静注安定亚微乳的制备及其特征

PREPARATION AND CHARACTERIZATION OF SUBMICRONIZED O/W EMULSION OF DIAZEPAM FOR INTRAVENOUS INJECTION

应用泊洛沙姆108与精制豆磷脂为乳化剂,制成静注安定亚微乳剂。用单纯形优化法来优化处方中乳化剂的用量(最优化值分别为4%和0.3%)。粗乳经两步高压乳匀机处理后,得很细的单分散乳剂。乳剂用透射电子显微镜检查,粒径均小于364nm。亚微乳不溶血,毒性低,小鼠 LD_(50)是市售安定注射液的2.5倍。药时曲线与市售安定注射液相似。

This emulsion was formulated with poloxamer 108 and purified soybean lecithin as emulsifying agents.An optimizing method(simplex method) was used to determine that 4% poloxamer 108 and 0.3% purified soybean lecithin were the optimum weight ratio.Primary emulsion was passed through a two stage pressure homogenizer,yielding a very fine monodispersed emulsion.It could be observed on TEM that the largest droplet size was 364 nm.The diazepam emulsion had no hemolysis and lower toxicity,LD_(50) was about 2.5 times of that of the diazepam injection.The drug concentration-time curves in rabbits after iv were the same with the both dosage forms.