Bioavailability study of a new, sinking, enteric-coated ursodeoxycholic acid formulation
| Autor: | Enrico Roda, C. Cerre, Patrizia Simoni, A Cipolla, C Polimeni, A. Pistillo, Aldo Roda, Giancarlo Ceschel |
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| Rok vydání: | 1995 |
| Předmět: |
Absorption (pharmacology)
Adult Male medicine.medical_specialty Time Factors Cmax Administration Oral Biological Availability Capsules Gastroenterology Intestinal absorption Oral administration Internal medicine medicine Humans Pharmacology Chromatography Gastric emptying Chemistry Ursodeoxycholic Acid Area under the curve Middle Aged Ursodeoxycholic acid Bioavailability Intestinal Absorption Delayed-Action Preparations Female Tablets Enteric-Coated medicine.drug |
| Zdroj: | Pharmacological research. 31(2) |
| ISSN: | 1043-6618 |
| Popis: | A new enteric-coated ursodeoxycholic acid (UDCA) formulation which sinks in the stomach and releases the drug only at a pH > or = 6.5 was developed. In 12 healthy subjects we measured, using a specific enzyme immunoassay, the serum levels of UDCA after a single oral dose of 450 mg of UDCA in three different formulations; enteric coated sinking tablet, stomach-floating enteric coated hard gelatin capsule and conventional gelatin capsule. The drug was given after a meal. Results are expressed as mean +/- SD. The area under the curve [AUC, mumol l-1 (8 h)] following oral administration of enteric-coated, sinking UDCA (39.0 +/- 8.5) was significantly higher than that obtained after both conventional UDCA (30.5 +/- 4.9) and floating enteric coated UDCA (29.3 +/- 3.4). Moreover, the maximum UDCA serum concentration (Cmax) was significantly higher with the enteric coated sinking UDCA formulation when compared to the other two formulations, while the time of maximum UDCA serum concentration (tmax) occurred later. These results may be explained by the hypothesis that the sinking tablet is expelled in the latter phase of gastric emptying along with the solid content. It therefore reaches the intestine at the highest alkalization phase caused by sustained biliary and pancreatic secretions. When released, the protonated insoluble UDCA is promptly solubilized by the alkaline pH thus giving a higher UDCA concentration gradient which facilitates its passive absorption. On the other hand, the floating capsule reaches the intestine too early, still in presence of an acidic pH; and in this condition UDCA is almost insoluble and consequently may be malabsorbed.(ABSTRACT TRUNCATED AT 250 WORDS) |
| Databáze: | OpenAIRE |
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