AIMTo study the chiral inversion of dextropantoprazole in human.

METHODSThree healthy Chinese male volunteers after an oral dose of 40 mg dextropantoprazole. An HPLC method was developed and used to determine the total plasma concentrations of each enantiomer. The ratios of the enantiomers in plasma samples were measured on a Chiral-AGP column. The plasma concentration of each enantiomer was then calculated using the ratios of enantiomers and total concentrations of the two enantiomers previously measured.

RESULTSThe AUC0-t of levopantoprazole was only 1.5% of the total AUC0-t of enantiomers.

CONCLUSIONThe chiral inversion from dextropantoprazole to levopantoprazole does not occur in the three healthy Chinese male volunteers after an oral dose of 40 mg dextropantoprazol.

2-Pyridinylmethylsulfinylbenzimidazoles ; Administration, Oral ; Adult ; Anti-Ulcer Agents ; blood ; chemistry ; pharmacokinetics ; Area Under Curve ; Benzimidazoles ; blood ; chemistry ; pharmacokinetics ; Chromatography, High Pressure Liquid ; Humans ; Male ; Omeprazole ; analogs & derivatives ; blood ; chemistry ; pharmacokinetics ; Stereoisomerism ; Sulfoxides ; blood ; chemistry ; pharmacokinetics

OBJECTIVETo investigate the antimicrobial activity of Pariet, Tekpron, Nexium, respectively, against Helicobacter pylori (H. pylori) in vitro.

METHODSAntimicrobial effects of these medicines were evaluated through detection of MICs for 3 H. pylori strains isolated from different countries.

RESULTSThe MIC(99) contents were 2.25 mg/L, 42.5 mg/L and 360 mg/L, respectively, for the three medicines. The strains under testing exhibited the same susceptibility to each medicine. Nexium did not inhibit the bacteria under the concentration of 3.6 - 36 mg/L with more and bigger H. pylori colonies seen when compared with controls.

CONCLUSIONSThe growth inhibitory activity appeared to be different among the three PPI medicines under investigation, with Rabeprazole the most potential agent of the three. Data suggested that the action of growth inhibition in vitro was resting on the characteristic of the given PPI as well as the supplements of the medicine.

2-Pyridinylmethylsulfinylbenzimidazoles ; Benzimidazoles ; pharmacology ; Enzyme Inhibitors ; pharmacology ; Esomeprazole ; analogs & derivatives ; pharmacology ; Helicobacter pylori ; drug effects ; Lansoprazole ; Microbial Sensitivity Tests ; Proton Pump Inhibitors ; Rabeprazole

OBJECTIVE: To investigate the effect of sulforaphane (SFN) on G METHODS: KG1a and KG1cells were treated by different concentrations of SFN for 48 h. Flow cytometry (FCM) was used to analyze the phase distribution of cell cycle. High-throughput sequencing was used to detect the effect of SFN on the expression of cell cycle related genes in KG1a cells. The mRNA expression of P53, P21, CDC2 and CyclinB1 were detected by qPCR. The protein expression of P53, CDC2, P-CDC2 and CyclinB1 were detected by Western blot. RESULTS: Cells in the G CONCLUSION SFN induces leukemia cells to block in G
Cell Cycle ; Humans ; Isothiocyanates/pharmacology* ; Leukemia, Myeloid, Acute ; Mitosis ; Sulfoxides

The objective of the present study was to establish the method of measurement of hydrogen peroxide and to estimate the anti-oxidative effect of genistein in the skin. UVB induced skin oxidation and anti-oxidative effect of genistein formulations were evaluated by determining levels of hydrogen peroxide. The mechanism involved in the determination of hydrogen peroxide is based on a color reaction between ferric ion (Fe3+) and xylenol orange, often called FOX assay and subsequent monitoring of absorbance values of the reactant at 540 nm. The reaction was to some extent pH-dependent and detection sensitivity was greatest at pH 1.75. Genistein liposomal gel demonstrated better anti-oxidative effect with regard to lowering hydrogen peroxide levels elevated by UVB irradiation compared to genistein-suspended gel. A linear relationship has been observed between anti-oxidative effect of genistein and drug deposition in the skin tissue. Genistein liposomal gel resulting in the localization of the drug in the deeper skin led to improved anti-oxidative effect compared to genistein gel. The suggested method for evaluation of oxidation of the skin can be used as a tool to screen effective anti-oxidative agents and their delivery systems acting on the skin.
Citrus sinensis ; Genistein ; Hydrogen Peroxide ; Hydrogen-Ion Concentration ; Phenols ; Skin ; Sulfoxides

