利多卡因微乳的制备及其质量评价  

Preparation and quality evaluation of lidocaine microemulsion

作　　者：杨齐 王聪聪 李渊源 徐风华[1] Yang Qi;Wang Cong-cong;Li Yuan-yuan;Xu Feng-hua(Department of Pharmacy,Medical Supplies Center,Chinese PLA General Hospital,Beijing 100853,China)

机构地区：[1]解放军总医院医疗保障中心药剂科,北京100853

出　　处：《中国药物应用与监测》2024年第1期50-54,共5页Chinese Journal of Drug Application and Monitoring

摘　　要：目的筛选利多卡因微乳的最优处方,制备利多卡因微乳并评价相关理化性质。方法通过伪三元相图法确定利多卡因微乳的处方配比,考察其粒径大小和稳定性,高效液相色谱法(HPLC)测定其载药量。结果筛选出利多卡因微乳处方为油酸乙酯/混合表面活性剂/蒸馏水(1∶9∶20),混合表面活性剂由聚山梨酯80和聚乙二醇400组成。微乳外观淡黄色,澄清、流动性好,呈球形,平均粒径大小19.70 nm,为水包油型微乳。HPLC测定利多卡因检测限为0.03μg·mL^(-1),定量限为0.1μg·mL^(-1),在60~160μg·mL^(-1)内线性良好(r=0.9992),不同方法制备的利多卡因微乳载药量为3.47%~7.38%。结论利多卡因微乳符合特征要求,处方制备工艺稳定可靠,最大载药量达7.38%,提高了利多卡因溶解度,为进一步临床应用奠定了良好基础。Objective To choose the optimal formulation of lidocaine microemulsion,prepare lidocaine microemulsion and examine its physical and chemical properties.Methods The composition of lidocaine microemulsion was determined by pseudo-ternary phase diagrams.The particle size and stability of lidocaine microemulsion were also investigated.The drug loading was determined by high performance liquid chromatography(HPLC).Results The formulation of lidocaine microemulsion encompassed ethyl oleate/mixed surfactant/distilled water(1∶9∶20).The mixed surfactant consisted of polysorbate 80 and polyethylene glycol 400.The microemulsion appeared spherical,clarified,and pale yellow,with good liquidity.The average particle size was 19.70 nm.The lidocaine microemulsion-1 was an oil-in-water type.By HPLC,the detection limit was 0.03μg·mL and the quantitation limit was 0.1μg·mL^(-1).The linear range was-1 from 60 to 160μg·mL(r=0.9992).The drug-loading range of lidocaine microemulsion prepared by different methods was between 3.47%and 7.38%.Conclusion Lidocaine microemulsion conformed to the characteristics of microemulsion and the preparation process was stable and reliable.The maximum drug loading of lidocaine microemulsion reached 7.38%,which improved the solubility of lidocaine.This research layed a good foundation for the further clinical application of lidocaine microemulsion.

关 键 词：利多卡因 微乳 伪三元相图 高效液相色谱法 载药量 

分 类 号：R943[医药卫生—药剂学]