FLASHMELT ORAL DOSAGE FORMULATION
First Claim
1. A flash-melt pharmaceutical dosage form comprising a medicament, a superdisintegrant, a dispersing agent and a binder wherein said medicament is aripiprazole and wherein said dispersing agent is calcium silicate and wherein said superdisintegrant is selected from the group of crospovidone and croscarmellose sodium.
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Accused Products
Abstract
There is provided granules for the production of flash-melt pharmaceutical oral dosage forms. In addition to one or more medicaments, the granules are composed of an excipient combination consisting of a superdisintegrant, a dispersing agent, a distributing agent, and a binder and may also include other conventional ingredients such as sweetening and flavoring agents. The subject granules are advantageous in that they are stable and can be prepared without the aid of solvents and without the need for special environments or handling. Dosage forms, especially tablets, prepared therefrom on conventional equipment disintegrate in the mouth in under about twenty five seconds.
7 Citations
22 Claims
- 1. A flash-melt pharmaceutical dosage form comprising a medicament, a superdisintegrant, a dispersing agent and a binder wherein said medicament is aripiprazole and wherein said dispersing agent is calcium silicate and wherein said superdisintegrant is selected from the group of crospovidone and croscarmellose sodium.
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18. A flash-melt pharmaceutical dosage form comprising a medicament, a superdisintegrant, a dispersing agent, a distributing agent and a binder wherein said medicament is aripiprazole and comprises not more than about 30 percent by weight of said medicament based on the total weight of said dosage form, said dispersing agent is calcium silicate having a surface area of 1.0 m2/gm to 210 m2/gm, bulk density of 0.075 g/cc to 0.90 g/cc, true density of 1.70 g/cc to 2.90 g/cc and volatile content of less than 1 percent to 14 percent w/w and which comprises from about 35 to about 45 percent by weight of said dispersing agent based on the total weight of said dosage form, said superdisintegrant is crospovidone and croscarmellose sodium, said crospovidone comprises from about 6 to about 8 percent by weight of said crospovidone based on the total weight of said dosage form and said croscarmellose sodium comprises from about 2 to about 4 percent by weight of said croscarmellose sodium based on the total weight of said dosage form and wherein said distributing agent is amorphous silica, fumed silica, diatomaceous earth, talc, kaolin or magnesium aluminum trisilicate and comprises from about 1 to about 10 percent by weight of said distributing agent based on the total weight of said dosage form.
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19. A flash-melt pharmaceutical dosage form comprising a medicament, a superdisintegrant, a dispersing agent, a distributing agent and a binder wherein said medicament is aripiprazole and comprises not more than about 30 percent by weight of said medicament based on the total weight of said dosage form, said dispersing agent is calcium silicate having a surface area of 1.0 m2/gm to 210 m2/gm, bulk density of 0.075 g/cc to 0.90 g/cc, true density of 1.70 g/cc to 2.90 g/cc and volatile content of less than 1 percent to 14 percent w/w and which comprises from about 35 to about 45 percent by weight of said dispersing agent based on the total weight of said dosage form, said superdisintegrant is crospovidone and croscarmellose sodium, wherein said crospovidone comprises about 7 percent by weight of said crospovidone based on the total weight of said dosage form and wherein said croscarmellose comprises about 3 percent by weight of said crospovidone based on the total weight of said dosage form, and wherein said distributing agent is amorphous silica, fumed silica, diatomaceous earth, talc, kaolin or magnesium aluminum trisilicate and comprises from about 10 to about 50 percent by weight of said distributing agent based on the total weight of said dosage form.
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20. A flash-melt pharmaceutical dosage form comprising a medicament, a superdisintegrant, a dispersing agent, a distributing agent and a binder wherein said medicament is aripiprazole and comprises not more than about 20 percent by weight of said medicament based on the total weight of said dosage form, said dispersing agent is calcium silicate having a surface area of 1.0 m2/gm to 210 m2/gm, bulk density of 0.075 g/cc to 0.90 g/cc, true density of 1.70 g/cc to 2.90 g/cc and volatile content of less than 1 percent to 14 percent w/w and which comprises from about 35 to about 45 percent by weight of said dispersing agent based on the total weight of said dosage form, said superdisintegrant is crospovidone and croscarmellose sodium, and wherein said crospovidone comprises about 7 percent by weight of said crospovidone based on the total weight of said dosage form and wherein said croscarmellose comprises about 3 percent by weight of said crospovidone based on the total weight of said dosage form, and wherein said distributing agent is amorphous silica, fumed silica, diatomaceous earth, talc, kaolin or magnesium aluminum trisilicate and comprises from about 10 to about 50 percent by weight of said distributing agent based on the total weight of said dosage form.
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21. A flash-melt pharmaceutical dosage form comprising a medicament, a superdisintegrant, a dispersing agent, a distributing agent and a binder wherein said medicament is aripiprazole and comprises not more than about 10 percent by weight of said medicament based on the total weight of said dosage form, said dispersing agent is calcium silicate having a surface area of 1.0 m2/gm to 210 m2/gm, bulk density of 0.075 g/cc to 0.90 g/cc, true density of 1.70 g/cc to 2.90 g/cc and volatile content of less than 1 percent to 14 percent w/w and which comprises from about 35 to about 45 percent by weight of said dispersing agent based on the total weight of said dosage form, said superdisintegrant is crospovidone and croscarmellose sodium and wherein said crospovidone comprises about 7 percent by weight of said crospovidone based on the total weight of said dosage form and wherein said croscarmellose sodium comprises about 3 percent by weight of said crospovidone based on the total weight of said dosage form.
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22. A flash-melt pharmaceutical dosage form comprising a medicament, a superdisintegrant, a dispersing agent, a distributing agent and a binder wherein said medicament is aripiprazole and comprises not more than about 5 percent by weight of said medicament based on the total weight of said dosage form, said dispersing agent is calcium silicate having a surface area of 1.0 m2/gm to 210 m2/gm, bulk density of 0.075 g/cc to 0.90 g/cc, true density of 1.70 g/cc to 2.90 g/cc and volatile content of less than 1 percent to 14 percent w/w and which comprises from about 35 to about 45 percent by weight of said dispersing agent based on the total weight of said dosage form, said superdisintegrant is crospovidone and croscarmellose sodium and wherein said crospovidone comprises about 7 percent by weight of said crospovidone based on the total weight of said dosage form and wherein said croscarmellose comprises about 3 percent by weight of said crospovidone based on the total weight of said dosage form.
Specification