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制备了含不同非甾体抗炎药(酮洛芬、吲哚美辛和双氯芬酸)及促透剂[月桂氮酮、薄荷醇、庚酸薄荷醇酯(M-HEP)或油酸薄荷醇酯(M-OA)]的压敏胶分散型贴剂。采用双室扩散池,以离体大鼠皮肤为屏障进行体外渗透试验,考察了压敏胶和促透剂的种类对贴剂中药物渗透行为的影响。结果表明,用Duro-TAK 87-4098型压敏胶制备的贴剂中酮洛芬的稳态渗透速率和24 h累积透过量显著高于用其他两种压敏胶(Duro-TAK 87-2677和87-2852)制备的贴剂。各促透剂对酮洛芬促渗透作用依序为:M-HEP>M-OA>薄荷醇>月桂氮酮;对吲哚美辛的促渗透作用依序为:M-HEP>M-OA>月桂氮酮≈薄荷醇;M-OA和月桂氮酮对双氯芬酸有显著的促渗透效果,前者的促渗效果较强,而薄荷醇及M-HEP无促渗透作用。
A solution containing different non-steroidal anti-inflammatory drugs (ketoprofen, indomethacin and diclofenac) and anti-hypertensive agents [Azone, menthol, menthol enanthate (M-HEP) (M-OA)] pressure sensitive adhesive dispersed patch. A two-compartment diffusion cell was used to in vitro rat skin penetration barrier test to investigate the pressure-sensitive adhesive and anti-permeability agents on the drug permeation behavior of the patch. The results showed that the steady-state permeation rate and the cumulative permeation rate of 24 hours for the patch prepared with Duro-TAK 87-4098 pressure-sensitive adhesive were significantly higher than those of the other two pressure-sensitive adhesives (Duro-TAK 87-2677 And 87-2852). The promoting effect of each enhancer on ketoprofen was M-HEP> M-OA> Menthol> Azone; the promoting effect on indomethacin was M-HEP> M-OA > Laurocapram ≈ menthol. M-OA and Azone were effective in promoting penetration of diclofenac. The former had a stronger permeation promoting effect, while menthol and M-HEP did not promote permeation.