Enalapril Maleate Research Articles

Development and Validation of Analytical Methods for Simultaneous Estimation of Lercanidipine Hydrochloride and Enalapril Maleate

The fixed dose of lercanidipine hydrochloride(LH) and enalapril maleate (EM) is used to provide more effective control of hypertension. The research work was aimed at the development and validation of simple and sensitive analytical methods for their quantification from tablets. The simultaneous equation, first-order derivative, and multivariate spectrophotometric methods were developed for the simultaneous estimation of LH and EM in tablets. The simultaneous equation method involves a determination of LH and EM at 236 nm and 207 nm, respectively. First order derivative UV spectrophotometry method involves using a zero crossing point of LH at 330 nm and EM at 219 nm. Both methods were validated as per ICH Q2 (R2) guidelines and found to be accurate and precise as they exhibited <2% relative standard deviation. The limit of detection (LOD) and limit of quantitation (LOQ) for LH were found to be 0.26 μg/ml and 0.78 μg/ml respectively whereas LOD and LOQ for EM were found to be 0.41 μg/ml and 1.24 μg/ml respectively for simultaneous equation method. The LOD and LOQ for LH were found to be 0.39 μg/ml and 1.19 μg/ml respectively whereas LOD and LOQ for EM were found to be 0.31 μg/ml and 0.97μg/ml respectively for the first-order derivative method. Three Chemometric methods namely classical least square (CLS), principal component regression (PCR), and partial least square (PLS) were studied for the simultaneous determination of LH and EM in tablets using spectrophotometry. A set of 25 standard mixtures containing both drugs were prepared in the range of 5–25 μg/ml for both drugs. The analytical figure of merit (FOM) was determined for all three chemometric methods. The LOD values for LH were found to be 0.97, 0.93, and 0.94 μg/ml and 0.90,0.88, and 0.89 μg/ml for EM using CLS, PCR, and PLS modeling techniques. The proposed methods were user-friendly, rapid, and sensitive enough for the determination of LH and EM.

Substantiation of the composition and technology for obtaining combined sustained-release tablets for the treatment of hypertension

Aim. To develop the composition and technology for obtaining the combined drug of indapamide with enalapril of the prolonged action. Materials and methods. Indapamide and enalapril maleate substances as active components, and polyvinylpyrrolidone, calcium stearate, lactose monohydrate, hydroxypropyl methylcellulose as excipients were used. The pharmaco-technological studies were conducted according to the methods of the State Pharmacopoeia of Ukraine (SPhU). Results and discussion. The pharmaco-technological properties of tablet mixtures and the quality of finished tablets were compared using direct pressing and preliminary wet granulation. Conclusions. It has been found that the use of the method of pre-granulation of the tablet mixture allows obtaining a finished product that fully meets the requirements of the SPhU.

Enalapril maleate as a green accelerator for zinc phosphating coating on low-carbon steel

In this study, enalapril maleate (EM), a green ingredient of an antihypertensive drug, was selected as an accelerator for phosphate coating promoting on low-carbon steel. The scanning electron microscope (SEM), X-ray diffraction (XRD), 3D morphologies, coating weight, coating thickness and free acidity (FA) as well as total acidity (TA) were characterized to analyze the coating performance. Copper sulfate titration, potentiodynamic polarization (PDP) and electrochemical impedance spectroscopy (EIS) were performed to evaluate corrosion resistance of phosphate coatings. The DFT computations were applied to explore the phosphating promoting mechanism. The results show that the EM optimal concentration is 1.6 g/L which lowers the operating temperature (form 80 ℃ to 40 ℃), generates the smoothest (Ra = 2.85 μm), the heaviest (28.35 g/cm2) and the thinnest (21.6 μm) coating, and reduces the corrosion rate from 1.099 mpy of blank to 0.0246 mpy. The density functional theory (DFT) results confirm that EM adsorbs on low-carbon steel by electrophilic sites (N10) as well as nucleophilic sites (C10), forms nucleated particles preferentially and accelerates the growth of crystals. Therefore, EM is a green organic compound with high phosphating promotion efficiency which has potential application prospects in industrial phosphating.

