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目的:本文的研究为临床用药和配制替硝唑(TNZ)外用药选择适宜药物浓度和促进剂浓度提供依据。方法:观察TNZ对小白鼠离体皮肤的透皮吸收,比较不同药物浓度的透皮吸收量及月桂氮酮(Azone)不同浓度的促渗作用。结果:0.2%,0.4%,1.0%TNZ,12h透皮吸收量分别为1.41,2.82,7.12mg·(50ml)-1,渗透系数分别为12.98×10-6,13.68×10-6,13.77×10-6。促渗剂Azone含量在5%以下时,TNZ透皮吸收百分率随着Azone浓度的提高而增加;当Azone含量达8%时,透皮吸收率反而下降。结论:TNZ可透过离体小白鼠皮肤,提高药物浓度可增加药物的透皮吸收量。促渗剂Azone用量以2%~5%为最佳
OBJECTIVE: This study provides the basis for selecting suitable drug concentration and promoting agent concentration for clinical use and topical tinidazole (TNZ) preparation. Methods: To observe the transdermal absorption of TNZ in isolated rat skin and compare the transdermal absorption of different concentrations of drug and the promoting effect of different concentrations of Azone. Results: The transdermal absorbances of 0.2%, 0.4%, 1.0% TNZ and 12h were 1.41, 2.82 and 7.12 mg · (50 ml) -1, respectively. The permeation coefficients were 12.98 × 10 -6, 13.68 × 10 -6, and 13.77 × 10 -6. When Azone content is below 5%, the transdermal absorption of TNZ increases with the increase of Azone concentration. When Azone content reaches 8%, transdermal absorption decreases. Conclusion: TNZ can penetrate the skin of isolated mice to increase the drug concentration and increase the transdermal absorption of the drug. Penetration enhancer Azone dosage of 2% to 5% is the best