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The objective was to prepare an Enalapril Maleate (EnM)-loaded floating microsphere with minimum particle size,maximum drug loading, and drug entrapment efficiency. Formulations were prepared by varying drug-to-polymerratio (A), solvent ratio (B), and stirring time (C). The solvent evaporation method was used to prepare the microsphere.“Box–Behnken’s design” (3 factors × 3 levels) was utilized for optimization. The independent variables were polymerto-drug ratio (A), solvent ratio (B), and stirring time (C), while particle size (R1), drug loading (R2), and entrapmentefficiency (R3) were considered as dependent variables. EnM-loaded alcohol microsphere (Formulation-A) wasprepared and optimized. Both Formulation-A and EnM-loaded acetonitrile microspheres (Formulation-B) weresubjected to morphological, micrometric, characterization, and in vitro release studies. The particle size, drug loading,and entrapment efficiency of Formulation-A and Formulation-B were 143 ± 27.75 µm, 37.31% ± 5.73%, and 76.89%± 4.97%, and 158.13 ± 25.1 µm, 40.13% ± 6.12%, and 99.19% ± 1.14%, respectively. The cumulative drug releasesof Formulation-A and Formulation-B were 90.52% ± 4.11% and 86.23% ± 3.81%, respectively. Both formulationsfollowed the Higuchi model of drug release. EnM-floating microsphere was effectively prepared and both formulationsshowed excellent continuous release properties for more than 12 hours.
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Abstract Background and objectives: Angioedema is a potentially fatal condition that may occur at any time in the perioperative period. It may result from histamine release, hypersensitivity reaction to drugs, or be triggered by bradykinin, in non-allergic reactions of hereditary or acquired etiology. The aim of this report is to report a case of angioedema in the early postoperative period in a patient on antihypertensive medication involving angiotensin-converting enzyme inhibitors. Case report: A 67-year-old male, Afro-descendant, hypertensive, and taken enalapril maleate underwent orthopedic shoulder surgery under general anesthesia combined with brachial plexus block. The procedure lasted 3 hours uneventfully. After discharge from the post-anesthesia care unit, the patient presented with angioedema and severe airway impairment. Tracheal intubation was attempted but it was impossible due to edema affecting the lips, tongue, and oropharyngeal region Emergency cricothyroidotomy was performed. The onset of angioedema had no causal relationship with the administration of any medication; there were no cutaneous manifestations and also not response to therapy for hypersensitivity reaction to drugs, such as antihistamines, corticoid, and adrenaline. It was considered to be mediated by bradykinin, as the patient had already had two similar episodes and was on regular medication (enalapril). The evolution was satisfactory. Conclusion: Angioedema is a potentially fatal condition when it affects the airway, and should be recognized by anesthesiologists and physicians working in the emergency departments.
Resumo Justificativa e objetivos: O angioedema é uma condição potencialmente fatal que pode surgir em qualquer momento no perioperatório. Pode decorrer da liberação de histamina, em uma reação de hipersensibilidade a drogas ou ser desencadeado pela bradicinina, em reações não alérgicas, de etiologia hereditária ou adquirida. O objetivo desse relato é descrever um caso de angioedema, no pós-operatório imediato, em um paciente em uso de medicação anti-hipertensiva da classe dos inibidores da enzima conversora da angiotensina. Relato de caso: Paciente de 67 anos, masculino, negro, hipertenso e em uso do maleato de enalapril, foi submetido a cirurgia ortopédica de ombro sob anestesia geral associada a bloqueio do plexo braquial. O procedimento durou 3 horas, sem intercorrências. Após a alta da sala de recuperação pós-anestésica, apresentou angioedema com grave comprometimento das vias aéreas. Tentou-se fazer intubação traqueal, mas foi impossível devido ao edema que acometia os lábios, a língua e região orofaringeana. Fez-se a cricotireoidostomia de emergência. O aparecimento do angioedema não apresentou relação causal com a administração de qualquer medicação, não houve manifestações cutâneas e também não respondeu à terapêutica para reação de hipersensibilidade a drogas, como anti-histamínicos, corticoide e adrenalina. Foi considerado como mediado pela bradicinina, pois o paciente já havia apresentado dois episódios semelhantes e estava em uso regular de medicação (enalapril). A evolução foi satisfatória. Conclusão: O angioedema é uma condição potencialmente fatal quando atinge as vias aéreas e deve ser de conhecimento do anestesiologista e dos médicos que trabalham nos setores de emergência.
