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Objective:To evaluate the clinical efficacy of Gushen Jianpi Huashi Decoction combined with irbesartan in the treatment of spleen and kidney deficiency syndrome of diabetic nephropathy (DN).Methods:According to random number table method, 97 patients with DN who met the inclusion criteria and from January 2018 to September 2020 were randomly divided into two groups, 48 in the control group and 49 in the study group. The control group took irbesartan on the basis of routine treatment of western medicine, and the study group took Gushen Jianpi Huashi Decoction on the basis of the control group. Both groups were treated for 14 days as a course of treatment, a total of 6 courses of treatment. Traditional Chinese Medicine (TCM) syndrome scores were performed before and after treatment, BUN and SCr levels were detected by automatic biochemical instrument, and serum IL-6, TNF-α, and CRP levels were detected by ELISA. The Urinary microalbumin excretion rate (UAER) was measured by radioimmunoassay, and the clinical efficacy was evaluated and adverse reactions were recorded.Results:The total effective rate was 91.8% (45/49) in the study group and 75.0% (36/48) in the control group, and there was significant difference between the two groups ( χ2=4.99, P=0.025). The scores of TCM syndrome in the study group was significantly lower than that of the control group ( t=29.75, P<0.01). After treatment, the serum BUN [(4.49 ± 0.68) mmol/L vs. (5.16 ± 0.61) mmol/L, t=5.11], SCr [(63.42 ± 4.09) μmol/L vs. (69.01 ± 4.35) μmol/L, t=6.52] and UAER [(72.58 ± 5.88) μg/min vs. (85.63 ± 6.49) μg/min, t=10.44] in the study group were significantly lower than those in the control group ( P<0.01), the serum IL-6, CRP and TNF-α levels in the study group were significantly lower than those in the control group ( t values were 9.44, 7.24 and 18.08, respectively, P<0.01). During the treatment, the incidence of adverse reactions was 14.6% (7/48) in the control group and 16.3% (8/49) in the study group, but there was no significant difference between two groups ( χ2=0.06, P=0.812). Conclusion:The Gushen Jianpi Huashi Decoction combined with irbesartan can improve the renal function of DN patients, reduce the level of inflammatory cytokines and improve the clinical effect.
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OBJECTIVE To explore the effects of irbesartan（Irb）combined with 5-fluorouracil（5-FU）on the proliferation and extracellular signal-regulated kinase （ERK）/peroxidase proliferator-activated receptor γ（PPARγ）signaling pathway of Lewis lung cancer cells. METHODS Lewis lung cancer cells from mice were divided into normal control （NC）group，Irb low-dose （LD）group（1×10－3 mmol/L），Irb high-dose （HD）group（1×10－1 mmol/L），5-FU group （10 μmol/L），Irb LD+ 5-FU group （Irb 1×10－3 mmol/L+5-FU 10 μmol/L）and Irb HD+ 5-FU group （Irb 1×10－1 mmol/L+5-FU 10 μmol/L）. MTT method was used to measure the activity of cell proliferation in each group. Plate colony formation experiment was used to determine the number of cell colonies formed in each group ；Western blot method was used to detect the expression levels of proliferating cell nuclear antigen （PCNA），p53，ERK1/2，p-ERK1/2 and PPAR γ protein in each group. RESULTS Compared with the NC group ，the cell proliferation activity ，the number of colonies formed and the protein levels of PCNA ，p-ERK1/2，and PPARγ were significantly reduced in the other five groups ，and the protein level of p 53 was significantly increased （P＜0.05）；the protein expression of ERK1/2 had no significant difference （P＞0.05）. The changes of above indexes in Irb LD+ 5-FU group and Irb HD+ 5-FU group were more significant than Irb LD group ，Irb HD group and 5-FU group （P＜0.05）. CONCLUSIONS Irb combined with 5-FU can inhibit the proliferation of Lewis lung cancer cell ，and the effect is better than that of the two alone. The mechanism may be related to the inhibition of ERK/PPARγ signal pathway.
