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irbesartan desmotropes:Solid-state characterization,thermodynamic study and dissolution properties

Journal of Pharmaceutical Analysis 2019年第5期9卷 339-346页

作者： Andrea Mariela Araya-Sibaja Carlos Eduardo Maduro de Campos Cinira Fandaruff Jose Roberto Vega-Baudrit Teodolito Guillen-Giron Mirtha Navarro-Hoyos Silvia Lucía Cuffini Laboratorio Nacional de Nanotecnología LANOTEC-CeNAT-CONARE 1174-1200 Pavas San Jose Costa Rica Escuela de Ciencia e Ingeniería de los Materiales Tecnologico de Costa Rica Cartago 159-7050 Costa Rica Escuela de Química Universidad de Costa Rica San Pedro de Montes de Oca 2060 San Jose Costa Rica Programa de Pos-Graduacao em Física Universidade Federal de Santa Catarina Florianopolis Brazil Independent Researcher 06472-005 Barueri Sao Paulo Brazil Laboratorio de Investigacion y Tecnología de Polímeros POLIUNA Escuela de Química Universidad Nacional de Costa Rica Heredia 86-3000 Costa Rica Instituto de Ciencia e Tecnica Universidade Federal de Sao Paulo Sao Jose dos Campos Sao Paulo Brazil

irbesartan (IBS) is a tetrazole derivative and antihypertensive drug that has two interconvertible structures, 1H- and 2H-tautomers. The difference between them lies in the protonation of the tetrazole ring. In the solid-state, both tautomers can be isolated as crystal forms A (1H-tautomer) and B (2H-tautomer). Studies have reported that IBS is a polymorphic system and its forms A and B are related monotropically. These reports indicate form B as the most stable and less soluble form. Therefore, the goal of this contribution is to demonstrate through a complete solid-state characterization, thermodynamic study and dissolution properties that the IBS forms are desmotropes that are not related monotropically. However, the intention is also to call attention to the importance of conducting strict chemical and in solid-state quality controls on the IBS raw materials. Hence, powder X-ray diffraction (PXRD) and Raman spectroscopy (RS) at ambient and non-ambient conditions, differential scanning calorimetry (DSC), hot stage microscopy (HSM), Fourier transform infrared (FT-IR) and scanning electron microscopy (SEM) techniques were applied. Furthermore, intrinsic dissolution rate (IDR) and structural stability studies at 98% relative humidity (RH), 25℃ and 40 ℃ were conducted as well. The results show that in fact, form A is approximately four-fold more soluble than form B. In addition, both IBS forms are stable at ambient conditions. Nevertheless, structural and/or chemical instability was observed in form B at 40℃ and 98% RH. IBS has been confirmed as a desmotropic system rather than a polymorphic one. Consequently, forms A and B are not related monotropically.

关键词： irbesartan Solid-state characterization Intrinsic dissolution rate Tautomerism Desmotropic forms

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Simultaneous determination of Repaglinide and irbesartan in biological plasmas using micellar enhanced excitation-emission matrix fluorescence coupled with ATLD method

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Science China Chemistry 2016年第7期59卷 816-823页

作者： Haiyan Fu Hedong Li Mei Shao Tianming Yang Xu Zhang Rujing Xu Yujuan Wei Shuhua Chen Chuang Ni Hailong Wu The Modernization Engineering Technology Research Center of Ethnic Minority Medicine of Hubei province College of PharmacySouth-Central University for NationalitiesWuhan 430074China State Key Laboratory of Chemo/Biosensing and Chemometrics College of Chemistry and Chemical Engineering Hunan UniversityChangsha 410082China

A highly sensitive and selective 3D excitation-emission fluorescence method has been proposed to rapidly quantify the combined antidiabetics Repaglinide(Re) and irbesartan(Ir) in rat and human plasmas with the aid of second-order calibration method based on alternating trilinear decomposition(ATLD) method. Re and Ir with weak fluorescence can be endowed with strong fluorescent property by changing the microenvironment in samples and improving the fluorescence quantum yield by using an appropriate micellar enhanced surfactant. The enhanced excitation-emission matrix fluorescence of Re and Ir can be accurately resolved and can simultaneously attain the optimal concentration even in the presence of a potentially strong intrinsic fluorescence from complex biological matrices, such as rat and human plasmas, by using the ATLD method, which completely exploits the "second-order advantage". The average recoveries of Re and Ir obtained from ATLD with the factor number of 3(N=3) were 101.0%±4.3% and 99.1%±4.1% for rat plasma and 100.5%±5.4% and 97.1%±3.6% for human plasma. Several statistical methods, including Student's t-test, figures of merit, and elliptical joint confidence region, have been utilized to evaluate the accuracy of the proposed method. Results show that the developed method can maintain second-order advantage in simultaneous determinations of the weak fluorescent analytes of interest in different biological plasma matrices.

