摘要
目的建立左布比卡因原位凝胶的体外释放方法,研究影响体外释放的因素和其筛选处方的能力。方法以左布比卡因为主药,制备以乙酸异丁酸蔗糖酯和聚乳酸-羟基乙酸共聚物为基质的原位凝胶。开发基于聚乙烯醇薄膜的自制适配器的桨法测定体外释放度,并考察影响释放的因素及其筛选处方的能力。通过小鼠热板测痛实验考察其体内镇痛效果。结果适配器的直径、上样体积和转速影响原位凝胶的体外释放;处方中有机溶剂的种类、用量、释放调节剂的用量等影响体外释放度。原位凝胶在小鼠体内具有一定的长效镇痛效果。结论本研究建立的体外释放方法适用于左布比卡因原位凝胶的体外评价,可为长效原位凝胶制剂的开发提供一定的参考。
Objective To establish an in vitro release method for levobupivacaine in situ gel and to determine the factors affecting in vitro release and its ability to screen prescriptions.Methods In situ gel formulations based on sucrose acetate isobutyrate and poly(lactic-co-glycolic acid)copolymers were prepared with levobupivacaine as the main drug.We developed a paddle method based on polyvinyl alcohol film with the adapter to assess the in vitro release degree and examine the factors affecting the release and its ability to screen the prescriptions.The in vivo analgesic effect was determined by hot plate analgesia test in mice.Results The diameter of the adapter,the sample volume,and the paddle speed influenced the in vitro release.The type and content of organic solvents,along with the presence of release modifiers greatly impacted the in vitro release results.In situ gel showed long-lasting analgesic effect in mice.Conclusion The in vitro release method fits the in vitro evaluation of levobupivacaine in situ gel and provides reference for the development of long-acting in situ gel.
作者
范哲
张帅
郝贵周
刘忠
尚萍萍
FAN Zhe;ZHANG Shuai;HAO Gui-zhou;LIU Zhong;SHANG Ping-ping(School of Medicine,Ocean University of China,Qingdao Shandong 266003;Shandong New Times Pharmaceutical Co.,Ltd.,Linyi Shandong 273400;Shandong Engineering Research Center of Complex Injectables,Linyi Shandong 273400)
出处
《中南药学》
2025年第9期2588-2593,共6页
Central South Pharmacy
基金
山东省重点研发计划(重大科技创新工程)项目(No.2020CXGC010506)。
关键词
左布比卡因
长效原位凝胶
适配器
桨法
体外释放
levobupivacaine
long-acting in situ gel formulation
adapter
paddle method
in vitro release
