Esomeprazole Research Articles

Prediction of In-vivo Performance of Naproxen and Esomeprazole Magnesium Delayed-Release Tablets using Biorelevant Dissolution Tests

Main objective of this research work was to develop a biorelevant dissolution method by correlating the in-vivo behavior of Naproxen and Esomeprazole magnesium delayed release tablets 500/20mg, when administered orally under pre-prandial condition. The target dissolution profile for bio-relevant dissolution media was derived, by deconvoluting mean blood plasma concentration time profile of Naproxen and Esomeprazole, achieved after oral administration under pre-prandial condition. The dissolution media volume and RPM were optimized using full factorial design of experiment. The dissolution profile observed with office of generic drugs recommended dissolution media was faster in release for Naproxen part and slower in release for Esomeprazole part in comparison to target release of bio-relevant dissolution method, with the F 2 value of 31 for Naproxen and 29 for Esomeprazole. USP Apparatus-I with fasted state simulated gastro intestinal change over dissolution media were used for method development. Based on ANOVA results, for Naproxen part, 250ml of fasting change over dissolution medium, and 50RPM, with the desirability factor of 0.508 was concluded as bio relevant dissolution medium. For esomeprazole part, the 900ml of fasting change over dissolution medium, and 100RPM, with the desirability factor of 0.479 was concluded as bio-relevant dissolution medium. The F 2 value observed between in-vitro and in-vivo dissolution profile is 64 and 63, the regression co-efficient (R 2 ) value of 0.987 and 0.997 for Naproxen and Esomeprazole respectively demonstrates a very good in-vitro/in-vivo correlation under pre-prandial condition. The developed method shall be used as a predictive in-vitro tool for evaluation Naproxen from Naproxen and Esomeprazole magnesium delayed release tablets, and also gives the advantage for claiming bio-waiver for remaining strengths.

Tu1503 ENDOSCOPIC AND HISTOLOGICAL CHARACTERISTICS OF NEW GASTRIC FINDINGS THAT APPEARED WITH STRONG ACID SECRETION SUPPRESSOR (P-CAB).

Since the number of H.pylori-infected persons decreases rapidly, it is expected that acid-related diseases will continue to increase in Japan. The need for gastric acid secretion suppressors is expected to increase in the future. There are several known gastric findings associated with the use of conventional proton pump inhibitors (PPIs). However, there are no reports of gastric findings associated with the use of potassium competitive acid blocker (P-CAB) a more potent gastric acid secretion suppressor. This time we found a new gastric finding associated with the use of P-CAB. This gastric finding is white granular findings with slight elevation similar the White Glove Appearance (WGA) which is known as gastric cancer cases. Since we named this finding White Granule with Small Elevation (WGSE), we introduce WGSE of this finding with endoscopic and histological analysis. <Case 1> A 57-year-old woman was given esomeprazole (EPZ) 20 mg / day and steroid for eosinophilic gastroenteritis. When esomeprazole was changed to Vonoprazan (VPZ) 20 mg / day because erosive gastritis was apparent by endoscopy, WGSE was observed in the gastric fundic gland area. WGSE worsened with continuing VPZ and the dose was reduced to 10 mg / day. Then WGSE gradually decreased and finally disappeared when medicine was changed to famotidine 40 mg / day. <Case 2> A 75-year-old woman was started on VPZ 20 mg for severe reflux esophagitis and maintenance therapy was performed at 10 mg / day. WGSE was observed in the gastric fundic gland area. The change to EPZ 20mg / day is being considered if symptoms are stable in the future. The WGSE histological findings were so similar the WGA observed in gastric cancer cases. Its characteristic finding showed a cystic dilated duct with accumulated gastric secretions. It could be detected WGSE under only continuous P-CAB use, not observed when using PPI. In addition, WGSE decreased with tapering of P–CAB. WGSE were completely disappeared with the change to H2 receptor antagonist. Therefore, we consider that WGSE is to be a specific change with continued use of P-CAB. Previous reports have said that WGA is sometimes observed in autoimmune gastritis with hypergastrinemia, so we have been believed that hypergastrinemia due to strong gastric acid suppression is the most important cause of WGSE. The highest serum gastrin levels of our cases were 1,750 pg/ml and 4,500 pg/ml, those were markedly high level. Although hypergastrinemia occurs with continued PPI use too, no WGSE has been reported. In other words, it is thought to be a gastric finding peculiar to continued use of P-CAB with severe hypergastrinemia. When using P-CAB in the future, it is necessary to pay attention to the appearance of WGSE. Our study found WGSE, the first stomach finding that was especially apparent when using P-CAB.View Large Image Figure ViewerDownload Hi-res image Download (PPT)

The Evaluation of Potential Cytotoxic Effect of Different Proton Pump Inhibitors on Different Human Cancer Cell Lines.

