Abstract
The quaternary salt berberine can be delivered to the brain by injecting the lipoidal dihydroberberine, which is converted in vivo to berberine. The efflux from the brain of the berberine formed in situ is much slower than its rate of elimination from the general circulatory system. This inherent specificity for the brain of this redox delivery system can further be enhanced by slowly infusing the dihydroberberine instead of an i.v. bolus injection. It was found that by controlling infusion of dihydroberberine, the concentration of berberine (relative to its concentration after i.v. bolus) rose specifically in the brain while it fell in other tissues. It is suggested that a combination of the redox-delivery system with controlled infusion (or other controlled release techniques) will result in maximal brain-specific delivery.
- Received February 3, 1983.
- Accepted June 14, 1983.
- Copyright © Parenteral Drug Association. All rights reserved.
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