ABSTRACT
SUMMARY Objective: Myocardial infarction has unfavorable effect on structural and functional properties of the myocardium, referred to as cardiac remodeling. Left ventricular mass, left ventricular mass index, and relative wall thickness are important predictors of cardiac remodeling. In this study, we investigated the effect of candesartan treatment in comparison with zofenopril treatment on echocardiographic indices of cardiac remodeling in post myocardial infarction patients. Material and Methods: In this prospective study, patients who underwent successful percutaneous coronary intervention were randomly assigned to a candesartan or zofenopril treatment. After randomization, echocardiographic indices of cardiac remodeling including left ventricular mass, left ventricular mass index, and relative wall thickness were evaluated before the start of treatment along with 1- and 6-month follow-ups. Results: According to our study, candesartan group showed significant reduction of estimated left ventricular mass and left ventricular mass index at 6-month follow-up visit compared to baseline values (199.53±38.51 g vs. 212.69±40.82 g; 99.05 g/m2 (90.00-116.5) vs. 106.0 g/m2 (96.0∼123.00), p<0.05, respectively). This trend was also observed in zofenopril group during the 6-month period (201.22±40.07 g vs. 207.52±41.61 g; 101.0 g/m2 (92.25-111.75.0) vs. 104.50 g/m2 (95.0∼116.75), p<0.05, respectively). Although both classes of drugs had favorable effects on post-myocardial infarction cardiac remodeling, the absolute benefit was more prominent in candesartan group as compared to zofenopril group (p<0.05). Conclusion: Our results suggest that candesartan treatment following myocardial infarction may potentially be useful in terms of improving post-myocardial infarction cardiac remodeling.
ABSTRACT
Aim:Some generics were reported to be counterfeit and inferior quality than the innovators. This study was aimed to make sure about the compliance with standard specifications and evaluation of the quality of different selected brands (generic and innovator),after performing different pharmacopeial quality control tests, of Candesartan cilexetil tablets (16 mg) commercially available in Saudi Arabia for hypertensive patients Study Design:In vitrostudy of tablets.Place and Duration of Study: Collegeof Pharmacy, Jazan University, Jazan, KSA, between September 2018 and May 2019.Methodology:The different generic brands of Candesartan cilexetil (CC) and innovator brand (16 mg) were subjected to weight variation, hardness, friability, assay, and disintegration tests following the established protocols. The purity of active ingredient was authenticated by comparative analysis of FT-IR spectra with pure drug. In vitro bioequivalence was studied after analyzing the results of dissolution summaries in phosphate buffer (pH 6.5) mixed with polysorbate 20 (0.35% v/v).Results:The results of the tests conducted for evaluation of the tablets were found to be in acceptable limits for all the selected brands. After comparative analysis of FT-IR spectra with pure drug, it was inferred that correct active ingredient was used for the preparation of tablets. The drug release profile exhibited 96.89 –101.97% of release of CC from all generic brands, in comparison to 99.4% for innovator brand after 60 min of study. The assessment of difference factor (f1<15) and similarity factor (f2>50) revealed the resemblance of generic brands with that of innovator brand. Furthermore, the dissolution efficiency (DE = ±10% of the innovator value) of all generic brands (73.12 –73.25%) exhibited equivalency with that of innovator brand (70.45%). Conclusion:The selected generics were considered to be biopharmaceutically equivalent to the innovator and maintained their efficacy. As a consequence, these brands can be used interchangeably by the hypertensive patients in Saudi Arabia
ABSTRACT
