Bisphosphonate prodrugs

Bisphosphonates (BP) are pyrophosphate analogs having a P-C-P backbone. The oral bioavailability of BPs is ca. 1%, due to high ionisation at physiological pH. Using the prodrug approach, oral absorption can be increased by masking one or more ionizable groups (clodronate, etidronate), or using a tar...

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Bibliographic Details
Published in:	Current medicinal chemistry Vol. 9; no. 12; p. 1201
Main Author:	Vepsäläinen, Jouko J
Format:	Journal Article
Language:	English
Published:	United Arab Emirates 01-06-2002
Subjects:	Administration, Oral Animals Biological Availability Clodronic Acid - analogs & derivatives Diphosphonates - chemical synthesis Diphosphonates - chemistry Diphosphonates - pharmacokinetics Drug Delivery Systems Etidronic Acid - analogs & derivatives Humans Hydrogen-Ion Concentration Hydrolysis Intestinal Absorption Prodrugs - chemical synthesis Prodrugs - chemistry Prodrugs - pharmacokinetics Structure-Activity Relationship Tissue Distribution
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Summary:	Bisphosphonates (BP) are pyrophosphate analogs having a P-C-P backbone. The oral bioavailability of BPs is ca. 1%, due to high ionisation at physiological pH. Using the prodrug approach, oral absorption can be increased by masking one or more ionizable groups (clodronate, etidronate), or using a targeting carrier system (alendronate, pamitronate).
ISSN:	0929-8673
DOI:	10.2174/0929867023369998