CROSS-LINKED POLYALLYLAMINE TABLET CORE
A method and a composition for making a composition, tablet, or tablet core having cross-linked polyallylamine salts such as sevelamer hydrochloride, sevelamer carbonate, or colesevelam hydrochloride, that may be used for treating hyperphosphatemia or reducing cholesterol. The method involves blending of a cross-linked polyallylamine salt with a water soluble excipient, optionally with water, an additive and/or a lubricant, and further tableting the resulting blend to form tablets and tablet cores.
1 . A pharmaceutical composition useful to treat hyperphosphatemia or reduce cholesterol comprising:
at least one cross-linked polyallylamine salt, and at least one water soluble excipient that is a polyol.
2 . A method of making a tablet blend composition comprising at least one cross-linked polyallylamine salt useful to treat hyperphosphatemia and or reducing cholesterol, comprising the steps:
(a) milling the substantially dry cross-linked polyallylamine salt to a desired particle size,
(b) blending with at least one water soluble excipient,
(c) optionally blending with water after the step (a) or (b), and
(d) optionally blending the mixture obtained in step (c) with an additive and or lubricant.
3 . The method of claim 2 , wherein step (a) further comprises reducing the particle size of said cross-linked polyallylamine to less than 400 microns.
4 . The method of claim 2 , further comprising adding water to the cross-linked polyallylamine salt.
5 . The composition of claim 1 , further comprising at least one lubricant.
6 . The composition of claim 1 , further comprising at least one additive.
7 . The composition of claim 1 , further comprising water.
8 . The composition of claim 1 , wherein the cross-linked polyallylamine salt is sevelamer hydrochloride.
9 . The composition of claim 1 , wherein the cross-linked polyallylamine salt is sevelamer carbonate.
10 . The composition of claim 1 , wherein the cross-linked polyallylamine salt is colesevelam hydrochloride.
11 . The composition of claim 5 , wherein the lubricant is selected from a group consisting of stearic acid, sodium stearate, magnesium stearate, calcium stearate, zinc stearate, or sodium stearylfumarate, or a combination thereof.
12 . The composition of claim 6 , wherein the additive is selected from a group consisting of silicon dioxide, sodium chloride, or sodium carbonate, or a combination thereof.
13 . The composition of claim 1 , wherein said composition is directly compressed into a tablet or tablet core.
14 . The composition of claim 1 , wherein the amount of cross-linked polyallylamine salt is about 60% to 90% by weight.
15 . The composition of claim 1 , wherein the amount of at least one excipient is about 5% to 35% by weight.
16 . The composition of claim 1 , wherein said at least one excipient is selected from a group consisting of sorbitol, xylitol, maltitol, Mannitol, dextrose, sucrose, dextrate, Isomalt, maltose, lactitol, maltodextrin, polyethylene glycol, monosaccharide, or disaccharide.
17 . The composition of claim 13 , wherein said tablet or tablet core is coated.
18 . The method of claim 2 , wherein said at least one water soluble excipient is selected from the group consisting of sorbitol, xylitol, maltitol, Mannitol, dextrose, sucrose, dextrate, polyethylene glycol, monosaccharide, or disaccharide, or a combination thereof.
19 . The method of claim 2 , further comprising: blending the mixture of step (a) or step (b) with water.
20 . The method of claim 19 , further comprising blending the mixture obtained in step (c) with an additive or lubricant, or both.
21 . A pharmaceutical composition comprising:
at least one cross-linked polyallylamine salt useful to treat hyperphosphatemia or reducing cholesterol, and at least one water soluble excipient.
22 . The method of claim 2 , wherein said cross-linked polyallylamine salt has a water content of less than 3%.