Background: Antihypertensive agents like Angiotensin-Converting Enzyme Inhibitors (ACEIs) and Angiotensin-Converting Enzyme Blockers (ARBs) are commonly indicated for patients with both hypertension and diabetes. However, the effect of these agents on blood sugar level or glycated hemoglobin (HbA1c) is still controversial. This study aims at investigating theshort, and long term effects of ACEIs and ARBs on blood sugar level and HbA1c of a group of streptozocin (STZ)-induced NIDDM rats when given in combination with Glimepiride (antidiabetic drug from Sulfonylureas group).Methods: Diabetes mellitus (DM) was induced in 100 Wistar albino adult male and female laboratory rats above 8 weeks old, and weigh between 250-300 gm by the administration of Streptozocin 75% α-anomer. Two weeks later, the100 rats were then randomized into four groups (25 rats each). Groupone was the untreated control group (received placebo only), while other groups (II, III, and IV) were treated by Glimepiride only, Glimepiride plus ARB (Candesartan), and Glimepiride plus ACEI (Enalapril)respectively. HbA1C levels were measured at baseline (pre-test/directly after randomization) to ensure that there was no significant difference between study groups at the baseline, post-test (after two weeks), and delayed-post-test (12 weeks after randomization/ 10 weeks after post-test) to measure short and long-term changes in the study groups.Results: There was no significant difference (p-values >0.05) between the four groups (groups I, II, III, and IV) in the HbA1C mean level at the beginning of this study (two-weeks after randomization and injection of STZ) (mean = 7.62 ±SD = 0.41, 7.72 ±SD = 0.48, 7.66 ±SD = 0.47, and 7.52 ±SD = 0.51respectively). However, two weeks later, treated groups (groups II, III, and IV) showed moderate reduction of HbA1C mean level compared to the untreated (placebo) group I, that was significant in groups III, and IV, and insignificant in group II (mean =7.43±SD 0.54, 6.97±SD 0.33, 6.72±SD 0.26, and 7.71 ±SD 0.44 respectively). Furthermore, treated groups (groups II, III, and IV) showed significant dramatic reduction of HbA1C mean level when compared to the untreated group (group I) (mean = 6.22 ±SD 0.51, 5.24 ±SD 0.62, 5.22 ±SD 0.13, and 7.62 ±SD 0.42 respectively).Overall, treated groups showed significantly lower HbA1C level than placebo groups. Moreover, Glimepiride + Enalapril combination showed a stronger hypoglycemic effect than the Glimepiride + Candesartan combination at post, and post-delayed tests, however, these differences were not significant.Conclusion: The addition of either ACEIs like Enalapril, or ARBs like Candesartan to Sulfonylureas like Glimepiride to in NIDDM patients will synergize its anti-diabetic effect in NIDDM subjects, and might increase the possibility of hypoglycemia. Caution and/or dose adjustment should be considered upon using these agentstogether in patients with hypertension along with diabetes
ABSTRACT
OBJECTIVE： To provide reference for the evaluation of the correlation between drugs and adverse drug reaction （ADR） and the implementation of medication therapy management （MTM）. METHODS： Clinical information of a elderly patient with chronic disease （hypertension and coronary heart disease） whose suffered from leukocyte and platelet counts reduction and abnormal liver biochemical examination after taking candesartan were analyzed retrospectively in outpatient department of Tianjin Third Central Hospital. MTM pharmacists analyzed the correlation of candesartan with ADR using Naranjo evaluation scale method. The reasons for abnormal liver biochemical examination were analyzed by Naranjo evaluation scale method combined with Roussel Uclaf causality analysis method （called RUCAM method for short）. The medication reconciliation was conducted according to the results， and pharmacists cooperated with doctors to set individualized medication regimen and follow-up. RESULTS： By Naranjo evaluation scale method， analysis results showed that candesartan was “probably related” to ADR. By RUCAM method， analysis results showed that candesartan was “probably related” to liver biochemical abnormalities. MTM pharmacists suggested that candesartan should be stopped in time and the patient’s medication should be adjusted. The physician and the patient adopted the pharmacist’s advice. After 38 days of drug withdrawal， the patient’s ADR symptoms disappeared， and leukocyte count， platelet count and liver biochemical examination were normal. After adjustment of medication， the patient was followed up for 6 months with normal blood pressure. CONCLUSIONS： Naranjo evaluation scale method and RUCAM are simple and feasible in evaluating the correlation of drugs with ADR and hepatotoxicity. The two methods are consistent in evaluating the correlation between drugs and hepatotoxicity. Naranjo scale method and RUCAM method can be combined to analyze the correlation between drugs and ADR with abnormal liver biochemical examination.
