Aim To evaluate the pharmacokinetics and bioequivalence of domestic pantoprazole sodium enteric-coated tablets as compared with imported pantoprazole enteric-coated tablets. Methods This was an open randomized, two pe...Aim To evaluate the pharmacokinetics and bioequivalence of domestic pantoprazole sodium enteric-coated tablets as compared with imported pantoprazole enteric-coated tablets. Methods This was an open randomized, two periods cross over study on twenty healthy male volunteers. The pantoprazole concentrations in plasma after an oral dose of 40 mg pantoprzaole preparations were determined by a HPLC-UV method. Non-compartmental method was used for the calculation of pharmacokinetic parameters. Logarithm-transformed Cmax and A UC were analyzed by the analysis of variance (ANOVA) with 90% confidence intervals. Results The main pharmacokinetics parameters of domestic pantoprazole sodium enteric-coated tablets and imported pantoprazole sodium enteric-coated tablets were as following: Cmax (3610 ± 956), (3466 ± 1209) ng·mL^-1, tmax (3.00 ± 0.40), (3.00 ± 0.46) h, AUC0-t (8140 ± 5065), (8390 ± 5474) ng·h·mL^-1, AUC0-∞ (8293 ± 5094), (8625 ± 5606) ng·h·mL^-1, t1/2 (1.61 ± 0.28), (1.85 ± 0.27) h, respectively. Conclusion Domestic pantoprazole sodium enteric-coated tablets were bioequivalent with the imported pantoprazole sodium enteric-coated tablets.展开更多
AIM: To compare the effi cacy and tolerability of S-pan- toprazole (20 mg once a day) versus racemic Panto- prazole (40 mg once a day) in the treatment of gastro- esophageal reflux disease (GERD). METHODS: This multi-...AIM: To compare the effi cacy and tolerability of S-pan- toprazole (20 mg once a day) versus racemic Panto- prazole (40 mg once a day) in the treatment of gastro- esophageal reflux disease (GERD). METHODS: This multi-centre, randomized, double-blind clinical trial consisted of 369 patients of either sex suf- fering from GERD. Patients were randomly assigned to receive either one tablet (20 mg) of S-pantoprazole once a day (test group) or 40 mg racemic pantoprazole once a day (reference group) for 28 d. Patients were evaluated for reduction in baseline on d 0, GERD symptom score on d 14 and 28, occurrence of any adverse effect during the course of therapy. Gastrointestinal (GI) endoscopy was performed in 54 patients enrolled at one of the study centers at baseline and on d 28. RESULTS: Signifi cant reduction in the scores (mean and median) for heart burn (P < 0.0001), acid regurgitation (P < 0.0001), bloating (P < 0.0001), nausea (P < 0.0001) and dysphagia (P < 0.001) was achieved in both groups on d 14 with further reduction on continuing the therapy till 28 d. There was a statistically signifi cant difference in the proportion of patients showing improvement in acid regurgitation and bloating on d 14 and 28 (P = 0.004 for acid regurgitation; P = 0.03 for bloating) and heart burn on d 28 (P = 0.01) between the two groups, with a higher proportion in the test group than in the refer- ence group. Absolute risk reductions for heartburn/acid regurgitation/bloating were approximately 15% on d 14 and 10% on d 28. The relative risk reductions were 26%-33% on d 14 and 15% on d 28. GI endoscopy showed no signifi cant difference in healing of esophagitis (P = 1) and gastric erosions (P = 0.27) between the two groups. None of the patients in either group reported any adverse effect during the course of therapy.CONCLUSION: In GERD, S-pantoprazole (20 mg) is more effective than racemic pantoprazole (40 mg) in improving symptoms of heartburn, acid regurgitation, bloating and equally effective in healing esophagitis and gastric erosions. The relative risk reduction is 15%-33%. Both drugs are safe and well tolerated.展开更多
AIM: To clarify whether there is any difference in the symptom relief in patients with reflux esophagitis following the administration of four Proton pump inhibitors (PPIs). METHODS: Two hundred and seventy-four patie...AIM: To clarify whether there is any difference in the symptom relief in patients with reflux esophagitis following the administration of four Proton pump inhibitors (PPIs). METHODS: Two hundred and seventy-four patients with erosive reflux esophagitis were randomized to receive 8 wk of 20 mg omeprazole (n = 68), 30 mg of lansoprazole (n = 69), 40 mg of pantoprazole (n = 69), 40 mg of esomeprazole (n = 68) once a day in the morning. Daily changes in heartburn and acid reflux symptoms in the first 7 d of administration were assessed using a six-point scale (0: none; 1: mild; 2: mild-moderate; 3: moderate; 4: moderate-severe; 5: severe). RESULTS: The mean heartburn score in patients treated with esomeprazole more rapidly decreased than those receiving other PPI. Complete resolution of heartburn was also more rapid in patients treated with esomeprazole for 5 d compared with omeprazole (P = 0.0018, P = 0.0098, P = 0.0027, P = 0.0137, P = 0.0069, respectively), lansoprazole (P = 0.0020, P = 0.0046, P = 0.0037, P = 0.0016, P = 0.0076, respectively), and pantoprazole (P = 0.0006, P = 0.0005, P = 0.0009, P = 0.0031, P = 0.0119, respectively). There were no significant differences between the four groups in the rate of endoscopic healing of reflux esophagitis at week 8. CONCLUSION: Esomeprazole may be more effective than omeprazole, lansoprazole, and pantoprazole for the rapid relief of heartburn symptoms and acid reflux symptoms in patients with reflux esophagitis.展开更多
AIM: To define the prevalence of gastroesophageal reflux disease (GERD) in mild persistent asthma and to value the effect of pantoprazole therapy on asthmatic symptoms.METHODS: Seven of thirty-four asthmatic patie...AIM: To define the prevalence of gastroesophageal reflux disease (GERD) in mild persistent asthma and to value the effect of pantoprazole therapy on asthmatic symptoms.METHODS: Seven of thirty-four asthmatic patients without GERD served as the non-GERD control group. Twenty-seven of thirty-four asthmatic patients had GERD (7/27 also had erosive esophagitis, sixteen of them presented GERD symptoms. An upper gastrointestinal endoscopy was performed in all the subjects to obtain five biopsy specimens from the lower 5 cm of the esophagus. Patients were considered to have GERD when they had a dilation of intercellular space (DIS)〉0.74 μm at transmission electron microscopy. Patients with GERD were treated with pantoprazole, 80 mg/day. Forced expiratory volume in one second (FEV1) was performed at entry and after 6 mo of treatment. Asthmatic symptoms were recorded. The required frequency of inhaling rapid acting β2-agonists was self-recorded in the patients' diaries.RESULTS: Seven symptomatic patients presented erosive esophagitis. Among the 18 asymptomatic patients, 11 presented DIS, while all symptomatic patients showed ultrastructural esophageal damage. Seven asymptomatic patients did not present DIS. At entry the mean of FEV1 was 1.91 L in symptomatic GERD patients and 1.88 L in asymptomatic GERD patients. After the treatment, 25 patients had a complete recovery of DIS and reflux symptoms. Twenty-three patients presented a regression of asthmatic symptoms with normalization of FEV1. Four patients reported a significant improvement of symptoms and their FEV1 was over 80%.CONCLUSION: GERD is a highly prevalent condition in asthma patients. Treatment with pantoprazole (80 mg/day) determines their improvement and complete regression.展开更多
