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In vitro dissolution profiles of enteric‐coated microsphere/microtablet pancreatin preparations at different pH values
Author(s) -
GAN K.H.,
GEUS W. P.,
BAKKER W.,
LAMERS C. B. H. W.,
HEIJERMAN H. G. M.
Publication year - 1996
Publication title -
alimentary pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 3.308
H-Index - 177
eISSN - 1365-2036
pISSN - 0269-2813
DOI - 10.1046/j.1365-2036.1996.55197000.x
Subject(s) - dissolution , duodenum , chromatography , chemistry , dosage form , enteric coated , dissolution testing , in vitro , microsphere , medicine , pharmacology , gastroenterology , biochemistry , biopharmaceutics classification system , chemical engineering , engineering
Objectives : Enteric‐coated microsphere/microtablet pancreatin should stay intact in the stomach and dissolve promptly on entering the duodenum. Post‐prandial 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 °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.