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Objective:To investigate the efficacy of tripterygium glycoside tablets combined with irbesartan for chronic nephritis and its effect on 24-hour urine protein and inflammatory factor levels.Methods:Ninety patients with chronic nephritis who received treatment at The Second People's Hospital of Liaocheng from April 2018 to January 2020 were included in this study. They were randomly divided into an observation group and a control group, with 45 patients in each group. The control group was treated with irbesartan. The observation group was treated with tripterygium glycoside tablets combined with irbesartan. All patients were treated for 3 successive months. Clinical efficacy and adverse reactions were compared between the two groups. Changes in 24-hour urine protein level, symptom score, and inflammatory factor levels after treatment relative to those before treatment were compared between the two groups.Results:Response rate in the observation group was significantly higher than that in the control group [95.6% (43/45) vs. 80.0% (36/45), χ2 = 5.07, P = 0.024). Before treatment, there were no significant differences in 24-hour urine protein level, symptom score, and inflammatory factor level between the two groups (all P > 0.05). After treatment, the 24-hour urine protein level in the observation group was significantly lower than that in the control group [(1.42±0.01) g/24 hours vs. (1.95 ± 0.05) g/24 hours, t = 69.72, P = 0.012). The symptom score in the observation group was significantly lower than that in the control group [(0.78 ± 0.01) points vs. (1.33 ± 0.12) points, t = 30.64, P = 0.001]. Serum levels of C-reactive protein, interleukin-6, and tumor necrosis factor-α in the observation group were significantly lower than those in the control group ( t = 15.70, P = 0.006; t = 96.55, P = 0.003; t = 43.41, P = 0.002). There was no significant difference in the incidence of adverse reactions between the two groups ( P = 0.694). Conclusion:Tripterygium glycoside tablets combined with irbesartan is highly effective on chronic nephritis. The combined therapy can remarkably decrease 24-hour urine protein levels, reduce symptom scores, and decrease inflammatory factor levels.
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Objective To explore the effects of irbesartan combined with hemodialysis on renal function,inflammatory factors and renal hemodynamics in patients with renal proteinuria.Methods A total of 106 patients with renal proteinuria who underwent hemodialysis in Changzheng Hospital Affiliated to Naval Medical University from May 2016 to May 2018 were selected for the study and were divided into observation group and control group according to the random number table method.The two groups were given hemodialysis,and observation group was given irbesartan on this basis.Kidney-related examination indexes [24 h urine protein quantitation,24 h urine volume,serum creatinine (Scr),urea nitrogen (BUN)],inflammatory factors [C-reactive protein (CRP),interleukin-8 (IL-8),intercellular adhesion molecule-1 (ICAM-1),monocyte chemoattractant protein-1 (MCP-1)],bilateral renal interlobar artery resistance index (RI),hemorheology (whole blood viscosity,low-shear viscosity,high-shear viscosity,erythrocyte aggregation index)were observed in the two groups before and after treatment.Results After 3 months of treatment,the levels of urine protein quantitation,serum Scr,BUN,CRP,IL-8,ICAM-1 and MCP-1 in the two groups were lower than those before treatment,and the levels in observation group were lower than those in control group (P ＜ 0.05);the 24h urine volume was more than that before treatment,and the level in observation group was more than that in control group (P ＜ 0.05).The RI values of bilateral kidney in the two groups were lower than those before treatment,and the value in observation group was lower than that in control group (P ＜ 0.05).The whole blood viscosity,low-shear viscosity,high-shear viscosity and erythrocyte aggregation index in the two groups were lower than those before treatment,and the indexes in observation group were lower than those in control group (P ＜ 0.05).Conclusions Addition of irbesartan in patients with renal proteinuria treated by hemodialysis can effectively improve renal function,reduce inflammation and blood viscosity,and improve renal hemodynamics,and promote the disease outcomes.
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Objective: The mass characterization of five trace level related impurities of Irbesartan was performed through the “nMS2” technique of triple quadrupole mass spectrometer and also to Correlated to the impurity origin. Methods: A simple and effective patented process was applied to get the impurity profile, and mass characterization was performed through the “nMS2” technique of triple quadrupole mass spectrometer analyser. Results: The simple production scan in differential collision energies is coined as “nMS2” technique of the triple quadrupole analyzer. The molecular ion fragmentation occurs with multiple collision energies and provides meaningful MSMS fragments for characterizing five trace level impurities less than 0.5% of angiotensin II receptor antagonist-Irbesartan. The origin of the impurity formation in the synthetic process was successfully related to the Spiro ketones. Conclusion: The results obtained in this research clearly indicates the approach of “nMS2” technique was very useful in the identification and structural prediction of trace level related impurities of Irbesrtan.
