Pharmacological compositions comprising pectins having high molecular weights and low degrees of methoxylation
View Patent ↗The inventions disclosed herein relate to compositions for the sustained release of pharmacological agents comprising pectins having a combination of both a high molecular weight and a low degree of methoxylation.
1. A composition for the sustained release of a pharmacological agent comprising:
at least one pharmacological agent; and
a pectin having a degree of methylation of less than 10% and an average molecular weight higher than 1×10 6 Daltons.
2. The composition of claim 1 further comprising a carrier.
3. The composition of claim 2 wherein the carrier comprises water, saline, buffered aqueous solution, emulsion, or adjuvant.
4. The composition of claim 1 , wherein the pectin is a polygalacturonic acid.
5. The composition of claim 1 , wherein the pectin is an Aloe pectin.
6. The composition of claim 1 , wherein the concentration of the pectin is from about 0.5 mg/ml to about 40 mg/ml.
7. The composition of claim 1 wherein the pectin, when dissolved in 0.1 M NaCl at a concentration of 0.0005–0.2% (w/v), has an intrinsic viscosity greater than 550 ml/g.
8. The composition of claim 1 wherein the pectin has a galacturonic acid content of greater than 70% by weight.
9. The composition of claim 1 wherein the pectin has a rhamnose content from about 3% to about 15% by mole.
10. The composition of claim 1 wherein the pectin has a galacturonic acid content of greater than 70% by weight and a rhamnose content from about 3% to about 6% by mole.
11. The composition of claim 1 wherein the pectin comprises 3-OMe Rhamnose at greater than about 0.1% by mole.
12. The composition of claim 1 wherein the pharmacological agent is a protein.
13. The composition of claim 1 wherein the pharmacological agent is a vaccine.
14. The composition of claim 1 wherein the pharmacological agent is an antigen or antibody.
15. The composition of claim 1 further comprising calcium cations.
16. The composition of claim 15 in the form of a bead that encapsulates the pharmacological agent.
17. The composition of claim 1 further comprising an aqueous carrier, wherein the pectin is dissolved in the aqueous carrier to form a first solution, and wherein the pectin is present in an amount sufficient to form gel beads by dropping the first solution into a second solution comprising calcium cations.
18. The composition of claim 1 further comprising an aqueous carrier, wherein the pectin is dissolved in the aqueous carrier to form a solution, and wherein the pectin is present at a concentration from about 10 mg/ml to about 15 mg/ml.
19. The composition of claim 1 further comprising an aqueous carrier, wherein the pectin is dissolved in the aqueous carrier to form a solution, and wherein the pectin is present at a concentration from about 1 mg/ml and about 5 mg/ml.
20. The composition of claim 1 further comprising an aqueous carrier and a monovalent cation salt, in the form of a solution.
21. The composition of claim 20 wherein the pectin is present at a concentration from about 1 mg/ml and about 5 mg/ml.
22. The composition of claim 20 in the form of a gel.
23. The composition of claim 20 wherein the monovalent cation salt is a sodium salt, and the composition does not comprise a divalent cation salt.
24. The composition of claim 23 in the form of a gel.
25. The composition of claim 1 wherein the pectin has a rhamnose content from about 2% to about 15% by mole.
26. A composition for the sustained release of a pharmacological agent comprising:
at least one pharmacological agent; and
a pectin having a degree of methylation of about 17.5% or less and an average molecular weight about 6.08×10 5 Daltons or higher.