To assess the differential cytotoxic activity of PPIs on different human cancer cell lines; namely A549 lung cancer, CACO-2 colorectal cancer, MCF-7 breast cancer, and PANC-1 pancreatic cancer, A375 skin melanoma. In this study, the five human cancer cell lines and human non-cancerous fibroblasts were treated with increasing concentration of PPIs Omeprazole (OMP), Esomeprazole (ESOM), and Lansoprazole (LANSO) (50-300μM), over 24h, 48h, and 72h. Cell viability was determined using 3-(4,5- Dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide (MTT) assay and the IC50 values of PPIs were measured. The most sensitive cell line A375 was used for further investigation. The cytotoxic effects of LANSO on these cells were assessed using Annexin-V Propidium Iodide (AV-PI) flow cytometry. As of action mechanism; anti-inflammatory effects of each PPIs and PPIs-DOXO combination therapy on LPS-stimulated RAW 264.7 mouse macrophages were assessed. Dose and time dependence cytotoxic activity of PPIs on human cancer cell lines was founded. Unlike DOXO; All PPIs had a selective cytotoxic effect in the normal fibroblasts. Unlike the equipotent OMP and ESOM; LANSO was the most potent drug with IC50 values at 72h of 99, 217, 272, 208, 181μM against A375, A549, CACO-2, MCF-7, and PANC-1, respectively. AV-PI flow cytometry revealed dose-dependent apoptotic effects of LANSO alone and substantially enhanced in DOXO-co-treatments. Interestingly unlike ESOM and OMP, LANSO proved more effective than indomethacin in LPS-stimulated RAW 264.7 macrophages. None of the tested compounds, as well as indomethacin, exerted any cytotoxicity against RAW 264.7 macrophages. PPIs-DOXO lacked potential synergistic combination antiinflammation therapies. This study provides the evidence that PPIs induce a direct and differential cytotoxic activity against human cancer cell line by the induction of the apoptosis. Moreover, PPIs increase cancer cell lines sensitivity to doxorubicin via apoptosis augmentation. Nevertheless, PPIs-DOXO lacked potential synergistic combination therapies in either antiproliferation or anti-inflammation.

Post‐exposure treatment with esomeprazole protects pregnant mice from mortality and from compromised fetal growth after exposure to chlorine gas.

Exposure to Chlorine (Cl2) and Bromine (Br2) causes significant cardiopulmonary injury to mice, rats, rabbits and humans triggering extensive systemic injury. After exposure to Br2 pregnant mice develop preeclampsia‐like symptoms and increased mortality as compared to identically exposed male or non‐pregnant female mice (Lambert et al Hypertension 2018). Heme oxygenase (HO‐1), which has been shown recently to be induced by proton pump inhibitors such as esomeprazole (ESO), has been implicated as a protective molecule against halogen inhalation induced injury in non‐pregnant animals and, additionally, against the development of symptoms in models of preeclampsia in pregnant mice.Timed pregnant C57BL/6 mice were exposed to 400ppm Cl2 for 10min at E14.5, then treated with vehicle or with 30mg/kg ESO by gavage 6h post exposure, then at every 24h thereafter. Survival and body weights were monitored until E18.5. Fetal weights were recorded at E18.5 after euthanasia. Finally, using nuclear factor (erythroid‐derived 2)–like 2 (Nrf2)‐knock out and Nrf2 competent murine transformed club cells (mtCC) we tested whether HO‐1 production was induced via Nrf2.Survival was significantly higher (P=0.0056) in Cl2 exposed pregnant mice that received ESO (88.9% survival, n=9) compared to the vehicle treated animals (29.4% survival, n=17). Maternal exposure to Cl2 severely compromises fetal growth (0.6366g±0.0666 (S.E.M.), n=5) when compared to normal fetuses (1.167g±0.0399 (S.E.M.), n=5) (P&lt;0.0001). However, the weight of fetuses collected from Cl2 exposed pregnant mice that received ESO (0.9264g±0.0542 (S.E.M.), n=8) compared to weights of fetuses from vehicle treated animals (0.6366g±0.0666 (S.E.M.), n=5) was significantly higher (P=0.0058). Finally, maternal weight, as normalized to weight recorded preexposure, in Cl2 exposed ESO treated pregnant mice (93.64%±4.038% (S.E.M.), n=8) compared with the vehicle treated animals (81.31%±5.717% (S.E.M.), n=5) was not significantly different (P=0.1772). Additionally, we found that HO‐1 gene expression is induced in a dose dependent manner by ESO only in Nrf2‐competent cells (p&lt;0.001).Our results suggest that ESO may be an effective countermeasure to increase maternal survival and improve fetal growth post halogen inhalation in pregnancy. Further mechanistic studies will have to explore organ/tissue specific role of HO‐1 induction in the protective effect.Support or Funding InformationThis work was supported by: 5U01ES027697 (to Tamas Jilling) and 5U01ES026458 (to Sadis Matalon)

