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OBJECTIVE To understand the safety of Ilaprazole sodium for injection in clinical practice. METHODS From Jan. 1st 2019 to Feb. 29th 2020， the data of 3 926 valid hospitalized patients receiving Ilaprazole sodium for injection were collected prospectively from 5 third-level hospitals through CHPS， and the post-marketing safety analysis was performed by using retrospective multicenter single cohort study. At the same time， a nested case-control study （the ratio of trial group and control group was 1∶4） was used to confirm the baseline stability of this study cohort and the correlation between adverse reactions and Ilaprazole sodium for injection. RESULTS Among 3 926 patients， 3 patients experienced 5 adverse drug events after using Ilaprazole sodium for injection， with the incidence of 0.076%. There was no serious adverse event， and the occurrence time was 2 days after medication； adverse drug events mainly include elevated liver function indicators （alanine transaminase， aspartate transaminase， total bilirubin）， which were mild and untreated， and all adverse drug events were improved. The results of the nested case-control study showed that the trial group and the control group belonged to the same background baseline， and the occurrence of adverse drug events was more closely related to Ilaprazole sodium for injection. CONCLUSIONS The overall safety of Ilaprazole sodium for injection is relatively high， and the occurrence of adverse events is more related to it.
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Objective To evaluate the efficacy and safety of Ilaprazole Enteric-Coated Tablets in the treatment of RE. Methods The databases of CNKI, VIP, Wanfang Data, PubMed, Embase, and The Cochrane Library were searched to collect all the randomized controlled trials (RCTs) of Ilaprazole in the treatment of RE published before April 2021. After data extraction and quality evaluation, the RCTs meeting the inclusion criteria were performed, and the meta-analysis was conducted by RevMan 5.4. Results Nine RCTs were included, with a total of 1115 patients of RE. The results of the meta-analysis showed that Ilaprazole Enteric-Coated Tablets were comparable to Esomeprazole Enteric-Coated Tablets in both endoscopic efficiency (90.08% vs. 90.00%, P > 0.05) and symptom relief rates (91.79% vs. 91.23%, P > 0.05), and there was no statistically significant difference in the incidence of adverse reactions (7.99% vs. 8.66%, P > 0.05). Conclusion Ilaprazole Enteric-Coated Tablets with lower doses were comparable to Esomeprazole Enteric-Coated Tablets which showed good efficacy and safety in the treatment of reflux esophagitis.
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Objective:To explore the efficacy and safety of intermittent infusion of ilaprazole sodium and high-dose continuous infusion of esomeprazole sodium in preventing rebleeding in patients with peptic ulcer bleeding after successful endoscopic hemostasis.Methods:This is a multi-center, interval randomized, double-blind, double-dummy, parallel controlled study. From March 3rd to June 15th, 2021, 151 patients with high risk of peptic ulcer bleeding and successfully underwent endoscopic hemostasis from 33 hospitals including the First Affiliated Hospital of Zhejiang University School of Medicine were enrolled. Patients were interval randomly divided into the trial group (74 cases) and the control group (77 cases). Patients in the trial group received intermittent intravenous infusion of ilaprazole sodium once daily (20 mg administered as a 60 min intravenous infusion on day 1, and 10 mg administered as a 30 min intravenous infusion on day 2 and 3); patients in the control group received continuous intravenous infusion of esomeprazole sodium for 72 h (esomeprazole sodium 80 mg at first dose in half an hour, and 8 mg per hour continuous intravenous infusion for 71.5 h). After intravenous infusion treatment, patients of both groups were given oral ilaprazole enteric-coated tablets, 10 mg each time, once a day for 4 d. The rebleeding rate after 72 h and within 7 d after treatment and the proportion of patients who received endoscopic retreatment or surgery due to rebleeding within 72 h after treatment were analysised based on the full analysis set (72 cases in the trial group and 75 cases in the control group); and the incidence rate of adverse reactions was observed in the two groups based on the safety analysis set (74 cases in the trial