关键词： Repaglinide irbesartan micellar enhanced fluorescence alternating trilinear decomposition

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Antioxidative Capacity of irbesartan

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Chemical Research in Chinese Universities 2011年第1期27卷 75-79页

作者： WANG Mei-xue ZHAO Xue-zhong GAI Chun-yu LIU Hong-min XU Yan-ping LI Jing The First Hospital 2. School of Public Health Jilin University Changchun 130021 P. R. China The Second Hospital Jilin University Changchun 130041 P. R. China

The author investigated the antioxidant effect of irbesartan[2-butyl-3-（{4-[2-（2H-l,2,3,4-tetrazol-5-yl）. phenyl]phenyl}methyl）-1,3-diazaspiro[4.4]non-1-en-4-one], an angiotensin receptor blocker（ARB）, on the oxidation of erythrocytes induced by 2,2-[azobis（2-amidinopropane） hydrochloride]（AAPH） and H2O2 The value of half concentration（IC50） of irbesartan to scavenge radicals was measured by reacting it with 2,2-[azinobis（3-ethylbenzothia- zoline-6-sulfonate） radical eation]（ABTS＋）. Activities of the catalase（CAT）, superoxide dismutase（SOD）, glutathione peroxidase（GSH-Px） and the content of malondialdehyde（MDA） in liver tissue and blood serum of normal-rats were measured by means of speetrophotometry to study the antioxidation function of irbesartan. Results of experiments show that irbesartan can scavenge ABTS＋ and superoxide radicals effectively as well as inhibit AAPH-, H2O2-induced hemolysis of erythrocytes. irbesartan can also increase the activities of GSH-Px, SOD, CAT and decrease the content of MDA of normal rats. So irbesartan is a good antioxidant.

关键词： irbesartan Antioxidant Oxidative stress Radical

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Effect and mechanism of irbesartan on occurrence of ventricular arrhythmias in rats with myocardial ischemia through connexin43(cx43)

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Asian Pacific Journal of Tropical Medicine 2016年第10期9卷 985-990页

作者： Tao Wu Dan Wu Qinghua Wu Bing Zou Xiao Huang Xiaoshu Cheng Yanqing Wu Kui Hong Ping Li Department of Cardiovascular Medicine the Second Affiliated Hospital of Nanchang University Jiangxi Health Vocational College

Objective: To explore the effect and mechanism of angiotensin II receptor blockers-irbesartan on occurrence of ventricular arrhythmias in rats with myocardial ischemia. Methods: Rats with embryonic cardiomyocytes-H9c2 were randomly divided into control group. ischemia group. irbesartan group and irbesartan+ischemia group. The cell viability of rats in each group was tested using MTT. Real-time PCR was employed to detect the expression of connexin43 (Cx43) mRNA and western blot to detect the expression of Cx43 and phosphorylated Cx43. SD rats were randomly divided into the sham-operation group (SO). myocardial infarction group (MI). irbesartan group and MI+ irbesartan group, with 10 rats in each group. HE staining was employed to observe the change in the pathomorpholouy of left ventricular tissue and TUNEL method to analyze the cell apoptosis in the tissue. The immunofluorescence was adopted to observe the expression and distribution of Cx43 in the left ventricular myocardium and study the change in the expression of Cx43 in the cardiac muscular tissue at mRNA and protein level. Results: The intervention of lrbesartan in the condition of ischemia indicated the significant decrease in the number of necrotic cells. The expression of Cx43 was significantly decreased under the culture of ischemia (Pirbesartan, the expression of Cx43 was increased compared with the ischemia group (pirbesartan group and MI group (P<0.05). The expression of Cx43 in the cardiac muscular tissue in MI group was significantly decreased (P<0.01(US) SO group). But

关键词： irbesartan Myocardial lschemia Cx43 Connexin Arrhythmias

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Study on the Pharmacokinetics and Relative Bioavailability of irbesartan Capsules in Healthy Volunteers

