应用化学2025，Vol.42Issue(8)：1105-1114,10.DOI:10.19894/j.issn.1000-0518.250026
布比卡因微乳凝胶制剂的研制及质量评价
Preparation and Quality Evaluation of Bupivacaine Microemulsion Gel
摘要
Abstract
Bupivacaine is an amide-type local anesthetic with strong anesthetic effect.However,due to its short half-life,single injection analgesic time is limited,increasing the dose is easy to cause adverse reactions,and continuous small-dose infusion will aggravate the patient's discomfort and the burden of medical care,which limits its clinical application.To address the above problems,bupivacaine microemulsion was prepared by spontaneous emulsification,and a bupivacaine microemulsion gel for transdermal route of administration was prepared using hydroxypropyl methyl cellulose(HPMC)as the gel matrix.The prescription process of the microemulsion gel was optimized in terms of particle size,drug loading capacity and other physicochemical indexes,and a pharmacodynamic study was carried out.The results showed that the optimal prescription of the microemulsion gel was:pharmaceutical soybean oil-Tween 80-Span 80-anhydrous ethanol-water phase ratio of 9∶10.5∶4.5∶10∶66;HPMC mass fraction of 0.4％.The optimized microemulsion had a particle size of(64.58±0.29)nm,a PDI of 0.198±0.096,a drug loading capacity of 96.95 mg/g,a viscosity of(8.43±0.28)Pa·s,a pH value of 7.49,a good stability,and a spherical morphology as shown by transmission electron microscopy.The transdermal penetration of the microemulsion and microemulsion gel was significantly higher compared with the free drug,and the microemulsion gel prolonged the pain threshold in mice without skin irritation.Bupivacaine microemulsion gel is easy and controllable to prepare,and the finished product is stable,excellent spreading and non-irritating,so it is expected to have a good prospect for clinical application.关键词
布比卡因/伪三元相图/微乳凝胶/局部麻醉/质量评价Key words
Bupivacaine/Pseudoternary phase diagram/Microemulsion gel/Local anesthesia/Quality evaluation分类
化学化工引用本文复制引用
邢梓鑫,马秀兰,刘哲鹏,傅鹏琨,宋慧荞,杨昳津,聂丽蓉..布比卡因微乳凝胶制剂的研制及质量评价[J].应用化学,2025,42(8):1105-1114,10.基金项目
国家自然科学基金面上项目(No.32372307)资助 Supported by the National Natural Science Foundation of China(No.32372307) （No.32372307）