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Irbesartan (IBS) is a tetrazole derivative and antihypertensive drug that has two interconvertible struc-tures, 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 ?C and 40 ?C 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 ?C 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.
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Objective To compare the effects of losartan and irbesartan on blood pressure,blood uric acid,insulin sensitivity and insulin resistance in female hypertensive patients complicated with hyperuricemia.Methods From August 2015 to December 2017,100 females of hypertension complicated with hyperuricemia who hospitalized in the Third People's Hospital of Ningxia were enrolled in the study.All the patients were divided into two groups according to the random digital table,with 50 cases in each group.The observation group was treated with losartan,and the control group was treated with irbesartan for 8 weeks.The total effective rate and adverse reactions were compared between the two groups.Also the changes of blood pressure,serum uric acid,fasting glucose (FBG),fasting insulin (FINS),high sensitivity C-reactive protein (hs-CRP),insulin sensitivity index (ISI) and insulin resistance index (HOMA-IR) were compared between the two groups after treatment.Results There was no statistically significant difference in the total effective rate between the two groups [92.0％ (46/50) vs.90.0％ (45/50)] (P ＞ 0.05).Before treatment,there were no statistically significant differences in blood pressure,serum uric acid,FBG,FINS,hs-CRP,ISI and HOMA-IR between the two groups (all P ＞ 0.05).After treatment,the systolic blood pressure and diastolic blood pressure in the two groups were (133.09 ± 10.11) mmHg vs.(131.54 ± 11.01) mmHg and (82.76 ± 6.23) mmHg vs.(83.75 ± 6.88) mmHg,which were lower than those before treatment (observation group:t =19.742,10.606,control group:t =18.925,-9.956,all P ＜ 0.05).But there were no statistically significant differences between the two groups (all P ＞ 0.05).After treatment,the serum uric acid in the observation group was lower than that in the control group [(387.21 ± 25.56) μmol/L vs.(429.67 ± 27.44) μmol/L] (t =8.006,P ＜ 0.05).The hs-CRP,FINS,HOMA-IR,ISI in the observation group were (4.92 ± 1.02) rmg/L,(15.92 ± 3.01) mU/L,(1.71 ± 0.24),(1.047 ± 0.095),which in the control group were (4.54 ± 1.00) mg/L,(17.23 ± 3.20) mU/L,(1.65 ± 0.27),(1.140 ± 0.083).After treatment,the hs-CRP,FINS,HOMA-IR in the two groups were decreased (all P ＜ 0.05),while ISI was increased (P ＜ 0.05).Furthermore,the improvement of FINS,ISI and HOMA-IR in the observation group was better than those in the control group (t =2.109,-5.213,3.191,all P ＜ 0.05).Conclusion Both losartan and irbesartan can improve clinical symptoms,lower blood pressure and improve insulin resistance in female hypertension patients complicated with hyperuricemia,and losartan is more effective than irbesartan.
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Objective To investigate the clinical effect of nifedipine combined with irbesartan in the treatment of diabetes mellitus with hypertension.Methods From August 2015 to January 2017,66 diabetes mellitus patients with hypertension in the First People's Hospital of Yongkang were selected in the study and randomly divided into control group and observation group,with 33 cases in each group.The control group was treated with nifedipine,and the observation group was treated with nifedipine combined with irbesartan for 2 months.The changes of blood pressure,blood sugar and adverse reactions of the two groups were observed.Results After treatment,the diastolic blood pressure,systolic blood pressure,postprandial blood glucose,fasting blood glucose,psychological score,physiological score,social relation score,substance life score in the observation group were (72.71 ± 4.04)mmHg,(121.78 ± 4.22) mmHg,(7.55 ± 1.26) mmol/L,(5.25 ± 0.79) mmol/L,(88.22 ± 4.31) points,(86.75 ± 3.82) points,(82.38 ± 3.23) points,(81.85 ± 2.79) points,respectively,which were better than those of the control group [(88.95 ± 3.71) mmHg,(138.44 ± 5.25) mmHg,(11.50 ± 2.12) mmol/L,(7.33 ± 0.70) mmol/L,(74.58 ± 3.93) points,(73.71 ± 4.04) points,(74.62 ± 3.93) points,(75.76 ± 3.32) points],the differences were statistically significant(t =15.94,13.32,8.63,10.61,13.43,13.47,8.76,8.07,all P ＜ 0.05).The incidence rate of adverse events was 18.18％ in the control group,which in the observation group was 12.12％,there was no statistically significant difference between the two groups(P ＞ 0.05).Condusion Nifedipine combined with irbesartan is superior to nifedipine in the treatment of diabetes mellitus with hypertension.
