摘要
Resumen Introducción: Una encuesta nacional en población abierta mostró que la enfermedad por reflujo gastroesofágico (ERGE) tiene alta prevalencia en México. Objetivo: Comparar la eficacia y seguridad de dos isómeros, dexrabeprazol (10 mg) versus esomeprazol (20 mg), en el tratamiento de la ERGE durante cuatro semanas. Métodos: Ensayo clínico fase III, aleatorizado, multicéntrico, prospectivo, doble ciego, en dos grupos que incluyeron 230 pacientes. Resultados: Con ambos tratamientos se observó disminución estadísticamente significativa en la severidad de los síntomas de ERGE (pirosis, regurgitación, dolor epigástrico y disfagia), evaluados mediante una escala visual análoga. La puntuación promedio de dexrabeprazol en el Cuestionario de Carlsson-Dent a los 28 días fue de 2.12 y la de esomeprazol de 3.02. Ambos tratamientos fueron efectivos, sin diferencia estadísticamente significativa (p < 0.05). En el Cuestionario de Salud SF-36 se observó que ambos mejoraron la puntuación en la calidad de vida, sin diferencia significativa. Ambos medicamentos fueron bien tolerados y el perfil de incidencia de eventos adversos fue bajo. Conclusiones: En el tratamiento de ERGE no erosiva, el uso de 10 mg/día de dexrabeprazol es tan efectivo como 20 mg/día de esomeprazol, con la ventaja de que la dosis es menor con un adecuado perfil de seguridad.
Abstract Introduction: A national survey in the general population showed that gastroesophageal reflux disease (GERD) is highly prevalent in Mexico. Objective: To compare the efficacy and safety of two isomers, dexrabeprazole (10 mg) vs. esomeprazole (20 mg), in the treatment of GERD for four weeks. Methods: Randomized, multicenter, prospective, double-blind phase III clinical trial in two groups that included 230 patients. Results: A statistically significant decrease in the severity of GERD symptoms (heartburn, regurgitation, epigastric pain and dysphagia), evaluated using a visual analogue scale, was observed with both treatments. Mean score for dexrabeprazole on Carlsson-Dent questionnaire at 28 days was 2.12, and for esomeprazole, 3.02. Both treatments were effective, with no statistically significant difference being recorded (p < 0.05). On SF-36 health questionnaire, both were observed to improve the quality-of-life score, with no significant difference being identified. Both drugs were well tolerated, and the adverse event incidence profile was low. Conclusions: In the treatment of non-erosive GERD, the use of dexrabeprazole at 10 mg/day is as effective as esomeprazole 20 mg/day, with the advantage that the dose is lower with an appropriate safety profile.
摘要
The aim of the work is to improve the synthetic process of dexrabeprazole sodium,enhance quality and yield of the product,simplify synthetic steps,and offer a stable and feasible process. Starting from 2-[[[4-(3-methoxypropoxy)-3-methylpyridine-2-yl]methyl]thio]-1 H-benzimidazole,dexrabeprazole was produced by asym-metric oxidation reaction with oxidant cumene hydroperoxide in the presence of chiral catalyst tetraisopropyl titan-ate and L-(+)-tartaric acid diethyl ester. Dexrabeprazole sodium was obtained by the reaction of purified dexrabeprazole with sodium hydroxide in a total yield of 79%with an HPLC purity of >99. 5%. The structure of dexrabeprazole sodium was confirmed by NMR,IR,elemental analysis and LC-MS. The improved process of dexrabeprazole sodium possesses simple operations,good yield and high purity,which is feasible for industrializa-tion.