高载药量萘普生凝胶透皮给药制剂的研制  

Investigation of naproxen gel with high drug content for transdermal delivery

作　　者：徐珍[1] 田青平[1] 李鹏[1] 李菁[1] 谢茵[1] 

机构地区：[1]山西医科大学药学院,山西太原030001

出　　处：《中国医院药学杂志》2009年第19期1636-1638,共3页Chinese Journal of Hospital Pharmacy

摘　　要：目的:制备含药量高的萘普生凝胶剂,并对其进行体外经皮渗透研究。方法:用药物透皮扩散试验仪进行萘普生凝胶剂经离体兔皮的体外渗透实验,用HPLC法测定萘普生的累积渗透量。以稳态渗透速率为评价指标,用正交设计法筛选卡波姆980、丙二醇和甘油的最佳用量。研究月桂氮卓芯酮、油酸、卡必醇对萘普生凝胶剂的促渗作用,考查卡必醇用量对萘普生载药量和促渗效果的影响。结果:正交实验筛选出的优化处方组成为:2%的卡波姆980、20%的丙二醇、含药1%的凝胶剂稳态渗透速率为110.3μg·cm-2·h-1。卡必醇为萘普生凝胶剂的优良渗透促进剂,加入5%的卡必醇,渗透速率可提高2.43倍。卡必醇的最佳用量为25%,所得凝胶剂的载药量可达4%,制剂均匀、细腻、透明,稳态渗透速率高达324.1μg·cm-2·h-1。结论:以卡必醇为促渗剂和增溶剂制得的萘普生凝胶剂载药量高、渗透速率快,有望成为萘普生的新型给药制剂。OBJECTIVE To prepare naproxen gel with high drug content and investigate its in vitro transdermal delivery ability. METHODS Naproxen gel diffusion was performed with rabbit skin using a drug diffusion apparatus. The contents of naproxen were measured by HPLC. The results of orthogonal experiments were evaluated by steady-state permeation rate （Js） of naproxen, and the formulation of gel with high permeation rate was screened. The effect of enhancers such as azone, oleic acid and transcutol was investigated through in vitro penetrable performance. The influence of content of transcutol on content of drug incorporated and permeation rate were studied. RESULTS The optimum formulation screened by orthogonal experiments was 2% earbopol 980 and 20% propytene glycol, its Js was 110. 3 g· cm^- 2· h^- 1. Transcutol was effective enhancer for naproxen gel. Adding 5 % transcutol in optimum formulation, Js of naproxen gel increased 2. 43 times. The best content of transcutol was selected as 25%, with which naproxen gel prepared was uniform, exquisite and transparent, the obtained Js was 324. 1 g·cm^- 2 ·h ^-1. CONCLUSION Naproxen gels prepared by selected transcutol as enhancer and solubilizing agent can obtain high drug content and exhibit high percutaneous ahsorbtion, which may be a promising new dosage form for transdermal delivery of naproxen.

关 键 词：萘普生 凝胶 卡波姆980 卡必醇 经皮给药 

分 类 号：R943[医药卫生—药剂学]