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In vitro dissolution profiles of enteric-coated microsphere/microtablet pancreatin preparations at different pH
1Adult Cystic Fibrosis Centre, Leyenburg Hospital, The Hague, The Netherlands.
Alimentary Pharmacology & Therapeutics
|October 1, 1996
Summary
Enteric-coated pancreatin preparations show suboptimal dissolution in vitro, especially at lower duodenal pH levels common in pancreatic insufficiency. Higher lipase formulations demonstrate improved, though not ideal, performance at pH 5.4 and below.
Area of Science:
- Gastroenterology
- Pharmacology
- Drug Delivery Systems
Background:
- Enteric-coated pancreatin microspheres/microtablets are designed for stomach stability and rapid duodenal dissolution.
- Duodenal pH in exocrine pancreatic insufficiency (EPI) is lower than the typical postprandial 5.75.
- Optimal dissolution is crucial for effective enzyme release and nutrient absorption in EPI patients.
Purpose of the Study:
- To evaluate the in vitro dissolution profiles of five enteric-coated pancreatin preparations.
- To assess dissolution times across a range of pH values (4.0-6.0) relevant to duodenal conditions, including those in EPI.
- To compare the performance of conventional and high lipase pancreatin formulations.
Main Methods:
- Five enteric-coated pancreatin preparations (Creon, Creon Forte, Pancrease, Pancrease HL, Panzytrat) were tested.
- Dissolution testing was performed in USP apparatus at 37°C using buffer solutions from pH 4.0 to 6.0.
- Dissolution rates were monitored by measuring extinction at 280 nm at regular intervals over 30 minutes.
Main Results:
- No preparations dissolved at pH 4.0.
- At pH 5.0, Pancrease HL showed 43% dissolution, while others showed ≤15%.
- Panzytrat and Pancrease HL exceeded 50% dissolution at pH 5.2; Creon Forte, Panzytrat, and Pancrease HL exceeded 90% at pH 5.6.
Conclusions:
- Conventional enteric-coated pancreatin preparations exhibit suboptimal in vitro dissolution profiles for treating EPI.
- Higher lipase preparations, like Pancrease HL, demonstrate better dissolution at lower pH levels (≤5.4) but are still not optimal.
- Further development of enteric coatings is needed to ensure adequate pancreatin release across a wider range of duodenal pH conditions in EPI patients.