原创力文档design, formulation and evaluation of transdermal drug delivery system of budesonide透皮给药系统的设计、制定和评价布地奈德.pdfVIP
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design, formulation and evaluation of transdermal drug delivery system of budesonide透皮给药系统的设计、制定和评价布地奈德
Pharmacology Pharmacy, 2011, 2, 199-211 199
doi:10.4236/pp.2011.23029 Published Online July 2011 (/journal/pp)
Design, Formulation and Evaluation of
Transdermal Drug Delivery System of Budesonide
* *
Updesh B. Lade , Yogesh M. Amgaonkar, Rupesh V. Chikhale , Dinesh M. Biyani, Milind J. Umekar
Department of Pharmaceutics, Smt. Kishoritai Bhoyar College of Pharmacy, Sadashivrao Patil Shikshan Sanstha, New Kamptee,
Nagpur (M.S), India.
*
Email: yamgaonkar123@, rupeshchikhale7@
Received January 24th, 2011; revised March 30th, 2011; accepted May 28th, 2011.
ABSTRACT
Budesonide is a highly potent synthetic, nonhalogenated corticosteroid. The mechanism of action of corticosteroids in
allergic rhinitis remains unknown, but may involve reductions in number of various mediator cells such as basophils,
eosinophils, T-helper cells, mast cells, and neutrophils. In the nasal mucosa, nasal reactivity to allergens, and release
of inflammatory mediators and proteolytic enzymes. Budesonide is very effective and quikly acting as it is rapidly and
almost completely absorbed after oral administration, but has poor systemic availability (about 10%) due to extensive
first-pass metabolism in the liver , mainly by the cytochrome P450 isoenzyme CYP3A4. The major metabolites, 6-β-
hydroxybudesonide and 16-α-hydroxyprednisolone have less than 1% of the glucocorticoid activity of unchanged drug
with a terminal half-life of about 2 - 4 hours. Polymeric films containing Eudragit RL 100: Eudragit RS: drug (7:3:1, 7:
2:1) and Ethyl cellulose: PVP: drug (7:3:1, 7:2:1) were selected for transdermal administration based on evaluation
studies. These polymeric films were prepared by mercury substrat
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