Pantoprazole sodium, a substituted benzimidazole derivative, is an irreversible proton pump inhibitor which is primarily used for the treatment of duodenal ulcers, gastric ulcers, and gastroesophageal reflux disease (...Pantoprazole sodium, a substituted benzimidazole derivative, is an irreversible proton pump inhibitor which is primarily used for the treatment of duodenal ulcers, gastric ulcers, and gastroesophageal reflux disease (GERD). The monographs of European Pharmacopoeia (Ph. Eur.) and United States Pharmacopoeia (USP) specify six impurities, viz.;impurities A, B, C, D, E and F, respectively for its active pharmaceutical ingredient (API). The identification and synthesis of all impurities except impurity E are well described in the literature;however, there is no report related to impurity E. The prospects to the formation and controlling of impurity E up to -0.03% in the synthesis of pantoprazole sodium sesquihydrate (PAN) were discussed in detail for the first time. The present work described the journey towards the successful development of an optimal preparation procedure of dimer impurity E. The most plausible mechanism involved in the formation of impurity E has been proposed.展开更多
AIM: To evaluate esophageal mucosal defense mechanisms at an epithelial level to establish if pantoprazole treatment can induce ultrastructural healing and improvement in the proliferation activity of the esophageal e...AIM: To evaluate esophageal mucosal defense mechanisms at an epithelial level to establish if pantoprazole treatment can induce ultrastructural healing and improvement in the proliferation activity of the esophageal epithelium in gastroesophageal reflux disease (GERD). METHODS: This was a single-blinded study for pHmonitoring, and histological, ultrastructural and MIB1 immunostaining evaluation. Fifty eight patients with GERD were enrolled and underwent 24 h pH-monitoring and endoscopy. Patients were treated for 12 and 24 mo with pantoprazole. Esophageal specimens were taken for histological and ultrastructural evaluation, before and after the treatment. RESULTS: With transmission electron microscopy, all patients with GERD showed ultrastructural signs of damage with dilation of intercellular spaces (DIS). After 3 mo of therapy the mean DIS values showed asignificant reduction and the mean MIB1-LI values of GERD showed an increase in cell proliferation. A further 3 mo of therapy significantly increased cell proliferation only in the erosive esophagitis (ERD) group. CONCLUSION: Three months of pantoprazole therapy induced ultrastructural healing of mucosal damage in 89% and 93% of ERD and non-erosion patients, respectively. Moreover, long-term pantoprazole treatment may be helpful in increasing the capability for esophageal cell proliferation in GERD, particularly in ERD patients.展开更多
Background: This study evaluated the effect of omeprazole or pantoprazole on platelet reactivity in non-STsegment elevation acute coronary syndrome(NSTE-ACS) patients receiving clopidogrel.Methods: Consecutive patient...Background: This study evaluated the effect of omeprazole or pantoprazole on platelet reactivity in non-STsegment elevation acute coronary syndrome(NSTE-ACS) patients receiving clopidogrel.Methods: Consecutive patients with NSTE-ACS(n =620) from general hospital of Shenyang Military Command were randomized to the omeprazole or pantoprazole(20mg/d) group(1:1), and received routine dual antiplatelet treatment. Patients' reversion rate of adenosine diphosphate-induced platelet aggregation(ADP-PA) was assessed at baseline, 12 to 24 h after administration of medication, and after 72 h of percutaneous coronary intervention(PCI). The primary endpoint of the study was platelet reactivity assessed with ADP-PA at 30 days after PCI. Adverse events(AEs) were recorded for 30-day and 180-day follow-up periods.Results: There were no significant differences between both the groups in platelet response to clopidogrel at 12–24h after drug administration(54.09%±18.90% vs. 51.62%±19.85%, P=0.12), 72 h after PCI(52.15%±19.45% vs. 49.66%±20.05%, P=0.18), and 30 days after PCI(50.44%±14.54% vs. 48.52%±15.08%, P=0.17). The rate of AEs did not differ significantly between groups during the 30-day(15.2% vs. 14.8%, P=0.91) and 180-day(16.5% vs. 14.5%, P=0.50) follow-up periods after PCI.Conclusion: The addition of omeprazole or pantoprazole to clopidogrel did not restrict the effect of platelet aggregation by reducing the conversion of clopidogrel. Compared with clopidogrel alone, pantoprazole-clopidogrel and omeprazoleclopidogrel combinations did not increase the incidence of adverse clinical events during 30-day and 180-day follow-up periods after PCI.展开更多
AIM:To investigate the in vitro effects of pantoprazole on rat lower esophageal sphincter(LES)tone.METHODS:Rats weighing 250-300 g,provided by the Yeditepe University Experimental Research Center(Yü-DETAM),were u...AIM:To investigate the in vitro effects of pantoprazole on rat lower esophageal sphincter(LES)tone.METHODS:Rats weighing 250-300 g,provided by the Yeditepe University Experimental Research Center(Yü-DETAM),were used throughout the study.They were anesthetized before decapitation.LES tissues whose mucosal lining were removed were placed in a stan-dard 30-mL organ bath with a modif ied Krebs solution and continuously aerated with 95% oxygen-5% carbon dioxide gas mixture and kept at room temperature.The tissues were allowed to stabilize for 60 min.Sub-sequently,the contractile response to 10-6 mol/L carba-chol was obtained.Different concentrations of freshly prepared pantoprazole were added directly to the tis-sue bath to generate cumulative concentrations of 5×10-6 mol/L,5×10-5 mol/L,and 1.5×10-4 mol/L.Activi-ties were recorded on an online computer via a 4-channeltransducer data acquisition system using the software BSL PRO v 3.7,which also analyzed the data.RESULTS:Pantoprazole at 5×10-6 mol/L caused a small,but statistically insignif icant,relaxation in the car-bachol-contracted LES(2.23% vs 3.95%).The 5×10-5 mol/L concentration,however,caused a signif icant relax-ation of 10.47% compared with the control.1.5×10-4 mol/L concentration of pantoprazol caused a 19.89% relaxation in the carbachol contracted LES(P<0.001).CONCLUSION:This is the fi rst study to demonstrate that pantoprazole has a relaxing effect in isolated LESs.These results might have signif icant clinical implications for the subset of patients using proton pump inhibitors who do not receive full symptomatic alleviation from gastroesophageal reflux disease.展开更多