ABSTRACT
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.
ABSTRACT
Abstract A simple, sensitive, rapid and highly efficient LC-MS/MS method was developed for the determination of Candesartan and Hydrochlorothiazide simultaneously in human plasma. The method employed Zorbax eclipse C18 (150 X 4.6 mm, 5µ) column using acetate buffer: acetonitrile (25:75%, v/v) as the mobile phase. The mobile phase flow rate is 1 mL/min which was delivered into the mass spectrometer electron spray ionization chamber. The Liquid/liquid extraction procedure was used in the method for the extraction of analytes. The chromatograph was attached to a negative ion mode tandem mass spectrometer and the method was validated for all the parameters as per the guidelines of US-FDA. The ions were detected in multiple reaction monitoring mode and the transitions are m/z 439.00®309.10 and 295.80®268.80 for candesartan and hydrochlorothiazide respectively. Isotopic standards were used as internal standards for effective recovery of the analytes. The drugs were analyzed over a calibration range of 1.027-302.047 ng/mL for candesartan and 1.044-306.945 ng/mL for hydrochlorothiazide respectively with regression coefficient greater than 0.99. The mean extraction recoveries are 96.95±5.61 and 100.55±4.82 for candesartan and hydrochlorothiazide respectively. The precision and accuracy values for all the studies were within the range of ≤15% and 85-115%. The performed stability studies indicate that the developed method is stable in plasma for 15 h at room temperature (bench top); 52 h (in injector); for 112 days at -70 ºC for long term stability; five successive freeze and thaw cycles. The developed method could be successfully employed for the determination of selected drugs in biological samples.
Subject(s)
Plasma , Hydrochlorothiazide/analysis , Mass Spectrometry/methods , Chromatography, Liquid/methods , Validation StudyABSTRACT
Objective To explore the influence of candesartan (an angiotensin II receptor 1 antagonist,AT1R) in radioresistance of human nasopharyngeal carcinoma CNE1 cells.Methods Cell growth of CNE1 with or without candesartan treatment was measured in vitro by MTT method;radiosensitivity of CNE1 with or without candesartan treatment was tested under normoxic or hypoxic conditions by clone formation assay.The expression of hypoxia-induced factor 1α(HIF-1α)in CNE1 cells was analysed by western blotting.Results Candesartan did not significantly inhibit the growth of CNE 1 cells in both normoxic and hypoxic conditions.Candesartan also did not influence the radiosensitivity of CNE1 cells in normoxic condition;however,it significantly increased the radiosensitivity of CNE1 cells in hypoxic condition.The expression of hypoxia-induced factor 1 α (HIF-1 α)in hypoxic CNE1 cells was significantly inhibited by candesartan treatment.Conclusion Candesartan does not significantly influence the proliferation of CNE1 cells in both normoxic and bypoxic conditions but significantly enhances the radiosensitivity of hypoxic CNE1 cells,in which the mechanisn may be involved in its inhibiting HIF1α expression in hypoxic CNE1 cells.