Preventing cardiotoxicity in patients with breast cancer and lymphoma: protocol for a multicentre randomised controlled trial (PROACT)

IntroductionAnthracyclines are included in chemotherapy regimens to treat several different types of cancer and are extremely effective. However, it is recognised that a significant side effect is cardiotoxicity; anthracyclines can...

Fused Deposition Modeling (FDM) 3D Printing of the Thermo-Sensitive Peptidomimetic Drug Enalapril Maleate.

Fused deposition modeling (FDM) 3D printing was used to produce 3D printed tablets with the thermo-sensitive model peptidomimetic drug enalapril maleate (EM). Two different formulations were prepared to investigate the degradation of enalapril maleate during the FDM 3D printing process. Soluplus® and Eudragit® E PO were chosen as polymers. After hot-melt extrusion (HME) and FDM 3D printing, both formulations were characterised regarding their solid-state properties using DSC and XRD. The degradation of the drug was analysed by determination of the content in the extrudates and 3D printed tablets, and dissolution was assessed. Various approaches have been attempted to prevent degradation of enalapril maleate, including utilization of a larger nozzle diameter and higher printing speeds to reduce heat exposition. None of these approaches were successful in preventing drug degradation. However, significant differences in the amount of degradation between the two formulations with different polymers could be observed. Thus, the FDM 3D printing process was not feasible without any degradation for the thermo-sensitive drug enalapril maleate. A maximum of 85.55 ± 1.48% enalapril was recovered in Eudragit® E PO tablets printed with a 0.4 mm nozzle at a temperature of 180 °C and with a speed of 30 mm/s.

Hot-Melt Extrusion of the Thermo-Sensitive Peptidomimetic Drug Enalapril Maleate.

The aim of this research was the production of extrudates for the treatment of hypertension and heart failure and the investigation of the degradation of the peptidomimetic drug enalapril maleate (EM) during hot-melt extrusion (HME). A fast HPLC method was developed to quantify enalapril maleate and possible degradation products. Screening experiments revealed that the diketopiperazine derivative (Impurity D) was the main degradation product. Hot-melt extrusion of enalapril maleate with the polymer Soluplus® enabled extrusion at 100 °C, whereas a formulation with the polymer Eudragit® E PO could be extruded at only 70 °C. Extrusion at 70 °C prevented thermal degradation. A stabilizing molecular interaction between enalapril maleate and Eudragit® E PO was identified via FT-IR spectroscopy. Dissolution studies were carried out to study the influence of the formulation on the dissolution behavior of enalapril maleate. These promising results can be transferred to other thermo-sensitive and peptidomimetic drugs to produce extrudates which can be used, for instance, as feedstock material for the production of patient-specific dosage forms via Fused Deposition Modeling (FDM) 3D printing.

