Oral absorption enhancement of carboxylic acid pharmaceuticals using (5-alkyl-2-oxo-1,3-dioxolen-4-yl)methyl ester group
First Claim
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1. The (5-C1 -C6 -alkyl-2-oxo-1,3-dioxolen-4-yl)methyl ester of a carboxylic acid selected from the group consisting of (+)-α
- -(fluoromethyl)histidine hydrochloride;
(6,7-dichloro-2-cyclopentyl-2-methyl-1-oxo-5-indanyloxy)acetic acid;
3-fluoro-D-alanine-2-deuterium labeled;
10,11-dihydro-5-(1-methyl-4-piperidinylidine)-5H-dibenzo (a,d)cycloheptene-3-carboxylic acid hydrochloride;
N-formimidoyl thienamycin monohydrate;
(Z)-7(R)-[(2-amino-2-carboxyethyl-thio]-2-(S)-[(2,2-dimethylcyclopropyl) carbonyl]amino-2-heptenoic acid;
N-[(S)-1-(carboxyl)-3-phenylpropyl]-L-alanyl-L-proline maleate;
N2 -[1-(S)-carboxy-3-phenyl-propyl]-L-lysyl-L-proline;
N-[1(S)-carboxy-3-phenylpropyl]-L-alanine-L-proline;
dihydroxyphosphine carboxylic acid oxide;
moxalactam;
somatostatin;
thienamycin;
cefmetazole;
cefmenoxime;
7β
-[D-(31 )-α
-(4(5)-carboxyimidazole5(4)-carboxamidophenylacetamido]-3-(4-.beta.-sulfoethylpyridinium)-methyl-3-cephem-4-carboxylic acid;
7-[D-α
-[3-(2'"'"'-amino-sulfonylanilino-4-hydroxy-5-pyrimidinyl)ureido]-p-hydrophenylacetamido]-3-[1-methytetrazo-5-yl)thiomethyl]-ceph-3-em carboxylic acid;
ceforanide;
ceftizoxime;
ceftazidime;
cefotetan;
cefsulodin;
7-[D(-)-α
-(4-hydroxy-6-methylpyridine-3-carboxyamido)-α
-(4-hydroxyphenyl-acetamido-3-(1-methyl-1H-tetrazol-5-yl)thiomethyl]-3-cephem-4-carboxylic acid;
cefatriaxon;
cefaperazone;
7β
-(D-2-amino-2-carboxyethylthio)-acetamido-7α
methoxy-3-[(1-methyl-1H-tetrazol-5-yl)thiomethyl]ceph-3-em-4-carboxyic acid;
cefotaxime;
cephalexin;
furosemide;
ibuprofen;
aspirin;
sodium levothyroxine;
fenoprofen;
7-theophyllineacetic acid;
tolmetin;
clofibric acid;
cefaclor;
pirprofen;
isoxepac;
benoxaprofen;
suprofen;
diclofenac sodium;
corprofen;
flurbiprofen; and
naprosyn.
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Abstract
The (5-R-2-oxo-1,3-dioxolen-4-yl)methyl moiety: ##STR1## wherein R is loweralkyl of 1-6 carbon atoms, especially methyl or t-butyl; when utilized as an ester on a pharmaceutical having a carboxylic acid functionality, enhances oral absorption of the pharmaceutical. This effect is applicable to a broad range of pharmaceutically active substances, including antibiotics, and antihypertensives as well as other classes of therapeutic agents.
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Citations
2 Claims
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1. The (5-C1 -C6 -alkyl-2-oxo-1,3-dioxolen-4-yl)methyl ester of a carboxylic acid selected from the group consisting of (+)-α
- -(fluoromethyl)histidine hydrochloride;
(6,7-dichloro-2-cyclopentyl-2-methyl-1-oxo-5-indanyloxy)acetic acid;
3-fluoro-D-alanine-2-deuterium labeled;
10,11-dihydro-5-(1-methyl-4-piperidinylidine)-5H-dibenzo (a,d)cycloheptene-3-carboxylic acid hydrochloride;
N-formimidoyl thienamycin monohydrate;
(Z)-7(R)-[(2-amino-2-carboxyethyl-thio]-2-(S)-[(2,2-dimethylcyclopropyl) carbonyl]amino-2-heptenoic acid;
N-[(S)-1-(carboxyl)-3-phenylpropyl]-L-alanyl-L-proline maleate;
N2 -[1-(S)-carboxy-3-phenyl-propyl]-L-lysyl-L-proline;
N-[1(S)-carboxy-3-phenylpropyl]-L-alanine-L-proline;
dihydroxyphosphine carboxylic acid oxide;
moxalactam;
somatostatin;
thienamycin;
cefmetazole;
cefmenoxime;
7β
-[D-(31 )-α
-(4(5)-carboxyimidazole5(4)-carboxamidophenylacetamido]-3-(4-.beta.-sulfoethylpyridinium)-methyl-3-cephem-4-carboxylic acid;
7-[D-α
-[3-(2'"'"'-amino-sulfonylanilino-4-hydroxy-5-pyrimidinyl)ureido]-p-hydrophenylacetamido]-3-[1-methytetrazo-5-yl)thiomethyl]-ceph-3-em carboxylic acid;
ceforanide;
ceftizoxime;
ceftazidime;
cefotetan;
cefsulodin;
7-[D(-)-α
-(4-hydroxy-6-methylpyridine-3-carboxyamido)-α
-(4-hydroxyphenyl-acetamido-3-(1-methyl-1H-tetrazol-5-yl)thiomethyl]-3-cephem-4-carboxylic acid;
cefatriaxon;
cefaperazone;
7β
-(D-2-amino-2-carboxyethylthio)-acetamido-7α
methoxy-3-[(1-methyl-1H-tetrazol-5-yl)thiomethyl]ceph-3-em-4-carboxyic acid;
cefotaxime;
cephalexin;
furosemide;
ibuprofen;
aspirin;
sodium levothyroxine;
fenoprofen;
7-theophyllineacetic acid;
tolmetin;
clofibric acid;
cefaclor;
pirprofen;
isoxepac;
benoxaprofen;
suprofen;
diclofenac sodium;
corprofen;
flurbiprofen; and
naprosyn. - View Dependent Claims (2)
- -(fluoromethyl)histidine hydrochloride;
Specification