| Title | Tissues Distribution of R-(-)- and S-(+)-m-Nisoldipine after Single Enantiomer Administration in Rats. | | Author(s) | Li M, Wang Q, Wang C, Jing X, Duan K, Chen X, Xu L, Tian Y, Zhang L, Du Y, Zhang X, Sheng X | | Institution | Department of Pharmaceutical Analysis, School of Pharmacy, Hebei Medical University, Shijiazhuang, P.R. China. | | Source | Drug Dev Ind Pharm 2008 Sep 27.:1-8. | | Abstract | Rapid, sensitive, and selective high-performance liquid chromatography methods were developed and validated for determination of m-nisoldipine enantiomers in rat tissues. All of the samples were prepared based on a simple and efficient liquid-liquid extraction method. After validating that no racemation occurred by ULTRON ES-OVM (Japan), m-nisoldipine enantiomers were determined, respectively, on a reverse-phase C(18) column (5 mum, 250 x 4.6 mm). This method was applied to study tissue distribution of m-nisoldipine enantiomers in rats after a single administration of m-nisoldipine enantiomers. By the two-sample t test, there were basically no significant differences between the two enantiomers in each tissue ( p > .05), which indicates that they may have the same potency in rats. In small intestine, lung, liver, and spleen, the concentrations of R-(-)- and S-(+)-m-nisoldipine were high at 30 and 150 min than that at 90 min, which showed that m-nisoldipine enantiomers may have the phenomenon of hepatoenteral circulation. A small quantity of the prototype of R-(-)- and S-(+)-m-nisoldipine in brain showed that they can cross the blood-brain barrier to arrive at the brain tissue. The high quantity of distribution in lung and brain implied that the lipophilicity of the drug was powerful. | | Language | ENG | | Pub Type(s) | JOURNAL ARTICLE
| | PubMed ID | 18821195 |
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