Process for removing bile salts from a patient and alkylated compositions therefor
View Patent ↗The invention relates to a method for reducing serum cholesterol in a patient in need thereof and alkylated and crosslinked poly(allylamine) polymers useful in the method. The alkylated and crosslinked poly(allylamine) polymers are crosslinked with epichlorohydrin and comprise at least some n-decyl substituted nitrogen atoms and at least some hexyltrimethyl ammonium substituted nitrogen atoms.
1. An alkylated and crossliniced poly(allylamine)polymer salt, comprising:
(a) at least some n-decyl substituted nitrogen attoms; and
(b) at least some hexyltrimethylammonium substitutcd nitrogen atoms, wherein the hexyltrimethylammonium has the structural formula —CH 2 (CH 2 ) 5 N − (CH 3 ) 3 and
wherein the alkylated and crosslinked poly(allylamine)polymer salt is crosslinked with epichlorohydrin.
2. The alkylated and crosslinked poly(allylamine)polymer salt of claim 1 , having halide counterions.
3. The alkylated and crosslinked poly(allylamine)polymer salt of claim 2 , having countetons selected from the group consisting of Cl − ; Br − , and mixtures. thereof.
4. The alkylated and crosslinked poly(allylamine)polymer salt of claim 3 , wherein the epichlorohydrin crosslinks between about 0.5 and 20% of the amine groups of the alkylated and crosslinked poly(allylamine)polymer salt.
5. The alkylated and crosslinked poly(allylamine)polymer salt of claim 4 , having halide counterions.
6. The alkylated and crosslinked poly(allylamine)polymer salt of claim 5 , having counterions selected from the group consisting of Cl − , Br − , and mixtures thereof.
7. A pharmaceutical composition comprising:
(a) a pharmaceutically acceptable carrier, and
(b) an alkylated and crosslinked poly(allylamine)polymer salt including:
(i) at least some n-decyl substituted nitrogen atoms; and
(ii) at least some hexyltrimethylammonium substituted nitrogen atoms, wherein the hexyltrimethylammonium has the structural formula —CH 2 (CH 2 ) 5 N − (CH 3 ) 3 and
wherein the alkylated and crosslinked poly(allylamine)polymer salt is crosslinked with epichlorohydrin.
8. The pharmaceutical composition of claim 7 , wherein the alkylated and crosslinked poly(allylamine)polymer salt has halide counterions.
9. The pharmaceutical composition of claim 8 , wherein the alkylated and crosslinked poly(allylamine)polymer salt has counterions selected from the group consisting of Cl − , Br − , and mixtures thereof.
10. The pharmaceutical composition of claim 7 , wherein the epichlorohydrin crosslinks between about 0.5 and 20% at the amine groups of the alkylated and crosslinked poly(allylamine)polymer salt.
11. The pharmaceutical composition of claim 10 , wherein the alkylated and crosslinKed poly(allylamine)polymer salt has halide counterions.
12. The pharmaceutical composition of claim 11 , wherein the alkylated and crosslinked poly(allylamine)polymer salt has counterions selected from the group consisting of Cl − , Br − , and mixtures thereof.
13. A method of reducing the serum cholesterol of a patient, comprising orally administering to said patient a therapeutically effective amount of an alkylated and crosslinked poly(allylamine)polymer salt, comprising;
(a) at least some n-decyl substituted nitrogen atoms; and
(b) at least some hexyltrimethylammonium substituted nitrogen atoms, wherein the hexyltrimethylammonium has the structural formula —CH 2 (CH 2 ) 5 N − (CH 3 ) 3 and
wherein the alkylated and crosslinked poly(allylamine)polymer salt is crosslinked with epichlorohydrin.
14. The method of claim 13 , wherein the alkylated and crosslinked poly(allylamine)polymer has halide counterions.
15. The method of claim 14 , wherein the alkylated and crosslinked poly(allylamine)polymer has counterions selected from the group consisting of Cl − ; Br − , and mixtures thereof.
16. The method of claim 13 , wherein the epichlorohydrin crosslinks between about 0.5 and 2% of the amine groups of the alkylated and crosslinked poly(allylamine)polymer salt.
17. The method of claim 6 , wherein the alkylated and crosslinked poly(allylamine)polymer has halide counterions.
18. The method of claim 17 , wherein the alkylated and crosslinked poly(allylamine)polymer has counterions selected from the group consisting of Cl − , Br − , and mixtures thereof.