A specific, precise and stability indicating high-performance thin-layer chromatographic method for simultaneous estimation of pantoprazole sodium and itopride hydrochloride in pharmaceutical formulations was develope...A specific, precise and stability indicating high-performance thin-layer chromatographic method for simultaneous estimation of pantoprazole sodium and itopride hydrochloride in pharmaceutical formulations was developed and validated. The method employed TLC aluminium plates precoated with silica gel 60F254 as the stationary phase. The solvent system consisted of methanol:water:ammonium acetate; 4.0:1.0:0.5 (v/v/v). This system was found to give compact and dense spots for both itopride hydrochloride (Rf value of 0.55__+0.02) and pantoprazole sodium (Rf value of 0.85+0.04). Densitometric analysis of both drugs was carried out in the reflectance- absorbance mode at 289 nm. The linear regression analysis data for the calibration plots showed a good linear relationship with R2=0.9988___0.0012 in the concentration range of 100--400 ng for pantoprazole sodium. Also, the linear regression analysis data for the calibration plots showed a good linear relationship with R2=0.9990_+0.0008 in the concentration range of 200-1200 ng for itopride hydrochloride. The method was validated for specificity, precision, robustness and recovery. Statistical analysis proves that the method is repeatable and selective for the estimation of both the said drugs. As the method could effectively separate the drug from its degradation products, it can be employed as a stability indicating method.展开更多
BACKGROUND Peptic ulcer(PU)is an abnormal phenomenon in which there is rupture of the mucosa of the digestive tract,which not only affects patients'normal life but also causes an economic burden due to its high me...BACKGROUND Peptic ulcer(PU)is an abnormal phenomenon in which there is rupture of the mucosa of the digestive tract,which not only affects patients'normal life but also causes an economic burden due to its high medical costs.AIM To investigate the efficacy of pantoprazole(PPZ)plus perforation repair in patients with PU and its effect on the stress response.METHODS The study subjects were 108 PU patients admitted between July 2018 and July 2022,including 58 patients receiving PPZ plus perforation repair[research group(RG)]and 50 patients given simple perforation repair[control group(CG)].The efficacy,somatostatin(SS)concentration,stress reaction[malondialdehyde(MDA),lipid peroxide(LPO)],inflammatory indices[tumor necrosis factor(TNF)-α,C-reactive protein(CRP),interleukin(IL)-1β],recurrence,and complications(perforation,hemorrhage,and pyloric obstruction)were compared.RESULTS The overall response rate was higher in the RG than in the CG.Patients in the RG and IL-1β were significantly reduced to lower levels than those in the CG.Lower recurrence and complication rates were identified in the RG group.CONCLUSION Therefore,PPZ plus perforation repair is conducive to enhancing treatment outcomes in PU patients,reducing oxidative stress injury and excessive inflammatory reactions,and contributing to low recurrence and complication rates.展开更多
BACKGROUND:This study aimed to compare pantoprazole,a proton-pomp inhibitors(PPIs),and ranitidine,a H2 receptor antagonists(H2RA),in ceasing dyspeptic symptoms in the emergency department(ED).METHODS:This randomized,d...BACKGROUND:This study aimed to compare pantoprazole,a proton-pomp inhibitors(PPIs),and ranitidine,a H2 receptor antagonists(H2RA),in ceasing dyspeptic symptoms in the emergency department(ED).METHODS:This randomized,double-blinded study compared the effectiveness of 50 mg ranitidine(Ulcuran®)and 40 mg pantoprazole(Pantpas®),given in a 100 m L saline solution by an intravenous rapid infusion within 2–4 minutes in patients with dyspepsia presented to the ED.Pain intensity was measured at baseline,30 and 60 minutes after the drug administration.RESULTS:A total of 72 patients were eligible for the study.Of these patients,2 were excluded from the study because the initial visual analogue scale(VAS)scores were under 20 mm and 4 were excluded from the statistical analysis because of being diagnosed as having other causes of epigastric pain despite being allocated to one of the study groups.Thirty-three patients in the pantoprazole group and 33 patients in the ranitidine group were analyzed ultimately.The mean age of the patients was36.6±15 years,and 26(39.4%)patients were male.Both of the groups reduced pain effectively at 30[27.6±28(18 to 37)vs.28.3±23(20 to 37),respectively]and 60 minutes[39.6±39(26 to 53)vs.42.3±25(33 to 51),respectively].There were 13(39.4%)patients in the pantoprazole group and 8(24.2%)patients in the ranitidine group who required additional drug at the end of the study(P=0.186).CONCLUSION:Intravenous pantoprazole and ranitidine are not superior to each other in ceasing dyspeptic symptoms at 30 and 60 minutes in the ED.展开更多
The objective of this study was to investigate the pantoprazole and rebamipide efficiency on NSAIDs (nonsteroidal anti-inflammatory drugs)-gastropathy restoring and healing in patients with coronary heart disease, s...The objective of this study was to investigate the pantoprazole and rebamipide efficiency on NSAIDs (nonsteroidal anti-inflammatory drugs)-gastropathy restoring and healing in patients with coronary heart disease, stable angina, who have been taking aspirin for a long time period. The study included three groups of patients according to the treatment they have got: ASA (acetylsalicylic acid) in the first group; ASA and pantoprazole in the second; ASA, pantoprazole and rebamipide in the third one. To obtain the results, endoscopic method and proinflammatory cytokines LTB4 and protective prostaglandin E2 determination in the blood were used. The research demonstrated no ulcer effects in the group of patients who were treated by rebamipide, and significantly fewer gastroduodenal erosions, in comparison to the group, where treatment contained ASA and pantoprazole. The LTB4 (leukotriene B4) level decreased in pantoprazole and rebamipide treatment groups, but the PGE2 (prostaglandin E2) level increased only after rebamipide therapy. Therefore, rebamipide should be included to the therapy for the better NSAIDs-gastropathy treatment, in reason of its good reparative and gastroprotective properties.展开更多
