Document Detail


Tissue distribution and targeting evaluation of TMP after oral administration of TMP-loaded microemulsion to mice.
MedLine Citation:
PMID:  23034007     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
The aim of this study was to quantify the oral delivery systems of Tetramethylpyrazine Microemulsion (TMP ME) to heart, liver, spleen, lung, kidney and brain by comparing TMP level after oral administration at a dose of 100 mg kg(-1) with those of TMP tablet suspension (TMP SWW). This study was taken in mice to develop a suitable analytical methodology in pharmacokinetics studies and to manipulate the tissue distribution and targeting evaluation. Drug concentrations in tissues were determined at different times post-mortem. An HPLC method for separation and quantification of TMP was developed and validated by studying mice tissues. Following oral administration, TMP concentrations in different tissues were constantly detected for quite a long time and finally differed significantly from each other. The AUC rank order 3 of ME group is AUC(liver )> AUC(brain) > AUC(lung )> AUC(spleen) > AUC(heart )> AUC(kidney), while the SWW group is AUC(liver) > AUC(lung) > AUC(spleen) > AUC(heart) > AUC(brain )> AUC(spleen). Especially, the AUC value in brain region (AUC(brain)) of ME is 6.06-fold of SWW. The drug relative overall targeting efficiency (RTE) are calculated: heart (7.49%), liver (3.54%), spleen (12.60%), lung (6.02%), kidney (2.86%) and brain (12.51%). The results from ME directly showed obvious targeting transport to the brain. These results indicated that this new family of pharmaceutical carriers can be used for the solubilization and targeted delivery of poorly soluble drugs to various pathological sites in the body.
Authors:
Li Ma; Yanni Fan; Hongfei Wu; Sha Na; Lei Wang; Chuanhua Lu
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-10-4
Journal Detail:
Title:  Drug development and industrial pharmacy     Volume:  -     ISSN:  1520-5762     ISO Abbreviation:  Drug Dev Ind Pharm     Publication Date:  2012 Oct 
Date Detail:
Created Date:  2012-10-4     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7802620     Medline TA:  Drug Dev Ind Pharm     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Affiliation:
Department of Pharmaceutics, Anhui University of Traditional Chinese Medicine , Anhui Province , China.
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