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Current advances in technology of proton pump inhibitor formulations

机译:质子泵抑制剂配方技术的最新进展

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Since the identification of gastro erosive reflux disease and peptic ulcer in the early 1900's, the line of treatment of the disease has evolved reasonably. The antisecretory agents used in the treatment regime have developed, beginning with the introduction of cimetidine in the mid-1970s to proton pump inhibitor (PPI) omeprazole in 1989 and subsequently dexlansoprazole dual delayed release in 2009. This development was done to address the unmet needs of patients suffering from severe esophagitis and nocturnal acid breakthrough (NAB). The available PPI formulations which had short plasma elimination half life of less than 2 hours could not inhibit the proton pumps synthesized in the nighttime hours. The inadequacy in symptom control and high prevalence of NAB in patients with more severe gastro esophageal disease still prevailed after medication. This was identified as the unmet needs of PPI formulations. Although novel formulations, including immediate release omeprazole may offer some advantages over existing formulations, it does not address many of the potential unmet needs of patients with these disorders. However, these needs are addressed by dual delayed release technology which delivers dose in a pulsatile manner and provides acid suppression for prolonged period of time.
机译:自从在1900年代早期发现胃糜烂性反流病和消化性溃疡以来,该病的治疗方法已经得到合理发展。从1970年代中期将西咪替丁于1989年引入质子泵抑制剂(PPI)奥美拉唑,随后于2009年引入右兰索拉唑双重缓释以来,已经开发出了用于治疗方案的抗分泌剂。患有严重食管炎和夜间酸突破(NAB)的患者。血浆消除半衰期短于2小时的可用PPI配方不能抑制夜间合成的质子泵。药物治疗后,重度胃食管疾病患者的症状控制不足和NAB患病率较高。这被确定为PPI配方的未满足需求。尽管包括速释奥美拉唑在内的新型制剂可能比现有制剂具有一些优势,但它不能解决这些疾病患者的许多潜在未满足需求。但是,双重延迟释放技术满足了这些需求,该技术以脉冲方式释放剂量并长时间提供酸抑制作用。

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