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Objective: This study involves the synthesis of Gum tragacanth (gt) based interpenetrating polymer network (ipn) and its utilization for sustained release of anti-ulcerative drug i.e. pantoprazole sodium. Methods: IPN was synthesized from Gum tragacanth, polyacrylic acid (gt-cl-paa) hydrogel. gt-cl-paa was kept in distilled water. Further, acryamide (aam) and methylmethacrylate (mma) was added and then kept for overnight. Later on, lipase and glutaraldehyde were added. Homopolymers and the unreacted monomers were removed using acetone. Synthesized IPN was dried at 50 °C for further study. Synthesized ipn was swelled in water and the drug was added to it. The drug was entrapped in the pores of the synthesized ipn and then drug release behavior was studied using uv-vis spectrophotometer. Results: Gt, paa and mma based crosslinked IPN were synthesized using lipase-glutaraldehyde as initiator-crosslinker system. The synthesized IPN was pH sensitive and possessed the desired swelling capacity required for the controlled and systematic liberation of pantoprazole sodium at 37 °C. The kinetic of drug release was studied and found that lateral diffusion (DL) of drug was higher as compared to the initial diffusion (DI). The prepared IPN can be used as prospective carrier for prolonged drug delivery. Conclusion: A novel pH sensitive and colon targeted IPN was synthesized. It acts as an effective device for the controlled release of drug pantoprazole sodium.
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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 Pharmaco-poeia (USP) specify six impurities, viz.; impurities A, B, C, D, E and F, respectively for its active phar-maceutical 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 for-mation 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.
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Objective:To establish a method to determine the contents of pantoprazole sodium bioadhesive tablets. Methods:An HPLC method was adopted. The determination was performed on a HYPERSIL ODS-2 (150 mm × 4. 6 mm, 5μm) column with mobile phase consisting of 0. 01 mol·L-1 dipotassium phosphate solution –methanol (60 ∶40) at the flow rate of 1. 0 ml·min-1 . The de-tection wavelength was set at 289 nm, the column temperature was maintained at 30 ℃ and the sample size was 20 μl. Results:The linear range of pantoprazole sodium was 1. 28-20. 60μg·ml-1,(r=0. 999 8) . The average recovery was 99. 52%(RSD=1. 43%, n=9). Conclusion:The method is simple, accurate and reliable, and can be used for determining the content of pantoprazole sodium bioadhesive tablets.
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OBJECTIVE: To establish an LC-MS/MS method to determine (S)-pantoprazole sodium in dog plasma and investigate its toxicokinetics. METHODS: After protein precipitation with acetonitrile, the analyte and internal standard were separated on CHIRALCEL OJ-RH column (4.6 mm ×150 mm, 5 μm) with acetonitrile-water (28∶72) as mobile phase eluted at a flow rate of 0.6 mL·min-1. Detection was carried out by electrospray positive ionization mass spectrometry in the multiple reaction monitoring (MRM) mode. The MRM transitions of m/z 384.0/199.8 and m/z 180.0/110.0 were used to quantify (S)-pantoprazole sodium and phenacetin, respectively. Beagle dogs were intravenously given (S)-pantoprazole sodium for 4 weeks at low, medium, and high dosages (10, 20, 40 mg·kg-1·d-1). RESULTS: The calibration curve was linear over the concentration range of 50-30 000 ng·mL-1. The RSDs were less than 15%, and the accuracy was in the range of 85%-115%. The AUC0-4 h and ρmax of (S)-pantoprazole sodium were proportional to the dosages. CONCLUSION: The established method can be applied to the determination of (S)-pantoprazole sodium in plasma of dogs and is suitable for the toxicokinetic study.
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Objective To investigate the clinical efficacy and safety of Danhong injection combined with pantoprazole sodium on patients with acute exacerbation of respiratory failure. Methods 104 patients with acute exacerbation of respiratory failure were treated in our hospital from January 2016 to January 2017. They were selected and equally divided into two groups with the method of random number table. The two groups were given the same basic treatment, and the control group was treated with pantoprazole sodium on this basis. The treatment group was treated with Danhong injection on the basis of the control group. The clinical efficacy and adverse reactions of two groups were recorded. Results After 15 days of the treatment, the total effective rate of the treatment group was 94.2%, which was significantly higher than that of the control group 71.2%(P<0.05). There was no significant difference in the incidence of adverse reactions between the control group and the treatment group. Conclusion Danhong injection combined with pantoprazole sodium is effective and safe in the treatment of acute exacerbations of respiratory failure, which is worthy of clinical practice and popularization.
