Purpose: Ranitidine hydrochloride (HCl) remains an important medication for treating acid-peptic ailments such as Gastroesophageal reflux disease (GERD). The main objective of this Post Marketing Surveillance (PMS) cl...Purpose: Ranitidine hydrochloride (HCl) remains an important medication for treating acid-peptic ailments such as Gastroesophageal reflux disease (GERD). The main objective of this Post Marketing Surveillance (PMS) clinical study was to test the efficacy and safety of Ranitidine HCl in Indian patients suffering from GERD. Patients and Methods: Data of 2446 patients (1307 males;1121 females) from 21 centers across India were analyzed. Patients received either of the three treatments: Ranitidine HCl 150 mg twice a day (BID) (ARM-A), Ranitidine HCl 300 mg once daily (OD) or BID (ARM-B), and Ranitidine HCl 300 mg OD (ARM-C). Gastroesophageal Reflux Disease Symptom Assessment Scale (GSAS) score and Heartburn Severity score were used to assess the drug’s efficacy. The adverse events reported by patients or investigators were analyzed to assess the safety profile of Ranitidine. Results: Of the 2446 subjects screened, 2428 were enrolled. There was a significant reduction in GSAS scores from baseline to the end of the study visit in all three ARMs. The GSAS scores reduced from 2.02 to 0.23 in ARM-A, 2.01 to 0.24 in ARM-B, and 2.07 to 0.26 in ARM-C patients. In ARM A, 72.82% had 24 hours heartburn-free days, and 66.89% had 7 consecutive heartburn-free days, which was more significant than the other two ARMs. 128 (5.27%) patients reported ADRs due to Ranitidine HCl at different doses. The most frequently reported ADR was constipation (17.18%), followed by oliguria (14.06%), cold (13.28%), and dysuria (12.5%). Of 128 ADRs, 113 (88.28%) were mild, and only 11 (8.59%) ADRs were related to the study drug. No severe ADRs were reported during the study. Conclusion: Ranitidine HCl 150/300 mg tablet was found to be an effective and safe H2-receptor antagonist for treating GERD in Indian Patients.展开更多
AIM： To evaluate the bioequivalence of ranitidine and bismuth derived from two compound preparations. METHODS： The bioavailability was measured in 20 healthy male Chinese volunteers following a single oral dose （eq...AIM： To evaluate the bioequivalence of ranitidine and bismuth derived from two compound preparations. METHODS： The bioavailability was measured in 20 healthy male Chinese volunteers following a single oral dose （equivalent to 200 mg of ranitidine and 220 mg of bismuth） of the test or reference products in the fasting state. Then blood samples were collected for 24 h. Plasma concentrations of ranitidine and bismuth were analyzed by high-performance liquid chromatography and inductively coupled plasma-mass spectrometry （ICPMS）, respectively. The non-compartmental method was used for pharmacokinetic analysis. Log-transformed Cmax, AUC（0-t） and AUC（0-∞） were tested for bioequivalence using ANOVA and Schuirmann two-one sided t-test. Tmax was analyzed by Wilcoxon＇s test. RESULTS： Various pharmacokinetic parameters of ranitidine derived from the two compound preparations, including Cmax, AUC（0-t）, AUC（0-∞）, Tmax and T1/2, were nearly consistent with previous observations. These parameters derived from test and reference drug were as follows： Cmax（0.67 ± 0.21 vs 0.68 ± 0.22 mg/L）, AUC（0-t）（3.1 ± 0.6 vs 3.0 ± 0.7 mg/L per hour）, AUC（0-∞）（3.3 ± 0.6 vs 3.2 ± 0.8 mg/L per hour）, Tmax （2.3 ± 0.9 VS 2.1 ± 0.9 h） and T1/2 （2.8 ± 0.3 vs 3.1 ± 0.4 h）. In addition, double-peak absorption profiles of ranitidine were found in some Chinese volunteers. For bismuth, those parameters derived from test and reference drug were as follows： Cmax （11.80 ± 7.36 vs 11.40 ± 6.55 μg/L）, AUC（0-t） （46.65 ± 16.97 vs 47.03 ± 21.49 μg/L per hour）, Tmax （0.50 ± 0.20 vs 0.50 ± 0.20 h） and T1/2 （10.2 ± 2.3 vs 13.0 ± 6.9 h）. Ninety percent of confidence intervals for the test/reference ratio of Cmax, AUC（0-t） and AUC（0-∞） derived from both ranitidine and bismuth were found within the bioequivalence acceptable range of 80%-125%. No significant difference was found in Tmax derived from both ranitidine and bismuth. CONCLUSION： The two compound preparations are bioequivalent and may be prescribed interchangeably.展开更多
