摘要
目的研制盐酸利多卡因(lidocaine hydrochloride,LDH)脂质体凝胶剂,并进行质量评价。方法通过均匀实验设计优化利多卡因脂质体的处方和制备工艺,以逆相蒸发-超声法制备LDH脂质体,再用卡波普为基质制成凝胶剂;以体外经皮渗透释药法,比较LDH脂质体凝胶剂及LDH凝胶剂中的经皮渗透规律。结果LDH脂质体平均粒径为88.31 nm,平均包封率为(66.21±4.8)%;LDH从凝胶剂的渗透符合Higuchi方程,其中脂质体凝胶剂24 h内药物渗透速率为761.49 μg·h-1,明显高于游离药物凝胶渗透率275.08 μg·h-1。结论载药脂质体凝胶剂可显著促进药物经皮吸收,为经皮吸收药物的理想载体。
OBJECTIVE: To prepare a liposomal gel of LDH and to evaluate it. METHODS: The prescription of formulation and preparation process were screened by the uniform design. The LDH liposome was prepared by the reverse-phase evaporation and ultrasound method, the carbopol was added as a support base for the preparation of the liposomeal gel. The permeation rate of LDH liposomal gel was assessed by Franz-diffiusion, and compared with conventional hydrogel. RESULTS: Mean diameter of the LDH liposome was (88.31 ± 6.82) nm and mean entrapment efficiency was (66.21 ± 4.8)%. The permeation rate (716.49 μg·h-1) of liposome gel was significantly higher than that (275.08 μg·h-1) of conventional gel in 24 h in vitro. The release pattern of drugs from two-type gels were coincident with Higuchi function. CONCLUSION: Liposomal gel has the ability to enhance LDH transcutaneous permeation. It is effective vehicle for transdermal therapeutic drugs.
出处
《中国药学杂志》
EI
CAS
CSCD
北大核心
2005年第11期839-842,共4页
Chinese Pharmaceutical Journal
关键词
利多卡因
脂质体
凝胶剂
包封率
均匀设计
Evaporation
Hydrochloric acid
Pattern recognition
Ultrasonic applications
