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Home Gene Therapy Rectally-absorbable-form-of-L-dopa

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 Rectally absorbable form of L-dopa

Details
Inventors: Repta, A. J.;
Assignee: Merck & Co., Inc. (Rahway, NJ)
Primary Examiner: Friedman; Stanley J.
Assistant Examiner:
Attorney, Agent or Firm: Polk; Manfred, Sudol; Michael C.

The invention relates to compositions and methods of enhancing rectal absorption of L-dopa via the formation of an ester prodrug and optionally with a decarboxylase inhibitor.

DETAILED DESCRIPTION What is claimed is: 1.
A method of enhancing the rate of absorption of a rectally administered composition comprising a therapeutically effective dosage amount of an ester of L-dopa having the structural formula: ##STR2## wherein R=alkyl(C.
sub.
1 -C.
sub.
20); aryl(C.
sub.
6 -C.
sub.
9); substituted and unsubstituted mono, di or polyhydroxyalkly(C.
sub.
1 -C.
sub.
20); substituted and unsubstituted aralkyl(C.
sub.
7 -C.
sub.
20) and pharmaceutically acceptable organic or inorganic counterion salts thereof and a pharmaceutically acceptable amount of a decarboxylase inhibitor selected from the group consisting of carbidopa and benserazide 2.
A method of enhancing the rate of absorption of a rectally administered composition comprising a therapeutically effective dosage amount of an ester of L-dopa having the structural formula: ##STR3## wherein R=alkyl(C.
sub.
1 -C.
sub.
20), aryl(C.
sub.
6 -C.
sub.
9), substituted and unsubstituted mono, di or polyhydroxyalkyl(C.
sub.
1 -C.
sub.
20); substituted and unsubstituted aralkyl(C.
sub.
7 -C.
sub.
20) and pharmaceutically acceptable organic or inorganic counterion salts.
wherein R=alkyl(C.
sub.
1 -C.
sub.
20), aryl(C.
sub.
6 -C.
sub.
9), substituted and unsubstituted mono, di or polyhydroxyalkyl(C.
sub.
1 -C.
sub.
20); substituted and unsubstituted aralkyl(C.
sub.
7 -C.
sub.
20) and pharmaceutically acceptable organic or inorganic counterion salts.
3.
The method of claim 1, wherein R is alkyl selected from the group consisting of methyl, ethyl, propyl, butyl and hexadecyl; aryl selected from the group consisting of phenyl and tolyl; substituted and unsubstituted mono, di or polyhydroxyalkyl selected from the group consisting of 4-hydroxybutyl, 2-hydroxypropyl, 2,3-dihydropropyl, 1,3-dihydropropyl, 6-hydroxyhexyl, 4-hydroxy-2-methoxybutyl, 5-hydroxypentyl and 2-hydroxy-4-diethylaminobutyl; or said substituted and unsubstituted aralkyl is selected from the group consisting of benzyl, o, m and p-methoxybenzyl and phenylethyl.
4.
The method of claim 3, wherein said alkyl is ethyl or isopropyl or butyl; said aryl is tolyl, said substituted and unsubstituted mono, di or polyhydroxyalkyl is 4-hydroxybutyl or 2-hydroxypropyl; and said substituted and unsubstituted aralkyl is phenylethyl or p-methoxybenzyl



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