کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8515013 | 1556513 | 2016 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Enhanced Activity of Topical Hydrocortisone by Competitive Binding of Corticosteroid-Binding Globulin
ترجمه فارسی عنوان
فعالیت پیشرفته هیدروکورتیزون موضعی توسط اتصال رقابتی گلووبولین کورتیکواستروئید
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کلمات کلیدی
OTCCBGTransdermalLoteprednol etabonateAUC - AUCover-the-counter - بیش از حد ضدStability - ثباتDrug transport - حمل مواد مخدرDrug design - طراحی دارو Metabolism - متابولیسم area under the curve - منطقه تحت منحنیHydrocortisone - هیدروکورتیزونProtein binding - پیوند پروتئینglucocorticoid receptor - گیرنده گلوکوکورتیکوئید
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
چکیده انگلیسی
Atopic dermatitis of sensitive areas such as the face, particularly in children, is a difficult disease to treat as the standard therapeutic, topical steroids, is contraindicated for this application in children. Hydrocortisone (HC) can be used in these instances because it has been shown to be safe, but is often ineffective as it is a relatively weak steroid, especially at over-the-counter concentrations. To enhance the local topical activity of HC, the terminal inactive metabolite of prednisolone, Î1-cortienic acid (Î1-CA), is added to HC, as Î1-CA preferentially binds transcortin, liberating more HC to elicit its therapeutic effect. Skin blanching studies, which are used to evaluate the potency of topical steroids, were employed to assess the ability of Î1-CA to enhance the activity of HC. The results demonstrate that Î1-CA, when applied in combination with HC, does indeed potentiate the vasoconstriction effect of topically applied HC, while having no effect alone. Thus, addition of the inert prednisolone metabolite Î1-CA can increase the therapeutic effect of over-the-counter concentrations of HC when applied topically.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 105, Issue 9, September 2016, Pages 2873-2878
Journal: Journal of Pharmaceutical Sciences - Volume 105, Issue 9, September 2016, Pages 2873-2878
نویسندگان
Erik T. Bodor, Whei-Mei Wu, V. Ravi Chandran, Nicholas Bodor,