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口服肠溶包衣奥美拉唑颗粒后有效的胃酸抑制作用。

Effective gastric acid suppression after oral administration of enteric-coated omeprazole granules.

作者信息

Mohiuddin M A, Pursnani K G, Katzka D A, Gideon R M, Castell J A, Castell D O

机构信息

Graduate Hospital, Department of Medicine, Philadelphia, Pennsylvania 19146, USA.

出版信息

Dig Dis Sci. 1997 Apr;42(4):715-9. doi: 10.1023/a:1018839425118.

DOI:10.1023/a:1018839425118
PMID:9125637
Abstract

Omeprazole is inactivated by exposure to gastric acid and is formulated as a gelatin capsule containing enteric-coated granules that release the drug in alkaline medium. In clinical situations where patients are unable to take the capsule orally, the optimum means of administration is uncertain. Eleven normal volunteers were given omeprazole 20 mg every day for one week before breakfast in random order as either a 20-mg capsule with water or free enteric-coated granules with either 8 oz of orange juice, 8 oz of water with 2 Alka-Seltzer antacid tablets (aspirin free), or 1 teaspoon of apple sauce. On day 7 of each regimen, an 8-hr intragastric pH study was performed following omeprazole 20 mg and standard breakfast. The median percentage of time of gastric acid pH > 4 after an omeprazole capsule was 68.5 (25-100); after granules with orange juice 59 (43-100); after granules in Alka-Seltzer solution 63 (31-100), and after granules in apple sauce 65 (30-99), with no significant differences (ANOVA). The time for the gastric pH to reach <4' after having been above was also similar for all four regimens (ANOVA). Omeprazole granules administered orally in a variety of ways achieve gastric acid suppression as effectively as the intact capsule.

摘要

奥美拉唑遇胃酸会失活,其剂型为明胶胶囊,内含肠溶包衣颗粒,该颗粒在碱性介质中释放药物。在临床情况下,若患者无法口服胶囊,最佳给药方式尚不确定。11名正常志愿者被随机安排在早餐前每天服用20毫克奥美拉唑,为期一周,服用方式分别为用水送服20毫克胶囊、用8盎司橙汁送服游离的肠溶包衣颗粒、用8盎司水加2片不含阿司匹林的阿耳卡-塞耳策抗酸片送服游离的肠溶包衣颗粒或用1茶匙苹果酱送服游离的肠溶包衣颗粒。在每种给药方案的第7天,在服用20毫克奥美拉唑和标准早餐后进行了8小时的胃内pH值研究。服用奥美拉唑胶囊后胃酸pH值>4的时间中位数为68.5(25 - 100);用橙汁送服颗粒后为59(43 - 100);用阿耳卡-塞耳策溶液送服颗粒后为63(31 - 100),用苹果酱送服颗粒后为65(30 - 99),差异无统计学意义(方差分析)。对于所有四种给药方案,胃酸pH值从高于4降至<4的时间也相似(方差分析)。以多种方式口服的奥美拉唑颗粒抑制胃酸的效果与完整胶囊一样有效。

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本文引用的文献

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Optimal dosing of omeprazole 40 mg daily: effects on gastric and esophageal pH and serum gastrin in healthy controls.每日40毫克奥美拉唑的最佳剂量:对健康对照者胃和食管pH值及血清胃泌素的影响。
Am J Gastroenterol. 1996 Aug;91(8):1532-8.
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Bioavailability and efficacy of omeprazole given orally and by nasogastric tube.口服和经鼻胃管给予奥美拉唑的生物利用度和疗效。
Dig Dis Sci. 1996 Mar;41(3):475-9. doi: 10.1007/BF02282321.
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Gut. 1983 Apr;24(4):270-6. doi: 10.1136/gut.24.4.270.
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The effect of omeprazole on gastric emptying in patients with duodenal ulcer disease.奥美拉唑对十二指肠溃疡病患者胃排空的影响。
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Dose-response study of omeprazole on meal-stimulated gastric acid secretion and gastrin release.奥美拉唑对进餐刺激胃酸分泌和胃泌素释放的剂量反应研究。
Gastroenterology. 1983 Dec;85(6):1373-8.
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Intravenous omeprazole rapidly raises intragastric pH.静脉注射奥美拉唑可迅速提高胃内pH值。
Gut. 1985 Sep;26(9):902-6. doi: 10.1136/gut.26.9.902.
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The effect of omeprazole on insulin induced gastric secretion in man.
Scott Med J. 1985 Apr;30(2):96-100. doi: 10.1177/003693308503000205.
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Omeprazole: a study of its inhibition of gastric pH and oral pharmacokinetics after morning or evening dosage.奥美拉唑:早晨或晚上给药后对胃内pH值的抑制作用及口服药代动力学研究。
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