局部使用的阿昔洛韦软膏无法穿透人体皮肤。
Failure of topical acyclovir in ointment to penetrate human skin.
作者信息
Freeman D J, Sheth N V, Spruance S L
出版信息
Antimicrob Agents Chemother. 1986 May;29(5):730-2. doi: 10.1128/AAC.29.5.730.
Abstract
Topical acyclovir (ACV) in polyethylene glycol (PEG) ointment has been disappointing in the treatment of recurrent herpes simplex virus infections in immunocompetent patients. To investigate the possible role of poor drug delivery from this formulation, we studied the penetration of ACV through excised human skin from three vehicles; PEG ointment, modified aqueous cream, and dimethyl sulfoxide. A second antiviral agent, idoxuridine, was studied in the same formulations, and drug delivery through excised guinea pig skin was also assessed for comparison. The delivery of ACV from PEG ointment was very slow for both human and guinea pig skin (drug flux, 0.055 and 0.047 microgram/cm2 per h, respectively). Formulation of ACV in modified aqueous cream and in dimethyl sulfoxide resulted in an 8- and 60-fold increase, respectively, in the flux of ACV through human skin. Idoxuridine behaved similarly to ACV in the three vehicles. The poor clinical results seen with topical use of ACV ointment may be due in part to retarded drug delivery from this formulation.
摘要
局部用阿昔洛韦（ACV）聚乙二醇（PEG）软膏在治疗免疫功能正常患者的复发性单纯疱疹病毒感染方面效果不佳。为了研究该制剂药物递送不佳的可能作用，我们研究了阿昔洛韦从三种载体透过离体人皮肤的渗透情况；PEG软膏、改良水性乳膏和二甲基亚砜。还在相同制剂中研究了另一种抗病毒药物碘苷，并评估了其透过离体豚鼠皮肤的药物递送情况以作比较。对于人皮肤和豚鼠皮肤，阿昔洛韦从PEG软膏中的递送都非常缓慢（药物通量分别为每小时0.055和0.047微克/平方厘米）。阿昔洛韦制成改良水性乳膏和二甲基亚砜制剂后，其透过人皮肤的通量分别增加了8倍和60倍。碘苷在三种载体中的表现与阿昔洛韦相似。局部使用阿昔洛韦软膏临床效果不佳可能部分归因于该制剂药物递送延迟。
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Treatment of herpes simplex labialis with topical acyclovir in polyethylene glycol.用聚乙二醇中的局部阿昔洛韦治疗唇疱疹。
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Treatment of recurrent genital herpes simplex infections with oral acyclovir. A controlled trial.口服阿昔洛韦治疗复发性生殖器单纯疱疹感染。一项对照试验。
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