group and 76 cases in the control group). Chi-square test or Fisher exact probability test was used for statistical analysis.Results:There was no rebleeding case in the trial group within 72 h and 1 case of rebleeding within 7 d (1.39%, 1/72). In the control group, there was 1 case of rebleeding (1.33%, 1/75) within 72 h and 4 cases of rebleeding (5.33%, 4/75) within 7 d. There was no significant difference in rebleeding rate either after 72 h or within 7 d after treatment between the two groups (both P>0.05). Within 72 h of treatment, no patients in both groups needed endoscopic or surgical retreatment due to rebleeding. Adverse reactions occurred in 5 cases (6.8%, 5/74) and 6 cases (7.9%, 6/76) in the trial group and control group, respectively, which recovered spontaneously without treatment. No serious adverse reactions occurred in both groups. Conclusion:In patients with high-risk peptic ulcer bleeding with successful endoscopic hemostasis, intermittent intravenous infusion of ilaprazole sodium has similar efficacy and safety as continuous high-dose intravenous infusion of esomeprazole sodium, but the dosage of intermitten regimen is less, the administration is more convenient, and it is worthy of clinical promotion.
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OBJECTIVE: To rapidly evaluate the efficacy, safety and economical efficiency of ilaprazole enteric-coated tablets in the treatment of duodenal ulcer, so as to provide evidence-based evidence for clinical rational drug use. METHODS: PubMed, Embase, the Cochrane Library, CNKI, WanFang database and health technology assessment (HTA) organization websites were searched systematically. HTA reports, systematic reviews/Meta-analysis and pharmacoeconomic studies comparing ilaprazole with other drugs for duodenal ulcer treatment were included. Qualitative and descriptive analysis were performed on the included studies. RESULTS: A total of 10 literatures were included, including five systematic reviews/Meta-analysis and six pharmacoeconomic research (one systematic reviews/Meta-analysis also carried out pharmacoeconomic research). The efficacy of ilaprazole (10 mg•d-1) was comparable to other PPIs regimens in the treatment of duodenal ulcer, and there was no statistically significant difference in the efficacy of ilaprazole (10 mg•d-1) and ilaprazole (5 mg•d-1). Compared with H2 receptor antagonists, ilaprazole (10 mg•d-1) was significantly better than ranitidine and famotidine in the treatment of duodenal ulcer. In terms of safety, there was no statistical difference in the incidence of adverse reactions between ilaprazole (10 mg•d-1) and other PPIs or H2 receptor antagonists. In terms of the economics of treating duodenal ulcer, ilaprazole (10 mg•d-1) was not economical compared to esmeprazole (40 mg•d-1), while ilaprazole (5 mg•d-1) was more economical than rabeprazole (10 mg•d-1). CONCLUSION: Ilaprazole enteric-coated tablets are safe and effective in the treatment of duodenal ulcer, not inferior to other PPIs, and have economic advantages compared with rabeprazole. Because ilaprazole (10 mg•d-1) and ilaprazole (5 mg•d-1) have comparable efficacy, a low-dose regimen could be considered clinically to further improve its safety and cost performance. At the same time, it is necessary to further carry out clinical and pharmacoeconomic studies of low-dose ilaprazole in the treatment of duodenal ulcer to improve the relevant evidence.
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In Korea and China, ilaprazole is a widely used proton pump inhibitor in the treatment of gastric ulcers. In this study, a specific and sensitive LC-MS/MS method has been developed and validated for the quantification of ilaprazole enantiomers in the rat plasma, using R-lansoprazole as the internal standard. The enantioseparation was achieved on a CHIRALPAK AS-RH column (4.6 mm × 150 mm, i.d. 5μm), with a mobile phase composed of 10 mM ammonium acetate aqueous solution and acetonitrile (60:40, V/V), at a flow-rate of 0.5 mL/min. The method was validated over the concentration range of 0.5-300 ng/mL for both, R- and S -ilaprazole. The lower limit of quantification was 0.5 ng/mL for both enantiomers. The relative standard deviation (RSD) of intra- and inter-day precision of R-ilaprazole and S-ilaprazole was less than 10.9％, and the relative error accuracy (RE) ranged from -0.5％-2.0％. Finally, the method was successfully evaluated in rats in a stereoselective pharmacokinetic study of the ilaprazole racemate.
