论文部分内容阅读
目的:制备载药量高、渗透效果好的萘普生凝胶并考查其抗炎、镇痛作用。方法:以卡波姆980为凝胶基质、丙二醇为保湿剂、卡必醇为促渗剂和增溶剂制备不同载药量的萘普生凝胶。用二甲苯诱导小鼠耳廓肿胀,卡拉胶诱发大鼠足跖肿胀,考查萘普生凝胶的抗炎作用;用热板法和扭体法观察萘普生凝胶对小鼠的镇痛作用。以1%的双氯芬酸钠凝胶剂作为阳性对照药,1%、2%和4%的萘普生凝胶分组给药。结果:加入25%的卡必醇后,所制凝胶的载药量可达4%,其稳态渗透速率可达324.1μg.cm-2.h-1。2%和4%萘普生凝胶对二甲苯引起的小鼠耳肿胀、卡拉胶所致大鼠足跖肿胀和醋酸引起的小鼠疼痛扭体反应均有较好的抑制作用,并能明显提高热板法小鼠的痛阈,改善痛阈提高百分率。与阳性药物组相比,2%、4%的萘普生凝胶剂组均显示相近或更好的抗炎镇痛作用。结论:以卡必醇为促渗剂和增溶剂所制的萘普生凝胶经皮给药制剂,对大鼠及小鼠的炎症及痛反应模型均有抑制作用,有望成为萘普生的新型给药制剂。
OBJECTIVE: To prepare naproxen gel with high drug loading and good osmotic effect and test its anti-inflammatory and analgesic effects. Methods: Naproxen gel with different drug loadings was prepared by using Carbopol 980 as matrix, propylene glycol as moisturizer, carbitol as penetration enhancer and solubilizer. Xylene-induced mouse ear swelling, carrageenan-induced rat paw edema, to examine the anti-inflammatory effect of naproxen gel; with hot plate method and writhing observed naproxen gel analgesia in mice effect. Diclofenac sodium gel 1% as a positive control drug, 1%, 2% and 4% Naproxen gel group administration. Results: After loading 25% carbitol, the drug loading reached 4%, and its steady-state permeation rate reached 324.1μg.cm-2.h-1.2% and 4% naproxen Gel-induced xylene-induced mouse ear swelling, rat paw edema caused by carrageenan and acetic acid-induced mouse writhing reaction have a good inhibitory effect, and can significantly improve the hot plate method in mice with pain Threshold, improve the pain threshold increase percentage. Compared with the positive drug group, 2%, 4% naproxen gel group showed similar or better anti-inflammatory analgesic effect. CONCLUSION: The naproxen gel transdermal delivery system with carbitol as penetration enhancer and solubilizer can inhibit the inflammation and pain response of rats and mice, and it is expected to become naproxen New formulations.