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Objective To investigate the efficacy and safety of Irbesartan Hydrochlorothiazide combined with Metoprolol as initial therapy in the treatment of heart failure in the elderly.Methods A total of 128 elderly patients with heart failure admitted into our hospital from September 2017 to August 2018 were randomly divided into Group A(n=64)and Group B(n=64).Group A was treated with oral Irbesartan Hydrochlorothiazide tablets.Group B was treated with sustained-release oral Metoprolol tablets in addition to what was given in Group A.Therapeutic effects were compared between the groups.Results Compared with Group A,the effectiveness rate of group B was significantly improved(93.8％ vs.81.3％,x2 =4.571,P=0.033).There was no significant difference in brain natriuretic peptide (BNP),interleukin (IL)-12,left ventricular ejection fraction (LVEF),left ventricular end-systolic diameter(LVESD),or left ventricular end-diastolic diameter(LVEDD)between the two groups before treatment (P＞0.05).Compared with Group B,BNP,IL-12,LVEF,LVESD and LVEDD had significantly better profiles in Group A after treatment (P ＜ 0.05).The time-domain measurements of heart rate variability such as sequential five-minute R-R interval means(SDANN),standard deviation of the N-N interval(SDNN),percent of differences between adjacent RR intervals ＞50ms(PNN50)and root mean square of the successive differences(RMSSD)were higher in Group B than in Group A after treatment.No serious adverse reactions were observed in either group,and there was no significant difference in the incidence of adverse reactions between the two groups(4.7％ vs.7.8 ％,x2 =0.533,P =0.465).Conclusions Irbesartan Hydrochlorothiazide combined with Metoprolol as initial therapy has good clinical effects in treating elderly heart failure.It can not only improve the clinical symptoms of patients,but also ensure clinical medication safety.
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Objective :To study therapeutic effect of irbesartan combined amlodipine on aged patients with diabetes mellitus complicated hypertension .Methods : A total of 94 aged patients with diabetes mellitus complicated hypertension ,who were treated in our hospital from Feb 2015 to Aug 2016 ,were selected .Patients were randomly and equally divided into amlodip‐ine group (received amlodipine based on routine treatment ) and combined treatment group (received irbesartan based on amlodipine group) ,both groups were treated for 12 weeks.Levels of blood pressure : SBP , DBP ,fasting plasma glucose (FPG) ,fasting insulin (FINS) and serum 25‐hydroxyl vitamin D3 [25‐(OH) D3] before and after treatment ,total effec‐tive rate and incidence rate of adverse reactions were observed and compared between two groups .Results : Total effective rate of combined treatment group was significantly higher than that of amlodipine group (91.49% vs.74.47%) , P＝0.028. Compared with before treatment ,after treatment ,there were significant reductions in levels of SBP ,DBP and FINS and significant rise in serum 25‐(OH) D3 level in two groups ,and significant reduction in FPG level in combined treatment group , P＝0.001 all.Compared with amlodipine group after treatment ,there were significant reductions in lev‐els of SBP [ (144.02 ± 11.24) mmHg vs.(129.75 ± 10.07) mmHg] ,DBP [ (85.20 ± 7.27) mmHg vs.(75.72 ± 8.13) mmHg] ,FPG [ (7.14 ± 0.47) mmol／L vs.(6.72 ± 0.51) mmol／L] and FINS [ (19.28 ± 3.24) μU／ml vs.(16.18 ± 2.39) μU／ml] ,and significant rise in serum 25‐(OH) D3 level [ (26.37 ± 3.87) μg／L vs.(32.48 ± 4.22) μg／L] in combined treatment group ,P＝0.001 all.There was no significant difference in incidence rate of adverse reactions between two groups ,P＝0.712. Conclusion : Irbesartan combined amlodipine possesses significant therapeutic effect on aged patients with diabetes mellitus complicated hypertension .It can significantly and effectively control blood pressure ,improve glucose metabolism with good safety ,which is worth extending .
