Document Detail


In situ absorption and protein binding characteristics of CDRI-85/92, an antiulcer pharmacophore.
MedLine Citation:
PMID:  12711165     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
CDRI-85/92, a new antiulcer drug, acts as a proton pump inhibitor arresting the secretion of acid in the stomach. The absorption kinetics of CDRI-85/92 was evaluated in situ using rat intestinal recirculation perfusion method. The experiment was conducted at pH 2.6 and 7.4 representing the acidic and the mild alkaline environment, which the drug experiences through the GIT during oral treatment. The rate of absorption was the same (0.12h(-1)) at pH 2.6 and 7.4, thus suggesting equal absorption profile of the CDRI-85/92 throughout the GIT irrespective of the pH. Equal rates of absorption can also be correlated with the presence of acidic and basic groups in the structure of CDRI-85/92. Protein binding studies of CDRI-85/92 using ultrafiltration were conducted in vitro and in vivo. Protein binding was found to be in the range of 31.49-32.91% both in in vitro and in vivo (employing 5-min post dose samples of rat serum after 20 mgkg(-1) i.v. treatment of CDRI-85/92). The binding was found to be linear in the concentration range of 156.25-2000 ngml(-1) (r(2)>0.99).
Authors:
Pratima Srivastava; R C Gupta
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  International journal of pharmaceutics     Volume:  257     ISSN:  0378-5173     ISO Abbreviation:  Int J Pharm     Publication Date:  2003 May 
Date Detail:
Created Date:  2003-04-24     Completed Date:  2003-05-29     Revised Date:  2009-11-03    
Medline Journal Info:
Nlm Unique ID:  7804127     Medline TA:  Int J Pharm     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  97-102     Citation Subset:  IM    
Affiliation:
Pharmacokinetics and Metabolism Division, Central Drug Research Institute, Chattar Manzil Palace, Post Box 173, Lucknow 226001, India.
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MeSH Terms
Descriptor/Qualifier:
Absorption
Animals
Anti-Ulcer Agents / pharmacokinetics*
Male
Oxazoles / pharmacokinetics*
Protein Binding
Rats
Rats, Sprague-Dawley
Chemical
Reg. No./Substance:
0/Anti-Ulcer Agents; 0/CDRI-85-92; 0/Oxazoles

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