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Plasma levels of diazepam in the dog and the rabbit after two different injection formulations, emulsion and solution
Author(s) -
Jeppsson R. I.
Publication year - 1976
Publication title -
journal of clinical pharmacy and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.622
H-Index - 73
eISSN - 1365-2710
pISSN - 0269-4727
DOI - 10.1111/j.1365-2710.1976.tb00064.x
Subject(s) - diazepam , emulsion , chemistry , chromatography , pharmacokinetics , lipid emulsion , drug , pharmacology , organic chemistry , medicine , surgery , parenteral nutrition
Summary Diazepam is almost insoluble in water but can be dissolved in soya bean oil. If the oil phase is homogenized to a fine emulsion, a formulation of low toxicity is obtained, suitable for intravenous injection. Intramuscularly or subcutaneously, oily vehicles of drugs can be used to prolong the drug action. In the present study the plasma elimination of diazepam has been compared in the dog and the rabbit after intravenous administration of emulsion formulations or a solution in ethanolpropylene glycol. The result showed that the drug release from the lipid particles is rapid, as the plasma elimination pattern was equal to that of the solution. Furthermore, the same result was noted when emulsions were used where the lipid particle elimination from plasma was very slow or very rapid. The finely dispersed oil phase has a very large total contact surface with the plasma and this was supposed to explain the rapid drug diffusion. Because of the similar plasma curves the diazepam emulsion is suggested as a less toxic alternative to the conventional ethanol‐propylene glycol solution.