ABSTRACT
Objective To investigate the effects of irbesartan hydrochlorothiazide combined with candesartan cilexetil in the treatment of elderly patients with hypertension and its protective effect on cardiac function.Methods 180 elderly patients with hypertension were selected,and they were randomly divided into observation group and control group according to the digital table,90 cases in each group.The observation group was given irbesartan hydrochlorothiazide combined with candesartan treatment,the control group was given candesartan.The heart function improvement after treatment,clinical efficacy and patients in hospitalization,complications,critical events and new death of the two groups were compared.Results After treatment,the heart rate,EVDD,SBP and other indicators of the two groups declined,which of the observation group[(56.14 ± 6.15)mm,(112.12 ± 20.12)mmHg,(70.45 ± 8.69/min)]were lower than the control group[(60.12 ± 6.78) mm(119.45 ± 21.45) mmHg,(82.12 ± 9.12/ min)],there were significant differences between the two groups (t1 =4.124,P =0.000;t2 =2.364,P =0.019;t3 =8.788,P =0.000).The total effective rate of the observation group was 93.33％,which was higher than 74.44％ of the control group,there was significant difference between the two groups (x2 =11.879,P =0.000).Conclusion Irbesartan hydrochlorothiazide combined with candesartan in the treatment of elderly hypertensive patients can effectively improve the heart function of patients,has significant effect.
ABSTRACT
Minimal hepatic encephalopathy is more common than the acute syndrome. Losartan, the first angiotensin-II receptor blocker (ARB), and candesartan, another widely-used ARB, have protected against developing fibrogenesis, but there is no clear data about their curative antifibrotic effects. The current study was designed to examine their effects in an already-established model of hepatic fibrosis and also their effects on the associated motor dysfunction. Low-grade chronic liver failure (CLF) was induced in 3-month old Sprague-Dawley male rats using thioacetamide (TAA, 50 mg·kg−1·day−1) intraperitoneally for 2 weeks. The TAA-CLF rats were randomly divided into five groups (n=8) treated orally for 14 days (mg·kg−1·day−1) as follows: TAA (distilled water), losartan (5 and 10 mg/kg), and candesartan (0.1 and 0.3 mg/kg). Rats were tested for rotarod and open-field tests. Serum and hepatic biochemical markers, and hepatic histopathological changes were evaluated by H&E and Masson's staining. The TAA-CLF rats showed significant increases of hepatic malondialdehyde, hepatic expression of tumor necrosis factor-α (TNF-α), and serum ammonia, alanine aminotransferase, γ-glutamyl transferase, TNF-α, and malondialdehyde levels as well as significant decreases of hepatic and serum glutathione levels. All treatments significantly reversed these changes. The histopathological changes were moderate in losartan-5 and candesartan-0.1 groups and mild in losartan-10 and candesartan-0.3 groups. Only candesartan significantly improved TAA-induced motor dysfunction. In conclusion, therapeutic antifibrotic effects of losartan and candesartan in thioacetamide-induced hepatic fibrosis in rats are possibly through angiotensin-II receptor blocking, antioxidant, and anti-inflammatory activities. Improved motor dysfunction by candesartan could be attributed to better brain penetration and slower "off-rate" from angiotensin-II receptors. Clinical trials are recommended.