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In this study, the relationships between 15N-NMR and 13C-NMR chemical shifts of omeprazole, lansoprazole, ilaprazole,pantoprazole, and rabeprazole and their physicochemical and pharmacokinetic properties, namely, pKa, half-life,tmax, logP, and protein binding were investigated. This study also presents the first report of 15N-NMR spectroscopicstudies of lansoprazole, pantoprazole, and ilaprazole. It was found that 15N-NMR chemical shifts of the doubly bondedbenzimidazole nitrogen of proton pump inhibitors showed correlation with pKa2, protein binding and logP, while 15NNMR chemical shifts of the pyridine nitrogen correlate with protein binding and tmax. Sum of 15N-NMR chemical shiftsand sum of 13C-NMR chemical shifts, both, exhibit correlation with half-life, logP, and tmax. The sum of 13C chemicalshifts of the pyridine moiety exhibits correlation with pKa1, while the sum of 13C chemical shifts of the benzimidazolemoiety exhibits correlation with half-life. NMR chemical shifts may, hence, be useful as molecular descriptors in thedevelopment of Quantitative Structure/Spectral Data Property Relationship models.
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Objective To evaluate the efficacy and safety of ilaprazole sodium for injection in the treatment of peptic ulcer bleeding.Methods It was designed as a multi-center,stratified randomized,double-blind,positive drug parallel controlled and non-inferiority study.From October 2014 to April 2015,at 40 hospitals,patients with peptic ulcer hemorrhage confirmed by gastroendoscopy were enrolled and divided into the ilaprazde sodium group (10 mg ilaprazole sodium for injection every 24 h,the first dose doubled) and the positive control group (40 mg of omeprazole sodium for injection every 12 h).The course of both treatment was 72 h.The hemostasis rate of overall group at 72 h,the clinical rebleeding rate at four to seven days,the blood transfusion rate,the incidence of switching to other treatments and the incidence of adverse reactions were compared between the two groups.A chi-square test or Fisher's exact probability method were performed for statistical analysis.Results A total of 533 patients with peptic ulcer bleeding were enrolled,355 patients in the ilaprazole sodium group and 178 patients in the positive control group.The hemostasis rates of ilaprazole sodium group and positive control group at 72 h were 97.69 ％ (339/347) and 97.14 ％ (170/175),respectively,and the difference was not statistically significant (P＞0.05).There were no rebleeding patients in both groups at four to seven days.The blood transfusion rates of ilaprazole sodium group and positive control group were 5.07 ％ (18/355) and 3.37 ％ (6/178).The incidence of switching to other treatments was 0.56％ (2/355) and 0.56％ (1/178),respectively,and the differences were not statistically significant (both P＞ 0.05).The incidence of adverse reactions in the ilaprazole sodium group was 3.94％ (14/355),which was lower than that of positive control group (8.43％,15/178).And the difference was statistically significant (Fisher's exact probability method,P=0.042).Conclusions The efficacy of ilaprazole sodium for injection in the treatment of peptic ulcer bleeding is similar to that of omeprazole sodium for injection.Moreover,the smaller the dose,the lower the frequency of administration and the better the safety.