Дослідження профілів розчинення таблеток Амлодипіну з еналаприлом

забезпечення якості при виробництві лікарських препаратів є всеохоплюючою концепцією. Якість лікарських засобів має бути гарантована на всіх стадіях виготовлення – від розроблення, дослідження й виробництва до впровадження та оптимального застосування. Все це закладено у вимоги низки належних практик: GMP, GLP, GCP, GDP, GPP, GSP. Велике значення при розробці твердих лікарських форм надається вивченню швидкості вивільнення діючих речовин та в середовищах з різним показником кислотності. Для оцінки якості розроблених комбінованих таблеток Амлодипіну з еналаприлом, прогнозування швидкості вивільнення діючих речовин з них, а відповідно прояву терапевтичної дії на організм. Метою роботи було вивчити профілі розчинення таблеток Амлодипіну з еналаприлом у порівнянні з оригінальними монопрепаратами. Обʼєктами дослідження були розроблений засіб Амлодипіну з еналаприлом, таблетки 5 мг/5 мг та відповідні оригінальні монопрепарати: Норваск (Pfizer Manufacturing Deutschland GmbH), таблетки 5 мг (амлодипін) та Берліприл (BERLIN-CHEMIE), таблетки 5 мг (еналаприл). Дослідження проводилися згідно Фармакопейних вимог з використанням приладу для розчинення USP I (лопаті). Середовища розчинення – 900 мл буферних розчинів рН 1,2, рН 4,5 і рН 6,8. Аналіз здійснювали методом високоефективної рідинної хроматографії. В якості рухомої фази застосовували розчин калію дигідрофосфату у воді (рН 4,0). Детектування проводили за довжини хвилі 215 нм. Було здійснено порівняльні дослідження кінетики розчинення засобу Амлодипін з еналаприлом, таблетки 5 мг/5 мг з кінетикою розчинення оригінальних монопрепаратів Норваск (Pfizer Manufacturing Deutschland GmbH), таблетки 5 мг та Берліприл (BERLIN-CHEMIE), таблетки 5 мг. Встановлено, що через 15 хв. в середовищі рН 6,8 еналаприлу малеат вивільняється з розроблених комбінованих таблеток лише на 83,6 %, а впродовж 30 хв. спостерігалося повне вивільнення обох активних фармацевтичних інгредієнтів у всіх досліджуваних середовищах. Виявлено високе значення фактора подібності профілю розчинення розроблюваного препарату Амлодіпин з еналаприлом, таблетки 5 мг/5 мг до оригінальних монопрепаратів: рН 1,2: амлодипін – 92,3, еналаприл – 86,5; рН 4,5: амлодипін – 94,8, еналаприл – 86,3; рН 6,8: амлодипін – 96,2, еналаприл – 80,2. Було визначено, що біофармацевтичні фактори, до яких належать фізико-хімічні властивості амлодипіну та еналаприлу, склад допоміжних речовин, особливості технологічного процесу, мають вплив на кінетику розчинення досліджуваного препарату на основі амлодипіну та еналаприлу. Отже, запропоновані комбіновані таблетки Амлодипіну з еналаприлом аналогічні відповідним референтним монопрепаратам і можуть бути використані в експериментальній і практичній медицині.

Standardized Analytical Procedure for Routine Testing of Amlodipine Besilate and Enalapril Maleate Simultaneously in In-vitro Samples

>This study develops a standardized methodology for routine analysis of in-vitro samples of amlodipine besilate and enalapril maleate concurrently in immediate-release tablet dosage forms. UV-detection was performed at absorption maxima of 237.20 nm and 217.00 nm for amlodipine besilate and enalapril maleate, respectively; 6.8 pH phosphate buffer was used as dissolution media for 30 mintues, on USP II (Paddle) dissolution apparatus, at 50 RPM and 37.0 ± 0.5oC. The fallouts of the analysis were endorsed statistically. Results were satisfactory in the arrays of 1–19 μg mL-1 for amlodipine besilate and 1–9 μg mL-1 for enalapril maleate. The analysis results exhibited that the projected simultaneous method is modest, swift, precise, and accurate and used for the repetitive analysis of dissolution samples of amlodipine besilate and enalapril maleate in combined pharmaceutical dosage forms (tablets).

UPLC method development and validation for simultaneous determination of amlodipine besylate and enalapril maleate in drug products

Objective: A simple, Accurate, precise method was developed for the simultaneous estimation of the Amlodipine besylate and Enalapril maleate in pharmaceutical dosage form. Methods: Chromatogram was run through BEH C18 column (2.1 × 50mm i.d., 1.7 μm particle size). Mobile phase containing methanol: 1N HCl (1:1) was pumped through column at a flow rate of 1ml/min. Temperature was maintained at Ambient. Optimized wavelength for Amlodipine besylate and Enalapril maleate was 272 nm. Results: Retention time of Amlodipine besylate and Enalapril maleate were found to be 1.04 min and 0.59 min. The % purity of Amlodipine besylate and Enalapril maleate was found to be 100.03 % and 99.75 % respectively. The system suitability parameters for Amlodipine besylate and Enalapril maleate such as theoretical plates were found to be 5659.11 and 3214.07. the resolution was found to be 4.58,2.91. The linearity study for Amlodipine besylate and Enalapril maleate was found in concentration range of 10μg-50 μg and 10 μg-50 μg and correlation coefficient (r2) was found to be 0.999 and 0.999, % mean recovery was found to be 97.41 % and 95.5 %, %RSD for repeatability was 0.73 and 0.66 %.

