Prodrugs for oral administration containing taxol or substituted

Details Prodrugs for oral administration containing taxol or substituted Prodrugs for oral administration containing taxol or substituted

1994-12-14

1996-01-16

Naff, David M.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

549430, 549510, 514 43, 514 50, 514885, 514 12, 514 2, 514 18, 514192, 514199, 514200, A01N 4302, A01N 4304, C07D30700, C07D30500

Patent

active

054848091

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 zaxol and taxol-related compounds. Potency of the lipid prodrugs is comparable to that of the corresponding nonderivatized drugs. In a preferred embodiment, taxol or substituted taxol is covalently bound to a phospholipid.

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