AIM： To evaluate the effect of ranitidine on gastric mucosal changes and on GI bleeding in long distance runhers. METHODS： Twenty-four long distance runners （M： 16, F： 8, age： 18.2＋ 1.5 years） participated in ...AIM： To evaluate the effect of ranitidine on gastric mucosal changes and on GI bleeding in long distance runhers. METHODS： Twenty-four long distance runners （M： 16, F： 8, age： 18.2＋ 1.5 years） participated in this study. A symptom questionnaire, stool hemoccult test, and upper gastrointestinal （GI） endoscopy were performed on the subjects prior to the study. The subjects took oral ranitidine （150 mg, b.i.d.） for two weeks. The upper GI endoscopy and stool Hemoccult tests were repeated after the treatment. RESULTS： Twenty-two of the 24 runners had at least one upper G1 mucosal lesion before the medication. The Endoscopic improvements were seen in eleven of the 14 cases of erosive gastritis and four of the 5 cases of esophagitis. Six subjects were Heine occult positive prior to the study, but only one was positive after the medication. CONCLUSION： Gastric mucosal lesions and GI bleeding in long distance runners seem to be associated to acidrelated factors mediated by the high level of regular running. Ranitidine seems to be and effective prophylaxis to prevent gastric mucosal lesions and GI bleeding.展开更多
AIM:To assess the efficacy and safety of ranitidine bismuth citrate plus clarithromycin given for 1 wk in Brazilian patients with peptic ulcer. METHODS: One hundred and twenty patients with peptic ulcer were randomize...AIM:To assess the efficacy and safety of ranitidine bismuth citrate plus clarithromycin given for 1 wk in Brazilian patients with peptic ulcer. METHODS: One hundred and twenty patients with peptic ulcer were randomized in two treatment groups: (1)1-wk regimen consisting of ranitidine bismuth citrate 400 mg b.i.d. with clarithromycin 500 mg b.i.d. or (2) 2-wk regimen of the same treatment. Eradication of the infection was considered when both the histologic examination and the urease test were negative for the infection 3 mo after treatment. RESULTS: By intention to treat analysis, Helicobacter pylori (H pylori) was eradicated in 73% and 76% of patients, respectively treated for 1 or 2 wk (P>0.05). By per protocol analysis, the eradication rates were 80% and 83%, respectively, in patients treated for 1 or 2 wk (P>0.05). Nine patients (8.2%) reported minor side effects. CONCLUSION: One-week therapy with ranitidine bismuth citrate and clarithromycin is safe, well tolerated and effective for treatment of H pylori infection, and appears to be comparable to the 2-wk regimen in terms of efficacy.x展开更多
A rapid and sensitive assay based on high performance liquid chromatography-tandem mass spectrometry（LC-MS/MS） was developed for the determination of ranitidine（RAN） in human plasma with codeine as internal stand...A rapid and sensitive assay based on high performance liquid chromatography-tandem mass spectrometry（LC-MS/MS） was developed for the determination of ranitidine（RAN） in human plasma with codeine as internal standard（IS）.After protein precipitation with acetonitrile,the analyte and IS were separated on a Zorbax SB-Aq C18 column（150 mm×4.6 mm i.d.,5 μm） eluted with a mobile phase consisting of methanol/acetonitrile/10 mmol/L ammonium acetate containing 1% formic acid（pH=2.4）（volume ratio 12.5：12.5：75） at a flow rate of 1.0 mL/min.Detection was performed by electrospray ionization in the positive ion mode followed by the multiple reaction monito-ring（MRM） of the transitions of RAN at m/z 315.1→176.3 and of IS at m/z 300.1→165.1.The method was linear over a concentration range of 1―1000 ng/mL（r=0.9991） with a lower limit of quantitation（LLOQ） of 1 ng/mL and a limit of detection（LOD） of 0.3 ng/mL.Accuracy as relative error was from-0.01% to-1.7% and intra-day and inter-day precisions as relative standard deviation were ≤8.9% and ≤5.5%,respectively.The method was successfully applied to a pharmacokinetic study of ranitidine,getting a single oral dose（160 mg） to healthy volunteers.展开更多
