کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2484519 | 1114314 | 2015 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Investigating Detrusor Muscle Concentrations of Oxybutynin After Intravesical Delivery in an Ex Vivo Porcine Model
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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
Intravesical oxybutynin is highly effective in the treatment of overactive bladder. Traditionally the mechanism of action was explained by antagonism of muscarinic receptors located in the detrusor, however evidence now suggests antimuscarinics may elicit their effect by modifying afferent pathways in the mucosal region. This study aimed to investigate the bladder wall distribution of oxybutynin in an ex vivo setting providing tissue - layer specific concentrations of drug achieved after intravesical delivery. Whole ex vivo porcine bladders were intravesically instilled with 0.167 mg mLâ 1 oxybutynin solution. After 60 min, tissue samples were excised, serially sectioned parallel to the urothelial surface and extracted drug quantified. Drug distribution into the urothelium, lamina propria and detrusor was determined. Oxybutynin permeated into the bladder wall at a higher rate than other drugs previously investigated (apparent transurothelial Kp = 1.36 Ã 10â 5 cm sâ 1). After 60 min intravesical instillation, concentrations achieved in the urothelium (298.69 μg gâ 1) and lamina propria (43.65 μg gâ 1) but not the detrusor (0.93 μg gâ 1) were greater than reported IC50 values for oxybutynin. This work adds to the increasing body of evidence suggesting antimuscarinics elicit their effects via mechanisms other than direct inhibition of detrusor contraction.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 104, Issue 7, July 2015, Pages 2233-2240
Journal: Journal of Pharmaceutical Sciences - Volume 104, Issue 7, July 2015, Pages 2233-2240
نویسندگان
Nicholas A. Williams, Kay M. Lee, Chris J. Allender, Jenna L. Bowen, Mark Gumbleton, Tim Harrah, Aditya Raja, Hrishi B. Joshi,