Examination of Aggregate Formation upon Simultaneous Dissolution of Methacrylic Acid Copolymer LD Enteric Coating Agent, Pharmaceutical Additives, and Zwitterionic Ingredients.

We previously showed that adhesive aggregates were formed when levofloxacin hydrate tablets and lansoprazole orally disintegrating (OD) tablets were suspended in water in the clinical context. In this study, we have clarified the factors causing aggregate formation, focusing on the role of pharmaceutical additives and electrostatic interaction. Co-suspension of enteric-coated proton pump inhibitor (PPI) esomeprazole magnesium hydrate with levofloxacin resulted in aggregate formation, whereas the non-enteric-coated PPI vonoprazan fumarate did not. A comparison of pharmaceutical additive in the two PPIs highlighted polysorbate 80 and methacrylic acid copolymer LD as candidates causing aggregation. When these pharmaceutical additives were added to levofloxacin, only methacrylic acid copolymer LD induced aggregate formation. Since levofloxacin is zwitterionic, we examined another zwitterionic ingredient, ampicillin sodium, and found that it also formed aggregates with methacrylic acid copolymer LD, while benzylpenicillin sodium, which is not zwitterionic, did not form aggregates. When we next examined a series of zwitterionic quinolone antimicrobial drugs, we found that ofloxacin, which is highly soluble, formed aggregates with lansoprazole OD tablets, whereas poorly soluble quinolone antimicrobial drugs did not form aggregates. Further, although cefepime hydrochloride and cephalexin did not form aggregates with methacrylic acid copolymer LD in tap water, aggregates were formed when a suspension of cefepime hydrochloride or cephalexin with methacrylic acid copolymer LD was adjusted to pH 7.0. Our results indicate that electrostatic interaction between zwitterionic ingredients and methacrylic acid copolymer LD can result in aggregate formation under conditions where the drug and methacrylic acid copolymer LD are both sufficiently soluble.

Development and Validation of Stability Indicating Method for Simultaneous Estimation of Esomeprazole and Levosulpiride by HPTLC using Experimental Design

The present study examines simultaneous multiple response optimization using desirability function for the development of an HPTLC method to detect esomeprazole magnesium trihydrate and levosulpiride in pharmaceutical dosage form. HPTLC separation was performed on aluminium plates pre-coated with silica gel 60 F254 as the stationary phase using ethyl acetate:methanol:toluene:ammonia (7:1.5:1.5:0.1% v/v/v) as the mobile phase. Full factorial design applied for the optimization of degradation condition. Esomeprazole magnesium trihydrate and levosulpiride were subjected to acid, alkali hydrolysis, oxidation and photodegradation. Experimental full factorial design has been used during forced degradation to determine significant factors responsible for degradation and to optimize degradation conditions reaching maximum degradation. 32 and 23 full factorial design has been used for optimization of chromatographic condition in acid and base degradation study, respectively. Quantification was achieved based on a densitometric analysis of esomeprazole magnesium trihydrate and levosulpiride over the concentration range of 800-4000 ng/band and 1500-7500 ng/band, respectively at 254 nm. The method yielded compact and well-resolved bands at Rf of 0.70 ± 0.02 and 0.32 ± 0.02 for esomeprazole magnesium trihydrate and levosulpiride, respectively. The linear regression analysis for the calibration plots produced r2 = 0.9967 and r2 = 0.9981 for esomeprazole magnesium trihydrate and levosulpiride, respectively. Method is validated as per ICH (Q2)R1 guideline.