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OBJECTIVE:To investigate the long-term economic consequences of candesartan cilexetilirbesartan and telmisartan in preventing stroke and myocardial infarction (MI) among hypertension patients using Markov model, to offer the reference for hypertension intervention. METHODS:A Markov state transition model was built based on the natural history of hypertension from the societal perspective to estimate the expected health care costs and the quality adjusted life years. Meanwhile, the incremental cost-effectiveness ratio was obtained. One year cycle length and 20 years horizon were adopted. The 5% yearly discount rate was applied to both health care costs and QALYs. One-way sensitivity analysis, second-order Monte-Carlo and probabilistic sensitivity analysis were performed. RESULTS:Candesartan cilexetil was at an absolute disadvantage because of the highest cost and the lowest effect in the baseline analysis. The incremental cost-effectiveness ratio for irbesartan versus telmisartan was 5 799.67 yuan/QALY. The sensitivity analysis was consistent with the baseline results. CONCLUSION:Irbesartan shows significant economic advantage at the threshold of 49 992 yuan/QALY compared with telmisartan. And candesartan cilexetil is with less economical.
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To study therapeutic effects of irbesartan combined amiodarone on heart failure (HF) patients with atrial fibrillation (AF) and its influence on cardiac function ,plasma levels of Ang‐Ⅱ,NE and BNP .Methods :A total of 98 HF patients with AF treated in our hospital from Sep 2016 to Sep 2017 were randomly divided into ami‐odarone group (received amiodarone based on routine treatment ) and combined treatment group (received irbesar‐ tan based on amiodarone group).Both group were treated for six months .HR ,BP ,cardiac function indexes ,plas‐ma levels of Ang‐Ⅱ,NE and BNP before and after treatment ,and incidence of adverse reactions were observed and compared between two groups .Results : Compared with before treatment ,after treatment ,there were significant reductions in HR ,BP ,LVEDd ,LVESd ,plasma levels of Ang‐Ⅱ,NE and BNP ,and significant rise in LVEF in two groups , P＜0. 05 or ＜0. 01. Compared with amiodarone group ,after treatment ,there were significant reduc‐tions in HR [(95. 6 ± 13.7) beats／min vs .(81. 4 ± 11. 8) beats／min] ,BP [(145. 7 ± 20.6)／(89.1 ± 11.4) mmHg vs.(132.3 ± 17.5)／(81.3 ± 10.2) mmHg] ,LVEDd [ (58.3 ± 5.2) mm vs.(53.2 ± 4.6) mm] ,LVESd [ (44. 2 ± 5. 1) mm vs.(38.1 ± 4.9) mm] ,plasma levels of Ang‐Ⅱ[(113.27 ± 10.14) pg／ml vs.(98.67 ± 8. 79) pg／ml] , NE [(1.90 ± 0. 31) pg／ml vs.(1.74 ± 0. 28) pg／ml] and BNP [(282.18 ± 54.16) pg／ml vs.(214. 36 ± 41. 25) pg／ml] ,and significant rise in LVEF [(39.8 ± 4.1)% vs.(48.6 ± 5. 5)%] in irbesartan group ,P＜0.01 all.There was no significant difference in incidence rate of adverse reactions during treatment between two groups , P＝ 0.712. Conclusion :Irbesartan combined amiodarone can effectively improve cardiac function ,reduce HR ,BP ,plasma lev‐els of Ang‐Ⅱ,NE and BNP with good safety in HF patients with AF .
