Document Detail


Improvement of the pulmonary absorption of (Asu1,7)-eel calcitonin by various absorption enhancers and their pulmonary toxicity in rats.
MedLine Citation:
PMID:  9344172     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The effects of absorption enhancers on the pulmonary absorption of (Asu1,7)-eel calcitonin (ECT) and their pulmonary toxicity were examined by means of in situ pulmonary experiments. The absorption of ECT from the lungs was estimated by its hypocalcemic effect. The pulmonary membrane toxicity of absorption enhancers was evaluated by the leakage of Evans Blue from the plasma into the lungs. In the absence of absorption enhancers, a slight hypocalcemic effect was obtained following intrapulmonary administration of ECT. However, we found significant hypocalcemic effects after the ECT administration with 10 mM n-lauryl beta-D-maltopyranoside (LM), 10 mM sodium glycocholate (NaGC), and 10 mM linoleic acid-HCO60 (hydrogenated caster oil) mixed micelle (MM). The plasma calcium levels decreased as the amount of LM coadministered with ECT increased. In contrast, 10 mM EDTA did not improve the pulmonary absorption of ECT. Overall, a correlation between the pulmonary absorption of ECT and local toxicity was observed in the presence of these additives. However, 1 mM LM, 10 mM NaGC, and 10 mM MM improve the pulmonary absorption of ECT with low pulmonary toxicity. These findings suggest that the use of these adjuvants would be a useful approach for improving the pulmonary absorption of ECT.
Authors:
A Yamamoto; S Okumura; Y Fukuda; M Fukui; K Takahashi; S Muranishi
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Journal of pharmaceutical sciences     Volume:  86     ISSN:  0022-3549     ISO Abbreviation:  J Pharm Sci     Publication Date:  1997 Oct 
Date Detail:
Created Date:  1998-02-02     Completed Date:  1998-02-02     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  2985195R     Medline TA:  J Pharm Sci     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  1144-7     Citation Subset:  IM    
Affiliation:
Department of Biopharmaceutics, Kyoto Pharmaceutical University, Japan.
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MeSH Terms
Descriptor/Qualifier:
Absorption / drug effects
Animals
Calcitonin / analogs & derivatives*,  pharmacokinetics,  toxicity
Calcium / blood
Castor Oil / analogs & derivatives*,  pharmacology
Glycocholic Acid / pharmacology*
Linoleic Acid / pharmacology*
Lung / drug effects,  metabolism*
Lung Neoplasms / chemically induced
Male
Maltose / pharmacology*
Micelles
Rats
Rats, Wistar
Surface-Active Agents / pharmacology
Chemical
Reg. No./Substance:
0/Micelles; 0/Surface-Active Agents; 0/n-lauryl beta-d-maltopyranoside; 2197-37-7/Linoleic Acid; 475-31-0/Glycocholic Acid; 60731-46-6/elcatonin; 61791-12-6/polyethoxylated castor oil; 69-79-4/Maltose; 7440-70-2/Calcium; 8001-79-4/Castor Oil; 9007-12-9/Calcitonin

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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