ANTIULCER ACTIVITY OF ELECTROHOMEOPATHIC DRUG (SPAGYRIC ESSENCE) CANCEROUS 15 - 3rd DILUTION AGAINST INDOMETHACIN-INDUCED GASTRIC ULCER IN RATS

Objective: To evaluate the curative protects activity of electrohomeopathic drug Cancerous15 (C15) against Indomethacin (IND)-induced gastric ulcer in albino rats. None of the data have been reported on antiulcer activity of C15 drug. Hence, the present study focuses on the scientific investigation of antiulcer activity of C15 against Indomethacin-induced peptic ulceration of rat models.&#x0D; Methods: A total number of 35 albino rats were divided into five groups equally. Pure water was given to Group 1 (normal). IND was given orally to Group 2 (ulcerated control). Cancerous15 third dilution was given to Group 3. IND was given to Group 4 and Group 5 animals, thereafter pretreatment with Esomeprazole (ESM) and C15-third dilution, respectively. The pretreatments were treated in each day’s interval for 21 days before IND administration. There was provision of food and water throughout the experimental period. On the 23rd day, the stomachs of the sacrificed rats were removed, and (1) ulcer index, (2) percentage of ulcer inhibition, (3) gastric volume, (4) pH, (5) pepsin activity, (6) mucin content, (7) malondialdehyde (MDA) concentration, and (8) stearidonic acid activity were studied.&#x0D; Results: The pre-treated animals with ESM and C15 shown as significantly decreases in ulcer index, gastric volume, pepsin activity and MDA concentration, and significant increase in the percentage ulcer inhibition, pH value, mucin content, and superoxide dismutase activity concentration in comparison to ulcer-induced rats.&#x0D; Conclusion: The study shows the significant ulcer protective activity of the C15 drug against IND-induced peptic ulceration in rats.

Efficacy and safety of rifabutin and furazolidone included triple regimen and minocycline plus furazolidone included quadruple regimen in eradicating refractory Helicobacter pylori infection

Objective To observe the efficacy and safety of rifabutin and furazolidone included triple regimen and minocycline plus furazolidone included quadruple regimen in eradicating refractory H. pylori infection. Methods A total of 146 patients who failed (≥two times) to treat H. pylori with standard anti-H.pylori therapy were selected and divided into esomeprazole, rifabutin and furazolidone treatment group (ERF group, n=74) and esomeprazole, minocycline, furazolidone and bismuth potassium citrate group (EMFB group, n=72). The duration of treatment were both 10 days. Liver and renal functions were examined within three days after therapy. 13C or 14C-urease breath test was performed one month after the medication withdrawal. The patients were followed up once every two weeks during the treatment period. The medication and adverse reactions were recorded in detail. The compliance and rates of adverse events in two groups were compared and analyzed. The eradication rates of the two groups and subgroups were compared by intention-to-treat (ITT) and per-protocol (PP) analyses. The cost-effectiveness of the two groups was evaluated with cost effectiveness analysis (CEA). The cost/effectiveness (C/E) ratio was calculated by PP. Chi-square test and t test were used for statistical analysis. Results There was no significant difference in complicance between ERF group and EMFB group (90.5% vs. 90.3%, P>0.05). There was no significant difference in H. pylori eradication rate between ERF group and EMFB group analyzed by ITT (82.4% vs. 84.7%, P>0.05). Analyzed by PP, there were no significant differences in H. pylori eradication rate between ERF group and EMFB group (91.0% vs. 93.8%), between male subgroup and female subgroup of ERF group (87.9% vs. 94.1%), between subgroup with age less than 60 years and subgroup with age over 60 years of ERF group (89.7% vs. 92.9%), between male subgroup and female subgroup of EMFB group (89.7% vs. 97.2%) and between subgroup with age less than 60 years and subgroup with age over 60 years of EMFB group (93.6% vs. 94.4%) (all P>0.05). There were no statistically significant differences in the rate of adverse events between ERF group and EMFB group (20.3% vs. 22.2%), between male subgroup and female subgroup of ERF group (25.0% vs. 15.8%), between subgroup with age less than 60 years and subgroup with age over 60 years of ERF group (26.2% vs. 12.5%), between male subgroup and female subgroup of EMFB group (19.4% vs. 24.4%) and between subgroup with age less than 60 years and subgroup with age over 60 years of EMFB group (24.5% vs. 15.8%) (all P>0.05). Fixed daily cost, total cost and C/E of ERF group was RMB 59.0 yuan, RMB 590.5 yuan and 648.9, respectively; and the eradication rate was 91.0%(61/67). Fixed daily cost, total cost and C/E of EMFB group was RMB 32.9 yuan, RMB 329.1 yuan and 350.9, respectively; and the eradication rate was 93.8%(61/65). Conclusions Rifabutin and furazolidone included triple regimen and minocycline plus furazolidone included quadruple regimen both have good efficacy, safety and compliance in the eradication of refractory H. pylori infection, and the latter is better. Key words: Rifabutin; Furazolidone; Minocycline; Refractory H. pylori infection; Efficacy