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Journal of Huazhong University of Science and Technology(Medical Sciences) 2002年第1期22卷 14-16页

作者：顾世芬陈汇邱应海师少军曾繁典 Institute of Clinical Pharmacology Tongji Medical College Huazhong University of Science and Technology Wuhan 430030 Institute of Medicine of Zhuhai Mintong Zhuhai 519041

The pharmacokinetics and relative bioavailability were studied in 18 healthy volunteers. A single oral dose of 150 mg irbesartan capsule (test) or tablet (reference) was given to each volunteer according to a randomized 2 way crossover study. The concentrations in plasma were determined by HPLC UV method. The main parameters of irbesartan capsules were: C max : 1.502±0.295 μg/ml, t max : 1.44±0.34 h, t 1/2 : 20.21±14.71 h, AUC 0 t : 11.087±3.443 μg/ml -1 ·h. The relative bioavailability of capsule to tablet was (101.4±28.9) %. The results of statistical analysis showed that two formulations were bioequivalent.

关键词： irbesartan pharmacokinetics bioavailability HPLC

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HPLC-UV method for simultaneous determination of irbesartan, candesartan, gliquidone and pioglitazone in formulations and in human serum

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Journal of Chinese Pharmaceutical Sciences 2018年第4期27卷 273-280页

作者： Agha Zeeshan Mirza Science and Technology Unit Umm Al-Qura University Makah 21955 KSA

In this study, we reported and validated a novel and sensitive reversed-phase liquid chromatographic method for the simultaneous determination of irbesartan, candesartan, gliquidone and pioglitazone. Separation was performed at 230 nm using a mobile phase consisting of methanol–water(90:10, v/v) with a flow rate of 1 mL/min. p H was adjusted to 3.5 with phosphoric acid. The concentration-response relationship was found linear over a concentration range of 5–25 μg/mL for all of the analytes tested. The limits of detection and quantification were 0.83 and 2.78 for irbesartan, 0.30 and 1.01 for candesartan, 1.11 and 3.93 for gliquidone, and 0.41 and 1.41 μg/mL for pioglitazone, respectively. Described method permitted the successful determination of these drugs in human serum. The developed method was simple, rapid, and it did not require extensive sample purification.

关键词： Candesartan Gliquidone irbesartan Pioglitazone RP-HPLC Method development

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Quantitative estimation of irbesartan in two different matrices and its application to human and dog bioavailability studies using LCeMS/MS

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Asian Journal of Pharmaceutical Sciences 2013年第6期8卷 346-355页

作者： Hari Krishan Tiwari Tausif Monif Priya Ranjan Prasad Verma Simrit Reyar Arshad Hussain Khuroo Sanjeev Mishra Department of Clinical Pharmacology and Pharmacokinetics Ranbaxy Research LaboratoriesPlot:GP-5Sec-18HSIIDCOld Delhi-Gurgaon RoadGurgaon 122015HaryanaIndia Birla Institute of Technology RanchiJharkhandIndia

A simple,rapid and robust high-throughput assay for the quantitative analysis of irbesartan in plasma from two species using liquid chromatography tandem mass spectrometric method was developed and *** phase extraction was used and quantification was achieved using a positive electrospray ionization interface under multiple reactions monitoring *** validation(as per recent regulatory requirements)was done using human *** same method was validated using dog plasma and the validation parameters met respective acceptance *** method has shorter run time of 3 *** will help in high *** low aliquot volume in the method helped us to take enough sampling time points for better pharmacokinetic *** calibration curve was shown to be linear from 12.1 to 6018.7 ng/ml in human plasma and 12.1 to 5987.2 ng/ml in dog *** method was successfully applied to samples collected during bioavailability studies of irbesartan in humans and dogs.

关键词： irbesartan Pharmacokinetics Solid phase extraction LCeMS/MS

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Pharmacokinetic interaction between irbesartan and Orthosiphon stamineus extract in rat plasma

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Asian Journal of Pharmaceutical Sciences 2016年第1期11卷 70-71页

作者： Nur Meilis Yahdiana Harahap Fadlina Chany Saputri Abdul Munim Rianto Setiabudy Pharmacy Department Faculty of Medicine and Health SciencesSyarif Hidayatullah State Islamic UniversityJakartaIndonesia Faculty of Pharmacy University of IndonesiaJakartaIndonesia Faculty of Medicine University of IndonesiaJakartaIndonesia

Orthosiphonstamineus commonly known as kumis kucing has been used traditionally for rheumatoid,gout,renal calculus,hypertension,diabetes,etc.[1].It is often used in combination with synthetic hypertensive drugs like ***,both effectiveness combination herbal medicine with modern pharmaceuticals,and the possible adverse effects from herb–drug interactions remain to be verified.