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Objective To investigate the clinical efficacy and safety of Danhong injection combined with pantoprazole sodium on patients with acute exacerbation of respiratory failure. Methods 104 patients with acute exacerbation of respiratory failure were treated in our hospital from January 2016 to January 2017. They were selected and equally divided into two groups with the method of random number table. The two groups were given the same basic treatment, and the control group was treated with pantoprazole sodium on this basis. The treatment group was treated with Danhong injection on the basis of the control group. The clinical efficacy and adverse reactions of two groups were recorded. Results After 15 days of the treatment, the total effective rate of the treatment group was 94.2%, which was significantly higher than that of the control group 71.2%(P<0.05). There was no significant difference in the incidence of adverse reactions between the control group and the treatment group. Conclusion Danhong injection combined with pantoprazole sodium is effective and safe in the treatment of acute exacerbations of respiratory failure, which is worthy of clinical practice and popularization.
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Objective To explore the effect of psychological intervention with pantoprazole sodium in treatment of gastric ulcer. Methods A total of 80 patients with gastric ulcer from March 2015 to January 2017 were randomly divided into two groups, control group and observation group; Two groups were treated with pantoprazole sodium, the control group received conventional care, while the observation group was given psychological care.The rehabilitation of the two groups was observed and compared . Results The effective rate of observation group was 92.5％, significantly higher than that of the control group(77.5％); The satisfaction rate of the observation group was 97.5％, significantly higher than that of the control group 72.5％; the differences between the two groups were statistically significant.Conclusion The implementation of psychological nursing of pantoprazole in treatment of gastric ulcer in the process, can consolidate the curative effect to be fully reflected, help patients recover in time, and improve patient care for acceptance,it is worthy of reference.
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OBJECTIVE:To establish a method for the determination of related substances in Pantoprazole sodium for injec-tions. METHODS:HPLC method was adopted. The determination was performed on Kromasil Hypersil ODS column with mobile phases consisting of 0.01 mol/L potassium dihydrogen phosphate buffer solution(pH adjusted to 7.0)-acetonitrile(gradient elution) at a flow rate of 1.0 mL/min. The detection wavelength was set at 290 nm,and the column temperature was 40 ℃,and injection volume was 20 μL. RESULTS:The linear ranges of impurity A,impurity B,impurity C+E,and impurity D were 0.4168-1.0420μg/mL(r=0.9998),0.1950-0.4875 μg/mL(r=0.9999),0.3890-0.9725 μg/mL(r=0.9998),0.1986-0.4965 μg/mL(r=0.9998), respectively. The limits of quantitation were 0.834,0.780,1.556,0.794 ng/mL;the limits of detection were 0.417,0.390,0.778, 0.397 ng/mL,respectively. RSD of precision test was lower than 1.0%;in repetitive test,RSD for total peak area of impurity was lower than 1.0% ;the recoveries were 98.81% -102.49%(RSD=1.18% ,n=9),95.31% -98.44%(RSD=0.91% ,n=9), 96.88%-98.44%(RSD=0.52%,n=9)and 97.87%-101.28%(RSD=1.05%,n=9). CONCLUSIONS:The method is convenient, accurate and suitable for the determination of related substance in Pantoprazole sodium for injection.
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[ ABSTRACT] AIM:To explore the inhibitory effects of pantoprazole sodium on epithelial-mesenchymal transition and cisplatin resistance in lung cancer cells and the underlying mechanism .METHODS: Using MTT method, wound healing assay , Transwell experiment , Western blot , the differences of morphology , invasion ability , migration ability , drug sensitivity and protein expression between A 549/DDP cells and A549 cells were determined .The effect of pantoprazole so-dium on morphology , invasion ability , migration ability , drug sensitivity and protein expression in A 549/DDP cells were al-so observed.RESULTS: Compared with A549 cells, A549/DDP cells had higher invasion and migration abilities , and lower drug sensitivity , exhibited mesenchymal phenotype and activated c-Met/AKT/mTOR pathway .Pantoprazole sodium inhibited the abilities of invasion and migration , and reversed the mesenchymal phenotype , drug resistance and the c-Met/AKT/mTOR pathway activation in A549/DDP cells.Treatment with c-Met inhibitor SU11274, PI3K inhibitor LY294002 and mTOR inhibitor rapamycin had the same effects on A 549/DDP cells as that of pantoprazole sodium .CONCLUSION:Pantoprazole sodium inhibits invasion , migration, epithelial-mesenchymal transition and cisplatin resistance in lung cancer cells by down-regulating c-Met/AKT/mTOR pathways .
