氟康唑的局部给药：以乳剂为剂型的体外皮肤渗透与透皮吸收
Topical delivery of fluconazole: in vitro skin penetration and permeation using emulsions as dosage forms.
作者信息
Ayub Alessandra C, Gomes Aline D M, Lima Marcus V C, Vianna-Soares Cristina D, Ferreira Lucas A M
机构信息
Department of Pharmaceutics, Faculty of Pharmacy, Federal University of Minas Gerais (UFMG), Av. Antonio Carlos, Belo Horizont (MG), Brazil.
出版信息
Drug Dev Ind Pharm. 2007 Mar;33(3):273-80. doi: 10.1080/03639040600829989.
We investigated in vitro skin penetration and permeation of fluconazole from emulsions containing different penetration enhancers. Fluconazole permeation was high (15-65% of the applied dose) across hairless mouse skin and low (8-9%) across pig ear skin. Permeation across mice skin from a formulation containing propyleneglycol and isopropyl myristate was significantly higher than that observed with the paraffin oil and propyleneglycol or Transcutol emulsions. With pig skin, the paraffin oil or isopropyl myristate and propyleneglycol emulsions showed similar skin permeation and penetration. However, these emulsions provided epidermal concentrations higher than the minimal inhibitory concentrations for most dermatophytes.
我们研究了含不同渗透促进剂的氟康唑乳剂的体外皮肤渗透情况。氟康唑在无毛小鼠皮肤上的渗透较高（占给药剂量的15 - 65%），而在猪耳皮肤上的渗透较低（8 - 9%）。含丙二醇和肉豆蔻酸异丙酯的制剂在小鼠皮肤上的渗透显著高于石蜡油与丙二醇或二甲基亚砜乳剂。对于猪皮，石蜡油或肉豆蔻酸异丙酯与丙二醇乳剂表现出相似的皮肤渗透情况。然而，这些乳剂在表皮中的浓度高于大多数皮肤癣菌的最低抑菌浓度。
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