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Humans , Male , Aged , Postoperative Complications/chemically induced , Angiotensin-Converting Enzyme Inhibitors/adverse effects , Angioedema/chemically inducedABSTRACT
Objective To explore the effects of Wenxin granule combined with conventional therapy on cardiac function,ventricular remodeling and local inflammatory response in patients with paroxysmal atrial fibrillation (PAF).Methods From February 2016 to February 2017,116 patients with PAF in the Integrated Traditional Chinese and Western Medicine Hospital of Taizhou were randomly divided into control group(55 cases) and combined group(61 cases) according to the digital table.The control group was treated with routine amiodarone hydrochloride tablets and enalapril maleate tablets,and the combined group was treated with Wenxin granule on the basis of the control group.The clinical efficacy of the two groups was compared,and the cardiac function,the level of inflammatory reaction and the index of ventricular remodeling before and after treatment were compared and analyzed in the two groups.The adverse reactions were observed and analyzed in the two groups.Results The total effective rate in the combined group was 93.44％,which was significantly higher than 76.36％ in the control group (x2 =6.745,P ＜ 0.05).After treatment,the left atrial diameter,the FS and CI levels in the combined group were significantly higher than those in the control group and before treatment (all P ＜ 0.05).The level of Pd in the combined group after treatment was (47.16 ± 0.80) ms,,which was significantly lower than that in the control group [(50.25 ± 0.75) ms] and that before treatment (t =21.395,48.318,all P ＜ 0.05).The levels of hs-CRP and BNP in the combined group were (7.12 ± 2.71) mg/L,(118.43 ± 11.16) ng/L,respectively,which were significantly lower than those in the control group [(11.21 ± 2.89) mg/L,(123.6 ± 11.27) ng/L] and before treatment (t =7.865,2.504,8.585,8.752,all P ＜0.05).After treatment,the LVEF level in the combined group was higher than that in the control group and before treatment (t =4.785,10.573,all P ＜ 0.05).The LVEDD and LVSV levels in the combined group were significantly lower than those in the control group and before treatment (t =9.089,2.313,10.890,4.299,all P ＜ 0.05).The total incidence rate of adverse reactions in the combined group was 6.56％,which was slightly lower than 7.28％ in the control group,but there was no statistically significant difference between the two groups(x2 =0.023,P＞0.05).Conclusion Wenxin granule combined with routine treatment in the treatment of PAF can significantly improve the clinical efficacy,improve the cardiac function obviously,delaye the ventricular remodeling,decrease the level of local inflammatory reaction significantly and the safety is high.
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OBJECTIVE: To investigate the effects of Enalapril maleate folic acid tablets on carotid atherosclerosis in H type hypertension patients with type 2 diabetes mellitus (T2DM) and its potential mechanism.METHODS: In prospective control study, 182 H type hypertension patients with T2DM were selected from Chongqing People's Hospital during Jan. 2014-Jan. 2016, and then randomly divided into observation group and control group, with 91 cases in each group. All patients received basic or hypoglycemic treatment of premixed insulin; observation group was additionally given Enalapril maleate folic acid tablets (containing enalapril maleate 10 mg, folic acid 0. 8 mg in each tablet) orally, one tablet, qd; control group was additionally given Enalapril maleate tablets (containing enalapril maleate 10 mg in each tablet) orally, one tablet, qd. Treatment course lasted for 12 months. The levels of blood pressure, plasma homocysteine (Hcy), fasting blood glucose (FBG), C-reactive protein (CRP) and carotid plaque score were detected in 2 groups before treatment, 12 months after treatment. RESULTS: Compared to before treatment, SBP and DBP of 2 groups were decreased significantly in 2 groups after 12 months of treatment (P<0. 05); there was no statistical significance between 2 groups (P>0. 05). The levels of plasma Hcy, FBG and CRP, carotid intima-media thickness and carotid plaque integral in observation group were significantly lower than control group (P<0. 05). CONCLUSIONS: Enalapril maleate folic acid tablets can relieve inflammation by reducing plasma Hcy, FBG and CRP so as to treat carotid atherosclerosis in H type hypertension patients with T2DM.
