Lipid prodrugs for oral administration

Details Lipid prodrugs for oral administration Lipid prodrugs for oral administration

1995-06-07

1998-04-28

Lankford, Jr., Leon B.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

514 43, 514 45, 544276, 558152, 558169, C07H 1900, A01N 1304, A61K 3170

Patent

active

057445923

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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