Effervescent bisphosphonate formulation
First Claim
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1. An effervescent pharmaceutical formulation comprising as an active ingredient a bisphosphonate selected from the groups consisting of:
- alendronate, cimadronate, clodronate, EB-1053, etidronate, ibandronate, neridronate, olpadronate, pamidronate, risedronate, tiludronate, YH 529, zoledronate, pharmaceutically acceptable salts and esters of the foregoing, and mixtures of the foregoing; and
an acid source selected from the group consisting of;
citric acid, tartaric acid, malic acid, fumaric acid, adipic acid, succinic acid;
an anhydride of said acids;
an acid salt selected from the group consisting of sodium dihydrogen phosphate, disodium dihydrogen pyrophosphate and sodium acid sulfite; and
mixtures of the acids, anhydrides and acid salts;
a carbonate source selected from the group consisting of;
sodium bicarbonate, sodium carbonate, potassium bicarbonate, potassium carbonate, sodium sesquicarbonate, sodium glycine carbonate, and mixtures thereof;
a binder selected from the group consisting of a non-reducing sugar, polyvinyl pyrrolidone, sodium chloride, sodium benzoate and sodium sulfate;
a lubricant selected from the group consist of stearic acid salts, powdered sodium benzoate, L-leucine, sodium laurel sulfate and PEG; and
optionally, one or more additional agents selected from the group consisting of flavoring agents, colorants, and sweeteners.
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Abstract
An effervescent formulation of alendronate contains an acid source, a carbonate source, a binder, a lubricant and optionally, flavoring agents, colorants and sweeteners.
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Citations
12 Claims
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1. An effervescent pharmaceutical formulation comprising as an active ingredient a bisphosphonate selected from the groups consisting of:
- alendronate, cimadronate, clodronate, EB-1053, etidronate, ibandronate, neridronate, olpadronate, pamidronate, risedronate, tiludronate, YH 529, zoledronate, pharmaceutically acceptable salts and esters of the foregoing, and mixtures of the foregoing; and
an acid source selected from the group consisting of;
citric acid, tartaric acid, malic acid, fumaric acid, adipic acid, succinic acid;
an anhydride of said acids;
an acid salt selected from the group consisting of sodium dihydrogen phosphate, disodium dihydrogen pyrophosphate and sodium acid sulfite; and
mixtures of the acids, anhydrides and acid salts;
a carbonate source selected from the group consisting of;
sodium bicarbonate, sodium carbonate, potassium bicarbonate, potassium carbonate, sodium sesquicarbonate, sodium glycine carbonate, and mixtures thereof;
a binder selected from the group consisting of a non-reducing sugar, polyvinyl pyrrolidone, sodium chloride, sodium benzoate and sodium sulfate;
a lubricant selected from the group consist of stearic acid salts, powdered sodium benzoate, L-leucine, sodium laurel sulfate and PEG; and
optionally, one or more additional agents selected from the group consisting of flavoring agents, colorants, and sweeteners. - View Dependent Claims (2, 3, 4, 5, 6, 7)
- alendronate, cimadronate, clodronate, EB-1053, etidronate, ibandronate, neridronate, olpadronate, pamidronate, risedronate, tiludronate, YH 529, zoledronate, pharmaceutically acceptable salts and esters of the foregoing, and mixtures of the foregoing; and
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8. A formulation comprising (in mg):
Alendronate sodium 5-10 mg (in mg alendronic acid) citric acid 600-750 sodium bicarbonate 300-500 sodium carbonate 20-60 sodium benzoate 5-15 water 0-5. - View Dependent Claims (9)
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10. A formulation comprising (in mg):
Alendronate sodium
5-10(in mg alendronic acid) citric acid 450-650 sodium bicarbonate (total)
800-1150.
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11. A formulation comprising (in mg):
Alendronate sodium 2.5-10 (in mg alendronic acid) citric acid 400-800 sodium bicarbonate 1000-2000 sodium carbonate 20-80 sodium benzoate
25-175xylitol
100-300.
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12. A formulation made by the process of combining:
Alendronate sodium 2.5-10 (in mg alendronic acid) citric acid 400-800 sodium bicarbonate 1000-2000 sodium carbonate 20-80 sodium benzoate
25-175xylitol
100-300.
Specification