Development and Validation of Genotoxic Impurity in Esomeprazole Magnesium Trihydrate Active Pharmaceutical Ingredient by LC-MS/MS

Development and Validation of Genotoxic Impurity in Esomeprazole Magnesium Trihydrate Active Pharmaceutical Ingredient by LC-MS/MS

Clinical study of mosapride and esomeprazole combined with flupentixol and melitracen tablets in the treatment of refractory gastroesophageal reflux disease

目的 回顾性研究莫沙必利与埃索美拉唑联合氟哌噻吨美利曲辛片治疗难治性胃食管反流病(RGERD)的效果。 方法 选取2016年3月至2017年9月运城市中心医院收治的RGERD患者68例为研究对象，按照治疗方案不同分为观察组(n=34)与对照组(n=34)。对照组予以莫沙必利+埃索美拉唑治疗，观察组予以莫沙必利+埃索美拉唑+氟哌噻吨美利曲辛片治疗，比较两组疗效、治疗前后反流性疾病问卷(RDQ)积分、抑郁自评量表(SDS)评分、焦虑自评量表(SAS)评分、食管测酸指标变化及食管测压指标变化。 结果 治疗后观察组RDQ积分改善情况优于对照组(P 0.05)；两组治疗前后食管测压指标差异无统计学意义(P>0.05)。 结论 采用莫沙必利与埃索美拉唑联合氟哌噻吨美利曲辛片治疗RGERD疗效显著，可缓解患者临床症状，改善其负性情绪，值得临床推广应用。

Experimental study and thermodynamic modeling of Esomeprazole (proton-pump inhibitor drug for stomach acid reduction) solubility in supercritical carbon dioxide

Production of micro- and nano-sized particles through supercritical fluid (SCF) technology needs substantial measurements of solubility data. In this work, for the first time, solubility of Esomeprazole (ESM) in supercritical carbon dioxide (SC−CO2) was determined at pressures and temperatures ranging within 12–27 MPa and 308.2–338.2 K, respectively. Under the applied conditions, mole fractions were obtained in the range of 1.11 × 10−5 to 9.10 × 10−4 . For correlating the drug solubility, six semi-empirical models and two equations of state (EoSs), with different modeling plans, were utilized. Furthermore, sublimation pressure of the solute was calculated by two different approaches: a predictive model and data fitting. Results showed high accuracy of Soave-Redlich-Kwong EoS combined with Renon mixing rule using the second approach. The results were further employed to derive a criterion for application of cubic EoSs in SCF as well as a methodology for prediction of Psub to 9.10 × 10−4

Formulation and evaluation of floating beads of esomeprazole magnesium USP

The aim of this study was to develop and evaluate floating beads of Esomrazole Magnesium USP. Floating beads of Esomeprazole was prepared by ionotropic gelatin method using sodium alginate as the polymer. Five different formulations were developed. The developed floating beads were evaluated for percentage yield, particle size, in vitro buoyancy, scanning electron microscopy and drug release. Stability studies were carried for 45 days. There are no significant change in the drug entrapment, buoyancy, and drug release of floating beads Esomeprazole Magnesium after 45 days. The polymer used was Sodium alginate. FTIR study results showed that there were no incompatibility between drug and polymer. Solubility study was performed and recorded the results. Results of our present study suggest that floating beads of Esomeprazole Magnesium can be successfully designed for controlled drug delivery which can reduce dosing frequency making the formulation an effective alternative to conventional dosage forms. Keywords: Floating beads, Esomeprazole magnesium, Buoyancy, In vitro.

