Proton Pump Inhibitors and Acid‐Related Diseases

Sachs, George

doi:10.1002/j.1875-9114.1997.tb03675.x

Cited by 147 publications

(1 citation statement)

References 84 publications

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“…Compared to commonly used gastric acid suppressant drugs like H2 receptor antagonists, PPIs offer great advantages in inhibiting gastric acid secretion with a completely inhibitory effect and rapid onset. Moreover, as an irreversible process, PPIs provide long-lasting inhibition and can inhibit the secretion of basic gastric acid and acid secretion caused by histamine, acetylcholine, gastrin, and food stimulation ( Sachs, 1997 ).…”

Section: Introductionmentioning

confidence: 99%

Integrated models of population pharmacokinetics and exposure response to optimize dosage regimen for anaprazole sodium in duodenal ulcer

Zhang,

Song,

Cui

et al. 2024

European Journal of Pharmaceutical Sciences

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Section: Introductionmentioning

confidence: 99%

Integrated models of population pharmacokinetics and exposure response to optimize dosage regimen for anaprazole sodium in duodenal ulcer

Zhang,

Song,

Cui

et al. 2024

European Journal of Pharmaceutical Sciences

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Liquid chromatographic–mass spectrometry analysis and pharmacokinetic studies of a novel rabeprazole formulation, sterile powder for injection, in dogs and rats

Shao

Sun

Xie

et al. 2007

Biopharm & Drug Disp

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Rabeprazole is among the most potent proton pump inhibitors (PPI) identified to date and it has been demonstrated that it is effective in such diseases as gastroesophageal reflux disease (GERD), duodenal ulcer and gastric ulcer. There is currently interest in developing a new formulation: rabeprazole sterile powder for injection (RSPI). This investigation was conducted to evaluate the preclinical pharmacokinetics of RSPI in rats and at the same time a comparative study was carried out in dogs between RSPI and Pariet tablets using liquid chromatographic-mass spectrometry analysis. The liquid chromatographic-mass spectrometry method was first conducted and validated as being specific, and having accuracy, precision, sensitivity and a satisfactory recovery. After intravenous administration of RSPI (i.v.: 2, 6 and 18 mg/kg) to rats, no significant dose-dependency was found in the CL (4.20-5.72 l/h/kg), V(area) (d) (0.94-1.32 l/kg), dose-normalized AUC (197.20-245.82 microg/l*h based on 1 mg/kg) and t(1/2) (p>0.05). In the dog, a randomized, open-label, crossover experiment was carried out to show that the mean area under the plasma concentration-time curve (AUC(0-infinity)) after i.v. administration of RSPI was at least four times larger than that following oral administration of Pariet tablet at an equivalent dose but the elimination half-life of these two formulation was similar (p>0.05). The results showed that the pharmacokinetics of RSPI was linear (r(2) = 0.98) in the dose range 2-18 mg/kg and the RSPI had a much higher AUC(0-infinity) and similar t(1/2) values compared with the enteric-coated tablet.

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Fertility and early embryonic development toxicity and toxicokinetic study of KFP‐H008 in Sprague–Dawley rats

Peng

Shao

et al. 2022

Birth Defects Research

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The novel potassium competitive acid blocker, KFP‐H008, developed to overcome the shortcomings of proton pump inhibitors. In this study, KFP‐H008 was administered by oral gavage at doses of 0 (control), 15, 45, and 150 mg/kg to Sprague–Dawley rats (24 animals per sex per group). Body weight, food consumption, mortality, sexual cycle, mating behavior, pregnancy, sperm motility, and relative organ weights were evaluated. In a concomitant toxicokinetic (TK) study (10 animals per sex per group), plasma TK parameters and tissue distribution of KFP‐H008 were tested. There were obvious effects at the dosage of 150 mg/kg to male rats with decreases of prostate weight and lower weight gain; to female rats with lower weight gain, hair off, and lower corpus luteum count. There were no effects on litter parameters. Time to reach maximum plasma concentrations for KFP‐H008 was between 0.5 and 1.0 hr for the 15 and 45 mg/kg groups, while for the 150 mg/kg group it had a delay to 2 hr. Overall, the NOAEL of KFP‐H008 was considered to be 45 mg/kg in both genders and the TK study shows that exposure (area under the curve) of male rats was about 1,091.0 ± 530.8 μg/Lhr and to female rats was 1,030.5 ± 512.5 μg/Lhr. Administration of KFP‐H008although reaches the reproductive organs, it demonstrated no significant effects on reproductive organs, it did not affect mating, fertility, pregnancy, growth, or morphologic development.

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Proton Pump Inhibitors and Acid‐Related Diseases

Cited by 147 publications

References 84 publications

Integrated models of population pharmacokinetics and exposure response to optimize dosage regimen for anaprazole sodium in duodenal ulcer

Integrated models of population pharmacokinetics and exposure response to optimize dosage regimen for anaprazole sodium in duodenal ulcer

Liquid chromatographic–mass spectrometry analysis and pharmacokinetic studies of a novel rabeprazole formulation, sterile powder for injection, in dogs and rats

Fertility and early embryonic development toxicity and toxicokinetic study of KFP‐H008 in Sprague–Dawley rats

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