摘要
目的:制备盐酸利多卡因长效局部注射剂,并建立其质量控制方法。方法:采用透明质酸钠凝胶为注射剂基质,并以聚乙二醇(PEG)为交联剂增强其缓释性能,制备盐酸利多卡因长效局部注射凝胶剂,建立HPLC法测定药物含量。采用透析袋法考察盐酸利多卡因长效局部注射凝胶剂的体外累积释放度。结果:最佳处方:注射剂凝胶基质透明酸钠含量为1%,交联剂PEG4000含量为0.07%,反应温度为60℃,主药含量为20 mg·ml^(-1)。以交联透明质酸钠为凝胶基质的注射剂在120 h的累积释放度达95%以上,以非交联透明质酸钠为凝胶基质的注射剂在120h时已释放完全。结论:该盐酸利多卡因长效局部注射凝胶剂制备工艺简单可行,且明显具有缓释作用,其质量控制方法简便可靠。
Objective： To prepare lidocaine hydrochloride sustained-release local gel for injection and establish the quality control methods. Methods： The Lidocaine hydrochloride sustained-release local gel for injection was prepared using sodium hyaluronate as the matrix of injection and PEG as the cross-linking agent to enhance sustained-release properties. An HPLC method was established to de- termine the drug content.. The in vitro accumulative release of lidoeaine hydrochloride sustained-release local gel for injection was in- vestigated by a dialysis bag method. Results： The best formula was as follows ： the content of sodium hyaluronate was 1%, the content of PEG4000 was 0.07% , the reaction temperature was 60~C , and the content of main drug was 20 mg·ml-1. The drug release from the injection with cross-linked sodium hyaluronate as the gel matrix was more than 87% in 120 h, while that from the injection with so- dium hyaluronate as the gel matrix was almost complete in 120 h. Conclusion： The preparation process of lidoeaine hydrochloride sustained-release local gel for injection is simple and feasible, and the injection has obvious sustained-release effect. The quality control method is simple and reliable.
作者
邱芳
陈鹰
胡慧芸
Qiu Fang;Chen Ying;Hu Huiyun(Department of Pharmacy,Wuhan General Hospital of PLA, Wuhan 430070, China;College of Pharmacy, Hubei University of Chinese Medicine)
出处
《中国药师》
CAS
2018年第4期630-634,共5页
China Pharmacist
关键词
盐酸利多卡因
局部注射剂
长效制剂
制备
质量控制
Lidocaine hydrochloride
Local gel for injection
Sustained-release
Preparation
Quality Control
