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US 6,642,276 B2Granted
Controlled release macrolide pharmaceutical formulations
AssigneeM/S Ind-Swift Limited
InventorHardeep Wadhwa
Life of this patent
Estimating the term…
Abstract
Disclosed is an oral controlled release macrolide pharmaceutical formulation. In a preferred embodiment, the formulation comprises a citrate salt of a preferred macrolide, clarithromycin. Also disclosed are methods for preparing, isolating and characterizing soluble and stable citrate salt of macrolides and use thereof in all solid dosage forms of macrolides.
Claims41
A controlled release pharmaceutical formulation comprising,
- a macrolide citrate salt;
- at least one hydrophilic polymer;
- a binder,
- a filler;
- and
- a lubricant;
- wherein said macrolide citrate salt is obtained by:
- dispersing a macrolide in an organic solvent;
- adding an aqueous solution comprising an equimolar amount of citric acid to said macrolide;
- and
- evaporating the organic solvent.
8 more elements
A method for producing a controlled release pharmaceutical formulation of macrolide citrate salt comprising:
- mixing multiple components comprising a macrolide citrate salt, a filler, and at least one hydrophilic polymer to form a first mixture of said multiple components;
- granulating the mixture in the presence of a binder to form granules which are dried and properly sized;
- and
- lubricating the granules to form an oral controlled release solid dosage formulation;
- wherein said granulating step is performed slowly, such that a solvent or a mixture of solvent and binder is added in small amounts to the first mixture.
2 more elements
A method of preparing a macrolide citrate salt, comprising:
- dispersing a macrolide in an organic solvent;
- adding an aqueous solution comprising citric acid to said macrolide organic solution with stirring to form a mixture;
- and
- removing the organic solvent from the mixture to form a macrolide ciliate salt;
- wherein the citric acid and macrolide are present in substantially equimolar quantities.
2 more elements
Dependencies are inferred from the claim text.