| Effects of amines on percutaneous absorption of alendronate. | |
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MedLine Citation:
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PMID: 21126206 Owner: NLM Status: In-Data-Review |
Abstract/OtherAbstract:
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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. |
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Authors:
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Jiae Whang; Hyesun Gwak |
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Publication Detail:
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Type: Journal Article Date: 2010-12-03 |
Journal Detail:
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Title: Drug development and industrial pharmacy Volume: 37 ISSN: 1520-5762 ISO Abbreviation: Drug Dev Ind Pharm Publication Date: 2011 May |
Date Detail:
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Created Date: 2011-04-07 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 7802620 Medline TA: Drug Dev Ind Pharm Country: England |
Other Details:
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Languages: eng Pagination: 491-7 Citation Subset: IM |
Affiliation:
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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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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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