The article describes the pantoprazole healing effect on the gastroduodenal mucosa in patients with NSAID gastropathy. Two groups of patients were compared, depending on the treatment they have got group, which was ta...The article describes the pantoprazole healing effect on the gastroduodenal mucosa in patients with NSAID gastropathy. Two groups of patients were compared, depending on the treatment they have got group, which was taking 75 mg of enteric aspirin per day and the group, where pantoprazole has been added to aspirin in the usual dose. Mucosa assessment was studied using fibrogastroduodenoscopy and Lanza score. Also, the relationship between aggression factors that cause NSAID gastropathy and mucosal protection agents has been studied. It was proved that the pantoprazole influence reduces the ulcerative-erosive lesions amount. Stomach erosive lesions percentage decreased from 58.18% to 42.42%, stomach ulcers from 14.55% to 6.06%, duodenum erosive lesions decreased from 34.55% to 24.24%, duodenum ulcers deceased from 9.09% to 3.03%. A positive correlation between LTB4 and Lanza scale was checked after pantoprazole treatment, indicating an impact on the LTB4 reduction in ulcers healing in patients with NSAID gastropathy.展开更多
Objective:Through the combination with hemocoagulase and pantoprazole on gastrointestinal bleeding, to observe the changes of serum BUN (blood urea nitrogen), LPO (LPO), NO (nitric oxide), TNF-α(TNF alpha), hs-CRP (h...Objective:Through the combination with hemocoagulase and pantoprazole on gastrointestinal bleeding, to observe the changes of serum BUN (blood urea nitrogen), LPO (LPO), NO (nitric oxide), TNF-α(TNF alpha), hs-CRP (high sensitivity C reactive protein) and cortisol levels, and to explore the mechanism of combination. Methods:110 cases of upper gastrointestinal bleeding in our hospital from January 2015 to September 2016 were selected and divided into the control group and the observation group, 55 cases for each group. Patients were treated with bed rest, fasting, intravenous nutrition, oxygen, and according to the individual situation actively supplement blood capacity, and the control group were treated with 40 mg intravenous pantoprazole treatment, 2 times/d;the patients in the observation group were treated with 2 kU hemocoagulase injection based on the treatment of control group, 2 times of intravenous injection per day, and all patients were treated for 3 d, and then the BUN, LPO, NO, TNF-α, hs-CRP and cortisol were detected. Results:(1) There were no significantly differences of the serum levels of BUN, LPO, and NO of the two groups before treatment (P>0.05). After treatment, the serum levels the two groups were significantly lower than before treatment, and LPO, BUN, and NO levels in the observation group were significantly better than the control group (P<0.05);(2) There were no significantly differences of the serum levels of TNF-α, hs-CRP, and cortisol of the two groups before treatment (P>0.05). After treatment, the serum levels in the two groups were significantly lower than before treatment, and TNF-α, hs-CRP, and cortisol levels in the observation group were significantly better than the control group (P<0.05). Conclusions:The treatment of patients with combined use of hemocoagulase and pantoprazole on gastrointestinal bleeding, can significantly improve the serum levels of BUN, LPO, NO, TNF-α, hs-CRP and cortisol levels, and further illustrates the synergistic effect of the combination, also shows that the combination of two drugs for patients with upper gastrointestinal bleeding can improve the symptoms of hemorrhage, reduce inflammation and stress, and improve the treatment effect.展开更多
Objective:To analyze the effect of pantoprazole and omeprazole in the treatment of patients with gastric ulcer.Methods:The treatment effect,recurrence rate,helicobacter pylori negative conversion rate,adverse reaction...Objective:To analyze the effect of pantoprazole and omeprazole in the treatment of patients with gastric ulcer.Methods:The treatment effect,recurrence rate,helicobacter pylori negative conversion rate,adverse reaction status and pain relief time of the two groups were compared.Results:The total effective rate of the experimental group(97.78%,44/45)was higher than that of the control group(84.44%,38/45),P<0.05;The recurrence rate(4.44%,2/45)and Helicobacter pylori negative conversion rate(95.56%,43/45)of the experimental group were significantly higher than those of the control group(P<0.05);The incidence of adverse reactions in the experimental group(11.11%,5/45)was lower than that in the control group(15.56%,7/45)(P>0.05);The pain relief time of the experimental group was(2.24±1.16)d,which was shorter than that of the control group(P<0.05).Conclusion:In the process of clinical treatment of gastric ulcer,pantoprazole has significant curative effect and low recurrence rate,which can eradicate Helicobacter pylori as soon as possible,shorten the pain time and make the treatment safer.展开更多
The aim of this work was to synthesize a pantoprazole-imprinted polymer(MIPs)and study its binding and release properties in an aqueous media.Methacrylic acid(MAA),methacrylamide(MAAM),hydroxyethyl methacrylate(HEMA),...The aim of this work was to synthesize a pantoprazole-imprinted polymer(MIPs)and study its binding and release properties in an aqueous media.Methacrylic acid(MAA),methacrylamide(MAAM),hydroxyethyl methacrylate(HEMA),and 4-vinyl pyridine(4VP)were tested as functional monomers.Different solvents were also applied as polymerization media under heat or UV radiation.The optimized MIP was prepared in chloroform as a solvent,4-vinyl pyridine as a functional monomer,and ethylene glycole dimethacrylate(EGDMA)as a crosslinker monomer under UV irradiation.Binding and release properties of MIP were studied in comparison with a non-imprinted polymer(NIP)in aqueous media,at different pH values.The protective effect of polymer for drugs against acidic conditions was evaluated at pH 2.Results indicated that the MIP had superior binding properties compared to NIP for pantoprazole.The percentage of drug released from MIP was significantly less than from NIP at all pH values,which was attributed to the presence of imprinted cavities in the MIP matrix.MIP also had a stronger protective effect for pantoprazole in acidic media,in comparison with NIP.展开更多
