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Effects of amines on percutaneous absorption of alendronate.
MedLine Citation:
PMID:  21126206     Owner:  NLM     Status:  In-Data-Review    
Objective: The aim of this study was to examine the effects of amines on the permeation of alendronate using solution formulations and pressure-sensitive adhesive (PSA) transdermal delivery systems (TDS). Materials and methods: Monoethanolamine (MEA), diethanolamine (DEA), triethanolamine (TEA), diethylamine (DEYA), and triethylamine (TEYA) at concentrations of 3, 6, and 10% were added to propylene glycol (PG) containing 6% caprylic acid. In vitro and in vivo experiments were conducted using alendronate solution and PSA TDS formulations. Results: When using saturated solution formulations, 3% TEA and 10% DEYA showed high permeation rates of 8.20 ± 0.80 and 7.87 ± 0.18 μg/cm(2)/h, respectively. The maximum permeation flux of 1.79 ± 0.28 μg/cm(2)/h from 1 mg/ml solution was obtained with the addition of 10% DEYA followed by the addition of 10% TEYA (1.72 ± 0.72 μg/cm(2)/h). The highest enhancement factor of 1.86 was obtained with alendronate PSA TDS containing 10% MEA compared with no amine. In the in vivo study, the amount remaining to be excreted (ARE) at time 0 (Ae(∞)) and ARE at time t [Ae(t)] differed between TDS and oral delivery significantly (P < 0.01). The TDS containing 10% MEA showed the highest Ae(∞) (19.5 ± 6.93 μg), which was 2.7- and 2.2-fold, compared with oral and no amine administration, respectively. Conclusion: Based on the results, TDS with 10% MEA in PG containing 6% caprylic acid could be a good candidate for the alendronate TDS.
Jiae Whang; Hyesun Gwak
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Publication Detail:
Type:  Journal Article     Date:  2010-12-03
Journal Detail:
Title:  Drug development and industrial pharmacy     Volume:  37     ISSN:  1520-5762     ISO Abbreviation:  Drug Dev Ind Pharm     Publication Date:  2011 May 
Date Detail:
Created Date:  2011-04-07     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7802620     Medline TA:  Drug Dev Ind Pharm     Country:  England    
Other Details:
Languages:  eng     Pagination:  491-7     Citation Subset:  IM    
College of Pharmacy and Division of Life and Pharmaceutical Sciences, Ewha Womans University, 11-1 Daehyun-Dong Seodaemun-Gu, Seoul 120-750, Korea.
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