| Autor: |
Fujisaki, Jiro, Tokunaga, Yuji, Takahashi, Toshiya, Murata, Saburo, Shimojo, Fumio, Hata, Takehisa |
| Zdroj: |
Journal of Pharmacy and Pharmacology; August 1996, Vol. 48 Issue: 8 p798-800, 3p |
| Abstrakt: |
Disodium (fluorescein-6−carbonyloxy)acetoaminomethylene bisphosphonate (CF-BP), a prodrug of 6−carboxy-fluorescein, is efficiently absorbed by the skeleton where it hydrolyses to carboxyfluorescein. An osteotropic drug-delivery system based on this bisphosphonic prodrug has been developed as a novel method for site-specific and controlled delivery of drugs to the bone. In this study the physicochemical properties of the prodrug have been characterized by investigating the affinity of CF-BP for hydroxyapatite and the hydrolysis of the compound to carboxyfluorescein.In the binding study, CF-BP bound very rapidly to hydroxyapatite without degradation and carboxyfluorescein was subsequently gradually released by hydrolysis of bound CF-BP. Hydrolysis of CF-BP in buffer solutions followed pseudo-first-order kinetics, and quantitative regeneration of carboxyfluorescein was observed. In addition, regeneration of carboxyfluorescein from CF-BP was accelerated in the presence of fresh rat plasma.These results suggest that CF-BP has the physicochemical properties required for site-specific and controlled delivery of carboxyfluorescein to bones. |
| Databáze: |
Supplemental Index |
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