Objective To compare the efficacy of Ranitidine and Pantoprazole for the prevention of haemorrhage from stress ulcer among critical care patients. Methods A total of 121 critically ill patients were included in this r...Objective To compare the efficacy of Ranitidine and Pantoprazole for the prevention of haemorrhage from stress ulcer among critical care patients. Methods A total of 121 critically ill patients were included in this retrospective study. The choice of pharmacologic stress ulcer prophylaxis were either Ranitidine or Pantoprazole. The primary outcome was the incidence of stress-related significant upper gastrointestinal bleeding, and the secondary outcome was the incidence of hospital acquired pneumonia (HAP). Results A total of 63 patients were given Ranitidine, and 58 patients were given Pantoprazole for stress ulcer bleeding prophylaxis. Nine patients (7.44%, 9/121) developed clinically-important upper gastrointestinal bleeding, including 5 (7.94%, 5/63) in the Ranitidine group, and 4 (6.90%,4/58) in the Pantoprazole group. The rate of HAP was 3.17% (2/63) in the Ranitidine group, and 15.52% (9/58) in the Pantoprazole group. Conclusion Ranitidine was associated with lower rates of HAP as compared with Pantoprazole, with no statistically significant difference in clinically-important gastrointestinal hemorrhage. Because of limited trial data, future well-designed and powerful randomized, clinical trials are warranted.展开更多
文摘Aim To evaluate the pharmacokinetics and bioequivalence of domestic pantoprazole sodium enteric-coated tablets as compared with imported pantoprazole enteric-coated tablets. Methods This was an open randomized, two periods cross over study on twenty healthy male volunteers. The pantoprazole concentrations in plasma after an oral dose of 40 mg pantoprzaole preparations were determined by a HPLC-UV method. Non-compartmental method was used for the calculation of pharmacokinetic parameters. Logarithm-transformed Cmax and A UC were analyzed by the analysis of variance (ANOVA) with 90% confidence intervals. Results The main pharmacokinetics parameters of domestic pantoprazole sodium enteric-coated tablets and imported pantoprazole sodium enteric-coated tablets were as following: Cmax (3610 ± 956), (3466 ± 1209) ng·mL^-1, tmax (3.00 ± 0.40), (3.00 ± 0.46) h, AUC0-t (8140 ± 5065), (8390 ± 5474) ng·h·mL^-1, AUC0-∞ (8293 ± 5094), (8625 ± 5606) ng·h·mL^-1, t1/2 (1.61 ± 0.28), (1.85 ± 0.27) h, respectively. Conclusion Domestic pantoprazole sodium enteric-coated tablets were bioequivalent with the imported pantoprazole sodium enteric-coated tablets.
文摘AIM: To compare the effi cacy and tolerability of S-pan- toprazole (20 mg once a day) versus racemic Panto- prazole (40 mg once a day) in the treatment of gastro- esophageal reflux disease (GERD). METHODS: This multi-centre, randomized, double-blind clinical trial consisted of 369 patients of either sex suf- fering from GERD. Patients were randomly assigned to receive either one tablet (20 mg) of S-pantoprazole once a day (test group) or 40 mg racemic pantoprazole once a day (reference group) for 28 d. Patients were evaluated for reduction in baseline on d 0, GERD symptom score on d 14 and 28, occurrence of any adverse effect during the course of therapy. Gastrointestinal (GI) endoscopy was performed in 54 patients enrolled at one of the study centers at baseline and on d 28. RESULTS: Signifi cant reduction in the scores (mean and median) for heart burn (P < 0.0001), acid regurgitation (P < 0.0001), bloating (P < 0.0001), nausea (P < 0.0001) and dysphagia (P < 0.001) was achieved in both groups on d 14 with further reduction on continuing the therapy till 28 d. There was a statistically signifi cant difference in the proportion of patients showing improvement in acid regurgitation and bloating on d 14 and 28 (P = 0.004 for acid regurgitation; P = 0.03 for bloating) and heart burn on d 28 (P = 0.01) between the two groups, with a higher proportion in the test group than in the refer- ence group. Absolute risk reductions for heartburn/acid regurgitation/bloating were approximately 15% on d 14 and 10% on d 28. The relative risk reductions were 26%-33% on d 14 and 15% on d 28. GI endoscopy showed no signifi cant difference in healing of esophagitis (P = 1) and gastric erosions (P = 0.27) between the two groups. None of the patients in either group reported any adverse effect during the course of therapy.CONCLUSION: In GERD, S-pantoprazole (20 mg) is more effective than racemic pantoprazole (40 mg) in improving symptoms of heartburn, acid regurgitation, bloating and equally effective in healing esophagitis and gastric erosions. The relative risk reduction is 15%-33%. Both drugs are safe and well tolerated.
文摘AIM: To clarify whether there is any difference in the symptom relief in patients with reflux esophagitis following the administration of four Proton pump inhibitors (PPIs). METHODS: Two hundred and seventy-four patients with erosive reflux esophagitis were randomized to receive 8 wk of 20 mg omeprazole (n = 68), 30 mg of lansoprazole (n = 69), 40 mg of pantoprazole (n = 69), 40 mg of esomeprazole (n = 68) once a day in the morning. Daily changes in heartburn and acid reflux symptoms in the first 7 d of administration were assessed using a six-point scale (0: none; 1: mild; 2: mild-moderate; 3: moderate; 4: moderate-severe; 5: severe). RESULTS: The mean heartburn score in patients treated with esomeprazole more rapidly decreased than those receiving other PPI. Complete resolution of heartburn was also more rapid in patients treated with esomeprazole for 5 d compared with omeprazole (P = 0.0018, P = 0.0098, P = 0.0027, P = 0.0137, P = 0.0069, respectively), lansoprazole (P = 0.0020, P = 0.0046, P = 0.0037, P = 0.0016, P = 0.0076, respectively), and pantoprazole (P = 0.0006, P = 0.0005, P = 0.0009, P = 0.0031, P = 0.0119, respectively). There were no significant differences between the four groups in the rate of endoscopic healing of reflux esophagitis at week 8. CONCLUSION: Esomeprazole may be more effective than omeprazole, lansoprazole, and pantoprazole for the rapid relief of heartburn symptoms and acid reflux symptoms in patients with reflux esophagitis.
