利多卡因——卵磷脂微乳处方的初步研究

Studies of lidocaine-lecithin microemulsion

目的 :以卵磷脂微乳为载体 ,制备利多卡因透皮给药系统。方法 :伪三元相图考察油包水型微乳形成区域 ;测定微乳黏度 ,正交分析法筛选微乳处方 ;紫外分光光度法直接测定微乳中盐酸利多卡因浓度。结果 :助表面活性剂的种类和Km(表面活性剂 /助表面活性剂用量比 )对微乳形成区域有显著性影响 ,正丙醇和异丙醇所形成的微乳区较大 ;低纯卵磷脂微乳形成区域较高纯卵磷脂大 ;醇的种类对微乳的黏度均有显著的影响 ,Km 对微乳的黏度有较大影响。选定紫外检测波长为 2 6 2nm ,盐酸利多卡因浓度在 0 .0 2～ 0 .5mg/mL范围内线性关系良好 (R =0 .9999)。平均回收率 ( 10 0 .17± 0 .16 ) %。日内差与日间差分别为 0 0 137±0 0 12 1,0 0 119± 0 0 115。结论 :选择混合表面活性剂利于制备微乳 ,醇的种类与用量对于利多卡因透皮微乳体系处方的选择具有重要意义。

Objective: To study the formation of transdermal delivery system of lidocaine with lecithin microemulsions as delivery system.Methods:Area of water in oil microemulsions was investigated through pseudo ternary phase diagrams. Viscosity of microemulsions were measured to select the the right formulation using orthogonal test method. The content of hydrochloride lidocaine in microemulsions was measured by spectrophotometric. Results:Nature of cosurfactant and K m showed predominant influence on the area of microemulsions, area of microemulsions in propanol and iso propanol system were larger. The area of microemulsions was larger in low purity lecithin system. Cosurfactant showed predominant influence on the viscosity of the microemulsion. Content of lidocaine was measured at 262nm, the standard curve was linear in the range of 0.02～0.5mg/mL, the average recovery was (100.17±0.16)%, the within day and between day precision of determination of lidocaine was 0.0137±0.0121, 0.0119±0.0115. Conclusion:Choosing mixed surfactant will help the formation of microemulsion. Nature and potent of alcohol have very important effect on selection of the formulation of lidocaine transdermal microemulsions.