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Objective To evaluate the efficacy of Yangsheng-Yishen decoction combined with irbesartan in the treatment of early diabetic nephropathy (DN).Methods A total of 95 patients with early DN who met the inclusion criteria were randomly divided into control group (47 cases) and treatment group (48 cases).The control group was treated with irbesartan,while the treatment group was given Yangsheng-Yishen decoction on the basis of the control group.The two groups were treated for 6 months.The FBG,HbAlc,urinary albumin excretion rate (UAER),Scr,TG,TC,LDL-C and HDL-C were detected by automatic biochemical analyzer.The level of vascular endothelial growth factor (VEGF),platelet derived growth factor (PDGF),tumor necrosis TNF-α and transforming growth TGF-β were measured by elisa assay,and the clinical efficacy was evaluated.Results After treatment,the levels of FBG,HbAlc,UAER and SCr in the treatment group was significantly lower than those in the control group (t=3.886,4.056,9.346,8.806,all P＜0.01).After treatment,the serum TG,TC and LDL-C of the treatment group were significantly lower than those of the control group (t=8.294,12.800,6.153,all P＜0.001),and HDL-C was significantly higher than that of the control group (t=4.293,P＜0.01).The levels of serum VEGF,PDGF,TNF-α and TGF-β in the treatment group was significantly lower than those in the control group (t=13.585,11.613,10.774,10.490 respectively,all P＜0.01).Conclusions The Yangsheng-Yishen decoction combined with irbesartan can reduce blood sugar,blood lipid and urinary protein level in early DN patients,improve renal function.
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OBJECTIVE@#To investigate the effects and mechanisms of irbesartan on myocardial injury in diabetic rats, and to analyze the changes of Notch1 signaling pathway in it.@*METHODS@#Thirty rats were randomly divided into four groups:normal control group (CON, =6), high calorie group (HC, =6) and diabetes mellitus group (DM, =9), irbesartan + diabetes group (Ir + DM, =9). After modeling 8 weeks later, the body weight ratio and left ventricular weight index were measured and the serum levels of triglyceride (TG) and total cholesterol (TC) were measured by automatic biochemical analyzer. The changes of superoxide dismutase (SOD) activity and malondialdehyde (MDA) content in myocardium of rats were determined by the kit and the expressions of B-cell lymphoma-2 (Bcl-2) and Bcl-2 assaciated X protein (Bax) protein in myocardium were detected by immunohistochemistry. The expressions of Notch1, Hes-1 and jagged-1 in myocardium of rats were detected by Western blot.@*RESULTS@#Compared with CON group, the levels of heart weight/body weight (H/B), left ventricular weight index(LVWI) and fasting blood glucose(FBG) in HC group were not significantly changed, while the levels of blood lipids, MDA and Bax were increased significantly, and the expressions of SOD, Bcl-2 and Notch1, Hes-1 and Jagged-1 were decreased. Compared with HC group, the levels of H/B, LVWI, FBG, MDA and Bax in DM group were increased significantly, and the levels of SOD, Bcl-2 and Notch1, Hes-1 and Jagged-1 were decreased. The expression of H/B, LVWI, Notch1, Hes-1 and Jagged-1 in Ir+DM group were increased, but there was no significant difference between the other indexes. The H/B and LVWI in Ir + DM group were significantly lower than those in DM group, the levels of blood lipid and blood glucose did not change significantly, but the incidence of oxidative stress and apoptosis was reduced. While Notch1, Hes-1, Jagged -1 protein expressions were increased.@*CONCLUSIONS@#Diabetes can induce myocardial injury, and irbesartan has myocardial protective effects through activation of Notch1.