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PURPOSE: Patients with gastroesophageal reflux disease without esophagitis show varying responses to proton pump inhibitors (PPIs). The aim of this study was to objectively evaluate the effect of a new PPI, ilaprazole, on patients with heartburn but without reflux esophagitis. MATERIALS AND METHODS: This prospective study was performed on 20 patients with heartburn but without reflux esophagitis. All patients underwent upper endoscopy and 24-hr combined multichannel intraluminal impedance and pH esophageal monitoring (MII-pH). They were then treated with ilaprazole (20 mg) once daily for 4 weeks. The GerdQ questionnaire, histologic findings, and inflammatory biomarkers were used for assessment before and after ilaprazole. RESULTS: Among the 20 patients, 13 (65%) showed GerdQ score ≥8. Based on MII-pH results, patients were classified as true nonerosive reflux disease (n=2), hypersensitive esophagus (n=10), and functional heartburn (n=8). After treatment, patients showed a statistically significant improvement in GerdQ score (p < 0.001). Among histopathologic findings, basal cell hyperplasia, papillary elongation, and infiltration of intraepithelial T lymphocytes improved significantly (p=0.008, p=0.021, and p=0.008; respectively). Expression of TNF-α, IL-8, TRPV1, and MCP-1 decreased marginally after treatment (p=0.049, p=0.046, p=0.045, and p=0.042; respectively). CONCLUSION: Daily ilaprazole (20 mg) is efficacious in improving symptom scores, histopathologic findings, and inflammatory biomarkers in patients with heartburn but no reflux esophagitis.
Subject(s)
Humans , Arm , Biomarkers , Electric Impedance , Endoscopy , Esophagitis , Esophagitis, Peptic , Esophagus , Gastroesophageal Reflux , Heartburn , Hydrogen-Ion Concentration , Hyperplasia , Interleukin-8 , Prospective Studies , Proton Pump Inhibitors , T-LymphocytesABSTRACT
Objective To investigate the clinical efficacy of ilaprazole and bismuth combined ten-day standard quadruple therapy and sequential therapy in the treatment of patients with Helicobacter pylori (H .pylori)infected chronic gastritis.Methods A total of 200 patients with H .pylori-positive chronic gastritis diagnosed by gastroendoscopy examination and rapid urease test (RUT)were randomly divided into standard quadruple therapy group and sequential therapy group,100 cases in each group.One group received ilaprazole,bismuth,amoxicillin-clavulanatepotassium and ofloxacin 10-day standard quadruple therapy, and the other group received ilaprazole, amoxicillin-clavulanatepotassium, ofloxacin and furazolidone 10-day sequential therapy.In four to six weeks after the therapy,the condition of H .pylori eradication was detected by a 14 C-urea breath test.The improvement of clinical symptoms and adverse effects were also observed. Normal distributed and variance homogenized measurement data were compared by t test,while unordered categorical data were analyzed by chi-square test and the exact probability method,and categorical data were compared by two independent sample rank sum test.Results The per-protocol analysis values of H .pylori eradication rates of the standard quadruple therapy group and the sequential therapy group were 88.54%(85/96)and 87.23%(82/94),respectively,while the intention-to-treat analysis values were 85 .00%(85/100)and 82.00%(82/100 ),respectively.The effective rates of symptomatic relief of upper abdominal pain,acid regurgitation,heart burning in the standard quadruple therapy group and the sequential therapy group were 95 .83%(92/96)and 95 .74%(90/94),respectively. The incidence of adverse effects which weve very mild was 6.25 % (6/96 ) and 7.44% (7/94 ), respectively.There was no statistically significant difference in the above three factors between the two groups (all P >0.05).Conclusions Ilaprazole and bismuth combined 10-day standard quadruple therapy and sequential therapy in the treatment of patients with H .pylori positive chronic gastritis both achieves high rates of H .pylori eradication and symptom relief with mild adverse effects.
