Abstract:
:The in vitro diffusion of a series of substituted acetanilides across the hamster cheek pouch was studied. The keratinized epithelial layer of the cheek pouch appeared to provide the major barrier to diffusion of these compounds. Linear relationships were found for plots of log epithelial permeability (Pe) versus the log of the octanol-buffer partition coefficient (PCoct; r = 0.712), and log Pe versus the log of the isooctane-buffer partition coefficient (PCiso; r = 0.869). Comparison of the in vitro data with in vivo data obtained in humans using the buccal absorption test showed good correlation (r = 0.878) between Pe and percent buccal absorption in 5 min. These results suggest that diffusion across the hamster cheek pouch may have some utility in the prediction of human buccal absorption.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Garren KW,Repta AJdoi
10.1002/jps.2600780218subject
Has Abstractpub_date
1989-02-01 00:00:00pages
160-4issue
2eissn
0022-3549issn
1520-6017pii
S0022-3549(15)47892-Xjournal_volume
78pub_type
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abstract::Eight analogs of the fentanyl-type analgesics, in which the piperidine ring is restricted into a boat conformation, were evaluated for analgesic activity. All analogs were less active than fentanyl, but interesting conformational and structural relationships were observed. Results of the study are discussed. ...
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journal_title:Journal of pharmaceutical sciences
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journal_title:Journal of pharmaceutical sciences
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journal_title:Journal of pharmaceutical sciences
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更新日期:2009-06-01 00:00:00
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journal_title:Journal of pharmaceutical sciences
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