کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5550878 | 1557302 | 2016 | 6 صفحه PDF | دانلود رایگان |

Brivaracetam, or (2S)-2-[(4R)-2-oxo-4-propyl-pyrrolidin-1-yl] butanamide, is an active pharmaceutical ingredient designed for the treatment of epilepsy. During the development of the IV administration mode, a liquid-liquid miscibility gap has been observed with pure water, isotonic and hypertonic solutions (vehicle at 0.9% w/w and 5%w/w NaCl respectively). The study reveals that the NaCl concentration has a direct impact on the extent of the demixing domain; from a sub-micronic demixing in pure water towards a macroscopic miscibility gap in hypertonic aqueous solutions. The thorough exploration of these heterogeneous equilibria led to define experimental parameters for safe IV injections without risk of liquid - liquid miscibility gap at 37 °C.
The intravenous formulations of brivaracetam, a new antiepileptic drug, marketed under the name Briviact® are explored by means of a thermodynamic investigation and the impact of sodium chloride in isotonic and hypertonic solutions is established with respect to the formation of liquid-liquid miscibility gaps in the respective phase diagrams.81
Journal: International Journal of Pharmaceutics - Volume 515, Issues 1â2, 30 December 2016, Pages 702-707