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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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Influence of irbesartan on expression of ILK and its relationship with epithelial-mesenchymal transition in mice with unilateral ureteral obstruction

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Acta Pharmacologica Sinica 2007年第11期28卷 1810-1818页

作者： Bi-cheng LIU~1,Hui-ling XIA,Ji-ning WU,Xiao-liang ZHANG,Dian-ge LIU,Yu-xiang GONGInstitute of Nephrology,Zhong Da Hospital,Southeast University.Nanjing 210009,China Institute of Nephrology Zhong Da Hospital Southeast University Nanjing China

Aim:irbesartan,a new antagonist of the type Ⅰ angiotensin Ⅱ receptor,has beenproven to be renal protective in both diabetic and non-diabetic nephropathy,butits exact mechanism is still uncertain.Here we investigated the influence ofirbesartan on the expression of the integrin-linked kinase (ILK) and its relation-ship with epithelial-mesenchymal transition (EMT) in mice with unilateral ureteralobstruction (UUO).Methods:The mice were randomly divided into 3 groups:sham operation (C,n=20),UUO (n=40),and UUO with irbesartan treatment(UUO+irbesartan,n=40).irbesartan was given at a dose of 50 mg/kg body weightper day by gavage.The experimental animals in the control group received thesame volume of vehicle (0.9% saline solution).The animals were sacrificed at d 1,3,7,and 14,respectively,after the surgery.Results:The expression of the ILK atmRNA and protein levels were significantly increased in the UUO group 1 d afterthe surgery,which was significantly decreased by treatment with irbesartan (Pirbesartan significantly abrogated such effects (Pirbesartan attenuated renaltubulointerstitial fibrosis in UUO mice,which may be related to the inhibition ofILK expression,subsequently preventing the tubular EMT.

关键词： irbesartan integrin-linked kinase epithelialmesenchymal transition tubulointerstitial fibrosis

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Effects of irbesartan on the expression of matrix metalloproteinase-2/ tissue inhibitor of metalloproteinase-2 in streptozotocin-induced diabetic rat kidney

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Chinese Medical Journal 2005年第12期118卷 1040-1044页

作者： LIUBi-cheng XUYan MAKun-ling HUANGHai-quan YINLian-fang LIUDian-ge InstituteofNephrology ZhongdaHospitalSoutheastUniversitySchoolofMedicineNanjing210009China

Glomerular hypertrophy and progressive expansion of extracelluar matrix (ECM) have been regarded as the early feature of diabetic nephropathy (DN), which leads to accumulation of ECM and thickening of glomerular basement membrane, and subsequently induces renal fibrosis. Both increasing synthesis and decreasing degradation of matrix components are responsible for matrix accumulation. The later may play more important role in DN that involves a number of matrix metalloproteinases (MMPs). MMPs are a family of proteolytic enzymes whose activity is tightly regulated by tissue inhibitor of metalloproteinases (TIMPs), and the MMP/TIMP ratio is critical for coordinating matrix production and degradation. 1 Recently, considerable evidence suggests that the intrarenal renin-angiotensin system plays an important role in the development of DN. 2 Blockade of the renin-angiotensin system (RAS) by angiotensin-coverting enzyme inhibitor (ACEI) or angiotensin Ⅱ receptor antagonist (AIIRA) delays the progression of renal injury associated with diabetes. 3 AIIRA has been regarded as the first line choice for DN therapy. However, the potential mechanism for AIIRA in the ECM degradative pathway has not been fully elucidated. The present study is to investigate the effect of irbesartan (Irb), a newly developed AIIRA, on renal expression of MMP-2 and TIMP-2 in streptozotocin (STZ)-induced diabetic rats.

关键词： irbesartan diabetic nephropathy matrix metalloproteinase-2 tissue inhibitor of metalloproteinase-2

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Chinese Medical Journal 2012年第8期125卷 1369-1375页

作者： MA Cong LU Xue-chun LUO Yun CAO Jian YANG Bo GAO Yan LIU Xian-feng FAN Li Department of Geriatric Cardiology Chinese People＇s Liberation Army General Hospital Beijing 100853 China Department of Geriatric Hematology Chinese People＇s Liberation Army General Hospital Beijing 100853 China Department of Geriatrics Laboratory Chinese People＇s Liberation Army General Hospital Beijing 100853 China

Background Angiogenesis occurs commonly in various physiological and pathological processes. Improving blood supply through promoting angiogenesis is a novel approach for treating ischemic diseases. Angiotensin II type 1 receptor blockers （ARBs） dominate the management of hypertension, but evidence of their role in angiogenesis is contradictory. Here we explored the angiogenic effects of ARBs through characterizing gene expression of the human umbilical vein endothelial cell line EA.hy926 exposed to irbesartan. Methods The human umbilical vein endothelial cell line EA.hy926 was grown for 72 hours after treatment with different concentrations of irbesartan. The cell proliferative capacity was assessed by CCK8 assay at 24, 48 and 72 hours. Gene expression levels in EA.hy926 cells responding to irbesartan were measured under optimal proliferation conditions by microarray analysis using Affymetrix U133 plus 2.0. The differential expression of genes involved in angiogenesis was identified through cluster analysis of the resulting microarray data. Quantitative RT-PCR and Western blotting analyses were used to validate differential gene expression related to the angiogenesis process. Results In the 104, 105, 106 mol/L treatment groups, cell proliferation studies revealed significantly increased proliferation in EA.hy926 cells after 24 hours of irbesartan treatment. However, after 48 and 72 hours of treatment with different concentrations of irbesartan, there was no significant difference in cell proliferation observed in any treatment group. We selected the group stimulated with irbersartan at a concentration of 10.6 mol/L for microarray experiments. Statistical analysis of the microarray data resulted in the identification of 56 gene transcripts whose expression patterns were significantly correlated, negatively or positively, with irbesartan treatment. Cluster analysis showed that these genes were involved in angiogenesis, extracellular stimulus, binding reactions and skeletal system morphogenesis. Of these 56 genes w

关键词： irbesartan angiogenesis angiotensin H type 1 receptor blockers receptor, angiotensin, type 1 receptor, angiotensin, type 2

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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 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) mR NA 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 pathomorphology 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 mR NA and protein level. Results: The intervention of irbesartan 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 vs SO group). But the expression of Cx43 was increased after the treatment

关键词： irbesartan Myocardial Ischemia Cx43 Connexin Arrhythmias

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Effects and Mechanism of irbesartan on Tubulointerstitial fibrosis in 5/6 Nephrectomized Rats

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Journal of Huazhong University of Science and Technology(Medical Sciences) 2010年第1期30卷 48-54页

作者：赵刚赵洪凃玲徐西振郑常龙姜美华汪培华汪道文 The Institute of Hypertension and Cardiovascular Division Department of Internal MedicineTongji HospitalTongji Medical CollegeHuazhong University of Science and Technology Department of Geriatric Medicine Tongji HospitalTongji Medical CollegeHuazhong University of Science and Technology

Tubulointerstitial fibrosis(TIF)is a common pathological feature of end-stage kidney disease.Previous studies showed that upregulation of TGFβ1 notably contributed to the chronic renal injury and irbesartan halted the development of TIF in rats with 5/6 renal mass reduction.This study was to investigate the effects of irbesartan on chronic TIF and the mechanism involved TGFβ1 in the rodent model of chronic renal failure involving 5/6 nephrectomy.The results showed that irbesartan significantly attenuated th...

关键词： chronic tubulointerstitial fibrosis irbesartan 5/6 nephrectomy signaling pathway

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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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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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