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Objective To investigate the therapeutic effect of Enalapril Maleate and Folic Acid Tablets in the treatment of type H hypertension complicated with coronary heart disease.MethodsA total of 80 patients with type H hypertension complicated with coronary heart disease admitted in our hospital from January 2014 to January 2016 were selected.They were randomly divided into control group and observation group.The control group was treated with enalapril maleate, while the observation group was treated with Enalapril Maleate and Folic Acid Tablets.The total effective rate of two groups of patients were analyzed and compared.ResultsAfter 6 months of treatment, the total effective rate of the observation group was significantly higher than that of the control group, the total effective rate of the observation group was 95.00%, and the total effective rate of the control group was 77.50%(P<0.05), the difference was statistically significant.ConclusionThe effect of Enalapril Maleate and Folic Acid Tablets in the treatment of type H hypertension complicated with coronary heart disease is obvious, and it can improve the total effective rate of the treatment.
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Objective To investigate the influence of Enalapril Maleate Tablets on serum micro inflammatory indexes and nutritional indexes in maintenance hemodialysis patients. Methods A total of 90 patients with chronic renal failure treated by maintenance hemodialysis in our hospital from April 2015 to October 2016 were randomly divided into control group and experimental group, with 45casesin each group. The control group was treated with atorvastatin,andthe observation group was treated with atorvastatin combined with enalaprilmaleate tablets. After treatment,the levels of the inflammatory markers of high sensitive C reactive protein (HS-CRP), tumor necrosis factor alpha (TNF-alpha), interleukin-8 (IL-8), interleukin 6 (IL-6) and the nutritional index of plasma albumin(ALB), prealbumin(PA) in two groups were analyzed. Results After treatment, the levels ofHS-CRP, TNF-alpha in the observation group were lower than those in control group, the difference was statistically significant (P<0.05); The levels of IL-6, IL-8 in the observation group were significantly lower than the control group, the difference was statistically significant (P<0.05). The indexes of ALB and PA in the observation group after treatment were higher than those in the control group, the difference was statistically significant (P<0.05). Conclusion For the patients with maintenance hemodialysis treatment, the clinical effect of using conventional atorvastatin treatment combined with Enalapril Maleate Tablets is good, high safety, with further clinical promotion and application significance.
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Objective To investigate and analyze the effect of serum micro inflammatory and nutritional indexes of psychological intervention combined with enalapril maleate tablets on the treatment of the patients with maintenance hemodialysis. Methods 100 patients with chronic renal failure in Jiande the first people's hospital from February 2015 to August 2016 were selected as the subjects, and randomly divided into the control group and the experimental group. The control group and the experimental group were given enalapril maleate tablets, at the same time, the experimental group were received psychological intervention. The changes of serum micro inflammation indexes and nutritional indexes in the the two groups were compared and analyzed. Results The HsCRP, TNF alpha levels in the experimental group decreased significantly than those in the control group, the differences had statistical significant (P<0.05). The levels of prealbumin and plasma albumin in the experimental group were significantly higher than those in the control group (P<0.05). After treatment, the SAS score in the experimental group was (42.3±5.2) points, and the SDS score was (40.1±5.9) points. The SAS score in the control group was (60.9±9.2) points, and the SDS score was (59.1±7.4) points. The scores of depression and anxiety in the experimental group were significantly lower than those in the control group (P<0.05). Conclusion Psychological intervention combined with enalapril maleate tablets used in maintenance hemodialysis patients, which can significantly improve patients' serum inflammation index, restore the nutritional status of patients, eliminate the negative emotion of patients, with further clinical promotion and application significance.