Subject(s)
Animals , Male , Angiotensin II Type 1 Receptor Blockers/therapeutic use , Benzimidazoles/therapeutic use , End Stage Liver Disease/complications , Losartan/therapeutic use , Motor Disorders/drug therapy , Tetrazoles/therapeutic use , Alanine Transaminase/blood , Ammonia/blood , Angiotensin II Type 1 Receptor Blockers/pharmacology , Benzimidazoles/pharmacology , Disease Models, Animal , End Stage Liver Disease/pathology , End Stage Liver Disease/physiopathology , Enzyme-Linked Immunosorbent Assay , gamma-Glutamyltransferase/blood , Glutathione/analysis , Liver Cirrhosis/complications , Liver Cirrhosis/pathology , Liver Cirrhosis/physiopathology , Liver/drug effects , Liver/pathology , Locomotion/physiology , Losartan/pharmacology , Malondialdehyde/analysis , Motor Disorders/etiology , Motor Disorders/physiopathology , Random Allocation , Rats, Sprague-Dawley , Reproducibility of Results , Reverse Transcriptase Polymerase Chain Reaction , Tetrazoles/pharmacology , Thioacetamide , Treatment Outcome , Tumor Necrosis Factor-alpha/bloodABSTRACT
BACKGROUND AND PURPOSE: Neurogenesis in the adult brain is important for memory and learning, and the alterations in neural stem cells (NSCs) may be an important aspect of Alzheimer's disease (AD) pathogenesis. The phosphatidylinositol 3-kinase (PI3K) pathway has been suggested to have an important role in neuronal cell survival and is highly involved in adult neurogenesis. Candesartan is an angiotensin II receptor antagonist used for the treatment of hypertension and several studies have reported that it also has some neuroprotective effects. We investigated whether candesartan could restore the amyloid-β(25–35) (Aβ₂₅₋₃₅) oligomer-inhibited proliferation of NSCs by focusing on the PI3K pathway. METHODS: To evaluate the effects of candesartan on the Aβ₂₅₋₃₅ oligomer-inhibited proliferation of NSCs, the NSCs were treated with several concentrations of candesartan and/or Aβ₂₅₋₃₅ oligomers, and MTT assay and trypan blue staining were performed. To evaluate the effect of candesartan on the Aβ-inhibited proliferation of NSCs, we performed a bromodeoxyuridine (BrdU) labeling assay. The levels of p85α PI3K, phosphorylated Akt (pAkt) (Ser473), phosphorylated glycogen sinthase kinase-3β (pGSK-3β) (Ser9), and heat shock transcription factor-1 (HSTF-1) were analyzed by Western blotting. RESULTS: The BrdU assays demonstrated that NSC proliferation decreased with Aβ25-35 oligomer treatment; however, a combined treatment with candesartan restored it. Western blotting displayed that candesartan treatment increased the expression levels of p85α PI3K, pAkt (Ser473), pGSK-3β (Ser9), and HSTF. The NSCs were pretreated with a PI3K inhibitor, LY294002; the effects of candesartan on the proliferation of NSCs inhibited by Aβ₂₅₋₃₅ oligomers were almost completely blocked. CONCLUSIONS: Together, these results suggest that candesartan restores the Aβ₂₅₋₃₅ oligomer-inhibited proliferation of NSCs by activating the PI3K pathway.
Subject(s)
Adult , Humans , Alzheimer Disease , Amyloid , Blotting, Western , Brain , Bromodeoxyuridine , Cell Survival , Glycogen , Hot Temperature , Hypertension , Learning , Memory , Neural Stem Cells , Neurogenesis , Neurons , Neuroprotective Agents , Phosphatidylinositol 3-Kinase , Phosphatidylinositols , Receptors, Angiotensin , Shock , Trypan BlueABSTRACT
Objective To investigate the comparison of clinical curative effect and inflammation factors between irbesartan hydrochlorothiazide and candesartan cilexetil in the treatment of patients with hypertension.Methods A total of 86 patients with hypertension in our hospital from June 2014 to October 2015 were collected and randomly divided into two groups, 43 cases in the control group were treated by candesartan cilexetil,43 cases in the experimental group were treated by irbesartan hydrochlorothiazide.The blood pressure, CRP, IL-6 and NO indexes were detected in the two groups and the clinical curative effect of the two groups was compared.Results The systolic pressure and diastolic pressure levels in the experimental group were significantly lower than the control group ( P <0.05 ); the serum CRP, IL -6 levels in experimental group were significantly lower than the control group, the NO level was significantly higher than the control group (P<0.05).Conclusion Irbesartan hydrochlorothiazide in the treatment of patients with hypertension has a better clinical curative effect, and higher security.
