Nyqvist-Mayer A A, Brodin A F, Frank S G
J Pharm Sci. 1985 Nov;74(11):1192-5. doi: 10.1002/jps.2600741112.
The distribution conditions in oil-water emulsions prepared by emulsifying a 1:1 eutectic mixture of lidocaine and prilocaine with a nonionic surfactant in water were studied by membrane and gel filtration methods. In this system, the local anesthetics are considered to be freely dissolved, surfactant solubilized, and emulsified in three separate phases. The dispersity of the oil phase was investigated by light microscopy and light-scatter spectroscopy. The majority of drops in the lidocaine-prilocaine emulsions were less than 1 micron in size. The concentration of freely dissolved drug in the aqueous phase of the emulsions was equal to the aqueous solubility of lidocaine-prilocaine in a 1:1 ratio. At constant lidocaine/prilocaine/surfactant ratio, increasing the total drug concentration in the emulsion resulted in an increase of the emulsified fraction of lidocaine-prilocaine, whereas the surfactant-solubilized fraction remained constant.
采用膜过滤和凝胶过滤法研究了在水中用非离子表面活性剂乳化利多卡因和丙胺卡因1:1共晶混合物所制备的油包水乳液中的分布情况。在该体系中，局部麻醉剂被认为以三种不同的相态自由溶解、被表面活性剂增溶和乳化。通过光学显微镜和光散射光谱法研究了油相的分散性。利多卡因 - 丙胺卡因乳液中的大多数液滴尺寸小于1微米。乳液水相中自由溶解药物的浓度等于1:1比例的利多卡因 - 丙胺卡因的水溶解度。在利多卡因/丙胺卡因/表面活性剂比例恒定的情况下，增加乳液中药物的总浓度会导致利多卡因 - 丙胺卡因乳化部分增加，而表面活性剂增溶部分保持不变。