The purpose of these experiments was to investigate the possible ionicbases for ranitidine （Ran） in isolated papillary muscles of the guinea pig.Ran,when the concentration was below 300μmol/L,had no influence on co...The purpose of these experiments was to investigate the possible ionicbases for ranitidine （Ran） in isolated papillary muscles of the guinea pig.Ran,when the concentration was below 300μmol/L,had no influence on contraction ofnormal muscles and only above 0.3 mmol/L,it showed weak negative inotropic ef-fect.The contractile activity elicited by histamine in potassium depolarized mus-cles was depressed by Ran markedly and dose-dependently.The IC<sub>50</sub> of Ran was0.273μmol/L.This depressant effect was reversed by an elevation of externalCa<sup>2+</sup>concentration to 7.7mmol/L.The contraction induced by isoproterenol inpotassium depolarized preparations was not altered by Ran.Ran at theconcentrations of 1,10 and 100μmol/L failed to show influences on fast actionpotentials.However,Ran at 0.5μmol/L time-dependently inhibited slow action po-tentials.It is concluded that the ionic mechanism of Ran might be attributed toantagonized H<sub>2</sub> receptor of myocardium which in turn decreases Ca<sup>2+</sup> inward cur-rent.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
文摘Purpose: Ranitidine hydrochloride (HCl) remains an important medication for treating acid-peptic ailments such as Gastroesophageal reflux disease (GERD). The main objective of this Post Marketing Surveillance (PMS) clinical study was to test the efficacy and safety of Ranitidine HCl in Indian patients suffering from GERD. Patients and Methods: Data of 2446 patients (1307 males;1121 females) from 21 centers across India were analyzed. Patients received either of the three treatments: Ranitidine HCl 150 mg twice a day (BID) (ARM-A), Ranitidine HCl 300 mg once daily (OD) or BID (ARM-B), and Ranitidine HCl 300 mg OD (ARM-C). Gastroesophageal Reflux Disease Symptom Assessment Scale (GSAS) score and Heartburn Severity score were used to assess the drug’s efficacy. The adverse events reported by patients or investigators were analyzed to assess the safety profile of Ranitidine. Results: Of the 2446 subjects screened, 2428 were enrolled. There was a significant reduction in GSAS scores from baseline to the end of the study visit in all three ARMs. The GSAS scores reduced from 2.02 to 0.23 in ARM-A, 2.01 to 0.24 in ARM-B, and 2.07 to 0.26 in ARM-C patients. In ARM A, 72.82% had 24 hours heartburn-free days, and 66.89% had 7 consecutive heartburn-free days, which was more significant than the other two ARMs. 128 (5.27%) patients reported ADRs due to Ranitidine HCl at different doses. The most frequently reported ADR was constipation (17.18%), followed by oliguria (14.06%), cold (13.28%), and dysuria (12.5%). Of 128 ADRs, 113 (88.28%) were mild, and only 11 (8.59%) ADRs were related to the study drug. No severe ADRs were reported during the study. Conclusion: Ranitidine HCl 150/300 mg tablet was found to be an effective and safe H2-receptor antagonist for treating GERD in Indian Patients.
文摘AIM： To evaluate the bioequivalence of ranitidine and bismuth derived from two compound preparations. METHODS： The bioavailability was measured in 20 healthy male Chinese volunteers following a single oral dose （equivalent to 200 mg of ranitidine and 220 mg of bismuth） of the test or reference products in the fasting state. Then blood samples were collected for 24 h. Plasma concentrations of ranitidine and bismuth were analyzed by high-performance liquid chromatography and inductively coupled plasma-mass spectrometry （ICPMS）, respectively. The non-compartmental method was used for pharmacokinetic analysis. Log-transformed Cmax, AUC（0-t） and AUC（0-∞） were tested for bioequivalence using ANOVA and Schuirmann two-one sided t-test. Tmax was analyzed by Wilcoxon＇s test. RESULTS： Various pharmacokinetic parameters of ranitidine derived from the two compound preparations, including Cmax, AUC（0-t）, AUC（0-∞）, Tmax and T1/2, were nearly consistent with previous observations. These parameters derived from test and reference drug were as follows： Cmax（0.67 ± 0.21 vs 0.68 ± 0.22 mg/L）, AUC（0-t）（3.1 ± 0.6 vs 3.0 ± 0.7 mg/L per hour）, AUC（0-∞）（3.3 ± 0.6 vs 3.2 ± 0.8 mg/L per hour）, Tmax （2.3 ± 0.9 VS 2.1 ± 0.9 h） and T1/2 （2.8 ± 0.3 vs 3.1 ± 0.4 h）. In addition, double-peak absorption profiles of ranitidine were found in some Chinese volunteers. For bismuth, those parameters derived from test and reference drug were as follows： Cmax （11.80 ± 7.36 vs 11.40 ± 6.55 μg/L）, AUC（0-t） （46.65 ± 16.97 vs 47.03 ± 21.49 μg/L per hour）, Tmax （0.50 ± 0.20 vs 0.50 ± 0.20 h） and T1/2 （10.2 ± 2.3 vs 13.0 ± 6.9 h）. Ninety percent of confidence intervals for the test/reference ratio of Cmax, AUC（0-t） and AUC（0-∞） derived from both ranitidine and bismuth were found within the bioequivalence acceptable range of 80%-125%. No significant difference was found in Tmax derived from both ranitidine and bismuth. CONCLUSION： The two compound preparations are bioequivalent and may be prescribed interchangeably.
