PARENTERAL FORMULATION FOR CARBAMAZEPINE

Award Information
Agency: Department of Health and Human Services
Branch: N/A
Contract: N/A
Agency Tracking Number: 16769
Amount: $500,000.00
Phase: Phase II
Program: SBIR
Awards Year: 1992
Solitcitation Year: N/A
Solitcitation Topic Code: N/A
Solitcitation Number: N/A
Small Business Information
Pharmatec Inc.
Box 730, Alachua, FL, 32615
Duns: N/A
Hubzone Owned: N
Woman Owned: N
Socially and Economically Disadvantaged: N
Principal Investigator
 Kerry Estes
 (904) 462-1210
Business Contact
Phone: () -
Research Institution
N/A
Abstract
THE FAVORABLE EFFICACY, TOXICITY AND ADVERSE SIDE-EFFECT PROFILES OF CARBAMAZEPINE (CBZ) CONTRIBUTE TO ITS WIDESPREADAND INCREASING USE TO CONTROL SEIZURES IN THE EPILETPTIC PATIENTS. HOWEVER, IN CASES WHEN ORAL DRUG TREATMENT IS NOTFEASIBLE, NO PARENTERAL FORMULATION IS AVAILABLE FOR CBZ. CURRENTLY EPILEPTIC PATIENTS WHO ARE UNABLE TO MAINTAIN ORALCBZ MUST BE TREATED WITH OTHER ANTICONVULSANTS FORMULATED FOR PARENTERAL ADMINISTRATION. THIS MULTIPLE DRUG APPROACH OFTEN LEADS TO UNPREDICTABLE SEIZURE CONTROL AND INCREASED DRUG TOXICITY IN CHRONICALLY CBZ TREATED PATIENTS. OUR PRELIMINARY STUDIES SHOWED FIRST THAT AQUEOUS SOLUTIONS OF CBZ CAN BE GIVEN INTRAVENOUSLY (IV). SECOND, ANTICONVULSANT ACTIVITY OF CBZ IS UNALTERED IN THE MOUSE MES(MAXIMAL ELECTROCONVULSANT SHOCK) MODEL WHEN GIVEN IN THE AQUEOUS FORMULATION. THIRD, THE IV TOTAL DAILY DOSE OF CBZ PROJECTED TO MAINTAIN SEIZURE CONTROL CAN BE FORMULATED IN AREASONABLE VOLUME. THIS APPROACH TO PARENTERAL FORMULATION OF CBZ IS BASED ON USING A WATER SOLUBLE EXCIPIENT WHICH IS KNOWN TO FORM AN INCLUSION COMPLEX WITH LIPOPHILIC DRUGS. THE EXCIPIENT HAS A FAVORABLE TOXICITY PROFILE FOR IV DOSINGAND THE SOLUTIONS ARE STABLE TO HEAT STERILIZATION. THE STUDIES WILL EXAMINE THE FEASIBILITY OF DEVELOPING A PARENTERAL FORMULATION OF CBZ BASED ON THIS LICENSED INCLUSION COMPLEX TECHNOLOGY. THE STUDIES WILL EXPLORE: FORMULATION STABILITY, COMPATIBILITY WITH OTHER IV FLUIDS, VENOUS IRRITATION, TOXICITY PROFILES AND MANUFACTURING REPRODUCABILITY. SUCCESSFUL DEVELOPMENT OF A CBZ FORMULATION FOR IV ADMINISTRATION WOULD BENEFIT THE EPILEPTIC PATIENT WHO IS UNABLE TO MAINTAIN ORAL CBZ THERAPY.

* information listed above is at the time of submission.

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