Effect of Enalapril Combined with Bisoprolol on Cardiac Function and Inflammatory Indexes in Patients with Acute Myocardial Infarction.

Objective The use of enalapril in combination with bisoprolol in patients with acute myocardial infarction (AMI) was studied for its effect on cardiac function and inflammatory parameters. Methods Sixty-two cases of AMI patients admitted to our clinic from November 2019 to November 2021 were selected for the study and grouped according to the random number table method, those enrolled were given conventional treatment such as oxygenation, absolute bed rest, and sedation, and administered low molecular heparin, aspirin, atorvastatin calcium tablets, clopidogrel, and nitrates. The control group (31 cases) was treated with enalapril maleate folic acid tablets, and the treatment group (31 cases) was treated with bisoprolol fumarate tablets on top of the control group, and the efficacy, adverse effects, cardiac function, inflammatory indexes, and oxidative stress indexes of the two arms were contrasted. Results The incidence of adverse reactions in the therapy cohort was 12.90% higher than that in the controlled arm, but the discrepancy was not medically relevant (P < 0.05). The SOD level was larger than the concentration in the corresponding drug therapy group, and the MDA level was lower than the concentration in the respective test cases (P < 0.05); the incidence of 12.90% adverse reactions in the treatment period was lower than that of 16.13% in the specific drug therapy group, but the variance was not scientifically evident (P > 0.05). Conclusion Enalapril application combined with bisoprolol in AMI patients is beneficial to boost the efficacy, promote the improvement of cardiac function, reduce the inflammatory response, and improve the oxidative stress with fewer adverse effects, which can ensure the therapeutic security.

Development of amlodipine and enalapril combined tablets based on quality by design and artificial neural network for confirming of qualitative composition

Using approaches of Quality by design, namely dispersion analysis, random balance method, regression analysis and neural networks, the composition and technology tablets based on amlodipine besylate and enalapril maleate have been developed. Using dispersion analysis was determined the effect of 30 excipients on 10 pharmaco-technological parameters of tablets. With the help of the desirability function, the leaders of the excipients were selected from 6 functional groups. It was confirmed that the composition with the best pharmaco-technological parameters, determined by using statistical methods, coincides with the results studies the synthesized Feed-forward neural network. The quantities of preferable excipients at 3 levels were identified by the random balance method. The relationship between the studied factors and the quality of the tablets was described by regression equations. Based on the placement of equal output lines, the optimal composition of amlodipine tablets with enalapril was established.

Implementation of a New Electronic Liquid Dispensing System for Individualized Compounding of Hard Capsules.

An automated compounding device can be a useful tool for the rapid and accurate production of small batches for personalized medicine as well as for clinical batches. A novel electronic liquid dispensing system (ELDS) was investigated to produce hard capsules with individualized dose strengths. An ethanol-based solvent system containing the antihypertensive enalapril maleate was extruded through a cannula into prefilled capsules. The capsules were prefilled with a powder bed of mesoporous silica (Syloid 244 FP) or synthetic dibasic calcium phosphate anhydrous (Fujicalin). The dosing accuracy as well as content uniformity of ELDS was compared with manual preparation using a Hamilton syringe (HS). Both methods met the pharmacopeia criteria for all formulations with an acceptance value (AV) less than 15. Drug adherence to the capsule shells was also investigated. A recovery rate of 98% of enalapril maleate showed almost no drug loss, but the appropriateness of the new dispensing method.