Developing a High-Performance Liquid Chromatography (HPLC) Method for Simultaneous Determination of Oxytetracycline, Tinidazole and Esomeprazole in Human Plasma

A high performance liquid chromatography method had been developed and validated for rapid simultaneous separation and determination of three anti-helicobacter drugs, oxytetracycline (OXY), tinidazole (TIN) and esomeprazole (ESM) in human plasma within 6minutes. Drugs extraction method from plasma was based on protein precipitation technique. Separation was carried out on a Equisil BDS C18 column (5μm, 150×4.60mm) using a mobile phase of acetonitrile: 0.025M KH2PO4 (25: 75, v/v) adjusted to pH3.50 with ortho-phosphoric acid at ambient temperature. The flow rate was 1mL/min and maximum absorption was measured using Diode Array (DAD) detector at 285nm. The retention times of OXY, TIN and ESM were recorded to be 2.68, 3.52 and 5.17minutes, respectively, indicating a shorter analysis time. Limits of detection were also reported to be 0.10, 0.07 and 0.04μg/mL for OXY, TIN and ESM, respectively, showing a high degree of the method sensitivity. The method was then validated according to FDA guidelines for the determination of the drugs clinically in human plasma specially regarding pharmacokinetic and bioequivalence studies.

A Study to Compare PK, PD and Safety of the AD-206 and Esomeprazole

A Study to Compare PK, PD and Safety of the AD-206 and Esomeprazole

PHARMACOKINETIC PROFILE AND INCURRED ESOMEPRAZOLE SAMPLE STABILITY IN PLASMA USING HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY - PHOTODIODE ARRAY

Objective: Esomeprazole (ESO) is one of the proton-pump inhibitors and is used to treat gastroesophageal reflux. It is sensitive to low pH, heat,moisture, and oxidation, which often means that ESO in clinical samples is degraded at the time of storage, affecting analysis results. This study aimedto analyze the in vivo stability of ESO in subjects’ plasma samples by testing the incurred sample stability (ISS) of ESO in plasma following 7, 14, and28 days of storage at two concentrations close to Cmax and one concentration in the elimination phase.Methods: Samples were analyzed using high-performance liquid chromatography with a C18 column with detection at 300 nm using a photodiodearray detector. Lansoprazole was used as an internal standard.Results: The ESO pharmacokinetics profile in the plasma samples yielded the values of Cmax 704.57–1425.85 ng/mL; tmax is 2.25 h; and AUC0-t is2444 ng.h/mL. ISS testing of plasma samples values were 6.50%, 5.73%, and 4.57% on first Cmax concentration; 3.55%, 4.84%, and 3.68% on 2nd Cmaxconcentration; and 4.04%, 4.80%, and 4.98% on elimination phase concentration.Conclusion: ISS testing results of plasma samples from six healthy subjects who were administered doses of 40 mg of ESO stored for 28 days showedthat it fulfilled the acceptance criteria (&lt;20%) of the 2011 EMEA Bioanalytical Guidelines with a %diff value in all incurred samples of 6.5%.

Asymptomatic respiratory dysfunction in patients with gastroesophageal reflux disease

