Key result
Amiodarone Lek reduces acute toxicity compared to Cordarone, increasing lethal dose by ~29% in preclinical models.
Why the study?
The toxicity profile of intravenous amiodarone formulations with altered particle size and excipient content was investigated to reduce acute toxic effects.
Does amiodarone nanosuspension reduce acute intravenous toxicity compared to standard amiodarone in mice and rats?
Does amiodarone nanosuspension reduce acute intravenous toxicity compared to standard amiodarone in mice and rats?
An amiodarone nanosuspension formulation demonstrated reduced acute intravenous toxicity compared to standard amiodarone in preclinical models, likely due to decreased excipient requirements.
Answers are grounded in this paper and cite their sources.
Test formulation may alter amiodarone acute toxicity margins in rodents; leaves open human i.v. safety implications.
The toxicity of amiodarone Lek formulation (test formulation) was investigated after a single intravenous (i.v.) administration to mice and rats. When compared to the reference item, Cordarone (Cordarone(®); Wyeth Pharmaceuticals Inc., Collegeville, Pennsylvania, USA), median lethal dose (LD(50)) after i.v. administration in female mice was 294.0 mg/kg body weight (b.w.) for the test formulation and 227.5 mg/kg b.w. for Cordarone. In female rats after i.v. administration, the LD(50) value was 269.9 mg/kg b.w. for the test formulation and 192.4 mg/kg b.w. for Cordarone. By altering the particle size of amiodarone in the Lek formulation, we were able to improve the solubility of amiodarone, thereby decreasing the number and quantity of excipients needed for preparation of the i.v. formulation and, consequently, reduced the acute toxic effects observed in the present study.
No takes yet. Share an insight, caveat, or question.
Barle et al. (2012) studied this question. Amiodarone Lek formulation vs. Cordarone was evaluated on Median lethal dose (LD50). Amiodarone Lek formulation had reduced acute toxicity versus Cordarone, with a higher median lethal dose in female mice (294.0 vs 227.5 mg/kg) and female rats (269.9 vs 192.4 mg/kg).
Synapse has enriched 10 related papers. Consider them for comparative context: