Relationship between lactone ratios of 9-nitrocamptothecin and their lactone/carboxylate equilibria in vitro and in vivo
The aim of this study was to evaluate the effect of lactone ratios on the lactone/carboxylate equilibria of 9-nitrocamptothecin (9-NC) in vitro and in vivo. The interconversion of lactone and carboxylate forms of 9-NC was studied. Then the lactone ratio vs time profiles of these 9-NC solutions were...
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Autores principales: | , , , , , , |
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Formato: | Articulo |
Lenguaje: | Inglés |
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2012
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Acceso en línea: | http://sedici.unlp.edu.ar/handle/10915/25743 http://www.latamjpharm.org/resumenes/31/7/LAJOP_31_7_1_10.pdf |
Aporte de: |
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I19-R120-10915-25743 |
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institution |
Universidad Nacional de La Plata |
institution_str |
I-19 |
repository_str |
R-120 |
collection |
SEDICI (UNLP) |
language |
Inglés |
topic |
Farmacia 9-nitrocamptothecin Intravenous injection Lactone Pharmacokinetics |
spellingShingle |
Farmacia 9-nitrocamptothecin Intravenous injection Lactone Pharmacokinetics Chen, Jun Hu, Rongrong Yang, Xixiong Tian, Rong Gu, Wei Chen, Zhipeng Cai, Baochang Relationship between lactone ratios of 9-nitrocamptothecin and their lactone/carboxylate equilibria in vitro and in vivo |
topic_facet |
Farmacia 9-nitrocamptothecin Intravenous injection Lactone Pharmacokinetics |
description |
The aim of this study was to evaluate the effect of lactone ratios on the lactone/carboxylate equilibria of 9-nitrocamptothecin (9-NC) in vitro and in vivo. The interconversion of lactone and carboxylate forms of 9-NC was studied. Then the lactone ratio vs time profiles of these 9-NC solutions were further investigated in pH 7.4 PBS, rat plasma and blood. 9-NC solutions with different lactone ratios (lactone ratios=100 %, 75 %, 50 %, 25 % and 0 %, respectively) were obtained by modifying the pH of solution and it was found that the effects on lactone/carboxylate equilibrium were in the order: blood cells > plasma albumin > pH. After i.v. administration, between the groups of 100 % and 75 % lactone ratios, the AUC0-t values of lactone 9-NC were almost equal. Therefore, there might be no difference between the anticancer activities of 9-NC solution in the range of 75~100 % lactone ratios. |
format |
Articulo Articulo |
author |
Chen, Jun Hu, Rongrong Yang, Xixiong Tian, Rong Gu, Wei Chen, Zhipeng Cai, Baochang |
author_facet |
Chen, Jun Hu, Rongrong Yang, Xixiong Tian, Rong Gu, Wei Chen, Zhipeng Cai, Baochang |
author_sort |
Chen, Jun |
title |
Relationship between lactone ratios of 9-nitrocamptothecin and their lactone/carboxylate equilibria in vitro and in vivo |
title_short |
Relationship between lactone ratios of 9-nitrocamptothecin and their lactone/carboxylate equilibria in vitro and in vivo |
title_full |
Relationship between lactone ratios of 9-nitrocamptothecin and their lactone/carboxylate equilibria in vitro and in vivo |
title_fullStr |
Relationship between lactone ratios of 9-nitrocamptothecin and their lactone/carboxylate equilibria in vitro and in vivo |
title_full_unstemmed |
Relationship between lactone ratios of 9-nitrocamptothecin and their lactone/carboxylate equilibria in vitro and in vivo |
title_sort |
relationship between lactone ratios of 9-nitrocamptothecin and their lactone/carboxylate equilibria in vitro and in vivo |
publishDate |
2012 |
url |
http://sedici.unlp.edu.ar/handle/10915/25743 http://www.latamjpharm.org/resumenes/31/7/LAJOP_31_7_1_10.pdf |
work_keys_str_mv |
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bdutipo_str |
Repositorios |
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1764820466890964993 |