苯磺酸氨氯地平压敏胶分散型贴剂的制备及体外经皮渗透性考察Preparation of drug-in adhesive patches of amlodipine besylate and its in vitro permeability through excised rat skin
蒋宇轩,马蕊,牛喜草,方亮
JIANG Yu-xuan,MA Rui,NIU Xi-cao,FANG Liang (School of Pharmacy
摘要(Abstract)：
目的制备苯磺酸氨氯地平压敏胶分散型贴剂并考察其体外经皮渗透性,为压敏胶分散型贴剂的制备与临床应用提供依据。方法将苯磺酸氨氯地平及各种渗透促进剂直接溶于自制压敏胶中制备压敏胶分散型贴剂;采用卧式双室扩散池研究苯磺酸氨氯地平贴剂的体外经皮渗透行为。结果贴剂中含药量越高,稳态渗透速率越快;加入各种渗透促进剂后,促渗作用由大到小的排列顺序为:质量分数为5%的氮酮>质量分数为5%的肉豆蔻酸异丙酯>质量分数为2.5%的氮酮>质量分数为5%的油酸;药物含量质量分数为1.5%、氮酮含量质量分数为5%的苯磺酸氨氯地平贴剂,稳态渗透速率最快,且在7 d内可持续透过药物。结论应用自制胶制备的苯磺酸氨氯地平压敏胶分散型贴剂有望制成长效的降压制剂,值得进一步深入研究。
Objective To prepare drug-in adhesive patches for amlodipine besylate and evaluate its in vitro transdermal permeability.Methods Drug-in adhesive patches of amlodipine besylate were prepared by dissolving amlodipine besylate and different enhancers into the homemade pressure sensitive adhesive.Permeation characteristics of amlodipine besylate from patches were evaluated using 2-compartment horizontal diffusion cells.Results The greater dosage of amlodipine besylate was used,the higher steady-state flux would occur.The effectiveness of permeation enhancement of different enhancers was in the following order:5%(m∶m) azone>5%(m∶m) isopropyl myristate>2.5%(m∶m) azone>5%(m∶m) oleic acid.The highest steady-state flux was obtained when 1.5%(m∶m) amlodipine besylate and 5%(m∶m)azone were added,and amlodipine besylate could keep permeating through excised rat skin for seven days.Conclusions The drug-in adhesive patches of amlodipine besylate have the potential to become a long-acting transdermal drug delivery system for the treatment of hypertension and are worthy of further investigation.
关键词(KeyWords)：
苯磺酸氨氯地平;压敏胶分散型贴剂;经皮渗透;促进剂
amlodipine besylate;drug-in adhesive patch;skin permeation;enhancer
基金项目(Foundation):
作者(Author):
蒋宇轩,马蕊,牛喜草,方亮
JIANG Yu-xuan,MA Rui,NIU Xi-cao,FANG Liang (School of Pharmacy
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