Development of aqueous parenteral formulations for carbamazepine through the use of modified cyclodextrins.

Abstract:

:The poor aqueous solubility of carbamazepine was dramatically increased via complexation with various chemically modified beta-cyclodextrins and gamma-cyclodextrins. A preparation of carbamazepine and 2-hydroxypropyl-beta-cyclodextrin was found to be stable to steam sterilization and to storage under a variety of conditions. Carbamazepine, when solubilized in this manner, was found to exert potent anticonvulsant effects in various seizure models and the formulation was tolerated in animals at high doses (100 mg/kg carbamazepine and 1200 mg/kg of the cyclodextrin excipient). The onset of anticonvulsant action was rapid and consistent with almost instantaneous in vivo complex dissociation. The low toxicity of 2-hydroxypropyl-beta-cyclodextrin, when administered via the parenteral route, and its ability to enhance the aqueous solubility of carbamazipine highly favor the use of this excipient.

journal_name

J Pharm Sci

authors

Brewster ME,Anderson WR,Estes KS,Bodor N

doi

10.1002/jps.2600800420

subject

Has Abstract

pub_date

1991-04-01 00:00:00

pages

380-3

issue

4

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(15)48513-2

journal_volume

80

pub_type

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