In vitro dissolution profiles of enteric-coated microsphere/microtablet pancreatin preparations at different pH values
In vitro dissolution profiles of enteric-coated microsphere/microtablet pancreatin preparations at different pH values
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DOI：
10.1046/j.1365-2036.1996.55197000.x
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发表时间：
1996-10-01
影响因子：
7.6
通讯作者：
Heijerman, HGM
中科院分区：
文献类型：
--
作者：
Gan, KH;Geus, WP;Heijerman, HGM
目的：肠溶微球/微片胰酶应在胃内保持完整，并在进入十二指肠后迅速溶解。餐后十二指肠远端腔内pH值为5.75，外分泌胰功能不全时pH值更低。本研究的目的是测定5种目前可用的肠溶微球/微片胰酶制剂在pH为4.0-6.0的缓冲溶液中的体外溶出时间。方法：对Creon、Creon Forte、胰酶、胰酶HL、Panzytrat等制剂进行检测。两个胶囊在37℃的缓冲溶液中放置在USP溶解测试装置中。缓冲液的pH值在4.0 ~ 6.0之间。以125转/分的转速搅拌溶液，每隔一段时间取2 ml样品，在280 nm处测量消光度，监测溶解速度，重复测量6次，结果：所有制剂在pH 4.0下均不溶解。在pH 5.0时，胰酶HL在30分钟内溶出率为43%，其他制剂溶出率为15%或更少。Panzytrat和胰酶HL在pH 5.2条件下30 min溶出度大于50%，Panzytrat、胰酶HL和Creon Forte在pH 5.6条件下30 min溶出度大于90%，在pH 5.8及更高条件下30 min溶出度均大于90%。结论：对于治疗外分泌胰腺功能不全，常规强度肠溶微球/微片胰酶制剂没有最佳溶出度。较新的高脂酶制剂，如胰酶HL，在pH值为5.4或更低时表现更好，尽管仍不是最优。
Objectives: Enteric-coated microsphere/microtablet pancreatin should stay intact in the stomach and dissolve promptly on entering the duodenum. Postprandial intraluminal pH in the distal duodenum is 5.75 and is lower in exocrine pancreatic insufficiency. The aim of the study was to measure in vitro dissolution times in buffer solutions with pH 4.0-6.0 for five currently available enteric-coated microsphere/microtablet pancreatin preparations.Methods: The following preparations were tested: Creon, Creon Forte, Pancrease, Pancrease HL and Panzytrat. Two capsules were placed in the buffer solution at 37 degrees C in a USP dissolution testing apparatus. Buffer solutions with pH between 4.0 and 6.0 were used. Solutions were stirred at 125 r.p.m. and the rate of dissolution was monitored by taking 2-mL samples at regular intervals and measuring extinction at 280 nm, Measurements were repeated six times,Results: All preparations failed to dissolve at pH 4.0. At pH 5.0 Pancrease HL showed 43% dissolution within 30 min, all other preparations 15% or less. Panzytrat and Pancrease HL showed more than 50% dissolution within 30 min at pH 5.2, Panzytrat, Pancrease HL and Creon Forte had more than 90% dissolution within 30 min at pH 5.6, and all preparations more than 90% dissolution within 30 min at pH 5.8 and higher,Conclusions: For the treatment of exocrine panceatic insufficiency conventional strength enteric-coated microsphere/microtablet pancreatin preparations do not have an optimal dissolution profile. The newer, high lipase preparations such as Pancrease HL perform better, although still not optimally, at pH 5.4 and lower.