基金Supported by the 2005 research fund of Wonkwang University
文摘AIM： To evaluate the effect of ranitidine on gastric mucosal changes and on GI bleeding in long distance runhers. METHODS： Twenty-four long distance runners （M： 16, F： 8, age： 18.2＋ 1.5 years） participated in this study. A symptom questionnaire, stool hemoccult test, and upper gastrointestinal （GI） endoscopy were performed on the subjects prior to the study. The subjects took oral ranitidine （150 mg, b.i.d.） for two weeks. The upper GI endoscopy and stool Hemoccult tests were repeated after the treatment. RESULTS： Twenty-two of the 24 runners had at least one upper G1 mucosal lesion before the medication. The Endoscopic improvements were seen in eleven of the 14 cases of erosive gastritis and four of the 5 cases of esophagitis. Six subjects were Heine occult positive prior to the study, but only one was positive after the medication. CONCLUSION： Gastric mucosal lesions and GI bleeding in long distance runners seem to be associated to acidrelated factors mediated by the high level of regular running. Ranitidine seems to be and effective prophylaxis to prevent gastric mucosal lesions and GI bleeding.
文摘AIM:To assess the efficacy and safety of ranitidine bismuth citrate plus clarithromycin given for 1 wk in Brazilian patients with peptic ulcer. METHODS: One hundred and twenty patients with peptic ulcer were randomized in two treatment groups: (1)1-wk regimen consisting of ranitidine bismuth citrate 400 mg b.i.d. with clarithromycin 500 mg b.i.d. or (2) 2-wk regimen of the same treatment. Eradication of the infection was considered when both the histologic examination and the urease test were negative for the infection 3 mo after treatment. RESULTS: By intention to treat analysis, Helicobacter pylori (H pylori) was eradicated in 73% and 76% of patients, respectively treated for 1 or 2 wk (P>0.05). By per protocol analysis, the eradication rates were 80% and 83%, respectively, in patients treated for 1 or 2 wk (P>0.05). Nine patients (8.2%) reported minor side effects. CONCLUSION: One-week therapy with ranitidine bismuth citrate and clarithromycin is safe, well tolerated and effective for treatment of H pylori infection, and appears to be comparable to the 2-wk regimen in terms of efficacy.x
基金Supported by the National High-Tech Research and Development Program of China(Nos.2008BAI51B03,2006BAI098B0808)the National Natural Science Foundation of China(No.30772613)
文摘A rapid and sensitive assay based on high performance liquid chromatography-tandem mass spectrometry（LC-MS/MS） was developed for the determination of ranitidine（RAN） in human plasma with codeine as internal standard（IS）.After protein precipitation with acetonitrile,the analyte and IS were separated on a Zorbax SB-Aq C18 column（150 mm×4.6 mm i.d.,5 μm） eluted with a mobile phase consisting of methanol/acetonitrile/10 mmol/L ammonium acetate containing 1% formic acid（pH=2.4）（volume ratio 12.5：12.5：75） at a flow rate of 1.0 mL/min.Detection was performed by electrospray ionization in the positive ion mode followed by the multiple reaction monito-ring（MRM） of the transitions of RAN at m/z 315.1→176.3 and of IS at m/z 300.1→165.1.The method was linear over a concentration range of 1―1000 ng/mL（r=0.9991） with a lower limit of quantitation（LLOQ） of 1 ng/mL and a limit of detection（LOD） of 0.3 ng/mL.Accuracy as relative error was from-0.01% to-1.7% and intra-day and inter-day precisions as relative standard deviation were ≤8.9% and ≤5.5%,respectively.The method was successfully applied to a pharmacokinetic study of ranitidine,getting a single oral dose（160 mg） to healthy volunteers.
文摘The purpose of these experiments was to investigate the possible ionicbases for ranitidine （Ran） in isolated papillary muscles of the guinea pig.Ran,when the concentration was below 300μmol/L,had no influence on contraction ofnormal muscles and only above 0.3 mmol/L,it showed weak negative inotropic ef-fect.The contractile activity elicited by histamine in potassium depolarized mus-cles was depressed by Ran markedly and dose-dependently.The IC<sub>50</sub> of Ran was0.273μmol/L.This depressant effect was reversed by an elevation of externalCa<sup>2+</sup>concentration to 7.7mmol/L.The contraction induced by isoproterenol inpotassium depolarized preparations was not altered by Ran.Ran at theconcentrations of 1,10 and 100μmol/L failed to show influences on fast actionpotentials.However,Ran at 0.5μmol/L time-dependently inhibited slow action po-tentials.It is concluded that the ionic mechanism of Ran might be attributed toantagonized H<sub>2</sub> receptor of myocardium which in turn decreases Ca<sup>2+</sup> inward cur-rent.
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.