Anaphylaxis to proton pump inhibitors (PPIs) has rarely been reported. Different patterns of cross-reactivity between PPIs have also been demonstrated using skin tests. Here, we report a case of anaphylaxis to lansoprazole with tolerance to other commercially available PPIs, which was proved by skin tests and oral provocation tests (OPTs). A 47-year-old female patient visited our Emergency Department with a sudden onset of whole body urticaria, facial swelling, dyspnea, and loss of consciousness that developed 1 hour after ingestion of 30 mg of lansoprazole for her episodic epigastric soreness. The skin prick test (SPT) and the intradermal test (IDT) with lansoprazole, esomeprazole, rabeprazole, and pantoprazole were performed. Lansoprazole showed positive reactions in both the SPT (3 mg/mL) and the IDT (0.003 mg/mL). Rabeprazole (3 mg/mL) showed a positive reaction only in IDT. The SPT and the IDT with esomeprazole and pantoprazole were all negative. The OPT with 30 mg of lansoprazole was positive (showing generalized rash and facial swelling 30 minuites after ingestion), while OPTs with esomeprazole, pantoprazole, and rabeprazole were all negative. Other PPIs could be safe alternatives in cases of anaphylaxis to 1 PPI. Skin tests seem to be helpful to define cross-reactivity between PPIs.
Anaphylaxis* ; Dyspnea ; Eating ; Emergency Service, Hospital ; Esomeprazole ; Exanthema ; Female ; Humans ; Intradermal Tests ; Lansoprazole* ; Middle Aged ; Proton Pump Inhibitors* ; Rabeprazole ; Skin ; Skin Tests ; Unconsciousness ; Urticaria

Animals ; Apoptosis ; Cell Line, Tumor ; Cell Proliferation ; Disulfides ; Male ; Mice ; Mice, Inbred BALB C ; Phosphatidylinositol 3-Kinases ; Stomach Neoplasms/drug therapy* ; Sulfoxides

The organosulfur compound sulforaphane (SFN; C₆H₁₁NOS₂) is a potent cytoprotective agent promoting antioxidant, anti-inflammatory, antiglycative, and antimicrobial effects in in vitro and in vivo experimental models. Mitochondria are the major site of adenosine triphosphate (ATP) production due to the work of the oxidative phosphorylation (OXPHOS) system. They are also the main site of reactive oxygen species (ROS) production in nucleated human cells. Mitochondrial impairment is central in several human diseases, including neurodegeneration and metabolic disorders. In this paper, we describe and discuss the effects and mechanisms of action by which SFN modulates mitochondrial function and dynamics in mammalian cells. Mitochondria-related pro-apoptotic effects promoted by SFN in tumor cells are also discussed. SFN may be considered a cytoprotective agent, at least in part, because of the effects this organosulfur agent induces in mitochondria. Nonetheless, there are certain points that should be addressed in further experiments, indicated here as future directions, which may help researchers in this field of research.
Animals ; Antioxidants/pharmacology* ; Apoptosis/drug effects* ; Brain/ultrastructure* ; Carbon Monoxide Poisoning/metabolism* ; Cytoprotection ; Humans ; Isothiocyanates/pharmacology* ; Membrane Potential, Mitochondrial/drug effects* ; Mitochondria/metabolism* ; Sulfoxides

This work aimed to set up a high performance liquid chromatography (HPLC) method to determine the concentration of lansoprazole in human plasma and study the pharmacokinetic characters of lansoprazole in Chinese healthy volunteers after intravenous (IV) infusion. In accordance with double 3 x 3 Latin square design with self-crossover design, 12 volunteers were randomly divided into six groups, with half males and half females. The volunteers were administered with single dose of 15, 30, 60 mg of lansoprazole by IV infusion at a constant speed respectively, to study the clinical pharmacokinetics of lansoprazole. The linear range of lansoprazole in human plasma was 0.020-4.970 microg/ml (r = 0.9999); The intra-day and inter-day RSD were less than 10%. After receiving single doses of 15, 30 and 60 mg of lansoprazole, t(1/2) were (1.663 +/- 0.405) h, (1.541 +/- 0.339)h and (1.747 +/- 0.156) h; Cmax were (1.065 +/- 0.094) microg/ml, (2.104 +/- 0.312) microg/ml and (3.786 +/- 0.356) microg/ml; AUC(0-infinity) were (2.376 +/- 0. 432) microg x h/ ml, (4.722 +/- 0.753) microg x h/ml and (10.495 +/- 2.129) microg x h/ml respectively. The improved HPLC method is simple, rapid and reproducible. It could be used for determination of the concentration of lansoprazole in human plasma. The pharmacokinetics of lansoprazole for injection was found to fit the linear dynamics in vivo within the dose range of 15 to 60 mg. In addition, the results suggested that gender had no statistic significant effect on the pharmacokinetic process of lansoprazole after IV infusion of single dose.
2-Pyridinylmethylsulfinylbenzimidazoles ; administration & dosage ; blood ; pharmacokinetics ; Chromatography, High Pressure Liquid ; methods ; Female ; Humans ; Infusions, Intravenous ; Lansoprazole ; Male ; Proton Pump Inhibitors