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OBJECTIVE:To stndy the clinical efficacy and safety of somatostatin combined with pantoprazole sodium in the treatment of severe acute pancreatitis(SAP). METHODS:By retrospective analysis,98 patients with SAP were divided into control group and observation group by the different treatment. All patients were treated by routine treatment of SAP. Based on it,patients in control group were given Pantoprazole sodium for injection 40 mg adding into 0.9% sodium chloride injection 100 ml,iv,twice a day;patients in observation group were given Somatostatin for injection 3 mg adding into 0.9% sodium chloride injection 100 ml based on the treatment of control group,by micro intravenous continuous intravenous infusion,0.25 mg/h,twice a day.Both cours-es were 7 d. The clinical data was observed,including clinical efficacy,improvement time of signs and symptoms(remission time of stomachache,recovery time of gastrointestinal function,withdrawal time of ventilator) and tumor necrosis factor-α(TNF-α), high-sensitivity C-reactive protein (hs-CRP),interleukin-8 (IL-8) levels and the incidence of adverse reactions before and after treatment. RESULTS:The total effective rate in observation group was significantly higher than control group,and the improve-ment time of signs and symptoms was significantly shorter than control group,with significant differences(P<0.05). After treat-ment,the inflammatory cytokine levels in 2 groups were significantly lower than before,and observation group was lower than con-trol group,with significant differences(P<0.05). The incidence of adverse reactions in observation group was significantly lower than control group,with significant difference(P<0.05). CONCLUSIONS:Based on the routine treatment,somatostatin combined with pantoprazole sodium has better efficacy than only pantoprazole sodium,with better safety.
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Objective The aim of this study was to investigate the effect of left-handed pantoprazole sodium on rat models of gastric ulcer generated by pyloric ligation .Methods The rat models induced by pylorus ligation were treated with a single intravenous injection of left-handed pantoprazole sodium .The gastric ulcer inhibition rate , volume of gastric juice, activity of pepsin, and level of serum gastrin were determined and gastric mucosa tissue was examined by pathology . Results The gastric ulcer index , volume of gastric juice , activity of pepsin and level of serum gastrin in the rats pretreated with left-handed pantoprazole sodium (0.9, 1.8, 3.6 mg/kg, i.v.) were significantly lower than those in the model group .The lesions of gastric mucosa were also improved in the pantoprazole-treated groups .Conclusions Left-handed pantoprazole sodium has remarkable protective effects on the gastric mucosa in rat models of gastric ulcer induced by pyloric ligation.
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Objective:To establish a method for the content determination of pantoprazole sodium for injection by high performance capillary electrophoresis. Methods:The determination was performed on an uncoated elastic quartz capillary column, the running buff-er was 0. 01 mol·L-1 potassium dihydrogen phosphate buffer, the running voltage was 25kV,the column temperature was 25℃ and the detection wavelength was 289 nm. Results:The linear range was good within the concentration range of 20. 05-200. 51 μg·ml-1(r=0. 999 6). The average recovery was 99. 03%(RSD=0. 86%, n=9). Conclusion:The method is simple, sensitive and reproduci-ble, and can be used in the determination of pantoprazole sodium for injection.
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Objective To explore the efficacy of somatostatin and pantoprazole sodium in treatment of severe acute pancreatitis. Methods 124 cases with severe acute pancreatitis admitted in the People's Hospital of Zhoushan City from Jan 2011 to Jan 2014 were randomly divided into control group and combination group,each had 62 cases. Patients in control group were treated with pantoprazole sodium,while in combination group were treated with somatostatin and semi Pantoprazole sodium. Results The total effective rate in combination group was 95.16%,higher than 64.52% in control group. the difference was significant(P<0.05 ). The recovery time and the incidence of complication in combination group was significantly lower than control group (P <0.05 ). Conclusion Somatostatin and pantoprazole sodium can effectively improve the treatment efficiency of SAP patients,shorten recovery time,and reduce the incidence of complication.
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OBJECTIVE: The systemic toxicities of S-(-)-pantoprazole sodium in rats following intravenous injuction for 30 d were studied. METHODS: One hundred rats were divided randomly into 5 groups: vehicle control group, pantoprazole sodium control group and three S-(-)-pantoprazole sodium groups with different dosages, and received vehicle, pantoprazole sodium(80 mg·kg-1·d-1), S-(-)-pantoprazole sodium(80, 40 and 20 mg·kg-1·d-1) by i.v.via tail vein. Administrations were performed each day for consecutive 30 d. Haematological parameters, biochemical parameters, and histopathology analysis were determined at 30 d of treatments and 14 d after the withdrawal, respectively. RESULTS: The rats in the S-(-)-pantoprazole sodium group at 80 mg·kg-1·d-1 apperanced shortness of breath, unsteady gait, lying motionless and other symptoms. The levels of TC, Na+, Cl- in this group were significantly higher or lower than those in vehicle control group at 30 d(P<0.05), The change of these parameters regained to normal at 14 d after withdrawal. CONCLUSION: Intravenous administration of the S-(-)-pantoprazole sodium for 30 d at high dose could induce reversible damage to liver and electrolyte. The toxicity of S-(-)-pantoprazole sodium is similar with pantoprazole sodium at the same dosage.
