Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Patent
1988-02-26
1990-07-03
Schwartz, Richard A.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
514400, 514415, 514627, 548342, 548504, 548507, 560144, 564204, 564207, A61K 31165, A61K 3123
Patent
active
049391747
ABSTRACT:
The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug.
In a preferred embodiment, the carrier is 4,7,10,13,16,19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.
REFERENCES:
T. Higuchi et al., (editors) Prodrugs as Novel Drug Delivery Systems, ACS Symposium Series, vol. 14, ACS, Washington, 1975, pp. 14-15.
S. Iwakami et al., Chem. Pharm. Bull., 34(9), 3960-3963 (1986).
Chemical Abstracts 106: 90177x (1987) [Jpn. Kokai Tokyo Koho JP 61, 204, 136, 9/10/86].
Chemical Abstracts 76: 97365c (1972), [G. Dhopeshwarkar et al., Biochem. Biophys. ACTA 1972, 255, 572-579].
Chemical Abstracts 108: 92100g (1988), [R. Spector, J. Neurochem. 1988, 50(2), 639-643].
Chemical Abstracts 100: 156839z (1984), [EP 91,694, 10/19/83].
V. Shashoua et al., J. Med. Chem. 1984, 27, 659-664.
J. Jacob et al., J. Med. Chem. 28, 106-110 (1985).
G. Hesse et al., Neuropharm., 24, 139-146 (1985).
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