Controlled-release mucoadhesive pharmaceutical composition for the oral administration of furosemide
First Claim
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1. An oral dosage form containing an effective amount of furosemide for inducing diuresis in a human and having both control-release and mucoadhesive properties, said dosage form comprising:
- a) a multiplicity of controlled-release microgranules containing said furosemide and one or more granulation excipients having an overall Hydrophilic Lipophilic Balance (HLB) lower than 8;
said microgranules having substantially no mucoadhesive properties prior to coating with a mucoadhesive;
said granulation excipients being selected from the group consisting of saturated glycerides and polyglycolyzed glycerides;
b) a coating containing at least one mucoadhesive constituent, said coating having been applied to the surface of said microgranules to substantially completely envelop each microgranule, said coating having been applied in a manner so that it is non-swollen by water, the coating enveloping each microgranule being substantially detached from coatings enveloping other microgranules, and said coating ensuring adhesion of the coated microgranules to the mucous membrane of the gastrointestinal tract; and
c) extragranular excipients mixed with the mucoadhesive microgranules, facilitating non-aggregation and dispersion of the mucoadhesive microgranules over the mucous membrane of the gastrointestinal tract and detachment of the coating enveloping each microgranule from the coatings enveloping other microgranules.
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Abstract
Disclosed are controlled-release mucoadhesive pharmaceutical compositions for the oral administration of furosemide. This composition comprises a multiplicity of microgranules of lipophilic material which are coated with a mucoadhesive coating. This invention reduced or eliminates the diuresis peak and reduces inter-subject response variability which normally accompany conventional treatment with this drug.
101 Citations
27 Claims
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1. An oral dosage form containing an effective amount of furosemide for inducing diuresis in a human and having both control-release and mucoadhesive properties, said dosage form comprising:
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a) a multiplicity of controlled-release microgranules containing said furosemide and one or more granulation excipients having an overall Hydrophilic Lipophilic Balance (HLB) lower than 8;
said microgranules having substantially no mucoadhesive properties prior to coating with a mucoadhesive;
said granulation excipients being selected from the group consisting of saturated glycerides and polyglycolyzed glycerides;b) a coating containing at least one mucoadhesive constituent, said coating having been applied to the surface of said microgranules to substantially completely envelop each microgranule, said coating having been applied in a manner so that it is non-swollen by water, the coating enveloping each microgranule being substantially detached from coatings enveloping other microgranules, and said coating ensuring adhesion of the coated microgranules to the mucous membrane of the gastrointestinal tract; and c) extragranular excipients mixed with the mucoadhesive microgranules, facilitating non-aggregation and dispersion of the mucoadhesive microgranules over the mucous membrane of the gastrointestinal tract and detachment of the coating enveloping each microgranule from the coatings enveloping other microgranules. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 20, 21, 22, 23, 24, 25, 26, 27)
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19. A composition according to claim I wherein the granulation excipients comprise products of esterification of saturated fatty acids.
Specification