碘化钾微乳的制备及其体外透皮吸收作用考察

Study on the Preparation of KI Microemulsion and Its Percutaneous Absorption in vitro

目的:制备碘化钾微乳并考察其透皮吸收的效果。方法:以伪三元相图为基础,依据微乳区域大小,确定微乳的油相、乳化剂、助乳化剂和后二者的比例(Km),初步筛选微乳处方;采用改进的Franz扩散池和离体小鼠皮肤进行体外经皮渗透试验,比较所制5%、10%碘化钾微乳与5%碘化钾溶液单位面积的累积渗透量(Qn),并对微乳进行加速稳定性试验。结果:碘化钾微乳的最优处方为碘化钾10%(m/V)、水23%、混合乳化剂(月桂山梨坦-乙醇Km值为1∶1)61.6%、油相(丙二醇单辛酸酯)15.4%;所制微乳的渗透过程符合一级速率方程,3种样品的Q24 h分别为(5.40±0.28)、(8.75±0.42)、(2.12±0.20)mg/cm2;40℃下贮存4周后所制微乳与贮存前比较p H、含量、外观均未见明显变化。结论:成功制得具有透皮吸收作用的碘化钾微乳。

OBJECTIVE： To prepare KI microemulsion and study its percutaneous absorption in vitro. METHODS： Based on the pseudo-ternary phase diagram and according to the area of microemulsion, the oil phase, emulsifier, co-emulsifier and the ratio of the latter two （Kin value） were determined and the microemulsion formulation was preliminary screened. Improved Franz diffu- sion cell and isolated mice skin were used for the percutaneous penetration test in vitro, and the cumulative penetration amount （Qo） of unit area in prepared 5% and 10% KI microemulsion and 5% KI solution was compared. Accelerated stability test was used for microemulsion. RESULTS： The optimal formulation of KI microemulsion was KI 10% （m/V）, water 23 %, mix-emulsifi- er （laurel sorbitan-ethanol, Km= 1 ： 1 ） 61.6 % and oil phase （propylene glycol monocaprylate） 15.4 %. The permeation process of microemulsion was in line with the first-order rate equation and the Q24h of 3 kinds of samples were respectively （5.40 ± 0.28）, （8.75 ± 0.42）, （2.12± 0.20） mg/cm^2. There were no obvious changes of pH, content and appearance of microemulsion after 4 weeks storing in 40 ℃ and before storing. CONCLUSIONS： The KI microemulsion with permeation effects is successfully prepared.