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OBJECTIVE: To select appropriate liquid chromatography conditions to determine the correction factors for the related compounds A, B, C, D + F and E of pantoprazole thus to establish the determination method of the related substances. METHODS: The separation was achieved on a C18 column(4. 6 mm × 250 mm, 5 μm) utilizing a mobile phase of acetonitrile and 0.01 mol · mL-1 dipo-tassium hydrogen phosphate(0 min, 80:20; 40 min, 40:60; 45 min, 20:80)at a flow rate of 1.0 mL · min-1. The column temperature was set at 35°C. The compounds were monitored at 288 nm. RESULTS: Pantoprazole sodium and its impurities were well separated by the method. The correction factors of pantoprazole related compounds A, B, C, D + F and E were 0.94, 0.93, 0.67, 0.96 and 0.99. CONCLUSION: The method can be used for the quality control of pantoprazole sodium and its related substances in the preparations.
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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.
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A simple, sensitive and precise high performance liquid chromatographic method for the analysis of Pantoprazole sodium and lansoprazole has been developed, validated and used for the determination of compounds in commercial pharmaceutical products. The compounds were well separated an isocratically on a C18 column [Use Inertsil C18, 5m , 150 mm x 4.6 mm] utilizing a mobile phase consisting of acetonitrile: phosphate buffer (60:40, v/v, pH 7.0) at a flow rate of 1.0 ml/min with UV detection at 230 nm. The retention time of Pantoprazole sodium and lansoprazole was found to be 2.017 min and 2.538. The procedure was validated for linearity (Correlation coefficient = 0.999). The study showed that reversed-phase liquid chromatography is sensitive and selective for the determination of Pantoprazole sodium and lansoprazole using single mobile phase.
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Aim: To establish a method for the determination of pantoprazole sodium and its related substances. Methods: A column packed with octadecylsiance bonded silica gel (250 mm × 4. 6 mm, 5 pjn) was used. The 0. 01 mol/L monopotassium phosphate solution( adjusted with phosphoric acid to pH 7. 0) -acetonitrile were adopted as the mobile phase, a gradient elution was programmed as follows: 0→30 min(90:10-60:40), 30→45 min(60: 40→15: 85); the detection wavelength was 289 nm; the column temperature was 40 ℃; the flow rate was 1. 0 mL/min. Results: Pantoprazole sodium, the intermediates and its related substances could be well separated. A good linear relationship was obtained over the range of 6. 96-48. 72 μg/mL( r =0. 999 9). The limit detection and quantisation of pantoprazole sodium were 8.51 ng and 17.0 ng, respectively. Conclusion: This method can be applied to control the related substances of pantoprazole sodium and determine pantoprazole sodi-um.
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OBJECTIVE:To investigate the stability of injectable pantoprazole sodium in 4 kinds of infusions.METHODS: A HPLC method was adopted in this determination, the content change of injectable pantoprazole sodium was determined within 4 hours' mixing with 4 kinds of infusions and its change of color was observed; meanwhile the effects of pH value, potassium,magnesium,calcium ions on the stability of injectable pantoprazole sodium were investigated.RESULTS:No obvious changes were noted in terms of contents, appearances, pH value, UV - absorption maximum wavelength for the injectable pantoprazole sodium solution within 4 hours either in 4 kinds of common infusions or in potassium,magnesium,calcium ions water solutions.It was extremely unstable when pH value of pantoprazole sodium solution was lower than 7.0;when its pH value was 7.0, its color became yellowish yet without obvious loss of content; it is stable within 4h when its pH value was above 8.0.CONCLUSIONS:Injectable pantoprazole sodium remains stable within 4 hours either in 4 kinds of common infusions or in potassium, magnesium, calcium ions water solutions, the pH value has a great influence on the stability of pantoprazole sodium solution.
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AIM: To study pharmacokinetics and relative bioavailability of pantoprazole sodium enteric-coated test and reference tablets in healthy volunteers. METHODS: A single oral dose of 40 mg pantoprazole sodium enteric-coated test and reference tablets were given to 20 male healthy volunteers in a randomized two-way crossover design. Plasma concentrations of pantoprazole were determined by HPLC method. Pharmacokinetic parameters and relative bioavailability were calculated with DAS program to evaluate the bioequivalence of the two preparations. RESULTS: Plasma concentration-time profiles were adequately described by a two-compartment open model. The main pharmacokinetic parameters of pantoprazole sodium test and reference tablets were as follow: The values of Tmax were (3.18±0.54) and (3.30±0.47) h, Cmax were (2.98±0.83) and (2.91±0.87) mg·L-1, T1/2β were (1.86±0.41) and (1.72±0.48) h, AUC0-t were (9.51±3.71) and (9.77±4.55) mg·h·L-1, respectively. The relative bioavailability of test tablets was (102.3±19.6)%. CONCLUSION: The two preparations of pantoprazole sodium are bioequivalent.