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Objective To study the clinical effect of enalapril maleate and folic acid tablets in the treatment of H type hypertension, and to observe the blood homocysteine(Hcy), to provide the basis for clinical diagnosis and treatment.Methods 126 patients with H type hypertension were selected.They were divided into study group and control group according to the random number table method,63 cases in each group.The control group was given enalapril maleate, the study group was given enalapril maleate and folic acid tablets.The clinical efficacy of the two groups was compared.The systolic blood pressure, diastolic blood pressure and Hcy level before and after treatment in two groups were observed.Results The total effective rate of the study group was 90.5%(57/63),which of the control group was 74.6%(47/63),the difference was statistically significant(x2=15.371,P0.05).The systolic pressure after treatment of the two groups were (129.3±5.7)mmHg and (137.9±4.9)mmHg, the diastolic blood pressure were (81.5±3.6)mmHg and (89.6±5.1)mmHg, the differences were statistically significant compared with before treatment(t=8.969,7.851,7.343,6.987,all P0.05), after treatment Hcy levels of the two groups were (8.93±0.63)μmol/L and (15.35±0.57)μmol/L respectively, the differences were statistically significant compared with before treatment(t=8.097,8.031,all P<0.05),the difference between the two groups was statistically significant(t=7.573,P<0.05).Conclusion Enalapril maleate and folic acid tablets in the treatment of H type hypertension has good clinical effect, can significantly lower blood pressure, improve Hcy level.
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OBJECTIVE:To study the in vitro dissolution of Enalapril maleate and folic acid tablet. METHODS:HPLC was performed on the column of Agilent HC-C18 with mobile phase A of acetonitrle-phosphate buffer solution(70:30,V/V) and mobile phase B of acetonitrle-phosphate buffer solution(5:95,V/V)(gradient elution) at a flow rate of 1.0 ml/min,detection wavelength was 215 nm,column temperature was 50 ℃,and volume injection was 80 μl. Media were water,hydrochloric acid solution(pH 1.2),phosphate buffer solution(pH 5.0)and phosphate buffer solution(pH 6.8),medium volume was 900 ml and rotation speed was 50 r/min. The dissolution behavior of enalapril maleate in Enalapril maleate and folic acid tablet in 4 media were studied and compared with the dissolution behavior in vitro in original preparation of Enalapril maleate tablet,meanwhile,the dissolution behar-ior of folic acid in Enalapril maleate and folic acid tablet in phosphate buffer solution(pH 5.0)were studied and compared with dis-solution data of folic acid preparation in Japanese Orange Book to evaluate the intrinsic quality. RESULTS:The linear range was 0.561-14.03μg/ml for enalapril maleate(r=0.999 9)and 0.043-1.085μg/ml for folic acid(r=0.999 9),respectively;RSDs of pre-cision and stability tests were lower than 2.0%;recoveries of enalapril maleate in 4 media were 100.63%-102.33%(RSD=0.72%, n=9),99.27%-100.44%(RSD=0.41%,n=9),99.71%-100.29%(RSD=0.15%,n=9)and 96.74%-99.19%(RSD=0.79%,n=9),respectively. Recoveries of folic acid were 100.18%-101.63%(RSD=0.48%,n=9),97.73%-101.81%(RSD=1.32%,n=9),99.60%-102.24%(RSD=0.74%,n=9)and 100.00%-102.76%(RSD=0.90%,n=9),respectively. In 15 min,the dissolution of enalapril maleate of 2 preparations in 4 dissolution media were more than 85%;dissolution speed of folic acid in Enalapril male-ate and folic acid tablet was faster than that in folic acid preparation in phosphate buffer solution(pH 5.0). CONCLUSIONS:The method is suitable to determine the dissolution of Enalapril maleate and folic acid tablet;the in vitro dissolution curve of enalapril maleate in Enalapril maleate and folic acid tablet is similar to Renitec,and the in vitro dissolution of folic acid is better than folic acid preparation.
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Objective:To establish an HPLC method for the determination of related substances in enalapril maleate dispersible tablets.Methods:AKromasil100-SC8(250mm×4.6mm,5μm)columnwasused. ThemobilephaseAwas0.01mol·L-1potassi-um dihydrogen phosphate (adjusting pH to 2. 2 with phosphoric acid) and mobile phase B was acetonitrile with gradient elution,and the flow rate was 1. 0 ml· min-1 . The detection wavelength was 215nm,the column temperature was 40℃,and the injection volume was 20 μl. Results:The linear range of enalaprilat,enalapril maleate and eanlapril diketopiperazine was 14.64-43.92 μg·ml-1(r =0. 999 8), 9. 29-27. 87 μg·ml-1(r=0. 999 1)and 10. 80-32. 40 μg·ml-1(r=0. 999 5), respectively. Enalaprilat was not detec-ted out and enalapril diketone was 0. 2% using the method described in Chinese pharmacopeia, and the content of enalaprilat was 0. 1% and that of enalapril diketone was 0. 2% using the gradient elution. The related substances and enalapril maleate could be sepa-rated well. Conclusion:The method is sensitive, accurate and highly specific in the quality evaluation and control.
