Lenaerts C, Beraud N, Castaigne J P
Center Hospitalier, Universitaire D'Amiens, France.
J Pediatr Gastroenterol Nutr. 1988;7 Suppl 1:S18-21.
In order to avoid inactivation in the stomach, pancreatic enzymes have been prepared as pH-sensitive, enteric-coated microspheres (Pancrease). An in vitro study was performed to evaluate the pH-related dissolution of Pancrease and to confirm its resistance to gastric acidity. Two assay methods were used with three different batches of Pancrease: (a) Enzyme absorbency at 280 nm was measured at unit pH intervals from pH 1 to pH 8 and at 0.5 pH intervals from the start of dissolution to pH 8. (b) Proteolytic activity was measured at pH 6.8. Significant enzyme dissolution started at pH 5.5 and was maximal at pH 6.0. At pH 6.8, the pH of simulated intestinal fluid, dissolution was complete in less than 15 min. At pH 5.0, no dissolution occurred within the first 10 min and only 13% dissolution was observed after 2 h. At pH 7.0, 100% dissolution was seen within 10 min. Results of the two assay methods were comparable with all three enzyme batches assayed. This study confirmed the gastroresistance of Pancrease. Because of the enteric coating of Pancrease, liberation of enzymes occurs in the duodenum and jejunum, providing maximal enzymatic efficacy in exocrine pancreatic insufficiency.
为避免在胃中失活，胰酶已被制备成对pH敏感的肠溶微球（胰酶胶囊）。进行了一项体外研究，以评估胰酶胶囊与pH相关的溶出情况，并确认其对胃酸的耐受性。使用两种测定方法对三批不同的胰酶胶囊进行检测：（a）在pH值从1到8每隔1个单位pH值，以及从溶出开始到pH值8每隔0.5个单位pH值时，测量280nm处的酶吸光度。（b）在pH 6.8时测量蛋白水解活性。酶的显著溶出在pH 5.5时开始，并在pH 6.0时达到最大值。在模拟肠液的pH 6.8时，溶出在不到15分钟内完成。在pH 5.0时，最初10分钟内没有溶出发生，2小时后仅观察到13%的溶出。在pH 7.0时，10分钟内观察到100%的溶出。两种测定方法的结果与所检测的所有三批酶均具有可比性。该研究证实了胰酶胶囊的抗胃酸能力。由于胰酶胶囊的肠溶包衣，酶在十二指肠和空肠中释放，在外分泌性胰腺功能不全中提供最大的酶活性。
