protein excretion in clinic. However, it is unknown whether there is potential herb–drug interaction between losartan and TGT. The aim of this study was to investigate their potential herb–drug interaction, and clarify the mechanism of the effect of TGT on the pharmacokinetics of losartan and its metabolite EXP3174 in rats. The plasma concentrations of losartan and EXP3174 were determined by LC–MS, and the main pharmacokinetic parameters were calculated. The C max, t 1/2 and AUC(0–t ) of losartan became larger after co‐administration, while the C max and AUC(0–t ) of EXP3174 became smaller, suggesting that TGT could influence the pharmacokinetics of losartan and EXP3174. The effects of TGT and its main components on the metabolic rate of losartan were further investigated in rat liver microsomes. Results indicated that TGT and its two main ingredients could decrease the metabolic rate of losartan. Therefore, it was speculated that TGT might increase the plasma concentration of losartan and decrease the concentration of EXP3174 by inhibiting the metabolism of losartan. The results could provide references for clinical medication guidance of losartan and TGT to avoid the occurrence of adverse reactions. 相似文献
9.
Natalia Gabrielly Pereira dos Santos Deyber Arley Vargas Medina Fernando Mauro Lanças 《Journal of separation science》2023,46(17):2300214
The development of a fast, cost-effective, and efficient microextraction by packed sorbent setup was achieved by combining affordable laboratory-repackable devices of microextraction with a high-throughput cartesian robot. This setup was evaluated for the development of an analytical method to determine N-nitrosamines in losartan tablets. N-nitrosamines pose a significant concern in the pharmaceutical market due to their carcinogenic risk, necessitating their control and quantification in pharmaceutical products. The parameters influencing the performance of this sample preparation for N-nitrosamines were investigated through both univariate and multivariate experiments. Microextractions were performed using just 5.0 mg of carboxylic acid-modified polystyrene divinylbenzene copolymer as the extraction phase. Under the optimized conditions, the automated setup enabled the simultaneous treatment of six samples in less than 20 min, providing reliable analytical confidence for the proposed application. The analytical performance of the automated high-throughput microextraction by the packed sorbent method was evaluated using a matrix-matching calibration. Quantification was performed using ultra-high-performance liquid chromatography-tandem mass spectrometry with chemical ionization at atmospheric pressure. The method exhibited limits of detection as low as 50 ng/g, good linearity, and satisfactory intra-day (1.38–18.76) and inter-day (2.66–20.08) precision. Additionally, the method showed accuracy ranging from 80% to 136% for these impurities in pharmaceutical formulations. 相似文献
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