Claims
- 1. A pharmaceutical composition in the form of a dry powder comprising particles of a readily water soluble drug which when solubilized has a bitter taste and which particles are treated so that upon addition of water thereto, the particles are rendered less soluble or form an in-situ precipitate suspended in the water and are essentially free of bitter taste, wherein said drug is rendered free of bitter taste without use or need for polymer or wax coating or microencapsulation.
- 2. The pharmaceutical composition as defined in claim 1 further including one or more pH modifying agents which generate a pH environment in water to effect reduction in solubility of drug or precipitation of drug.
- 3. The pharmaceutical composition as defined in claim 1 wherein said pH modifying agent is an alkaline agent and provides a pH of the suspension greater than the drug pH in water or the pH modifying agent is an acidifying agent and provides a pH of the suspension lower than the drug pH in water
- 4. The pharmaceutical composition as defined in claim 1 wherein the drug is a quinolone-carboxylic acid derivative or a salt thereof, or a naphthyridone carboxylic acid derivative or a salt thereof.
- 5. The pharmaceutical composition as defined in claim 1 wherein the drug is
- 6. The pharmaceutical composition as defined in claim 1 wherein said drug is reduced in solubility or forms an in-situ precipitate when constituted with water.
- 7. The pharmaceutical composition as defined in claim 1 comprising a readily water soluble drug and one or more pH modifying agents which, upon addition of water to the formulation, adjust the pH of the mixture to cause reduction in solubility or in-situ precipitation of the drug, thereby rendering the drug substantially free of bitter taste.
- 8. The pharmaceutical composition as defined in claim 3 wherein said alkaline agent is one or more selected from the group consisting of L-arginine, L-lysine, sodium citrate and magnesium hydroxide, and the acidifying agent is one or more selected from the group consisting of fumaric acid, citric acid, tartaric acid, malic acid, maleic acid or succinic acid.
- 9. The pharmaceutical composition as defined in claim 8 wherein the drug is an acidic drug which forms a precipitate with an alkaline pH modifying agent or the drug is a basic drug which forms a precipitate with an acidic pH modifying agent.
- 10. The pharmaceutical composition as defined in claim 9 wherein said acidic drug is des-quinolone, norfloxacin, ciprofloxacin or ofloxacin, and the basic drug is sodium cloxacillin monohydrate, sodium dicloxicillin monohydrate or sodium ifetroban.
- 11. The pharmaceutical composition as defined in claim 1 wherein said composition further optionally includes one or more antioxidants, glidants, and/or suspending agents.
- 12. A pharmaceutical composition in the form of a drug powder formulation useful for the constitution with water into an oral suspension, said powder formulation comprising 1-cyclopropyl-8-(difluoromethoxy)-7-[(1R)-1-methyl-2,3-dihydro-1H-5-isoindolyl]-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid methanesulfonate, monohydrate sodium bisulfite, silicon dioxide, L-arginine, and sodium carboxymethylcellulose.
- 13. A pharmaceutical composition in the form of an oral suspension of a normally unpalatable drug, which suspension is substantially devoid of bitter taste, which comprises particles of a readily soluble drug which in solution has a bitter taste, and water for oral suspension, and one or more pH modifying agents mixed with the particles of drug which renders and maintains the drug in substantially insoluble form in the oral suspension, so that the bitter taste of the drug is masked without the use or need for polymer or wax coatings or microencapsulation.
- 14. The pharmaceutical composition as defined in claim 13 wherein the pH modifying agent adjusts suspension pH to cause reduction in solubility or in-situ precipitation of the drug in the suspension.
- 15. The pharmaceutical composition as defined in claim 13 comprising from about 10 mg to about 600 mg (per 5 ml of suspension) of readily water-soluble drug, from about 3 mg to about 200 mg of a pH modifying agent, and sufficient amount of water to provide 5 ml of suspension.
- 16. The pharmaceutical composition as defined in claim 13 in the form of an oral suspension comprising per 5 ml of constituted suspension, which comprises
drug in an amount within the range from about 10 mg to about 600 mg, pH modifying agent in an amount within the range from about 3 mg to about 200 mg, antioxidant in an amount within the range from about 0 to about 20 mg, glidant in an amount within the range from about 0 to about 100 mg, suspending agent in an amount within the range from about 0 to about 24 mg, and water as necessary to provide 5 ml of constituted suspension.
- 17. The pharmaceutical composition as defined in claim 16 wherein the drug is
1-cyclopropyl-8-(difluoromethoxy)-7-[(1R)-1-methyl-2,3-dihydro-1H-5-isoindolyl]-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid methanesulfonate monohydrate, the pH modifying agent is L-arginine, the antioxidant is sodium bisulfite, the glidant is silicon dioxide and the suspending agent is carboxymethyl cellulose.
- 18. A method for preparing an oral suspension of a drug which is substantially free of bitter taste, which comprises providing a readily water soluble drug which in solution has a bitter taste, mixing the drug with a one or more pH modifier capable of generating an environment in water which causes reduction in solubility or in-situ precipitation of the drug, and mixing the drug and pH modifier with water to form an oral suspension which is essentially free of bitter taste.
- 19. A method for masking the bitter or otherwise unpalatable taste of a water-soluble drug, which comprises providing a readily water-soluble drug in particulate form, mixing the drug with one or more pH modifying agents, whereby when the drug and pH modifying agents are mixed with water, the pH modifying agent provides a pH environment which renders and maintains the drug substantially insoluble in suspension so that the bitter taste of the drug is masked and/or substantially reduced.
- 20. The method as defined in claim 19 wherein said drug is des-quinolone and the pH modifying agent is selected from the group consisting of L-arginine, L-lysine, sodium citrate and magnesium hydroxide.
- 21. An oral suspension of des-quinolone
comprising des-quinolone, a pH modifying agent, optional excipients and water for suspension, the des-quinolone being rendered and maintained substantially insoluble in the water for suspension, whereby the oral suspension is substantially free of bitter taste.
Parent Case Info
[0001] This application claims priority from U.S. Provisional Application No. 60/363,704 filed Mar. 12, 2002 which is incorporated herein by reference.
Provisional Applications (1)
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Number |
Date |
Country |
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60363704 |
Mar 2002 |
US |