Method of converting a drug to an orally available form by coval

Details Method of converting a drug to an orally available form by coval Method of converting a drug to an orally available form by coval

1992-12-16

1995-05-02

Naff, David M.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

514 50, 514885, 514 12, 514 2, 514 18, 514192, 514199, 514200, A01N 4304, A01N 3718, A61K 3700, A61K 3143

Patent

active

054119472

ABSTRACT:
The oral delivery of many classes of drugs is facilitated by converting drugs having suitable functional groups to 1-O-alkyl-, 1-O-acyl-, 1-S-acyl, and 1-S-alkyl-sn-glycero-3-phosphate derivatives. The method confers the ability to be absorbed through the digestive tract to drugs that are not orally bioavailable in the non-derivatized state, and enhances the effectiveness of drugs that are poorly absorbed or rapidly eliminated. The method provides orally bioavailable lipid prodrugs of pharmaceutical compounds having diverse physiological activities, including anticancer and antiviral agents, anti-inflammatory agents, antihypertensives and antibiotics. Potency of the lipid prodrugs is comparable to that of the corresponding non-derivatized drugs.

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