Pharmacokinetics, Bioequivalence, and Safety Studies of Pantoprazole Sodium Enteric‐Coated Tablets in Healthy Subjects

Abstract

This study aimed to evaluate the bioequivalence of 2 pantoprazole sodium enteric‐coated tablet formulations, a generic formulation and a branded formulation, and to investigate their pharmacokinetic and safety profiles. The study was designed as a single‐center, randomized, open‐label, single‐dose, dual‐period, and 2‐sequence crossover trial, and was divided into fasting and postprandial human bioequivalence trials. In the first trial, 36 subjects were fasted overnight before they were given generic or branded tablets (during 2 separate administration periods). Separately, 42 subjects were provided a high‐fat meal 1 hour before the drugs were administered. Blood specimens of each subject were obtained up to 24 hours after drug administration. No significant differences were observed between the pharmacokinetic profiles of the generic and branded pantoprazole sodium enteric‐coated tablets. Bioequivalence was evaluated using 90% confidence intervals for the ratio of test/reference log area under the concentration‐time curve over 24 hours, log area under the concentration‐time curve to infinity (AUC0‐∞), and log peak concentration (Cmax). The 90% confidence intervals of the least squares geometric mean ratio of Cmax, area under the concentration‐time curve from time zero to the last measurable concentration (AUC0‐t), and AUC0‐∞ of 36 subjects in the fasting trial and of 40 of 41 subjects in the postprandial trial (Cmax [41], AUC0‐t [41], and AUC0‐∞ [40]) were in accordance with the bioequivalence criteria. No severe adverse effects were detected. The generic and branded pantoprazole sodium enteric‐coated tablets were considered bioequivalent with similar safety profiles.

Influence of Storage Conditions on the Pantoprazole Dissolution Profile for Gastro-Resistant Tablet Formulations

“…antoprazole belongs to the group of proton pump inhibitors, together with omeprazole, lansoprazole, rabeprazole, and esomeprazole (1). Pantoprazole irreversibly binds to the proton pump H + /K + ATPase in the parietal cells of the stomach and reduces secretion of gastric acid (2,3). Therapeutic indications for the use of pantoprazole are gastro-oesophageal reflux disease, stomach and duodenal ulcers, and Zollinger Ellison syndrome.…”

“…Therapeutic indications for the use of pantoprazole are gastro-oesophageal reflux disease, stomach and duodenal ulcers, and Zollinger Ellison syndrome. It is also used as part of triple therapy for Helicobacter pylori eradication (3,4). Orally administered pantoprazole has an absolute bioavailability of 77 %; it is absorbed rapidly and does not accumulate with frequent use.…”

“…It is metabolized in the liver, the main metabolite being dimethylpantoprazole-P sulfate. These metabolites are primarily eliminated from the body by the kidneys (3,5). The optimal effective dose of pantoprazole for adults is 40 mg once per day (4).…”