文摘AIM: To define the prevalence of gastroesophageal reflux disease (GERD) in mild persistent asthma and to value the effect of pantoprazole therapy on asthmatic symptoms.METHODS: Seven of thirty-four asthmatic patients without GERD served as the non-GERD control group. Twenty-seven of thirty-four asthmatic patients had GERD (7/27 also had erosive esophagitis, sixteen of them presented GERD symptoms. An upper gastrointestinal endoscopy was performed in all the subjects to obtain five biopsy specimens from the lower 5 cm of the esophagus. Patients were considered to have GERD when they had a dilation of intercellular space (DIS)〉0.74 μm at transmission electron microscopy. Patients with GERD were treated with pantoprazole, 80 mg/day. Forced expiratory volume in one second (FEV1) was performed at entry and after 6 mo of treatment. Asthmatic symptoms were recorded. The required frequency of inhaling rapid acting β2-agonists was self-recorded in the patients' diaries.RESULTS: Seven symptomatic patients presented erosive esophagitis. Among the 18 asymptomatic patients, 11 presented DIS, while all symptomatic patients showed ultrastructural esophageal damage. Seven asymptomatic patients did not present DIS. At entry the mean of FEV1 was 1.91 L in symptomatic GERD patients and 1.88 L in asymptomatic GERD patients. After the treatment, 25 patients had a complete recovery of DIS and reflux symptoms. Twenty-three patients presented a regression of asthmatic symptoms with normalization of FEV1. Four patients reported a significant improvement of symptoms and their FEV1 was over 80%.CONCLUSION: GERD is a highly prevalent condition in asthma patients. Treatment with pantoprazole (80 mg/day) determines their improvement and complete regression.
文摘Pantoprazole sodium, a substituted benzimidazole derivative, is an irreversible proton pump inhibitor which is primarily used for the treatment of duodenal ulcers, gastric ulcers, and gastroesophageal reflux disease (GERD). The monographs of European Pharmacopoeia (Ph. Eur.) and United States Pharmacopoeia (USP) specify six impurities, viz.;impurities A, B, C, D, E and F, respectively for its active pharmaceutical ingredient (API). The identification and synthesis of all impurities except impurity E are well described in the literature;however, there is no report related to impurity E. The prospects to the formation and controlling of impurity E up to -0.03% in the synthesis of pantoprazole sodium sesquihydrate (PAN) were discussed in detail for the first time. The present work described the journey towards the successful development of an optimal preparation procedure of dimer impurity E. The most plausible mechanism involved in the formation of impurity E has been proposed.
基金Supported by A Grant from MURST ex 60% to GDF and CC and a grant from Nycomed Italy
文摘AIM: To evaluate esophageal mucosal defense mechanisms at an epithelial level to establish if pantoprazole treatment can induce ultrastructural healing and improvement in the proliferation activity of the esophageal epithelium in gastroesophageal reflux disease (GERD). METHODS: This was a single-blinded study for pHmonitoring, and histological, ultrastructural and MIB1 immunostaining evaluation. Fifty eight patients with GERD were enrolled and underwent 24 h pH-monitoring and endoscopy. Patients were treated for 12 and 24 mo with pantoprazole. Esophageal specimens were taken for histological and ultrastructural evaluation, before and after the treatment. RESULTS: With transmission electron microscopy, all patients with GERD showed ultrastructural signs of damage with dilation of intercellular spaces (DIS). After 3 mo of therapy the mean DIS values showed asignificant reduction and the mean MIB1-LI values of GERD showed an increase in cell proliferation. A further 3 mo of therapy significantly increased cell proliferation only in the erosive esophagitis (ERD) group. CONCLUSION: Three months of pantoprazole therapy induced ultrastructural healing of mucosal damage in 89% and 93% of ERD and non-erosion patients, respectively. Moreover, long-term pantoprazole treatment may be helpful in increasing the capability for esophageal cell proliferation in GERD, particularly in ERD patients.
基金supported by National Key Technology R&D Program in the "Twelfth Five-Year" Plan of China(2011BAI11B07)
文摘Background: This study evaluated the effect of omeprazole or pantoprazole on platelet reactivity in non-STsegment elevation acute coronary syndrome(NSTE-ACS) patients receiving clopidogrel.Methods: Consecutive patients with NSTE-ACS(n =620) from general hospital of Shenyang Military Command were randomized to the omeprazole or pantoprazole(20mg/d) group(1:1), and received routine dual antiplatelet treatment. Patients' reversion rate of adenosine diphosphate-induced platelet aggregation(ADP-PA) was assessed at baseline, 12 to 24 h after administration of medication, and after 72 h of percutaneous coronary intervention(PCI). The primary endpoint of the study was platelet reactivity assessed with ADP-PA at 30 days after PCI. Adverse events(AEs) were recorded for 30-day and 180-day follow-up periods.Results: There were no significant differences between both the groups in platelet response to clopidogrel at 12–24h after drug administration(54.09%±18.90% vs. 51.62%±19.85%, P=0.12), 72 h after PCI(52.15%±19.45% vs. 49.66%±20.05%, P=0.18), and 30 days after PCI(50.44%±14.54% vs. 48.52%±15.08%, P=0.17). The rate of AEs did not differ significantly between groups during the 30-day(15.2% vs. 14.8%, P=0.91) and 180-day(16.5% vs. 14.5%, P=0.50) follow-up periods after PCI.Conclusion: The addition of omeprazole or pantoprazole to clopidogrel did not restrict the effect of platelet aggregation by reducing the conversion of clopidogrel. Compared with clopidogrel alone, pantoprazole-clopidogrel and omeprazoleclopidogrel combinations did not increase the incidence of adverse clinical events during 30-day and 180-day follow-up periods after PCI.
