首页|利多卡因微乳的制备及其质量评价

利多卡因微乳的制备及其质量评价

Preparation and quality evaluation of lidocaine microemulsion

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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0.03 μg·mL-1,定量限为0.1 μg·mL-1,在60~160 μg·mL-1内线性良好(r = 0.999 2),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 was an oil-in-water type.By HPLC,the detection limit was 0.03 μg·mL-1 and the quantitation limit was 0.1 μg·mL-1.The linear range was from 60 to 160 μg·mL-1(r = 0.999 2).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.

LidocaineMicroemulsionPseudo-ternary phase diagramHigh performance liquid chromatographyDrug load

杨齐、王聪聪、李渊源、徐风华

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解放军总医院医疗保障中心药剂科,北京 100853

利多卡因 微乳 伪三元相图 高效液相色谱法 载药量

2024

中国药物应用与监测
中国人民解放军总医院

中国药物应用与监测

CSTPCD
影响因子:1.983
ISSN:1672-8157
年,卷(期):2024.21(1)
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