Roxatidine Acetate Hydrochloride

The RxAc drug loaded on Tween80-chitosan-TPP nanoparticles (NRxAc) has been characterized and probed by UV-Vis, PXRD, FTIR, DLS and SEM technique. The physicochemical characteristics of NRxAc have been employed and evaluated for formulation of drug, particle size, external morphology, drug content and in vitro drug release. Multi-spectroscopic (i.e. fluorescence, UV-Vis, CD spectroscopy) and molecular docking techniques were also used to study the interaction of BSA with RxAc and NRxAc. RxAc and NRxAc quenched the fluorescence emission of BSA via a static quenching mechanism. The experimental data of Fluorescence demonstrated that the binding constant of RxAc and NRxAc were found around 10⁴ L.mol^-1, which suggests moderate binding affinity with BSA via hydrophobic forces. Through the site marker displacement experiments and molecular docking, the probable binding location of RxAc and NRxAc has been suggested in subdomain IB (site III) of BSA. Altogether, the results of present study can provide an important insight and a great deal of helpful information for future design of antiulcer drugs. Hence, The RxAc-loaded chitosan nanoparticles produced might be utilized as a successful tool for developing and using antiulcer drugs.Communicated by Ramaswamy H. Sarma.

This study aimed to evaluate the bioequivalence between a generic roxatidine acetate hydrochloride (RAH) sustained‐release capsule and brand‐named formulation (ALTAT) under fasting and fed conditions. An open‐label, single‐center, randomized 2‐period crossover study with a 5‐day washout period was conducted. A single oral dose of 75‐mg generic RAH sustained‐release capsule (test drug) or a commercial capsule (reference drug) was given to healthy volunteers under fasting (n = 36) and fed conditions (n = 36). Blood samples were collected at baseline and during the 24 hours after dosing. The concentrations of roxatidine acetate (ROX) and bioactive metabolite roxatidine in plasma were detected using a validated high‐performance liquid chromatography–tandem mass spectrometry method. Pharmacokinetic parameters were analyzed with noncompartmental methods. As prodrug, RAH was dehydrochloric acid to ROX in body and further rapidly converted to roxatidine. Such a rapid metabolism resulted in ROX that was hardly detected in plasma. Active metabolism roxatidine was therefore used to evaluate the pharmacokinetic process. The major pharmacokinetic parameters of roxatidine including peak plasma concentration, area under the plasma concentration–time curve from time 0 to time t, and area under the plasma concentration–time curve from time 0 to infinity were similar between the 2 preparations under fasting and fed conditions. The generic RAH sustained‐release capsule is bioequivalent to the reference drug under fasting and fed conditions in healthy Chinese subjects.