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In the present work, oral dispersible tablets of Enalapril maleate were prepared using three different superdisintegrants and a co-processed superdisintegrant consisting of crospovidone and sodium starch glycolate in the ratio 1:1. Oral dispersible tablets of Enalapril maleate were prepared by employing direct compression technique using the above superdisintegrants, and evaluated for precompression as well as post-compression parameters, such as determination of weight variation, thickness, hardness, friability, wetting time, disintegration time, drug content, water absorption ratio, in vitro dispersion time, and in vitro drug release study. Formulation F-VII. F-VIII and F-IX were subjected to stability Studies as per ICH guidelines at temperatures and humidity of 25±5ºC/60±5%RH; 30±5ºC/65±5%RH and 40±5ºC/75±5%RH. Tablets didn’t reveal any appreciable changes in respect to hardness, disintegration time, drug content and dissolution profiles. From the results, it could be concluded that the formulation(F-VII) made with coprocessed super disintegrant (1:1) at a concentration of 5% w/w revealing a disintegrating time of 13.2 sec, and 97.84 % cumulative drug release emerged as the best formulation.
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A simple, precise and rapid reverse-phase HPLC method has been developed and subsequently validated for the simultaneous estimation of Amlodipine besylate and Enalapril maleate from their combination drug product. The proposed RP-HPLC method utilizes a Phenomenex C18, 5 μm, 250 mm × 4.6 mm i.d. column, at ambient temperature, optimum mobile phase consisted of Methanol: Acetonitrile : Water (40:50:10, v/v/v), effluent flow rate monitored at 1.0 mL min-1, and detection using PDA detector. The described method was linear over the range of 0.5-6.0 g/ml and 0.5-8.0 g/ml for Enalapril maleate and Amlodipine besylate, respectively. The mean recovery was found to be 100.06 ± 0.49 % and 99.98 ± 0.63 % for Enalapril maleate and Amlodipine besylate, respectively. The intermediate precision data obtained under different experimental setup, the calculated value of coefficient of variation (CV, %) was found to be less than critical value. The proposed method can be useful in the quality control of bulk manufacturing and pharmaceutical dosage forms.
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Objective To explore the clinical effects of diabetic nephropathy treated with enalapril and Yinxingdamo injection. Methods 80 patients were randomly recruited into a control group and a treatment group. The control group was treated with enalapril, and the treatment group was treated with Yinxingdamo injection on the basis of the control group. Results Comparing with the control group, the treatment group could be seen a obvious decrease of 24h UAE, BUN and Cr(P<0.01). Conclusion The therapeutic effects of combined using enalapril and Yinxingdamo injection is better than only using enalapril in treating diabetic nephropathy.
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Objetivo: Avaliar os efeitos do maleato de enalapril na regressão da hipertrofia ventricular esquerda (EVE) associada a hipertensão arterial. Casuística e Métodos: Quinze pacientes masculinos, idades entre 45 e 65 anos, média 56, com hipertensão arterial essencial leve ou moderada (pressão arterial diastólica, PAD, entre 90 e 114 mmHg) e HVE ao exame ecocardiográfico. A administração de enalapril iniciou-se com dose diária única de 20 mg, aumentada até o máximo de 40 mg, se a PAD permanecesse acima de 90 mmHg e não houvessem reações adversas...
Purpose: To evaluate the effects of enalapril maleate on the regression of left ventricular hypertrophy (LVH) associated to hypertension. Patients and Methods: Fifteen male, age between 45 and 65 years (mean age = 56 y) with diagnosis of mild-to-moderate essential hypertension (> diastolic blood pressure [DBP] < between 90 and 114 mmHg) and LHV at the echocardiogram. The administration of enalapril maleate was initiated with a 20 mg daily dosage and titrated up to a maximum of 40 mg daily, whenever DBP was maintained above 90 mmHg and no adverse experience occurred...