ABSTRACT
Background: Alzheimer’s disease (AD) is a major world-wide health problem. Much evidence points to a link between hypertension and AD. However, the exact effects of different antihypertensive drugs on AD need to be more assessed. The aim was to evaluate and compare the possible effects of perindopril, and candesartan on cognitive impairment, oxidative stress markers, and brain concentrations of amyloid beta-peptide (Aβ-P) in a rat model of induced dementia. Methods: Thirty-two adult male Wistar rats were distributed among 4 groups; (1) normal controls; (2) rats with dementia induced by intracerebroventricular administration of streptozotocin (ICV-STZ) and received no treatment; (3) ICV-STZ rats treated orally with perindopril for 3 weeks; and (4) ICV-STZ rats treated orally with candesartan for 3 weeks. The assessed parameters were spatial memory by Morris Water Maze test, brain tissue level of total antioxidant capacity (TAC), reduced glutathione (GSH), lipid peroxidation product (malondialdehyde [MDA]), and Aβ-P. Results: Both perindopril and candesartan attenuated STZ-induced memory impairment, caused a significant increase in TAC and GSH levels, reduced MDA levels, whereas only candesartan significantly reduced Aβ-P levels. Conclusions: This study reports that candesartan and perindopril can reverse the free radical induced damages and resultant memory defects, and may suggest candesartan as worthy drugs for prevention of Aβ-P deposition in this animal model of AD.
ABSTRACT
Objective To explore the treatment effect of candesartan capsule in the treatment of hypertension,and to provide evidence for clinical treatment of hypertension patients.Methods 133 patients with hypertension were randomly divided into the observation group and the control group.64 cases in the control group were given captopril,69 cases in observation group were given candesartan capsule on the basis of the control group.The treatment outcome after a period of treatment,the average treatment effect and adverse reaction of SBP and DBP were observed.Results The total effective rate of the observation group was 98.55 ％ (68/69),which was significantly higher than 90.62％ (58/64) of the control group (x2 =6.22,P ＜ 0.05).The ineffective rate of the observation group was 1.45％ (1/69),which was significantly lower than 9.38％ (6/64) of the control group (x2 =5.86,P ＜ 0.05).After treatment,the SBP and DBP of the observation group were (125.40 ± 5.94) mmHg and (85.24 ± 4.90) mmHg,which were significantly lower than (137.38 ± 6.71) mmHg and (89.68 ± 4.63) mmHg of the control group (t =5.94,6.02,all P ＜ 0.05).Cough,headache/vertigo,dose first hypotension and renal function injury of the two groups had no significant differences (x2 =1.38,1.22,1.06,1.53,all P ＞ 0.05).Conclusion Candesartan capsule in the treatment of hypertension has good antihypertensive effect,and has no adverse reaction of antihypertensive drugs.
ABSTRACT
Objective To compare the efficacy and safety of candesartan cilexetil and enalapril in the treatment of senile hypertension.Methods 100 patients with hypertension were randomly divided into the treatment group and control group according to digital table method.The treatment group were received candesartan cilexetil 4 ～ 8mg once daily for 8 weeks,and control group were received enalapril 10 ～ 20mg once daily for 8 weeks,and the efficacy and adverse reactions were watched.Results The SBP and DBP were (134.42 ± 6.39) mmHg and (82.00 ± 5.05) mmHg for candesartan cilexetil and (137.70 ± 5.27) mmHg and (81.76 ± 5.03) mmHg for enalapril after 8 weeks.A significant reduction of blood pressure was achieved in both groups than before treatment (tcan =35.85,30.88;tena =37.92,31.67,all P ＜ 0.01).After treatment pulse pressure was (56.06 ± 4.91)mmHg for candesartan cilexetil and (60.04 ± 4.40) mmHg for enalapril.Compared with before treatment,pulse pressure was significantly reduced in the treatment group (t =16.93,P ＜ 0.01) and was no significant difference in control group (t =6.34,P ＞ 0.05).The incidence of adverse reactions of patients with treatment group was obviously lower than that of the control group.Conclusion Candesartan cilexetil is effective and safe in senile hypertension patients,and it could be used as a first-line treatment.
