Relationship between Lactone Ratios of 9-Nitrocamptothecin and their Lactone/Carboxylate Equilibria In Vitro and In Vivo

被引：0
|
作者：
Chen, Jun [1 ]
Hu, Rongrong [1 ]
Yang, Xixiong [2 ]
Tian, Rong [1 ]
Gu, Wei [1 ]
Chen, Zhipeng [1 ]
Cai, Baochang [1 ]
机构：
[1] Nanjing Univ Chinese Med, Coll Pharm, Nanjing 210046, Jiangsu, Peoples R China
[2] Jingchu Univ Technol, Coll Chem Engn & Pharm, Jingmen 448000, Peoples R China
来源：
LATIN AMERICAN JOURNAL OF PHARMACY | 2012年 / 31卷 / 07期
关键词：
9-nitrocamptothecin; Intravenous injection; Lactone; Pharmacokinetics; CARBOXYLATE FORMS; CAMPTOTHECIN; DRUG;
D O I：
暂无
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
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 To 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 To and 75 % lactone ratios, the AUC(0-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 similar to 100 % lactone ratios.
引用
收藏
页码：990 / 998
页数：9
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