s-1743 and ilaprazole

Proton-pump inhibitors (PPIs) and vonoprazan are recommended as first-line therapies for erosive esophagitis (EE). However, it is uncertain how the magnitude of efficacy and safety of first-line therapy, the choice of individual PPIs or vonoprazan in the treatment of EE remains controversial. This study aimed to evaluate the efficacy and safety of vonoprazan and PPIs in healing esophageal mucosal injury in patients with EE.. Relevant databases were searched to collect randomized controlled trials of proton pump inhibitors and vonoprazan in the treatment of reflux esophagitis up to December 2021. Studies on standard-dose PPIs or vonoprazan that were published in Chinese or English and assessed healing effects in EE were included in the analysis. Stata16.0 was used to conduct a network Meta-analysis to evaluate the efficacy and safety of the treatment.. A total of 41 literatures were included with 11,592 enrolled patients. For the endoscopic cure rate, all the PPIs and vonoprazan significantly improve compared to Placebo; Based on the surface under the cumulative ranking curve, Ilaprazole ranked first, followed by esomeprazole, vonoprazan, pantoprazole, lansoprazole, omeprazole, rabeprazole and placebo therapy ranked the last. For the rate of adverse events, there was no significant difference among all the PPIs, vonoprazan, and placebo.. Ilaprazole, esomeprazole and vonoprazan have more advantages in mucosal erosion healing, there was no significant difference in the comparative safety among all interventions.

Topics: Abdominal Injuries; Esomeprazole; Esophagitis, Peptic; Humans; Network Meta-Analysis; Peptic Ulcer; Proton Pump Inhibitors; Rabeprazole

Although many case reports have described patients with proton pump inhibitor (PPI)-induced hypomagnesemia, the impact of PPI use on hypomagnesemia has not been fully clarified through comparative studies. We aimed to evaluate the association between the use of PPI and the risk of developing hypomagnesemia by conducting a systematic review with meta-analysis.. We conducted a systematic search of MEDLINE, EMBASE, and the Cochrane Library using the primary keywords "proton pump," "dexlansoprazole," "esomeprazole," "ilaprazole," "lansoprazole," "omeprazole," "pantoprazole," "rabeprazole," "hypomagnesemia," "hypomagnesaemia," and "magnesium." Studies were included if they evaluated the association between PPI use and hypomagnesemia and reported relative risks or odds ratios or provided data for their estimation. Pooled odds ratios with 95% confidence intervals were calculated using the random effects model. Statistical heterogeneity was assessed with Cochran's Q test and I2 statistics.. Nine studies including 115,455 patients were analyzed. The median Newcastle-Ottawa quality score for the included studies was seven (range, 6-9). Among patients taking PPIs, the median proportion of patients with hypomagnesemia was 27.1% (range, 11.3-55.2%) across all included studies. Among patients not taking PPIs, the median proportion of patients with hypomagnesemia was 18.4% (range, 4.3-52.7%). On meta-analysis, pooled odds ratio for PPI use was found to be 1.775 (95% confidence interval 1.077-2.924). Significant heterogeneity was identified using Cochran's Q test (df = 7, P<0.001, I2 = 98.0%).. PPI use may increase the risk of hypomagnesemia. However, significant heterogeneity among the included studies prevented us from reaching a definitive conclusion.

Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Dexlansoprazole; Esomeprazole; Humans; Lansoprazole; Magnesium; Odds Ratio; Omeprazole; Pantoprazole; Proton Pump Inhibitors; Rabeprazole; Risk Factors; Treatment Outcome

The aim of this study was to compare the efficacy and safety of ilaprazole and esomeprazole both in initial treatment regimen and retreatment regimen of H. pylori infection in chronic gastritis and to explore risk factors for eradication failure. A total of 330 patients with chronic gastritis who were confirmed of H. pylori infection were enrolled in this study. 290 of them were initially treated patients and the 40 remained were patients with retreatment. Eradication assessment was performed at least four weeks after the completion of eradication therapy. Results showed that the eradication rates of the ilaprazole group and esomeprazole group were 91.4 % and 88.4 % for per-protocol (PP) analysis (p=0.41) and 89.0 % and 86.2 % for intention-to-treat (ITT) analysis (p=0.48) in initially treated patients. Meanwhile, they were 75.0 % and 72.2 % for PP analysis (p=0.85) and 75.0 % and 70.0 % for ITT analysis (p=0.72) in patients with retreatment. The differences were not statistically significant. There was also no significant difference in safety between the two drugs. A multiple logistic regression analysis showed that demographic factors such as age, gender, alcohol, smoking, coronary heart disease (CHD), hypertension (HTN) and diabetes mellitus (DM) did not affect eradication rates. However, patients with higher DOB values and patients with atrophic gastritis had significantly lower eradication rates than patients with lower DOB values and with non-atrophic gastritis whether the proton pump inhibitor (PPI) in eradication regimens was ilaprazole or esomeprazole. In conclusion, our findings suggest that the efficacy and safety of ilaprazole and esomeprazole were not significantly different both in initial treatment regimen and retreatment regimen of H. pylori infection in chronic gastritis and DOB values and type of chronic gastritis were to be independent risk factors for eradication failure. In addition, we discovered that a new quadruple regimen containing furazolidone and minocycline which achieved good efficacy and safety can be a promising option for retreatment of H. pylori infection.

Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Adult; Anti-Bacterial Agents; Chronic Disease; Drug Therapy, Combination; Esomeprazole; Female; Furazolidone; Gastritis; Gastritis, Atrophic; Helicobacter Infections; Helicobacter pylori; Humans; Male; Middle Aged; Minocycline; Prospective Studies; Proton Pump Inhibitors; Retreatment; Treatment Failure; Treatment Outcome

The objectives were to investigate the pharmacokinetics, pharmacodynamics and safety of ilaprazole infusion in healthy subjects and patients with esomeprazole as positive control, and then recommend the dosage regimen for Phase 2b/3 studies.. Three clinical studies were performed. First, 16 healthy subjects received infusion of ilaprazole 30 mg or esomeprazole 80 mg. Second, 12 healthy subjects received ilaprazole 20 mg followed by 10 mg once daily for 2 days. Finally, 20 patients with duodenal ulcers received ilaprazole 20 mg followed by 10 mg for 2 days or esomeprazole 40 mg twice daily for 3 days. Serial blood samples were collected and intragastric pH was recorded.. The mean percentages time of intragastric pH >6 was 63.6 and 51.7% for healthy subjects after receiving ilaprazole 30 mg and esomeprazole 80 mg. Linear pharmacokinetics was observed when the dose was increased to 30 mg but the effect was saturated. Ilaprazole 20 mg followed by 10 mg for 2 days provided higher plasma exposure in healthy subjects than patients, but the effect was comparable. After multiple administrations, ilaprazole provided similar effect to esomeprazole. Ilaprazole infusion was safe and well tolerated without serious adverse events.. Ilaprazole provided comparable effect of pH control to esomeprazole, with lower dose and fewer times of administration. There was no significant difference of ilaprazole between healthy subjects and patients regarding intragastric acid inhibition. A loading dose of ilaprazole 20 mg followed by 10 mg once daily for 2 days was recommended for Phase 2b/3 studies.

Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Adult; China; Duodenal Ulcer; Duodenoscopy; Esomeprazole; Female; Gastric Acid; Gastric Acidity Determination; Healthy Volunteers; Humans; Infusions, Intravenous; Male; Middle Aged; Proton Pump Inhibitors; Treatment Outcome; Young Adult

Proton pump inhibitors (PPIs) are the main drugs for the treatment of reflux esophagitis. Phase II clinical trials showed that, compared with Esomeprazole, the new PPI Ilaparazole is great in terms of efficacy for reflux symptoms relief and curling for esophagitis. The aim of this study was to confirm suitable dose of Ilaparazole in the treatment of reflux esophagitis.. This study used a randomized, double-blind, parallel positive drug control, multi-center design. A total of 537patients diagnosed as reflux esophagitis by gastroscopy were randomly divided into Ilaparazole group (n = 322, Ilaparazole 10 mg QD) and esomeprazole group (n = 215, Esomeprazole 40 mg QD). The patients in the two groups were treated for 8 weeks. Heartburn and reflux symptoms prior to treatment, and 2, 4 and 8 weeks after the treatment were assessed. Gastroscopy was performed after 4 weeks of treatment. Unhealed patients within 4 weeks underwent gastroscopy again at the end of 8 weeks.. A total of 471 cases completed the treatment. In Esomeprazole and Ilaparazole groups. After 8 weeks treatment, the healing rate in Esomeprazole group and Ilaparazole group were 82.79% (94.94%) and 83.54% (92.50%), respectively. The corresponding rate difference [Ilaparazole-esomeprazole] was 0.75% (-2.44%) and the two-sided 95% CI was -5.72 to 7.22 (-6.90 to 2.01). The symptom disappearance rates for FAS (PPS) were 75.81% (82.02%) and 76.71% (80.36%) P = 0.8223 (0.7742). Adverse reactions related to the drugs were: 10.70% and 11.80%, (P = 0.7817).. The efficacy and safety of Ilaparazole (10 mg/day) in treating reflux esophagitis was similar to esomeprazole (40 mg/day). Ilaparazole (10 mg/day) can be used in the treatment of esophagitis. The clinical trial registration number of the study is NCT 02860624.

Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Adult; Double-Blind Method; Drug Monitoring; Esomeprazole; Esophagitis, Peptic; Female; Gastroscopy; Humans; Male; Middle Aged; Proton Pump Inhibitors; Symptom Assessment; Treatment Outcome

Proton pump inhibitors (PPIs) are the main drugs for the treatment of reflux esophagitis. Previous studies have indicated ilaprazole to be safer and more effective in treating duodenal ulcers as compared with omeprazole. Being a novel PPI, ilaprazole may be used in the treatment of reflux esophagitis. The purpose of this study was to evaluate the safety and efficacy of ilaprazole tablets in the treatment of reflux esophagitis.. This study used a randomized, double-blind, multi-center, active-comparison design. The patients were randomly divided into an ilaprazole group (10 mg once daily and 15 mg once daily) and an esomeprazole group (40 mg once daily). Both the groups were treated for 8 weeks. Heartburn and reflux symptoms prior to treatment, and 4 and 8 weeks after the treatment were assessed. Gastroscopy was performed after 4 and 8 weeks. The healing rate after 4 weeks treatment was compared. If esophagitis was healed at the end of 4 weeks, patients did not undergo gastroscopy at the end of 8 weeks.. Three hundred and twenty-five patients were enrolled in this study. The 4-week full analysis set (per-protocol set) healing rates in the esomeprazole 40-mg group, the ilaprazole 10-mg group, and the ilaprazole 15-mg group were: 71.43 % (78.89 %), 81.31 % (86.73 %), and 71.70 % (81.40 %), respectively, p = 0.1595 (0.4122); the 8-week healing rates were 84.76 % (93.33 %), 88.79 % (94.90 %), and 85.85 % (97.67 %), respectively, p = 0.6689 (0.4049). Drug-related adverse events rate were 10.48 %, 14.02 %, and 15.09 %, respectively, in the three groups (p = 0.6114).. The efficacy and safety of ilaprazole (10 mg/day, 15 mg/day) in treating reflux esophagitis was similar to esomeprazole (40 mg/day). Ilaprazole (10 mg/day) has a smaller dosage, hence it should be considered more in clinical uses.. ClinicalTrials.gov NCT01107938.

Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Adult; Double-Blind Method; Esomeprazole; Esophagitis, Peptic; Female; Heartburn; Humans; Male; Middle Aged; Proton Pump Inhibitors

Ilaprazole, a proton pump inhibitor (PPI) currently in clinical use, may provide improved acid suppression vs. other PPIs.. To compare the pharmacodynamic and pharmacokinetic profiles of ilaprazole and esomeprazole.. A phase 1, randomised, open-label, single-centre, 4-period crossover study was conducted in 40 healthy volunteers. Ilaprazole 10, 20 or 40 mg or esomeprazole 40 mg was administered once daily for 5 days with ≥5-day washout intervals. Pharmacokinetic blood samples and intragastric pH measurements were collected at scheduled timepoints for 24 h after dosing on Days 1 and 5.. Esomeprazole 40 mg provided significantly better pH control during the initial hours (0-4 h) after a single dose, but ilaprazole (particularly 20 and 40 mg) provided significantly better pH control for the entire 24-h period and during evening and overnight hours after single and multiple doses. Increasing ilaprazole doses resulted in dose-proportional increases in peak plasma concentration and area under the plasma concentration vs. time curve following single and multiple doses. Ilaprazole was safe and generally well tolerated; an unexpectedly high incidence of allergic eye and skin reactions were observed but were not specific to any dosing regimen. Plasma gastrin concentrations did not increase proportionately with increasing ilaprazole dose.. Ilaprazole provided significantly better pH control over 24 h and during evening and overnight hours compared with esomeprazole in healthy volunteers, which may translate to greater relief of night-time heartburn in the clinical setting for patients with gastric acid-related disorders.

Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Administration, Oral; Adult; Anti-Ulcer Agents; Cross-Over Studies; Esomeprazole; Female; Gastrins; Healthy Volunteers; Humans; Hydrogen-Ion Concentration; Male; Middle Aged; Proton Pump Inhibitors

At present, little information on the biopharmaceutical behaviour of proton pump inhibitors (PPIs) describing their absorption and biodistribution in vivo has been reported because the extreme instability of PPIs in the gastrointestinal environment makes it difficult to analyze such behaviour. In this work, a modified rat in situ intestinal perfusion model was employed to investigate absorption in the gastrointestinal tract and subsequent biodistribution of several PPIs (ilaprazole, esomeprazole and rabeprazole), which have different physicochemical properties. Our data indicated that PPIs exhibited significantly enhanced absorption rates in the whole intestine, including the duodenum, jejunum, ileum and colon, corresponding to the increase in the oil-water partition coefficient (LogP). PPIs and corresponding salt types showed no obvious differences in absorption, implying that solubility changes in the PPI have little effect on its absorption in the gastrointestinal tract. Among these PPIs, ilaprazole presented a more stable intestinal absorption behaviour, as well as more distribution and longer residence time in the stomach by HPLC-MS/MS analysis and radioactivity counts after

Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Absorption, Physicochemical; Adsorption; Animals; Biological Products; Chemical Phenomena; China; Esomeprazole; Female; Ileum; Intestinal Absorption; Jejunum; Male; Proton Pump Inhibitors; Rabeprazole; Rats; Rats, Sprague-Dawley; Tandem Mass Spectrometry; Tissue Distribution

We developed and validated a simple, convenient and reproducible method for simultaneous estimation of six proton-pump inhibitors (PPIs), omeprazole (OPZ), esomeprazole (EOPZ), lansoprazole (LPZ), pantoprazole (PPZ), rabeprazole (RPZ) and ilaprazole (IPZ) in pharmaceutical dosage forms by a single marker. Meanwhile, the stability of the cited PPIs in 0.9% sodium chloride injection stored in polypropylene syringes up to 48 hours for continuous infusion use was investigated.. Under these conditions, all cited PPIs were separated simultaneously at a retention time of 6.0, 7.3, 7.3, 9.9, 12.5 and 13.9 min for RPZ, OPZ, EOPZ, IPZ, PPZ and LPZ, respectively, with a total run time less than 20.0 min. Comparative analysis results indicated that there were no significant differences observed between the QAMS method and the external standard method. The percentage of initial concentration of each PPI gradually decreased during the storage time.. The proposed method, which is selective, economical and accurate, was applied successfully for determination of the cited PPIs in their respective pharmaceutical dosage forms. Admixtures of OPZ, EOPZ, PPZ, IPZ in 0.9% sodium chloride injection were stable for 24 hours and LPZ, RPZ in 0.9% sodium chloride injection were stable for 8 hours in polypropylene syringes.

Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Chromatography, High Pressure Liquid; Drugs, Investigational; Esomeprazole; Humans; Lansoprazole; Molecular Structure; Omeprazole; Pantoprazole; Polypropylenes; Proton Pump Inhibitors; Rabeprazole

proton pump inhibitors (PPI) have been widely used in the clinic but inappropriate prescribing has also increased dramatically.. to describe the prescribing patterns and assess the appropriateness of the prescribed PPI use in 45 hospitals in China.. PPI prescriptions for non-hospitalized patients were collected from hospitals in Beijing, Chengdu, Guangzhou and Hangzhou of China over a 40-day period in 2016. These data were analyzed using the prescription number, proportion and economic indicators (defined daily dose system [DDD], defined daily cost [DDC] and drug utilization index [DUI]). The evaluation criteria of PPI use was based on Martindale: The Complete Drug Reference, New Materia Medica and drug instructions.. in total, 357,687 prescriptions using oral PPI and 38,216 prescriptions using injectable PPI were assessed. The average age of PPI users was 53 years. The most commonly used oral PPI was rabeprazole, while the most common injectable PPI was pantoprazole. The DDD of oral rabeprazole and DDC of injectable rabeprazole were the highest. Meanwhile, only the DUI values of oral rabeprazole, lansoprazole and ilaprazole were less than 1.0. The clinical diagnosis of some users included well identified risky comorbidities such as kidney disease (2.9%). Furthermore, between 32.6% and 56.8% of the PPI prescriptions were used for inappropriate indications.. this survey demonstrated that PPI use was accompanied by unapproved indications and excessive dosages. Comprehensive measures are urgently needed to improve PPI use and reduce unnecessary drug costs.

Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Adolescent; Adult; China; Comorbidity; Esomeprazole; Female; Health Care Surveys; Hospitals; Humans; Inappropriate Prescribing; Lansoprazole; Male; Middle Aged; Pantoprazole; Proton Pump Inhibitors; Rabeprazole; Young Adult