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Objective To compare the clinical efficacy of ilaprazole standard triple therapy with omeprazole standard triple therapy in the treatment of patients with Helicobacter pylori ( Hp ) positive duodenal bulb ulcer. Methods 100 patients with Hp positive duodenal bulb ulcer were randomly divided into the two groups by lottery, given ilaprazole standard triple therapy and omeprazole standard triple therapy respectively.After 5 weeks of the course,take gastroscopy and the enzyme 13C-urea breath test,and the Hp eradication rate,clinical efficacy,ulcer heal-ing rate and adverse reactions were observed.Results The Hp eradication rate is better than the omeprazole group (92%vs 78%,χ2 =3.853,P0.05).Conclusion It is a good method in the treatment of Hp positive duodenal bulb ulcer for ilaprazole stand-ard triple therapy.
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The present study was an attempt to formulate and evaluate enteric coated tablets for Ilaprazole to reduce the gastrointestinal tract side effects. Four formulations of core tablets were prepared and one who shows rapid disintegration (near around three minutes) was selected for enteric coating. Ilaprazole which have an irritant effect on the stomach can be coated with a substance that will only dissolve in the small intestine. Enteric coat was optimized using two different polymers such as HPMCP 50 and Eudragit L 100 in different concentrations. The prepared tablets were evaluated in terms of their pre-compression parameters, physical characteristics and in-vitro release study. 2.5% seal coating on core tablets was optimized and 9% enteric coating on seal coated tablets was performed using HPMC P 50 (60%), triethyl citrate (10%) and IPA:DCM (60:40) which gives the highest dissolution release profile and f2 value.
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The present study was an attempt to formulate and evaluate enteric coated tablets for Ilaprazole to reduce the gastrointestinal tract side effects. Four formulations of core tablets were prepared and one who shows rapid disintegration (near around three minutes) was selected for enteric coating. Ilaprazole which have an irritant effect on the stomach can be coated with a substance that will only dissolve in the small intestine. Enteric coat was optimized using two different polymers such as HPMCP 50 and Eudragit L 100 in different concentrations. The prepared tablets were evaluated in terms of their pre-compression parameters, physical characteristics and in-vitro release study. 2.5% seal coating on core tablets was optimized and 9% enteric coating on seal coated tablets was performed using HPMC P 50 (60%), triethyl citrate (10%) and IPA:DCM (60:40) which gives the highest dissolution release profile and f2 value.
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Objective To observe the clinical effect of ilaprazole in the treatment of peptic ulcer.Methods 100 patients with peptic ulcer were randomly divided into omeprazole group and ilaprazole group,50 cases in each group.The patients were given omeprazole or ilaprazole combined with amoxicillin and clarithromycin.The treatment effects and clinical symptom relief satisfaction rate were compared between the two groups.Results After treatment,the results under gastroscopy:in ilaprazole group,20 cases cured,16 cases healed,9 cases were effective and 5 cases were invalid.Those in omeprazole group were 14 cases,12 cases,12 cases,12 cases respectively.The differences between the two groups were statistically significant(U =3.78,P ＜ 0.05).The removal rate of Helicobacter pylori and clinical symptom relief satisfaction rate of ilaprazole group were significantly higher than those of the omeprazole group(x2 =3.84,4.57,P ＜ 0.05).Conclusion Ilaprazole can obtain good clinical effect in treatment of peptic ulcer,with high symptom relief satisfaction rate and clearance of Helicobacter pylori.
