Vehicle Effects on Activity of an Anticonvulsant Compound
| Autor: | James L. Bloss, Dilip R. Sanvordeker |
|---|---|
| Rok vydání: | 1977 |
| Předmět: |
Male
Time Factors Pyridines medicine.medical_treatment Kinetics Pharmaceutical Science Pharmacology Piperazines Dosage form Mice chemistry.chemical_compound Suspensions Seizures In vivo medicine Animals Sorbitol Drug Interactions Mice Inbred ICR Dose-Response Relationship Drug Biological activity Solutions Piperazine Linear relationship Anticonvulsant chemistry Anticonvulsants Emulsions Pharmaceutical Vehicles |
| Zdroj: | Journal of Pharmaceutical Sciences. 66:82-85 |
| ISSN: | 0022-3549 |
| DOI: | 10.1002/jps.2600660120 |
| Popis: | The effect of several lipid and nonlipid pharmaceutical solvents on the in vivo activity of 1‐diphenylmethyl‐4‐[(6‐methyl‐2‐pyridyl)methyleneamino]piperazine (I) was evaluated in the mouse. The intensity of onset and the duration of anticonvulsant activity of the compound were affected depending on the type and form of liquid dosage preparation used. The rate of decline in anticonvulsant activity in the 80–20% response range followed apparent zero‐order kinetics. A linear relationship between the observed ED 50 and the concentration of sorbitol in the dosage form of I was observed. A reduction in the sorbitol content of the dosage form resulted in a proportional increase in the rapidity of onset and the duration of anticonvulsant activity of I. Emulsification restored both the onset and duration of pharmacological activity, which was virtually arrested when the compound was given orally as a solution in oil. |
| Databáze: | OpenAIRE |
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