以磷脂复合物为载体的泊沙康唑亚微乳处方及制备工艺研究

Study on the formulation and preparation of posaconazole microemulsion with phospholipid complex as the carrier

确定泊沙康唑磷脂复合物亚微乳的最佳处方及制备工艺,并对其进行确证。以磷脂复合物为载体,利用高压均质技术制备泊沙康唑磷脂复合物亚微乳。以外观性状、粒径、Zeta电位、离心稳定常数(Ke)、含量和包封率为主要评价指标,对影响亚微乳剂的处方因素及制备工艺因素进行单因素考察和正交优化,确定泊沙康唑磷脂复合物亚微乳的处方及制备工艺,并对其进行确证。按确定的处方工艺制备3批样品,各质量评价指标的平均值分别为:粒径0.186μm、Zeta电位-34.69mV、pH7.01、含量98.12%、包封率91.41%、渗透压302mOsmol/L,符合亚微乳剂质量要求。本处方及制备工艺简单可行,重现性好,制得的亚微乳包封率高,质量均匀、可控。

To determine the best prescription and preparation technology of posaconazole phospholipid composite submicroemulsion, and confirm it. Phospholipid complex was used as a carrier, and the high pressure homogenization was used to prepare posaconazole phospholipid complex submicron emulsion. Zeta potential, centrifugal stability constant （Ke）, content and entrapment efficiency were used as the main evaluation indexes. Single factor investigation and orthogonal optimization were performed on the prescription factors and preparation process factors that affect the submicroemulsion. The sulconazole phospholipid composite submicroemulsion formulation and the preparation process were confirmed. Three batches of samples were prepared according to the prescribed prescription process. The average values of the quality evaluation indexes were as follows： the particle size of 0.186pro, the Zeta potential of -34.69mV, pH at 7.01, the content of 98.12%, the encapsulation efficiency of 91.41%, the osmotic pressure of 302mOsmol/L, in line with submicroemulsion quality requirements. The prescription and the preparation process are simple and feasible, and the reproducibility is good. The prepared submicroemulsion has high encapsulation efficiency, uniform quality and controllability.