Water-soluble films comprising low-viscosity alginates
A film comprising as a film-forming agent an alginate salt of monovalent cation or a mixture of alginate salts containing at least one alginate salt of monovalent cation, the film-forming agent being such that a 10% aqueous solution thereof at a temperature of 20° C. has a viscosity of 100-1000 mPas, as measured at a shear rate of 20 rpm by use of a Brookfield viscometer with a spindle No. 2. A method of preparing the film. The film is useful for delivery of active ingredients to a mammal.
1. A bioadhesive water-soluble film comprising, as a film-forming agent, an alginate salt of a monovalent cation or a mixture of alginate salts containing at least one alginate salt of a monovalent cation, the film-forming agent having a mean guluronate (G) content of from 50% to 85% by weight, a mean mannuronate (M) content of from 15% to 50% by weight, a mean molecular weight of from 30,000 g/mol to 90,000 g/mol and being such that an aqueous solution of 10% thereof at a temperature of 20° C. has a viscosity of 100 mPas to 1000 mPas, as measured at a shear rate of 20 rpm by use of a Brookfield viscometer with a spindle No. 2.
2. The bioadhesive film according to claim 1 , wherein the monovalent cation is selected from the group consisting of Na + , K + and NH 4 + .
3. The bioadhesive film according to claim 1 , wherein the alginate salt of monovalent cation comprises from 25% to 35% by weight of β-D mannuronate.
4. The bioadhesive film according to claim 1 , wherein the alginate salt of monovalent cation comprises from 65% to 75% by weight of α-D guluronate.
5. The bioadhesive film according to claim 1 , further comprising a plasticizer.
6. The bioadhesive film according to claim 1 , further comprising a filler.
7. The bioadhesive film according to claim 1 , having a thickness of 0.1 mm to 2 mm.
8. The bioadhesive film according to claim 1 , when in contact with a moist surface, dissolves within a time period of less than 2 minutes.
9. The bioadhesive film according to claim 1 , further comprising at least one biologically active substance.
10. The bioadhesive film according to claim 1 , further comprising at least one therapeutically active substance.
11. The bioadhesive film according to claim 1 , further comprising at least one biologically active substance and/or therapeutically active substance selected from the group consisting of antimicrobial agents, histamine-2-receptor antagonists, proton pump inhibitors, serotonin receptor antagonists, anti-inflammatory substances, CNS-acting agents, peptides, proteins, nicotine, nicotine analogues and analgesics.
12. The bioadhesive film according to claim 11 , wherein the biologically and/or therapeutically active substance is at a concentration from 0.000001% by weight to 85% by weight of the total weight of the composition.
13. The bioadhesive film according to claim 11 , wherein the biologically and/or therapeutically active substance is at a concentration from 30% by weight to 80% by weight of the total weight of the composition.
14. The bioadhesive film according to claim 11 , wherein the biologically and/or therapeutically active substance is at a concentration from 50% by weight to 70% by weight of the total weight of the composition.
15. The bioadhesive film according to claim 1 , further comprising at least one pharmaceutically and/or physiologically acceptable additive.
16. The bioadhesive film according to claim 1 , wherein said bioadhesive film is a single dosage unit.
17. A method of manufacturing a bioadhesive water-soluble film, said method comprising: a) dissolving a film-forming agent in a solvent or a mixture of solvents to obtain a liquid composition wherein the film-forming agent comprises an alginate salt of a monovalent cation or a mixture of alginate salts containing at least one alginate salt of a monovalent cation, the film-forming agent having a mean guluronate (G) content of from 50% to 85% by weight, a mean mannuronate (M) content of from 15% to 50% by weight, a mean molecular weight of from 30,000 g/mol to 90,000 g/mol and being such that an aqueous solution of 10% thereof at a temperature of 20° C. has a viscosity of 100 mPas to 1000 mPas, as measured at a shear rate of 20 rpm by use of a Brookfield viscometer with a spindle No. 2; b) distributing the composition onto a solid surface; and c) permitting the composition to dry on the surface.
18. The method according to claim 17 , wherein the monovalent cation is selected from Na+, K + and NH 4 + .
19. The method according to claim 17 , wherein the alginate salt of monovalent cation comprises from 25% to 35% by weight β-D mannuronate.
20. The method according to claim 17 , wherein the alginate salt of monovalent cation comprises from 65 to 75% by weight of α-D guluronate.
21. The method according to claim 17 , wherein the composition further comprises a plasticizer.
22. The method according claim 17 , wherein the composition further comprises a filler.
23. The method according to claim 17 , wherein the composition further comprises at least one biologically active substance.
24. The method according to claim 17 , wherein the composition further comprises at least one therapeutically active substance.
25. The method according to claim 17 , wherein the composition further comprises at least one pharmaceutically and/or physiologically acceptable additive.
26. The method according to claim 17 , wherein the composition further comprises at least one biologically active substance selected from the group consisting of antimicrobial agents, histamine-2-receptor antagonists, proton pump inhibitors, serotonin receptor antagonists, anti-inflammatory substances, CNS-acting agents, peptides, proteins, nicotine, nicotine analogues and analgesics.
27. The method according to claim 17 , wherein the composition further comprises at least one biologically and/or therapeutically active substance at a concentration from 0.000001% by weight to 85% by weight of the total weight of the composition.
28. The method according to claim 17 wherein the composition further comprises at least one biologically and/or therapeutically active substance at a concentration from 30% by weight to 80% by weight of the total weight of the composition.
29. The method according to claim 17 , wherein the composition further comprises at least one biologically and/or therapeutically active substance at a concentration is from 50% by weight to 70% by weight of the total weight of the composition.
30. The method according to claim 17 , further comprising preparing the bioadhesive film in dosage units.
31. The method according to claim 17 , further comprising administering to a mammal said bioadhesive film.
32. A bioadhesive water-soluble film prepared by a method comprising:
a) dissolving a film-forming agent in a solvent or a mixture of solvents to obtain a liquid composition, wherein the film-forming agent comprises an alginate salt of a monovalent cation or a mixture of alginate salts containing at least one alginate salt of a monovalent cation, the film-forming agent having a mean guluronate (G) content of from 50% to 85% by weight, a mean mannuronate (M) content of from 15% to 50% by weight, a mean molecular weight of from 30,000 g/mol to 90,000 g/mol and being such that an aqueous solution of 10% thereof at a temperature of 20° C. has a viscosity of 100 mPas to 1000 mPas, as measured at a shear rate of 20 rpm by use of a Brookfield viscometer with a spindle No. 2;
b) distributing the composition onto a solid surface; and
c) permitting the composition to dry on the surface.