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Animals , Rats , Diabetes Mellitus, Experimental , Irbesartan , Myocardium , Rats, Sprague-Dawley , Receptor, Notch1 , Signal TransductionABSTRACT
AIM:To investigate the effect of irbesartan on the fatty liver of db/db mice and whether autophagy is involved in the process.METHODS:Male db/db mice(n=24)were randomly divided into model group and irbesar-tan group,and 12 db/m mice with similar age and weight were selected as normal control group.After 16 weeks of inter-vention respectively,the fatty liver-related parameters including body weight, liver index, blood lipid, liver function and pathological changes in the liver were observed.The protein levels of p-PI3K,p-Akt,and p-mTOR,as well as Atg-7,bec-lin-1 and LC3B in the liver tissues were detected by Western blot,and the autophagosomes in the liver were observed under electron microscope.RESULTS:Compared with the model group,the body weight,liver index,blood lipids,alanine and aspartate aminotransferase were decreased in irbesartan group(P<0.05).Moreover,the pathological changes in the liver were significantly ameliorated in irbesartan group than that of model group.Importantly, the protein levels of p-PI3K, p-Akt and p-mTOR were decreased with irbesartan administration,while the expression of Atg-7,beclin-1 and LC3B-Ⅱwas increased(P<0.05),which resulted in a distinct increase in autophagosomes.CONCLUSION:Irbesartan alleviates he-patic steatosis in db/db mice by inhibiting the PI3K/Akt/mTOR signaling pathway and upregulating the protein expression of Atg-7,beclin-1 and LC3B-Ⅱ,thereby inducing autophagy in hepatocytes.
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Objective :To explore therapeutic effect and safety of irbesartan hydrochlorothiazide (I+H) tablet combined am-lodipine besylate on young and middle-aged patients with hypertension .Methods : A total of 138 young and middle-aged pa-tients with hypertension ,who were treated in our hospital from Jan 2015 to Feb 2017 ,were selected .Patients were ran-domly and equally divided into group A (received I+ H therapy) ,group B (received amlodipine treatment ) and group C (received I+ H+ amlodipine treatment ) ,all groups were continuously treated for three months .Systolic blood pressure (SBP) ,diastolic blood pressure (DBP) and heart rate (HR) before and after treatment ,total effective rate and incidence rate of adverse reactions were measured and compared among three groups .Results :Compared with before treatment ,after treatment ,there were significant reductions in SBP ,DBP and HR in three groups , P＜0.05 or ＜0.01. Compared with group A after treatment ,there was significant reduction in SBP [ (133.1 ± 6.2) mmHgvs.(128.9 ± 6.0) mmHg vs. (122.0 ± 3.8) mmHg] in group B and C ,and that of group C was significantly lower than that of group B ,P＜0.01 all ;compared with group B after treatment ,there was significant reduction in DBP [ (91.7 ± 6.7) mmHg vs.(87.5 ± 4.8) mmHg vs.(79.3 ± 3.0) mmHg] in group A and C ,and that of group C was significantly lower than that of group A ,P＜0.01 all.Compared with group A and B ,there was significant rise in total effective rate (78.3% vs.73.9% vs.97.8%) in group C , P＜0.01 all.There was no significant difference in incidence rate of adverse reactions among three groups , P＝0.876 .Conclusion : Irbesartan hydrochlorothiazide tablet combined amlodipine besylate tablet can significantly improve blood pressure in young and middle-aged patients with hypertension , Its effect is better than that of two drugs alone use . Which is safe and reliable ,and is worth extending .
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ABSTRACT Irbesartan is an antihypertensive with limited bioavailability and solid lipid nanoparticles (SLN) is one of the approaches to improve bioavailability. Solid lipid nanoparticles were prepared using glyceryl monostearate by solvent emulsification method followed by probe sonication. Irbesartan loaded SLNs were characterized and optimized by parameters like particle size, zeta potential, surface morphology entrapment efficiency and in vitro release. The optimized formulation was then further evaluated for the pharmacokinetic studies in Wistar rats. Irbesartan-loaded SLN of particle size 523.7 nm and 73.8% entrapment efficiency showed good bioavailability in Wistar rats and also showed optimum stability in the studies. The SLN prepared using glyceryl monostearate by solvent emulsification method leads to improve bioavailability of the drug.
