US4663349A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Rectally absorbable form of L-dopa
Assignee: Merck and Co Inc
•
Filing: 1985-12-30
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Granted: 1987-05-05
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Expires: 2005-12-30
Abstract
Abstract 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.
Inventors
- 👤 A. J. Repta
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 17:52
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/21; A61K31/215; A61P; A61P25/00; A61P43/00
Claims Analysis
Total Claims: 23
Claim 1
Independent Claim
65 words
A method of enhancing the rate of absorption of a rectally administered composition comprising rectally administering to a patient a therapeutically effective dosage amount of an ester of L-dopa having the structural formula: ##STR2## wherein R is alkyl(C 1 -C 20 ), aryl(C 6 -C 9 ), unsubstituted aralkyl(C 7 -C 20 ) or pharmaceutically acceptable organic or inorganic counterion salts and pharmaceutically acceptable excipients.
Claim 2
Independent Claim
65 words
A method of enhancing the rate of absorption of a rectally administered composition comprising rectally administering to a patient a therapeutically effective dosage amount of an ester of L-dopa having the structural formula: ##STR2## wherein R is alkyl(C 1 -C 20 ), aryl(C 6 -C 9 ), unsubstituted aralkyl(C 7 -C 20 ) or pharmaceutically acceptable organic or inorganic counterion salts and pharmaceutically acceptable excipients.
Claim 3
Dependent Claim
9 words
The method of claim 1, wherein R is alkyl.
Claim 4
Dependent Claim
22 words
The method of claim 2, wherein said alkyl is selected from the group consisting of methyl, ethyl, isopropyl, pentyl, myristyl and palmityl.
Claim 5
Dependent Claim
10 words
The method of claim 3, wherein said alkyl is ethyl.
Claim 6
Dependent Claim
9 words
The method of claim 1, wherein R is aryl.
Claim 7
Dependent Claim
18 words
The method of claim 5, wherein said aryl is selected from the group consisting of phenyl and tolyl.
Claim 8
Dependent Claim
10 words
The method of claim 6, wherein said aryl is tolyl.
Claim 9
Dependent Claim
12 words
The method of claim 1, wherein R is substituted and unsubstituted aralkyl.
Claim 10
Dependent Claim
26 words
The method of claim 8 wherein said aralkyl is selected from the group consisting of benzyl, alkoxybenzyl(C 8 -C 14 ), phenylethyl, phenylpropyl, phenylisobutyl and phenyloctyl.
Claim 11
Dependent Claim
10 words
The method of claim 9, wherein said aralkyl is phenylethyl.
Claim 12
Dependent Claim
16 words
The method of claim 1, wherein said ester of L-dopa is in microenema or suppository form.
Claim 13
Dependent Claim
62 words
A pharmaceutical composition for enhancing rectal absorption of L-dopa by administering a formulation comprising a therapeutically effective dosage amount of an ester of L-dopa of the structural formula: ##STR3## wherein R is alkyl(C 1 -C 20 ), aryl(C 6 -C 9 ), unsubstituted aralkyl(C 7 -C 20 ) or pharmaceutically acceptable organic or inorganic counterion salts and suppository base or microenema excipients.
Claim 14
Dependent Claim
62 words
A pharmaceutical composition for enhancing rectal absorption of L-dopa by administering a formulation comprising a therapeutically effective dosage amount of an ester of L-dopa of the structural formula: ##STR3## wherein R is alkyl(C 1 -C 20 ), aryl(C 6 -C 9 ), unsubstituted aralkyl(C 7 -C 20 ) or pharmaceutically acceptable organic or inorganic counterion salts and suppository base or microenema excipients.
Claim 15
Dependent Claim
9 words
The composition of claim 2, wherein R is alkyl.
Claim 16
Dependent Claim
22 words
The composition of claim 3, wherein said alkyl is selected from the group consisting of methyl, ethyl, isopropyl, pentyl, myristyl and palmityl.
Claim 17
Dependent Claim
10 words
The composition of claim 14, wherein said alkyl is ethyl.
Claim 18
Dependent Claim
9 words
The composition of claim 12, wherein R is aryl.
Claim 19
Dependent Claim
18 words
The composition of claim 16, wherein said aryl is selected from the group consisting of phenyl and tolyl.
Claim 20
Dependent Claim
10 words
The composition of claim 17, wherein said aryl is tolyl.
Claim 21
Dependent Claim
12 words
The composition of claim 12, wherein R is substituted and unsubstituted aralkyl.
Claim 22
Dependent Claim
29 words
The composition of claim 19, wherein said substituted and unsubstituted aralkyl is selected from the group consisting of benzyl, alkoxybenzyl(C 8 -C 14 ), phenylethyl, phenylpropyl, phenylisobutyl and phenyloctyl.
Claim 23
Dependent Claim
10 words
The composition of claim 20, wherein said aralkyl is phenylethyl.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1990-05-04 | 1990-11-03 | 1991-05-05 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-05-04 | 1994-11-03 | 1995-05-05 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-05-04 | 1998-11-03 | 1999-05-05 | $7700.00 | Window Closed / Lapsed |