کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2487796 | 1114434 | 2006 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Enhancement of Transdermal Testosterone Delivery By Supersaturation
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
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چکیده انگلیسی
The objective was to evaluate supersaturation in the development of a spray formulation for transdermal testosterone delivery. The method of cosolvents was used to prepare supersaturated testosterone vehicles, the stability of which was evaluated. Drug delivery from selected formulations, and from a simpler spray, was then assessed across hairless rat skin in vitro. Supersaturated drug solutions were formed either by rapidly adding water to a drug-saturated 4:1:1 ethanol/propylene glycol (PG)/water mixture, or by maintaining the proportion of water constant, while varying the relative amounts of ethanol and PG. In the former case, only small degrees of saturation (DS) could be maintained, and drug flux was increased only modestly. The latter approach produced more stable formulations with DSâ=â2 to 4. A 1:1 ethanol/PG spray containing saturated testosterone delivered drug as efficiently as a supersaturated vehicle with DS = 2.5. Preparation of supersaturated testosterone formulations is possible, therefore, but significant amounts of water lead to rapid drug crystallization. As percentage PG increases, better stability results, but the practicality of using such vehicles in sprays and aerosols may be questioned. Nevertheless, a simple 1:1 ethanol/PG spray apparently induces supersaturation in situ, and further work to optimize the approach is warranted.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 95, Issue 11, November 2006, Pages 2373-2379
Journal: Journal of Pharmaceutical Sciences - Volume 95, Issue 11, November 2006, Pages 2373-2379
نویسندگان
Marie-Laure Leichtnam, Hervé Rolland, Patrick Wüthrich, Richard H. Guy,