文摘AIM:To investigate the in vitro effects of pantoprazole on rat lower esophageal sphincter(LES)tone.METHODS:Rats weighing 250-300 g,provided by the Yeditepe University Experimental Research Center(Yü-DETAM),were used throughout the study.They were anesthetized before decapitation.LES tissues whose mucosal lining were removed were placed in a stan-dard 30-mL organ bath with a modif ied Krebs solution and continuously aerated with 95% oxygen-5% carbon dioxide gas mixture and kept at room temperature.The tissues were allowed to stabilize for 60 min.Sub-sequently,the contractile response to 10-6 mol/L carba-chol was obtained.Different concentrations of freshly prepared pantoprazole were added directly to the tis-sue bath to generate cumulative concentrations of 5×10-6 mol/L,5×10-5 mol/L,and 1.5×10-4 mol/L.Activi-ties were recorded on an online computer via a 4-channeltransducer data acquisition system using the software BSL PRO v 3.7,which also analyzed the data.RESULTS:Pantoprazole at 5×10-6 mol/L caused a small,but statistically insignif icant,relaxation in the car-bachol-contracted LES(2.23% vs 3.95%).The 5×10-5 mol/L concentration,however,caused a signif icant relax-ation of 10.47% compared with the control.1.5×10-4 mol/L concentration of pantoprazol caused a 19.89% relaxation in the carbachol contracted LES(P<0.001).CONCLUSION:This is the fi rst study to demonstrate that pantoprazole has a relaxing effect in isolated LESs.These results might have signif icant clinical implications for the subset of patients using proton pump inhibitors who do not receive full symptomatic alleviation from gastroesophageal reflux disease.
文摘A specific, precise and stability indicating high-performance thin-layer chromatographic method for simultaneous estimation of pantoprazole sodium and itopride hydrochloride in pharmaceutical formulations was developed and validated. The method employed TLC aluminium plates precoated with silica gel 60F254 as the stationary phase. The solvent system consisted of methanol:water:ammonium acetate; 4.0:1.0:0.5 (v/v/v). This system was found to give compact and dense spots for both itopride hydrochloride (Rf value of 0.55__+0.02) and pantoprazole sodium (Rf value of 0.85+0.04). Densitometric analysis of both drugs was carried out in the reflectance- absorbance mode at 289 nm. The linear regression analysis data for the calibration plots showed a good linear relationship with R2=0.9988___0.0012 in the concentration range of 100--400 ng for pantoprazole sodium. Also, the linear regression analysis data for the calibration plots showed a good linear relationship with R2=0.9990_+0.0008 in the concentration range of 200-1200 ng for itopride hydrochloride. The method was validated for specificity, precision, robustness and recovery. Statistical analysis proves that the method is repeatable and selective for the estimation of both the said drugs. As the method could effectively separate the drug from its degradation products, it can be employed as a stability indicating method.
文摘BACKGROUND Peptic ulcer(PU)is an abnormal phenomenon in which there is rupture of the mucosa of the digestive tract,which not only affects patients'normal life but also causes an economic burden due to its high medical costs.AIM To investigate the efficacy of pantoprazole(PPZ)plus perforation repair in patients with PU and its effect on the stress response.METHODS The study subjects were 108 PU patients admitted between July 2018 and July 2022,including 58 patients receiving PPZ plus perforation repair[research group(RG)]and 50 patients given simple perforation repair[control group(CG)].The efficacy,somatostatin(SS)concentration,stress reaction[malondialdehyde(MDA),lipid peroxide(LPO)],inflammatory indices[tumor necrosis factor(TNF)-α,C-reactive protein(CRP),interleukin(IL)-1β],recurrence,and complications(perforation,hemorrhage,and pyloric obstruction)were compared.RESULTS The overall response rate was higher in the RG than in the CG.Patients in the RG and IL-1β were significantly reduced to lower levels than those in the CG.Lower recurrence and complication rates were identified in the RG group.CONCLUSION Therefore,PPZ plus perforation repair is conducive to enhancing treatment outcomes in PU patients,reducing oxidative stress injury and excessive inflammatory reactions,and contributing to low recurrence and complication rates.
文摘BACKGROUND:This study aimed to compare pantoprazole,a proton-pomp inhibitors(PPIs),and ranitidine,a H2 receptor antagonists(H2RA),in ceasing dyspeptic symptoms in the emergency department(ED).METHODS:This randomized,double-blinded study compared the effectiveness of 50 mg ranitidine(Ulcuran®)and 40 mg pantoprazole(Pantpas®),given in a 100 m L saline solution by an intravenous rapid infusion within 2–4 minutes in patients with dyspepsia presented to the ED.Pain intensity was measured at baseline,30 and 60 minutes after the drug administration.RESULTS:A total of 72 patients were eligible for the study.Of these patients,2 were excluded from the study because the initial visual analogue scale(VAS)scores were under 20 mm and 4 were excluded from the statistical analysis because of being diagnosed as having other causes of epigastric pain despite being allocated to one of the study groups.Thirty-three patients in the pantoprazole group and 33 patients in the ranitidine group were analyzed ultimately.The mean age of the patients was36.6±15 years,and 26(39.4%)patients were male.Both of the groups reduced pain effectively at 30[27.6±28(18 to 37)vs.28.3±23(20 to 37),respectively]and 60 minutes[39.6±39(26 to 53)vs.42.3±25(33 to 51),respectively].There were 13(39.4%)patients in the pantoprazole group and 8(24.2%)patients in the ranitidine group who required additional drug at the end of the study(P=0.186).CONCLUSION:Intravenous pantoprazole and ranitidine are not superior to each other in ceasing dyspeptic symptoms at 30 and 60 minutes in the ED.
文摘The objective of this study was to investigate the pantoprazole and rebamipide efficiency on NSAIDs (nonsteroidal anti-inflammatory drugs)-gastropathy restoring and healing in patients with coronary heart disease, stable angina, who have been taking aspirin for a long time period. The study included three groups of patients according to the treatment they have got: ASA (acetylsalicylic acid) in the first group; ASA and pantoprazole in the second; ASA, pantoprazole and rebamipide in the third one. To obtain the results, endoscopic method and proinflammatory cytokines LTB4 and protective prostaglandin E2 determination in the blood were used. The research demonstrated no ulcer effects in the group of patients who were treated by rebamipide, and significantly fewer gastroduodenal erosions, in comparison to the group, where treatment contained ASA and pantoprazole. The LTB4 (leukotriene B4) level decreased in pantoprazole and rebamipide treatment groups, but the PGE2 (prostaglandin E2) level increased only after rebamipide therapy. Therefore, rebamipide should be included to the therapy for the better NSAIDs-gastropathy treatment, in reason of its good reparative and gastroprotective properties.
