Pharmacokinetics of 5-aminosalicylic acid from controlled-release capsules in man
| Autor: | Dennis H. Giesing, M. B. Lanman, Scott J. Weir, L. S. Eichmeier, Robert C. Lanman, B. Morrill, Dale K. Yu |
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| Rok vydání: | 1995 |
| Předmět: |
Adult
Male Volunteers Time Factors Aminosalicylic acid Capsules Urine Pharmacology Dosage form chemistry.chemical_compound Drug Delivery Systems Pharmacokinetics medicine Humans Pharmacology (medical) Antipyretic Mesalamine Feces Gastrointestinal tract General Medicine Controlled release digestive system diseases Aminosalicylic Acids chemistry medicine.drug |
| Zdroj: | European Journal of Clinical Pharmacology. |
| ISSN: | 1432-1041 0031-6970 |
| DOI: | 10.1007/bf00198311 |
| Popis: | One gram single dose of Pentasa controlled-release capsules was administered to 24 healthy volunteers under fasting condition. Mean plasma 5-aminosalicylic acid (5-ASA) and acetyl 5-ASA concentrations peaked at 0.53 microgram.ml-1 and 1.33 micrograms.ml-1 from 3 to 4 hours following dosing, respectively. The half-lives of both compounds could not be determined as absorption of 5-ASA was continuous throughout the gastrointestinal tract. An average of 29.4% (CV: 27%) of the dose was excreted in the urine primarily as acetyl 5-ASA. Up to 91.1% of the dose was released from the capsules. Forty percent of the dose (CV: 40%) was eliminated in the feces, with 8.9% of the dose remained as formulation bounded 5-ASA, indicating that controlled-release capsules continue to release drug throughout the GI tract. 5-ASA contributed 46.7% of the salicylates eliminated in the feces and acetyl 5-ASA accounted for the balance. Controlled-release capsules produced three times more total salicylates and 10 times more total and free 5-ASA in the feces than did 5-ASA suspension. Thus, while lower systemic levels of salicylates were absorbed, greater therapeutic quantities of 5-ASA were available in the bowel. |
| Databáze: | OpenAIRE |
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