关键词： Orthosiphon stamineus irbesartan Pharmacokinetics interaction Herbs-drug interaction

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Effects of irbesartan on atrial cell electrophysiology

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Chinese Medical Journal 2005年第3期118卷 231-233页

作者： HUANGCong-xin CAOFeng JIANGHong WANGTeng LIXia DepartmentofCardiology RenminHospitalofWuhanUniversityWuhan430060China DepartmentofCardiology RenminHospitalofWuhanUniversityWuhan430060China

Atrial fibrillation (AF) is the most common sustained arrhythmia encounteredin clinical practice.1 Its incidence increases with age and the presence of structural heartdisease. It is a major cause of stroke, especially in the elderly. It has been shown thatangiotensin converting enzyme inhibitor (ACEI) can reduce the incidence of AF after acute myocardialinfarction.2 Several studies have shown that activation of the rennin-angiotensin system isassociated with the mechanisms of AF. irbesartan is a long-acting angiotensin II type 1 receptorantagonist used widely in the treatment of hypertension.3 In recent years, it has been demonstratedthat patients treated with amiodarone plus irbesartan had a lower rate of recurrence of atrialfibrillation than did patients treated with amiodarone alone.4 These findings suggest that theinhibition of angiotensin II may prevent AF, but its underlying electrophysiological mechanisms areobscure. The purpose of this study is to investigate the effects of irbesartan on atrial cellelectrophysiology.

关键词： irbesartan arrhythmia electrophysiology ion channels

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Effect of irbesartan on angiotensin Ⅱ-induced hypertrophy of human proximal tubular cells

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Chinese Medical Journal 2004年第4期117卷 547-551页

作者：刘必成孙静陈琪罗冬冬马坤岭阮雄中 Institute of Nephrology Department of Pathophysiology Centre for Nephrology

Background Intrarenal activation of the renin angiotensin system (RAS) plays an important role in mediating renal fibrosis. Both angiotensin converting enzyme inhibitors (ACEIs) and angiotensin Ⅱ (AngⅡ) receptor antagonists have been shown to exert a protective role against diabetic and non-diabetic nephropathy. However, the exact mechanism of how blocking local RAS prevents renal fibrosis is unclear. The present study was to investigate the influence of a new AngⅡ receptor antagonist, irbesartan (Irb), on AngⅡ-induced hypertrophy in human proximal tubular cell line (HK-2). Methods The cell line, HK-2, was grown in Dulbeccos’s Modified Eagle’s Medium containing 10% heat-inactivated fetal calf serum. After rested in serum-free medium for 24 hours, the effects of Irb on AngⅡ (10 -7 mol/L)-induced [ 3H]-leucine incorporation, total protein content (measured by the Coomassie brilliant blue G250 method), and change in cell size (determined by scanning electron microscopy) were observed. The influence of Irb on the cell cycle was analyzed by fluorescence activated cell sorter (FACS) flow cytometry. Results AngⅡ induced cell hypertrophy in a time and dose dependent manner. Stimulation of cells with AngⅡ for 48 hours resulted in a increase in [ 3H]-leucine incorporation [0 hour: (5584±1016) cpm/10 5cells vs 48 hours: (10741±802) cpm/10 5cells, P<0.05], which was significantly attenuated by treatment with Irb. AngⅡ significantly increased the total protein content in HK-2 cells [control: (0.169±0.011) mg/10 5cells vs AngⅡ group: (0.202±0.010) mg/10 5 cells, P<0.05], which was also markedly inhibited by cotreatment with Irb (P<0.01). Scanning electron microscopy showed that AngⅡ induced an increase in average physical cell size, which was significantly inhibited by Irb [control: (11.92±1.62) μm; AngⅡ group: (20.63±3.83) μm; AngⅡ+Irb group: (13.59±3.15) μm; P<0.01 vs control, respectively]. Furthermore, flow cytometry revealed that AngⅡ arrested cells in

关键词： irbesartan angiotensin Ⅱ hypertrophy epithelial cells

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