Formulation And Invitro, In Vivo Evaluation Of Mucoadhesive Buccal Tablet Of Enalapril Maleate

The buccal area of the mouth mucosal cavity provides an adorable route of administration for systemic and local medication distribution. Among the several transmucosal locations accessible, the mucosa of the buccal cavity was determined to be the most convenient and easily approachable site for the administration of therapeutic drugs as retentive dose forms delivery. The objective of the current research is based on to improve the bioavailability and efficacy of the Enalapril maleate (EM) a commonly used antihypertensive drug through buccal mucosal. The pure drug EM and excipient polymers such as, hydroxypropyl methylcellulose (HPMC K100), Carbopol 934p, Chitosan and polyvinyl pyrrolidone (PVP K30) were obtained from manufacturing industries. EM buccal tablets were prepared using direct compression. The powder blend formulation studies such as Bulk density, tapped density, Hausner ratio, Carr’s index and angle of repose were carried out, moisture absorption study was performed by using 5%W/V agar, residence time was carried out using porcine buccal mucosa, ex vivo permeation was performed using Franz diffusion cell and in vivo drug release for API and formulated tablets were studies using rabbits. The result of our study showed that the powder flow properties were found to be within the limits, moisture absorption study was 67.63%, residence time till 8.15 hrs, ex vivo permeation 99.12% and in vivo drug release was extended till 24 hrs. The bioregion in which it will remain in contact were perfectly done with appropriate evaluation techniques (Residence time), the moisture absorption study was carried out to check how much moisture the tablet can absorbed to release the drug and was found satisfactory. The ex vivo permeation study was performed by Franz diffusion cell to check the drug permeation through buccal mucosa. The in vivo studies were performed on New Zealand rabbits and can be concluded that the drug release from the formulated F6 was better than the marketed API.&#x0D;

Effect of enalapril maleate-folic acid tablets on inflammatory response and myocardial endoplasmic reticulum stress-related factors in hypertensive rats

Purpose: To determine the effect of enalapril maleate folate on inflammatory reaction and myocardial endoplasmic reticulum stress-related factors in hypertensive rats.Methods: Eighty (80) hypertensive rats with SBP &gt; 140 mmHg were equally assigned to control and study groups. Rats in control group were given normal saline by gavage, while the observation group was given enalapril maleate powder (10 mg/kg/day). After 4 weeks of treatment, 2 mL of inferior vena cava blood was collected from each of the two rat groups. The level of homocysteine (Hcy) was determined with Hcy assay kit, while C-reactive protein (CRP) levels in patients were determined by latex immunoturbidimetry. Serum FBG was assessed using automatic biochemical analyzer. The expression levels of GRP78, CRP94, chop and caspase-12 in aortic smooth muscle cells were assayed immunohistochemically.Results: Central arterial pressure (MAP), aortic media thickness, lvwi, HWI FBG and CRP were significantly higher in the study rats, while Hcy level was lower, than in controls (p &lt; 0.05). There were significantly lower levels of glucose regulatory protein 78 (GRP78), CRP94, CHOP and caspase-12 in study rats than in control rats (p &lt; 0.05).Conclusion: Enalapril maleate-folate slows down inflammatory reaction by reducing the levels of Hcy, CRP and FBG. It inhibits the expressions of GRP78, CRP94, CHOP and caspase-12 in myocardium, reduces damage to myocardial cells, and alleviates or reverses left ventricular hypertrophy in rats with high blood pressure. This provides new insight into the research and development of other drugs.

Paricalcitol Attenuates Metabolic Syndrome-Associated Heart Failure through Enhanced Mitochondrial Fusion.

