ORAL DELIVERY OF A SUSTAINED ESTRADIOL DELIVERY SYSTEM

Award Information
Agency:
Department of Health and Human Services
Branch
n/a
Amount:
$462,000.00
Award Year:
1988
Program:
SBIR
Phase:
Phase II
Contract:
n/a
Agency Tracking Number:
7203
Solicitation Year:
n/a
Solicitation Topic Code:
n/a
Solicitation Number:
n/a
Small Business Information
Pharmatec Inc.
Po Box 730, Alachua, FL, 32615
Hubzone Owned:
N
Socially and Economically Disadvantaged:
N
Woman Owned:
N
Duns:
n/a
Principal Investigator:
Kerry S Estes Phd
(904) 462-1210
Business Contact:
() -
Research Institution:
n/a
Abstract
STUDIES ARE PROPOSED TO EVALUATE THE FEASIBILITY OF ORAL 17BETA-ESTRADIOL (E2) ADMINISTRATION USING A NOVEL REDOX SYSTEM. THIS CHEMICAL DELIVERY SYSTEM (CDS) IS BASED ON AN INTERCONVERSION OF A LIPOPHILIC DIHYDROPYRIDINE TO A HYDROPHILIC PYRIDINIUM SALT, ANALOGOUS TO THE NADH NAD+ COENZYME SYSTEM. IT PERMITS ENHANCED ANDSUSTAINED DELIVERY OF E2 TO THE CENTRAL NERVOUS SYSTEM BY HYDROLYSIS OF A "LOCKED-IN," CHARGED PRECURSOR. SUSTAINED LEUTINIZING HORMONE (LH) INHIBITION AND INCREASED BRAIN DRUGCONCENTRATIONS WERE SHOWN IN RATS AFTER INTRAVENOUS (I.V.) E2-CDS TREATMENT. NO SERUM E2 CHANGE WAS DETECTED, INDICATING THAT E2 WAS RELEASED CENTRALLY FROM CHARGED E2-CDS AND DECREASED LH VIA CENTRAL ACTION AND/OR VIA PORTALVESSEL TRANSIT OF E2 TO THE PITUITARY. DEVELOPMENT OF AN ORAL FORMULATION FOR E2-CDS OFFERS SEVERALADVANTAGES OVER CURRENTLY AVAILABLE ESTROGEN THERAPIES INCLUDING: (1) DELIVERY OF A NATURALLY OCCURRING GONADAL STEROID, (2) DECREASED PERIPHERAL ESTROGEN ACTIVITY, AND (3) INCREASED DOSING INTERVALS. THE FIRST STUDY WILL ESTABLISH BIOAVAILABILITY OF THE DRUG. THE SECOND STUDY WILL COMPARE LH-INHIBITING ACTIVITY OF ORAL AND I.V. E2-CDS ADMINISTRATION. THE THIRD STUDY WILL EXAMINE THE TISSUE DISTRIBUTION OF DRUG AND SELECTED METABOLITES OVER TIME AFTER ORAL E2-CDS TREATMENT.

* information listed above is at the time of submission.

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