ABSTRACT
Objective To investigate the curative effect of Candesartan on chronic systolic heart failure in Tibetan pla?teau. Methods A total of 526 patients with chronic systolic heart failure were divided into two groups randomly (Treatment group N=252;Control group N=274). Regular medicines, such as cardiac, diuretic and vasodilator drugs , are given to pa?tients in both groups according to their primary underlined diseases. Additionally, enalapril is added in control group, while candesartan is added in treatment group. Improvement of cardiac function, LVEF, LVEDD and blood pressure were compared between these two groups after 8 weeks. Results There was no significant difference in effective rate (i.e., 45.2%in treat?ment group and 44.9% in control group, respectively), efficiency rate (i.e. 54.8% in treatment group and 55.1% in control group, respectively) and inefficiency rate (i.e. 2.0%in treatment group and 2.2%in control group, respectively) between treat?ment and control groups . After treatment, LVEF in the two groups are all improved, while LVEDD and blood pressure both de?creased with statistical significance. However, the difference between the two groups is not significant. Conclusion No sta?tistical difference was found in curative effect on chronic systolic heart failure in Tibetan Plateau between two groups.
ABSTRACT
OBJECTIVE:To observe the clinical efficacy and safety of candesartan cilexetil combined with hydrochlorothiazide in the treatment of elderly degenerative valvular heart disease heart failure. METHODS:120 patients with elderly degenerative val-vular heart disease heart failure were randomly divided into observation group,control group 1 and control group 2. All patients were given conventional treatment,including limited activity,limited salt,limited water,additional use of digitalis and nitrates car-diac drugs,etc. On this basis,observation group was orally treated with Candesartan cilexetil dispersible tablet 4 mg,once a day+Hydrochlorothiazide tablet 25 mg,once a day,took 10 d then stopped 2 d;control group 1 was orally treated with Enalapril male-ate tablet 10 mg,once a day+Hydrochlorothiazide tablet;control group 2 was orally treated with Metoprolol tartrate tablets 50 mg, twice a day+Hydrochlorothiazide tablet. All efficacies of patients were evaluated after one year,and the BNP,LVEF,LVEDD and SV before and after treatment,medication compliance and incidence of adverse reactions were observed. RESULTS:There was no significant difference in the total effective rate in each group(P>0.05). After treatment,the BNP and LVEDD were significantly lower than before,LVEF and SV were significantly higher than before,with significant difference(P0.05). CONCLUSIONS:Based on the conventional treatment,can-desartan cilexetil combined with hydrochlorothiazide has good clinical efficacy and safety in the treatment of elderly degenerative valvular heart disease heart failure.
ABSTRACT
Objective:To prepare and optimize candesartan cilexetil tablets,and study the stability preliminarily. Methods:The formula was optimized by Box-Behnken experiment design,the ratio of lactose to pregelatinized starch( X1 ),the amount of disintegrant ( X2 ,%)and the amount of lubricant( X3 ,%)were selected as the independent variables,and weight difference( Y1 ,%),friability ( Y2 ,%),disintegration time( Y3 ,%)and candesartan cilexetil dissolution( Y4 ,%)were the dependent variables. The release rate of candesartan cilexetil tablets and the reference tablets were compared by similarity factor( f2 value). Preliminary stability was studied by high-temperature test,high-humidity test and illumination test. Results:The optimal formula of the tablets was as follows:the ratio of lactose to pregelatinized starch was 7:1,the amount of disintegrant was 5. 5%,and the amount of lubricant was 0. 5%. The f2 for the candesartan cilexetil tablets and the reference tablets in different dissolution meda was 60. 62,73. 34,66. 95 and 68. 60,respec-tively. Conclusion:The formula design is reasonable,the preparation process is feasible and the quality can be controlled.