Objectives Transition from cardiac hypertrophy to failure involves adverse metabolic reprogramming involving mitochondrial dysfunction. We have earlier shown that vitamin D deficiency induces heart failure, at least in part, through insulin resistance. However, whether activation of vitamin D receptor (VDR) can attenuate heart failure and underlying metabolic phenotype requires investigation. Thus, we aimed to assess the cardioprotective potential of paricalcitol, a vitamin D receptor-activator, against cardiac hypertrophy and failure in high-fat high-fructose-fed rats. Methods Male Sprague Dawley rats were fed control (Con) or high-fat high-fructose (HFHFrD) diet for 20 weeks. After 12 weeks, rats from HFHFrD group were divided into the following: HFHFrD, HFHFrD+P (paricalcitol i.p. 0.08 μg/kg/day) and HFHFrD+E (enalapril maleate i.p. 10 mg/kg/day). Intraperitoneal glucose tolerance test, blood pressure measurement, and 2D echocardiography were performed. Cardiac fibrosis was assessed by Masson's trichrome staining of paraffin-embedded heart sections. Mitochondrial DNA and proteins, and citrate synthase activity were measured in rat hearts. VDR was silenced in H9c2 cardiomyoblasts, and immunoblotting was performed. Results Paricalcitol improved glucose tolerance, serum lipid profile, and blood pressure in high-fat high-fructose-fed rats. Paricalcitol reduced cardiac wall thickness and increased ejection fraction in high-fat high-fructose-fed rats but had no effect on perivascular fibrosis. PGC1-α was upregulated in the HFHFrD+P group compared to the HFHFrD group, but there was no significant difference in mitochondrial content. Citrate synthase activity was significantly higher in the HFHFrD+P group compared to the HFHFrD group. Rat hearts of the HFHFrD+P group had significantly higher expression of mitofusins. H9c2 cells with VDR knockdown showed significantly lower expression of Mfn2. Improvement in the HFHFrD+P group was comparable with that in the HFHFrD+E group. Conclusions Paricalcitol reverses cardiac dysfunction in rats with metabolic syndrome by enhancing mitochondrial fusion. We demonstrate repurposing potential of the drug currently used in end-stage kidney disease.

Metal Complexation of Arabinoxylan Engenders a Smart Material Offering pH, Solvents, and Salt Responsive On-Off Swelling with the Potential for Sustained Drug Delivery.

The present study aimed to develop a stable interconnected matrix as a sustained release drug delivery material. Arabinoxylan (AX) was extracted from ispaghula husk and then crosslinked with different concentrations, i.e., 0.5, 1.0, and 1.5 g of CaCl2 per 0.25 g of AX. The crosslinking was confirmed through Fourier transform infrared spectroscopy. The swelling capacity of crosslinked AX (CL-AX) was evaluated against buffer solutions of pH 1.2, 6.8, 7.4, and water. The swelling capacity increased from pH 1.2 to pH 7.4 and followed the second order swelling kinetics. The swelling study also revealed that CL-AX with 1.0 g CaCl2 showed maximum swelling capacity. The swelling–deswelling (on–off switching) behavior of CL-AX was evaluated in water–ethanol, water–0.9% NaCl solution, and buffer solutions of pH 7.4–1.2 and showed responsive swelling–deswelling behavior. Scanning electron microscopy revealed a highly porous nature of CL-AX with a mesh of thin fibrous networking. Hemocompatibility studies of CL-AX revealed its non-thrombogenic and nonhemolytic attributes. The CL-AX matrix tablet prolonged the release of enalapril maleate for 24 h, and the drug release followed the zero order kinetics and super case-II transport mechanism. Therefore, CL-AX can be recognized as a stimuli responsive and hemocompatible biomaterial with sustained drug release potential.

Explore the Role of the rs1801133-PPARG Pathway in the H-type Hypertension.

Both rs1801133 mutation on Methylenetetrahydrofolate reductase (MTHFR) gene and transcription factor peroxisome proliferator-activated gamma (PPARG) have been associated with plasma homocysteine (Hcy) levels and hypertension. However, their role in H-type hypertension remains unclear. In this study, we first tested the association between rs1801133 genotypes and Hcy level in H-type hypertension using clinical profiles collected from 203 patients before and after the treatment using enalapril maleate and folic acid tablets (EMFAT). Then, we constructed a literature-based pathway analysis to explore the role of the rs1801133-PPARG signaling pathway in H-type hypertension and its treatment. Although presented similar blood pressure, the patients with TT genotype of rs1801133 were much younger (p value <0.05) and significantly higher in Hcy levels (x2 = 6.11 and p < 0.005) than that in the CC and CT genotype groups. Pathway analysis showed that T-allele of rs1801133 could inhibit the expression of PPARG through the downregulation of folate levels and upregulation of Hcy levels, which increased the risk of hypertension and hyperhomocysteinemia. Treatment using EMFAT led to similarly decreased Hcy levels for all patients with different genotypes (x2 = 86.00; p < 0.36), which may occur partially through the activation of PPARG. Moreover, even after treatment, the patients with TT genotype still presented significantly higher Hcy levels (x2 = 7.87 and p < 0.001). Our results supported that rs1801133 mutation could play a role in H-type hypertension, which might be partially through the downregulation of PPARG. Moreover, PPARG might also be involved in treating H-type hypertension using EMFAT.