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Animals , Male , Angiotensins/antagonists & inhibitors , Nanoparticles/statistics & numerical data , Antihypertensive Agents/pharmacokinetics , Pharmacokinetics , Biological Availability , Emulsifying Agents/analysisABSTRACT
OBJECTIVE:To compare therapeutic efficacy and safety of indapamide separately combined with benazepril,irbe-sartan or amlodipine for grade 2 essential hypertension(EH). METHODS:A total of 150 patients with grade 2 EH were randomly divided into benazepril group(50 cases),irbesartan group(50 cases)and amlodipine group(50 cases). 3 groups were given Indap-amide tablet 2.5 mg orally,once a day. Benazepril group was additionally given Benazepril hydrochloride tablet 10 mg orally,once a day;irbesartan group was additionally given Irbesartan tablet 150 mg orally,once a day;amlodipine group was additionally giv-en Amlodipine tablet 5 mg orally,once a day. 3 groups were treated for 12 weeks. The levels of systolic pressure,diastolic pres-sure,heart rate,total cholesterol(TC),three triacylglycerol(TG)and serum potassium as well as the occurrence of ADR were ob-served in 3 groups before and after treatment. RESULTS:The total response rate of berazopril group,irbesartar group and a mloelip-ire group had no significant difference(90.0% vs. 88.0% vs. 92.0%,P>0.05). There were no statistical significances in the levels of systolic pressure,diastolic pressure,heart rate,TC,TG and serum potassium among 3 groups before treatment(P>0.05). Af-ter treatment,systolic pressure and diastolic pressure of 3 groups were significantly lower than before,with statistical significance (P0.05). There were no statistical significance in heart rate, TC,TG of 3 groups before and after treatment and the level of serum potassium in benazepril group and irbesartan group (P>0.05). After treatment,the level of serum potassium in amlodipine group was significantly lower than before,with statistical signifi-cance (P0.05). CONCLUSIONS:The indapamide separately combined with benazepril,irbesartan or amlodipine have similar therapeu-tic efficacy for grade 2 EH,but the safety of irbesartan is better than those of benazepril and amlodipine.
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Objective To observe the efficacy of irbesartan combined with metoprolol in the treatment of chronic congestive heart failure.Methods From April 2015 to April 2016,60 patients with chronic congestive heart failure in Central Hospital of Zhuji were randomly divided into the observation group and the control group,30 cases in each group.The two groups were given conventional treatment,the control group was treated with metoprolol,and the observation group was treated with irbesartan combined with metoprolol.The changes of left ventricular ejection fraction (LVEF),left ventricular end systolic diameter (LVESD),left ventricular end diastolic diameter (LVEDD),heart rate,systolic pressure and diastolic pressure before and after treatment in two groups were observed.And the clinical efficacy of the two groups was compared.Results After treatment,compared with the control group,the heart function index of the observation group changed obviously,LVEF increased (t=5.88,P＜0.01),LVESD and LVEDD significantly decreased (t=7.19,4.11,all P＜0.01).The heart rate of the observation group was significantly slowed down (t=2.72,P＜0.01),systolic blood pressure and diastolic blood pressure were also significantly reduced (t=2.93,3.98,all P＜0.01).The total effective rate of the observation group was 93.3％,which of the control group was 73.3％,the difference was statistically significant (χ2=4.32,P＜0.05).ConclusionIrbesartan combined with metoprolol in the treatment of chronic congestive heart failure has significant clinical efficacy,is conducive to ease the clinical symptoms and improve heart function effectively.
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Objective To study the clinical efficacy of irbesartan hydrochlorothiazide combined with small dose thyroxine in the treatment of severe heart failure in the elderly. Methods 100 elderly patients with severe heart failure were selected as the research object (from January 2013 to December 2016). They were randomly divided into the control group and the experimental group, with 50 patients in each group. Patients in the control group received routine treatment, including diuretic therapy, cardiac treatment, and anti heart failure treatment. The experimental group was treated with low-dose thyroxine combined with irbesartan and hydrochlorothiazide on this basis. The clinical effects of the two groups were compared and analyzed. Results After the corresponding treatment, the number of invalid cases in the experimental group was 6 cases, 16 cases were effective, 28 cases were effective,and the total effective number was 44 cases. In the control group, the number of invalid cases was 15. The effective rate of the treatment group was 88.0％, which was significantly higher than that of the control group 70％, which was statistically significant (P<0.05). After treatment, the left ventricular ejection fraction, the level of four and three, and the level of serum thyroid stimulating hormone in the experimental group were significantly higher than those before treatment, with statistical difference (P<0.05). Conclusion Small dose thyroxine combined with irbesartan and hydrochlorothiazide is effective in the treatment of severe heart failure in elderly patients, and can significantly improve the heart function of patients, and has the significance of further clinical promotion.