کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
5550878 1557302 2016 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Impact of sodium chloride on the expansion of a liquid-liquid miscibility gap in an API/water system. Case study of Brivaracetam
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی علوم دارویی
پیش نمایش صفحه اول مقاله
Impact of sodium chloride on the expansion of a liquid-liquid miscibility gap in an API/water system. Case study of Brivaracetam
چکیده انگلیسی

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

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: International Journal of Pharmaceutics - Volume 515, Issues 1–2, 30 December 2016, Pages 702-707
نویسندگان
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