DEVELOPMENT OF NANOPARTICLES SUSPENSION FOR PAEDIATRIC DRUG ADMINISTRATION

Objective: Enalapril maleate (EM) is an angiotensin-converting enzyme (ACE) inhibitor. It is generally prescribed for the treatment of hypertension, heart failure and chronic kidney diseases in adults and children. EM 2.5 mg, 5 mg, 10 mg and 20 mg tablets and EM injection 1.25 mg/ml are currently available in the market. But a liquid paediatric formulation of this medicine is not currently available. Also, it is a BCS class III drug, having a bioavailability of approximately 60%. The present study proposes a new strategy for improvement of drug bioavailability and taste masking: EM nanoencapsulation within polymeric nanoparticles suspensions prepared with Eudragit RS100 (ERS100) as polymer and Tween 80 as a stabilizer, aiming at obtaining a liquid dosage form suitable for paediatric administration.Methods: Nanoprecipitation method used for the preparation of nanoparticles suspension. The preparations were evaluated for drug content, entrapment efficiency, particle size, zeta potential, polydispersity index, pH, viscosity and in vitro drug release. Based on the entrapment efficiency, viscosity and in vitro drug release the optimized formulation was selected. Optimized formulation evaluated for taste, ex vivo intestinal permeation, differential scanning calorimetry, scanning electron microscopy and release kinetic studies.Results: The optimized nanoparticle formulation F8 having drug to polymer ratio of 1:100 showed satisfactory drug content (95.1%), entrapment efficiency (77.71%), particle size (198.47 nm), pH (6.36), viscosity (2.9 x〖10〗^(-3)Pa•s) and 81.2% drug release after 12 h. The formulation has taste-masking properties and shows 84.6% drug permeation through the goat intestine within 12 h.Conclusion: The prepared nanoparticles suspension of Enalapril maleate was found to be an effective liquid pharmaceutical dosage form for paediatric administration with taste-masking properties.

Influence of commonly used excipients on the chemical degradation of enalapril maleate in its solid state: The role of condensed water

The physicochemical stability of enalapril maleate was investigated in the presence of fourteen different excipients divided into four different classes. The extent of a drug-excipient interaction was investigated by following the chemical stability using HPLC. It was found that there is a certain order in the stability of enalapril maleate. Enalapril maleate remained most stable in the presence of: disaccharides > celluloses > starches > superdisintegrants. The amount of degradation can be related to the excipient characteristics. A material with a higher water sorption capacity and lower crystallinity presents a more reactive particle surface. It was revealed that the condensation layer deposited on the surface of the excipient is responsible for the degradation of enalapril maleate. A confirmation was found by changing the surface of the excipient and influencing the environmental humidity that allowed a variable build-up of the condensation layer. For this particle-particle interaction, the microenvironmental pH only presents a minor effect as it was found to not be a determining factor for degradation. Moreover, there appears to be a firm relationship between the degradation of enalapril maleate and the water sorption-activity of excipients.

Formulation of Enalapril-Loaded Microspheres Using Emulsion Solvent Evaporation Technique for Bitter Taste Masking

The aim of the present study was to formulate polymer microspheres using the emulsion solvent evaporation technique as an approach to mask the bitter taste of enalapril maleate. Five models were prepared with two water-insoluble polymers. Talc was used to stabilize the particle structure. Production yields ranged from 38 % to 53 %; drug loading varied between 17 % and 40 %; the mean particle size ranged from 140 μm to 339 μm. No interaction between enalapril and the polymers was estimated. A drug release study in artificial saliva indicated a negligible amount of enalapril dissolved in the test medium which demonstrated successful taste masking.