| Full text | |
| Author(s): |
Moraes, Carolina Morales
;
Abrami, Priscila
;
Paula, Eneida de
[3]
;
Braga, Angélica F. A.
;
Fraceto, Leonardo Fernandes
Total Authors: 5
|
| Document type: | Journal article |
| Source: | International Journal of Pharmaceutics; v. 331, n. 1, p. 99-106, Feb. 2007. |
| Field of knowledge: | Health Sciences - Dentistry |
| Abstract | |
Local anesthetics are substances able to induce pain relief by binding to the sodium channel of excitable membranes, blocking the influx of sodium ions and the propagation of nervous impulses. S(−) bupivacaine (S(−) bvc) is an amide type local anesthetic widely used in surgery and obstetrics for sustained peripheral and central nerve blockade. The present work focuses on the characterization of an inclusion complex of S(−) bvc in 2-hydroxypropyl-BETA-cyclodextrin (HP-BETA-CD). The complexation with HP-BETA-CD has been investigated using reversed-phase liquid chromatography and solubility isotherms. The retention behavior was analyzed on a reversed phase C18 column and the mobile phase used was acetonitrile-phosphate buffer pH 7.4 (10 mM), (45/55, v/v), in which HP-BETA-CD was incorporated as a mobile phase additive. The decrease in the retention times with increasing concentration of HP-BETA-CD enables the determination of the complex apparent stability constants by HPLC as a function of temperature. The solubility isotherms were studied as a function of pH (7.4 and 10.5) and temperature... (AU) | |