Pharmacokinetics and bioavailability of a sustained-release diltiazem formulation (Mono-Tildiem LP 300 mg) after repeated administration in healthy volunteers
| Autor: | P. Rosenzweig, G. Bianchetti, C. Dubruc, G. Houin, V. Sultana |
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| Rok vydání: | 1995 |
| Předmět: |
Adult
Male Volunteers Time Factors Administration Oral Biological Availability Pharmacology Bioequivalence Dosage form Diltiazem Drug Delivery Systems Pharmacokinetics Oral administration Healthy volunteers medicine Humans heterocyclic compounds Pharmacology (medical) Absolute bioavailability business.industry General Medicine musculoskeletal system Bioavailability Injections Intravenous cardiovascular system business circulatory and respiratory physiology medicine.drug |
| Zdroj: | European Journal of Clinical Pharmacology. |
| ISSN: | 1432-1041 0031-6970 |
| DOI: | 10.1007/bf00198308 |
| Popis: | The usual dosage regimen of diltiazem (Tildiem) is 60 mg 3-4 times a day. A sustained-release formulation has been developed (Mono-Tildiem LP 300 mg) in order to allow a single daily administration. Two repeated dosing studies were performed in healthy volunteers. The absolute bioavailability of sustained-release diltiazem LP 300 mg was investigated using concomitant i.v. administration of 13C-labelled drug: absolute bioavailability of the "once a day" formulation was 35%. The second study compared sustained-release diltiazem LP 300 mg with the standard formulation of diltiazem. The results showed that the diltiazem plasma concentrations obtained after the LP formulation remained stable between 2 and 14 h after administration and were compatible with a once a day administration. Relative bioavailability of sustained-release diltiazem LP 300 mg was 79.3% compared with diltiazem. Therefore, a unitary dose of sustained-release diltiazem LP 300 mg was chosen as the dose equivalent to the daily dose administered with the standard diltiazem formulation. |
| Databáze: | OpenAIRE |
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