Oral kinetics and bioavailability of the cholinesterase reactivator HI-6 after administration of 2 different formulations of tablets to dogs
| Autor: | Matej Maksimović, Veljko Kovačević, Dubravko Bokonjić, Dusan Jovanovic |
|---|---|
| Rok vydání: | 1987 |
| Předmět: |
Male
Cholinesterase Reactivators Chemistry Kinetics Administration Oral Biological Availability Pyridinium Compounds General Medicine Absorption (skin) Pharmacology Toxicology Bioavailability Gastrointestinal absorption Dogs Peak plasma Pharmacokinetics Injections Intravenous Oximes Animals Female Open model Cholinesterase reactivator Tablets |
| Zdroj: | Toxicology Letters. 39:85-91 |
| ISSN: | 0378-4274 |
| DOI: | 10.1016/0378-4274(87)90260-8 |
| Popis: | A one-compartment open model with first-order absorption was used for comparing new oral formulations of the potent acetylcholinesterase reactivating oxime HI-6. Although mean peak plasma levels did not differ between retard and conventional tablets (21.38 and 20.74 mumol/l), the time for reaching peak levels was significantly longer (5.5 h) with retard than with conventional tablets (2.86 h). Among other pharmacokinetic estimates only absorption half-lives and areas under the concentration-time curve (AUC) were significantly different (P less than 0.05). The AUC with retard tablets was 8.07% and that of conventional tablets 5.42% of intravenous AUC, indicating low bioavailability of oral HI-6 formulations. Potential therapeutic use of HI-6 requires, therefore, further investigations in order to improve its gastrointestinal absorption. |
| Databáze: | OpenAIRE |
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