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Objective To analyze the clinical effects and pharmacoeconomics of ilaprazole in the treatment of reflux esophagitis.Methods 80 reflux esophagitis patients were selected as research subjects,who were divided into observation group and the control group,each group 40 cases according to the random number table.The observation group was given ilaprazole treatment,the dose for the 10mg/d;the control group received esomeprazole treatment,the dose for the 40mg/d.After 8 weeks of treatment,the clinical efficacy and cost of treatment of the two groups were compared.The ilaprazole clinical efficacy and pharmacoeconomics treatment of reflux esophagitis was explored.Results (1) After 8 weeks of treatment,symptom scores in patients of the observation group(0.7 ± 0.3)point,compared with before treatment(3.1 ± 0.8) point was significantly lower,the difference was statistically significant (t =16.7,P ＜0.01).The control group patients after symptom score(0.4 ±0.3) than before treatment(3.2 ±0.9) was also significantly reduced,the difference was statistically significant (t =18.6,P ＜0.01) ;there was no statistically significant in score after 8 weeks of treatment between the two groups(t =0.00,P ＞0.05).35 cases in the observation group had markedly effectiveness in 2cases,the total effective rate was 92.5％ ;36 cases in control group had markedly effectiveness in 2 cases,the total rate was 95％ ;efficiency of treatment of the two groups of patients was compared with that difference was not statistically significant(x2 =0.21,P ＞0.05).3) The analysis found that the observation group 34 cases were cured,improved in 2 cases,total effective rate was 90％ ;the control group,35 cases were cured,2 cases improved endoscopic efficacy in two groups of patients after 8 weeks of treatment,the total was 92.5％ ;4) There was no statistically significant difference in the efficiency of treatment of the two groups (x2 =0.15,P ＞0.05).The cost of treatment between the two groups was not statistically significant (t =0.99,P ＞ 0.05).Conclusion Ilaprazole has the similar clinical effect and cost with esomeprazole in the treatment of reflux esophagitis,and ilaprazole is an effective drug for treatment of reflux esophagitis.
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Objective To systematically review the efficacy of ilaprazole in duodenal ulcer by Meta analysis.Methods Randomized controlled trial (RCT) comparing ilaprazole with other proton pump inhibitors in duodenal ulcer were searohed for Meta analysis.Results Six RCT met the inclusion criteria and 1319 patients were included.Meta analysis showed that the healing rate at 4-week in the dose of ilaprazole 10 mg/d was higher than that in control group [ 89.1％ (591/663 ) vs.86.4％ (426/493) ],but there was no significant difference (P＞ 0.05 ).When including high-quality literature,English literature,Chinese literature,or the literature using omeprazole as control,there was no significant difference either (P ＞ 0.05 ).The adverse rate in the two groups had no significant difference [ 9.7％ (64/663) vs.12.6％ (62/493)] (P ＞0.05 ).The 4-week healing rate between the doses of ilaprazole 5 mg/d and 10 mg/d had no significant difference [84.7％(138/163) vs.84.0％(131/156)](P＞0.05).Conclusions Ilaprazole has high healing rate for duodenal ulcer,with low adverse rate.The effect of the dose ot5 mg/d is comparable to 10 mg/d.
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Objective To evaluate the effect of ilaprazole enteric tablets on intragastric pH in duodenal ulcer patients. Methods A randomized, double blind, positive controlled clinical trial was carried out. A total of forty-two patients with duodenal ulcer were randomized into low dose ilaprazole group (5 mg/d), medium dose ilaprazole group (10 mg/d), high dose ilaprazole group(20 mg/d) and omeprazole group(20 mg/d). An ambulatory 24 hour intragastric pH study was performed at the fifth treatment day. Fraction time pH above 3, 4 or 5, median values of 24 hour diurnal pH and 12 hour nocturnal pH, the percentage of patients with total time pH above 3, 4 or 5 at least for 18 hours were evaluated. Results There were no significant differences of fraction time pH above 3 or 4, median values of 24 hour diurnal pH and 12 hour nocturnal pH and the percentage of patients with total time pH above 3, 4 or 5 at least for 18 hours among all the groups with different doses of ilaprazole and the omeprazole group. The fraction time pH above 5 in medium and high dose ilaprazole groups were (87.96 ± 12. 29)% and (89.86±15. 18)% respectively, which was higher than that in low dose ilaprazole group [(67. 17± 30. 16)%] and omeprazole group[(76. 14 ± 16. 75)%], P <0. 05. Conclusion Ilaprazole has a strong effect on intragastric acid control with a dose dependent trend.