文摘The article describes the pantoprazole healing effect on the gastroduodenal mucosa in patients with NSAID gastropathy. Two groups of patients were compared, depending on the treatment they have got group, which was taking 75 mg of enteric aspirin per day and the group, where pantoprazole has been added to aspirin in the usual dose. Mucosa assessment was studied using fibrogastroduodenoscopy and Lanza score. Also, the relationship between aggression factors that cause NSAID gastropathy and mucosal protection agents has been studied. It was proved that the pantoprazole influence reduces the ulcerative-erosive lesions amount. Stomach erosive lesions percentage decreased from 58.18% to 42.42%, stomach ulcers from 14.55% to 6.06%, duodenum erosive lesions decreased from 34.55% to 24.24%, duodenum ulcers deceased from 9.09% to 3.03%. A positive correlation between LTB4 and Lanza scale was checked after pantoprazole treatment, indicating an impact on the LTB4 reduction in ulcers healing in patients with NSAID gastropathy.
文摘Objective:Through the combination with hemocoagulase and pantoprazole on gastrointestinal bleeding, to observe the changes of serum BUN (blood urea nitrogen), LPO (LPO), NO (nitric oxide), TNF-α(TNF alpha), hs-CRP (high sensitivity C reactive protein) and cortisol levels, and to explore the mechanism of combination. Methods:110 cases of upper gastrointestinal bleeding in our hospital from January 2015 to September 2016 were selected and divided into the control group and the observation group, 55 cases for each group. Patients were treated with bed rest, fasting, intravenous nutrition, oxygen, and according to the individual situation actively supplement blood capacity, and the control group were treated with 40 mg intravenous pantoprazole treatment, 2 times/d;the patients in the observation group were treated with 2 kU hemocoagulase injection based on the treatment of control group, 2 times of intravenous injection per day, and all patients were treated for 3 d, and then the BUN, LPO, NO, TNF-α, hs-CRP and cortisol were detected. Results:(1) There were no significantly differences of the serum levels of BUN, LPO, and NO of the two groups before treatment (P>0.05). After treatment, the serum levels the two groups were significantly lower than before treatment, and LPO, BUN, and NO levels in the observation group were significantly better than the control group (P<0.05);(2) There were no significantly differences of the serum levels of TNF-α, hs-CRP, and cortisol of the two groups before treatment (P>0.05). After treatment, the serum levels in the two groups were significantly lower than before treatment, and TNF-α, hs-CRP, and cortisol levels in the observation group were significantly better than the control group (P<0.05). Conclusions:The treatment of patients with combined use of hemocoagulase and pantoprazole on gastrointestinal bleeding, can significantly improve the serum levels of BUN, LPO, NO, TNF-α, hs-CRP and cortisol levels, and further illustrates the synergistic effect of the combination, also shows that the combination of two drugs for patients with upper gastrointestinal bleeding can improve the symptoms of hemorrhage, reduce inflammation and stress, and improve the treatment effect.
文摘Objective:To analyze the effect of pantoprazole and omeprazole in the treatment of patients with gastric ulcer.Methods:The treatment effect,recurrence rate,helicobacter pylori negative conversion rate,adverse reaction status and pain relief time of the two groups were compared.Results:The total effective rate of the experimental group(97.78%,44/45)was higher than that of the control group(84.44%,38/45),P<0.05;The recurrence rate(4.44%,2/45)and Helicobacter pylori negative conversion rate(95.56%,43/45)of the experimental group were significantly higher than those of the control group(P<0.05);The incidence of adverse reactions in the experimental group(11.11%,5/45)was lower than that in the control group(15.56%,7/45)(P>0.05);The pain relief time of the experimental group was(2.24±1.16)d,which was shorter than that of the control group(P<0.05).Conclusion:In the process of clinical treatment of gastric ulcer,pantoprazole has significant curative effect and low recurrence rate,which can eradicate Helicobacter pylori as soon as possible,shorten the pain time and make the treatment safer.
基金the Vice Chancellor of Research,Mashhad University of Medical Sciences,for financial support through Grant 89434
文摘The aim of this work was to synthesize a pantoprazole-imprinted polymer(MIPs)and study its binding and release properties in an aqueous media.Methacrylic acid(MAA),methacrylamide(MAAM),hydroxyethyl methacrylate(HEMA),and 4-vinyl pyridine(4VP)were tested as functional monomers.Different solvents were also applied as polymerization media under heat or UV radiation.The optimized MIP was prepared in chloroform as a solvent,4-vinyl pyridine as a functional monomer,and ethylene glycole dimethacrylate(EGDMA)as a crosslinker monomer under UV irradiation.Binding and release properties of MIP were studied in comparison with a non-imprinted polymer(NIP)in aqueous media,at different pH values.The protective effect of polymer for drugs against acidic conditions was evaluated at pH 2.Results indicated that the MIP had superior binding properties compared to NIP for pantoprazole.The percentage of drug released from MIP was significantly less than from NIP at all pH values,which was attributed to the presence of imprinted cavities in the MIP matrix.MIP also had a stronger protective effect for pantoprazole in acidic media,in comparison with NIP.
文摘Objective To compare the efficacy of Ranitidine and Pantoprazole for the prevention of haemorrhage from stress ulcer among critical care patients. Methods A total of 121 critically ill patients were included in this retrospective study. The choice of pharmacologic stress ulcer prophylaxis were either Ranitidine or Pantoprazole. The primary outcome was the incidence of stress-related significant upper gastrointestinal bleeding, and the secondary outcome was the incidence of hospital acquired pneumonia (HAP). Results A total of 63 patients were given Ranitidine, and 58 patients were given Pantoprazole for stress ulcer bleeding prophylaxis. Nine patients (7.44%, 9/121) developed clinically-important upper gastrointestinal bleeding, including 5 (7.94%, 5/63) in the Ranitidine group, and 4 (6.90%,4/58) in the Pantoprazole group. The rate of HAP was 3.17% (2/63) in the Ranitidine group, and 15.52% (9/58) in the Pantoprazole group. Conclusion Ranitidine was associated with lower rates of HAP as compared with Pantoprazole, with no statistically significant difference in clinically-important gastrointestinal hemorrhage. Because of limited trial data, future well-designed and powerful randomized, clinical trials are warranted.