Asian Institute of Gastroenterology, Somajiguda, Hyderabad, India.
J Gastroenterol Hepatol. 2010 Jan;25(1):43-7. doi: 10.1111/j.1440-1746.2009.05994.x. Epub 2009 Oct 27.
A pH of more than 6 is required for clot stability and hemostasis. Intravenous proton pump inhibitors have a rapid onset of action compared to oral and have been preferred for management of non-variceal bleeding. Intravenous pantoprazole has been used extensively. Buffered esomeprazole (BE) is an oral preparation consisting of an inner core of non-enteric-coated esomeprazole with a shell of sodium bicarbonate. The buffer protects against acid degradation of esomeprazole in addition to immediate antacid action. The aim of this study was to assess the efficacy of BE for raising and maintaining an intragastric pH of more than 6 in comparison to i.v. pantoprazole in equivalent dosing.
A randomized two-way cross-over study was conducted. Ten healthy volunteers were randomized to twice daily BE 40 mg or pantoprazole 40 mg i.v. bolus. Intragastric pH was measured with a wireless pH radiotelemetry capsule (Bravo, Medtronic). A 2-week washout period was given between doses.
BE achieved a steady pH of more than 6 in a median time of 2 min (range 1-5 min) after the first dose. The mean % time that intragastric pH was more than 6.0 for BE was 96%, and 90% of the 24-h period compared to pantoprazole (47% and 18%), P = 0.000. A median pH (interquartile range) for the BE group was 6.2 (6.175-6.2) which was higher than i.v. pantoprazole 4.60 (4.5-5.0) (P = 0.005).
BE achieves and maintains a pH of more than 6 within minutes of administration. It was significantly superior to i.v. pantoprazole in equivalent dosing. This finding could have implications in the management of non-variceal bleed where a rapid and sustained pH of more than 6 is desirable.
凝血稳定和止血需要 pH 值超过 6。与口服相比，静脉质子泵抑制剂具有快速的作用起效时间，因此已被优先用于治疗非静脉曲张性出血。静脉注射泮托拉唑已被广泛使用。缓冲型埃索美拉唑（BE）是一种口服制剂，由非肠溶埃索美拉唑的内芯和碳酸氢钠外壳组成。该缓冲剂除了具有即刻抗酸作用外，还能防止埃索美拉唑的酸降解。本研究旨在评估 BE 在与等效剂量的静脉注射泮托拉唑相比时，提高和维持胃内 pH 值超过 6 的疗效。
进行了一项随机两向交叉研究。将 10 名健康志愿者随机分为每日两次口服 BE 40mg 或静脉注射泮托拉唑 40mg 推注。使用无线 pH 放射性遥测胶囊（Bravo，Medtronic）测量胃内 pH 值。两次剂量之间给予 2 周洗脱期。
BE 在首次给药后中位数 2 分钟（范围 1-5 分钟）内达到稳定的 pH 值超过 6。BE 的胃内 pH 值超过 6.0 的时间百分比中位数为 96%，24 小时内的时间百分比中位数为 90%，而泮托拉唑为 47%和 18%（P = 0.000）。BE 组的中位 pH 值（四分位距）为 6.2（6.175-6.2），高于静脉注射泮托拉唑 4.60（4.5-5.0）（P = 0.005）。
BE 在给药后数分钟内达到并维持 pH 值超过 6。与等效剂量的静脉注射泮托拉唑相比，BE 具有显著优势。这一发现可能对非静脉曲张性出血的治疗有影响，因为需要快速和持续的 pH 值超过 6。