BACKGROUND/AIMS: To compare efficacy and tolerability of rabeprazole (RAB) 10 mg versus omeprazole (OME) 20 mg in patients with duodenal ulcer. METHODS: This randomized, comparative, multicenter study was conducted at 10 centers in Korea, from February to September in 1999. Patients with active duodenal ulcer as proven by endoscopy were randomized to RAB (n=123) or OME (n=123) groups. One hundred-twenty-three patients received RAB 10 mg once daily, and 123 patients received OME 20 mg once daily for 2 or 4 weeks. Primary efficacy parameter was complete healing by endoscopy and secondary parameter was the improvement in the severity of clinical symptoms after the therapy. RESULTS: After 2 weeks, complete healing was achieved in 81.7% (85/104) of patients given RAB 10mg and in 81.1% (77/95) of patients given OME 20 mg (p=0.902). After 4 weeks, complete healing was documented in 97.1% (101/104) of patients given RAB 10 mg and in 93.7% (89/95) of patients given OME 20 mg (p=0.315). The percentages of patients resolved daytime pain and night-time pain at Day 4 were 87.5% and 90.1% in RAB group and 79.0% and 80.5% in OME group (p=0.138 and p=0.087 for day-time k night-time pain, respectively). No clinically meaningful changes or other between-group differences were observed in laboratory parameters and adverse events which were evaluated to be related with medication. CONCLUSIONS: In this study, rabeprazole 10 mg produced healing rates and symptom relief equivalent to omeprazole 20 mg at weeks 2 and 4 in patients with active duodenal ulcer and provided a tendency of faster symptom relief than omeprazole 20 mg, although it didn't reach statistical significance. Both the treatments were well tolerated.
Duodenal Ulcer* ; Endoscopy ; Humans ; Korea ; Omeprazole* ; Rabeprazole*

BACKGROUND/AIMS: Although intravenous proton pump inhibitor (PPI) has been used for the prevention of post endoscopic submucosal dissection (ESD) bleeding, the route of administration has not been confirmed. The aim of the present study was to compare the efficacy of intravenous and oral PPI administration for the prevention of delayed post ESD bleeding. METHODS: Total 166 consecutive patients were randomly assigned to 30 mg lansoprazol twice a day (PO group) and 120 mg pantoprazole intravenous injection (IV group) for 48 hours. Finally, 65 patients in PO group and 87 patients in IV group were analyzed. After ESD, all patients underwent follow up endoscopy after 24 hours and were observed the symptoms of bleeding up to 60 days after ESD. RESULTS: Age, sex and use of anticoagulants were not different between groups. At follow up endoscopy after 24 hours, oozing and exposed vessel was noted in 4.6% of PO group and 8.0% of IV group and there was no significant difference. Delayed bleeding occurred in 4 of 65 patients (6.2%) in the PO group and 8 of 87 patients (9.2%) in the IV group (p>0.999). By multivariate analysis, oozing or exposed vessels at follow up endoscopy were risk factors for delayed bleeding (OR=17.5, p=0.022). CONCLUSIONS: There was no significant difference in the delayed bleeding, length of hospital stay according to the administration route. Bleeding stigmata at follow up endoscopy was risk factor of delayed bleeding. Oral PPI administration can cost-effectively replace IV PPI for prevention of post ESD bleeding.
2-Pyridinylmethylsulfinylbenzimidazoles/therapeutic use ; *Administration, Oral ; Aged ; Anticoagulants/therapeutic use ; Endoscopic Mucosal Resection/*adverse effects ; Female ; Gastroscopy ; Humans ; *Injections, Intravenous ; Lansoprazole/therapeutic use ; Male ; Middle Aged ; Odds Ratio ; Postoperative Hemorrhage/etiology/*prevention & control ; Prospective Studies ; Proton Pump Inhibitors/*therapeutic use ; Risk Factors ; Stomach Neoplasms/surgery