Controlled Systemic Absorption and Increased Anesthetic Effect of Bupivacaine Following Epidural Administration of Bupivacaine-Hydroxypropyl-β-Cyclodextrin Complex

Pharmaceutical Research - Tập 13 Số 10 - Trang 1576-1580 - 1996
Fréville, Jean Christophe1, Dollo, Gilles1, Le Corre, Pascal1, Chevanne, François1, Le Verge, Roger1
1Laboratoire de Pharmacie Galénique et Biopharmacie, Faculté des Sciences Pharmaceutiques et Biologiques, Université de Rennes 1, Rennes Cedex, France

Tóm tắt

Purpose. To investigate the influence of complexation between bupivacaine and hydroxypropyl-β-cyclodextrin (HP-β-CD) on the systemic absorption and on the pharmacodynamic effect of bupivacaine following epidural administration in a rabbit model. Methods. Bupivacaine and bupivacaine-HP-β-CD complex were administered according to a randomized and cross-over design in six rabbits chronically instrumented with an epidural catheter. The plasma concentrations of bupivacaine and the duration and intensity of the motor blockade were evaluated. Results. Complexation with HP-β-CD led to a decrease in the maximum plasma concentration of bupivacaine. Individual absorption kinetics evaluated by Loo-Riegelman absorption analysis indicated that systemic absorption resulted from two parallel first-order processes. Only the faster absorption phase was slowed by complexation with HP-β-CD. The duration of the motor blockade was increased almost twice but the intensity was not modified. Conclusions. Complexation with HP-β-CD could be a promising drug delivery system to improve the therapeutic index of bupivacaine.

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Pharmaceutical Research

Tập 13 Số 10

1576-1580

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