ABSTRACT
OBJECTIVE:To observe the clinical efficacy and safety of candesartan combined with amlodipine besylate in the treatment of elderly hypertension. METHODS:Totally 156 elderly patients with hypertension were randomly divided into control group and observation group. Patients in control group were orally given Amlodipine besylate tablets 5 mg in the morning,once a day. Patients in observation group were orally given Candesartan tablets 8 mg based on the treatment of control group,once a day. The course of both was 8 weeks. The clinical data was observed,including clinical efficacy,systolic blood pressure(SBP)and dia-stolic blood pressure(DBP)before and after treatment,fasting blood glucose(FPG),insulin resistance index(HOMA-IR),24 h urinary albumin total(mAlb),serum creatinine(SCr)and the incidence of adverse reactions. RESULTS:The total effective rate in observation group was significantly higher than control group;the HOMA-IR,mAlb and SCr in observation group were significant-ly lower than control group,with significant difference(P0.05). There were no obvious adverse reactions during treatment. CONCLUSIONS:Candesartan combined with amlodipine besylate has better efficacy than only amlodipine besylate in the treatment of elderly hypertension,with similar safety.
ABSTRACT
OBJECTIVE:To observe therapeutic efficacy of candesartan combined with Sulodexide soft capsules in the treatment of persistent proteinuria of diabetic nephropathy. METHODS:180 patients with persistent proteinuria of diabetic ne-phropathy were randomly divided into control group and trial group,with 90 cases in each group. Control group was given can-desartan,8 mg/time,once a day;trial group was additionally given Sulodexide soft capsules on the basis of control group,250 LSU/time,twice a day. The indexes levels of both groups were compared before and after treatment,including systolic blood pressure(SBP),diastolic blood pressure(DBP),serum creatinine(Scr),blood urea nitrogen(BUN),urinary albumin excre-tion rate (UAER),24 hour urinary albumin (24hU-Alb) and urinary 2-microglobulin (β2-MG),α1 microglobulin (α1-MG), urine N-acetyl-β-D glucoside enzyme(NAG)and serum cystatin C(Cys-C). RESULTS:After treatment,there was no statisti-cal significance in the levels of SBP,DBP,Scr,BUN and UAER between 2 groups(P>0.05);24hU-Alb level of observation group was significantly betRter than that of control group,with statistical significance (P<0.05);after treatment,β2-MG,α1-MG,NAG and Cys-C of 2 groups were all improved significantly,and the trial group was more significant then the control group,with statistical significance (P<0.05). CONCLUSIONS:Candesartan combined with Sulodexide soft capsules in the treatment of persistent proteinuria of diabetic nephropathy can effectively improve renal function and reduce urinary microalbu-min.
ABSTRACT
Se presentan en este artículo los resultados del desarrollo y validación de una metodología analítica para la cuantificación de Candesartan Cilexetil en tabletas recubiertas para uso humano. El procedimiento consiste en una separación por cromatografía líquida de alta eficiencia en fase inversa y detector de arreglo de diodos, empleando como fase móvil una mezcla compuesta por un buffer de acetatos de pH 4,0 y acetonitrilo (30:70), una columna C18 a temperatura ambiente y detección a una longitud de onda de 306 nm. Se comprobó la selectividad, la precisión y la exactitud de la metodología. Estas características junto con su sencillez hacen el método adecuado y conveniente para el objetivo propuesto. La robustez de la metodología se investigó frente a la variación de algunas de las condiciones cromatográficas bajo las cuales se llevó a cabo la validación.
A reverse phase high performance liquid chromatographic method was developed for the quantitative assay of candesartan ciletexil in coated tablets for human use as hypotensor agent. The method was then validated for its quantitative determination assay in tablets as pharmaceutical specialties. A C18 column stabilized at room temperature was used and the detection was performed at 306 nm. A mixture of acetonitrile, acetate buffer pH 4,0 (30:70) was used as the mobile phase. The method is selective, linear and shows a good repeatability. The robustness was also studied. These properties besides the simplicity make the methodology convenient for the objective proposed.