BACKGROUND: Gastroesophageal reflux disease is the primary cause for many conditions affecting extraesophageal structures. OBJECTIVE: The objective of the study is to investigate the relation between reflux disease and asymptomatic respiratory dysfunction and examine correlation between the respiratory dysfunction with severity of gastroesophageal reflux disease (GERD) spectrum. METHODOLOGY: A total of 242 patients were subjected to pulmonary function test (PFT) using spirometer-G procedures. Forced expiratory volume 1 s (FEV1), forced vital capacity (FVC), FEV1/FV C ratio, and peak expiratory flow rate (PEFR) were measured. Patients in test group were treated with proton-pump inhibitor (PPI) and esomeprazole 40 mg twice daily for 3 months. They were subjected to PEFR at the end of the study. Analysis was performed using SPSS version. RESULTS: Age and PFT parameters FEV1, forced expiratory flow (FEF) 25–75, PEF, and PEFR were compared groupwise and were found to be statistically significant except FEV. As the severity of GERD increases, severity of pulmonary disorder also increases. In Group 1A, 56.5% patients had normal PEFR and 43.4% PEFR was reduced showing statistically significant. In patients with abnormal PFT, 74.2% had mild esophagitis, 15.1% had moderate esophagitis, and 10.6% had severe esophagitis showing statistically significant. Mean PEFR before treatment showed 344.1 ± 79.22. After 3 months of esomeprazole 40 mg, twice daily mean increased 409.08 ± 100.00. In Group 1B, PEFR before treatment noted 342.0 ± 53.77. Significant improvement was seen in PEFR with mean of 506.00 ± 52.64 with PPIs. CONCLUSIONS: GERD is associated with asymptomatic respiratory dysfunction. There is strong and direct relationship between the severity of respiratory disorders, detected by FEV1 and FEV1/FVC, FEF25–75, PEF, PEFR, and severity of GERD. This study demonstrated significant improvement in PEFR values, with adequate treatment of GERD.

Vonoprazan-Based Third-Line Therapy Has a Higher Eradication Rate against Sitafloxacin-Resistant Helicobacter pylori.

Eradication of Helicobacter pylori (H. pylori) is an effective strategy for preventing various gastrointestinal diseases such as gastric cancer and mucosa-associated lymphoid tissue (MALT) lymphoma. However, the eradication success rate is decreasing because of a recent increase in drug-resistant strains of H. pylori. Here, we evaluated the success rate of eradication therapy with vonoprazan (VPZ), a new potassium-competitive acid blocker, against drug-resistant H. pylori. In total, 793 patients who received H. pylori eradication therapy were investigated retrospectively. All underwent esomeprazole (EPZ)-based triple therapy (n = 386) or VPZ-based triple therapy (n = 407) for first-, second- and third-line H. pylori eradication for 7 days. The overall success rates of first- and third-line H. pylori eradication were significantly higher for VPZ-based triple therapy (88.4% and 93.0%, respectively, per protocol (PP)) than for EPZ-based triple therapy (69.5% and 56.5%, respectively, PP). Moreover, the success rates of first- and third-line eradication of clarithromycin (CLR)- and sitafloxacin (STFX)-resistant H. pylori were significantly higher for VPZ-based triple therapy (72.0% and 91.7%, PP) than for EPZ-based triple therapy (38.5% and 20.0%, PP). In addition, patient age did not affect the eradication rate of VPZ-based first-line therapy, whereas the success rate of EPZ-based therapy was lower in patients under 65 years of age. Our results clearly demonstrated that VPZ-based therapy achieved a higher eradication rate even against CLR- and STFX-resistant H. pylori, and that patient age did not affect the eradication rate of VPZ-based therapy. These findings suggest that dual therapy using VPZ and amoxicillin may be sufficient for standard H. pylori eradication, and may thus also be beneficial for avoiding antibiotic misuse.

Lek Esomeprazole Magnesium Trihydrate kao potencijalni neotrovni inhibitor korozije za meki čelik u kiselim medijima

The inhibiting effect of Esomeprazole Magnesium Trihydrate drug on the corrosion of mild steel (MS) in 1 M HCl was performed by chemical tests (weight loss (WL)) and electrochemical methods (Tafel polarization (TP), electrochemical frequency modulation (EFM) and AC impedance spectroscopy (EIS)). The adsorption isotherm of Esomeprazole Magnesium Trihydrate drug on the MS surface was found to follow Temkin adsorption isotherm. Some thermodynamic parameters were computed and discussed. The obtained data showed that the inhibition efficiency (IE) rises with increasing the dose of the Esomeprazole Magnesium Trihydrate and with raising the temperature. The morphology of MS surface was analyzed by using scanning electron microscope (SEM), atomic force microscopy (AFM), and Fourier transforms infrared spectroscopy (FTIR) techniques. All test methods were in good agreement with each other.

In Barrett esophagus, high- vs low-dose esomeprazole improved clinical outcomes; aspirin vs no aspirin did not.

Source Citation Jankowski JA, de Caestecker J, Love SB, et al. Esomeprazole and aspirin in Barrett's oesophagus (AspECT): a randomised factorial trial. Lancet. 2018;392:400-8. 30057104

Synthesis of Esomeprazole

Synthesis of Esomeprazole