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Topical and systemic availability of 5‐amino‐salicylate: comparisons of three controlled release preparations in man

The bioavailability of three pure 5‐aminosalicylic (5‐ASA) preparations (Asacol, Claversal, and Pentasa) was studied in 8 ileostomy patients and 12 normal subjects after 6 days of treatment with 2000 mg 5‐ASA. The local bioavailability, reflected by the 5‐ASA concentration was thereby measured at two clinically relevant areas of the gut: at the entrance to, and the exit from the colon. Estimates of the systemic bioavailability were obtained from the urinary excretions and the plasma values of 5‐ASA and Acetyl‐5‐ASA (Ac‐5‐ASA) during the three regimens. The three preparations studied are designed to release 5‐ASA at different levels in the intestine, but there was no significant difference in the 5‐ASA concentrations in the ileostomy effluents (Asacol 1.8 mmol/L, Claversal 3.4 mmol/L, Pentasa 2.0 mmol/L, median values). However, we found a smaller urinary excretion of 5‐ASA and Ac‐5‐ASA (5.2%vs Claversal 27.9% and Pentasa 23.0%, median values of ingested daily dose) and a lower concentration of Ac‐5‐ASA in the ileostomy effluents after Asacol treatment (0.8 mmol/L, median value) which indicates a more distal release from this preparation compared with Claversal (2.4 mmol/L, median value) and Pentasa (5.5 mmol/L, median value). In normal subjects a higher faecal water concentration of 5‐ASA was found after Asacol (9.8 mmol/L, median value) compared with Claversal (5.0 mmol/L, median value), whereas no difference between the faecal water concentrations of Ac‐5‐ASA was found (Asacol 21.5 mmol/L, Claversal 21.6 mmol/L, median values). This can be explained by a larger systemic absorption of 5‐ASA from Claversal, and accordingly Claversal treatment resulted in the largest urinary excretion of 5‐ASA and Ac‐5‐ ASA (43.7% us Asacol 35.6% and Pentasa 31.6 %, median values of ingested daily dose). The high Ac‐5‐ASA concentration in the ileostomy effluents and in the faeces after Pentasa, and the low plasma values, indicate a slow 5‐ASA release from this preparation throughout the small and large intestine. The results of the study indicate that Asacol is released in the distal part of the small intestine, that Pentasa is gradually released in the small and large intestine, and that Claversal shows an intermediate release pattern.