CA2439570A1 - In-situ gel formation of pectins - Google Patents
In-situ gel formation of pectins Download PDFInfo
- Publication number
- CA2439570A1 CA2439570A1 CA002439570A CA2439570A CA2439570A1 CA 2439570 A1 CA2439570 A1 CA 2439570A1 CA 002439570 A CA002439570 A CA 002439570A CA 2439570 A CA2439570 A CA 2439570A CA 2439570 A1 CA2439570 A1 CA 2439570A1
- Authority
- CA
- Canada
- Prior art keywords
- composition
- pectic substance
- physiologically active
- active agent
- pectic
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 229920001277 pectin Polymers 0.000 title claims abstract 18
- 235000010987 pectin Nutrition 0.000 title claims abstract 14
- 239000001814 pectin Substances 0.000 title claims abstract 14
- 238000011065 in-situ storage Methods 0.000 title claims abstract 9
- 230000015572 biosynthetic process Effects 0.000 title 1
- 239000000203 mixture Substances 0.000 claims abstract 65
- 238000000034 method Methods 0.000 claims abstract 39
- AEMOLEFTQBMNLQ-BKBMJHBISA-N alpha-D-galacturonic acid Chemical compound O[C@H]1O[C@H](C(O)=O)[C@H](O)[C@H](O)[C@H]1O AEMOLEFTQBMNLQ-BKBMJHBISA-N 0.000 claims abstract 32
- 239000013543 active substance Substances 0.000 claims abstract 29
- 235000011399 aloe vera Nutrition 0.000 claims abstract 8
- 238000013268 sustained release Methods 0.000 claims abstract 6
- 239000012730 sustained-release form Substances 0.000 claims abstract 6
- 239000002562 thickening agent Substances 0.000 claims 12
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 12
- 239000006185 dispersion Substances 0.000 claims 8
- 239000000243 solution Substances 0.000 claims 8
- 241001116389 Aloe Species 0.000 claims 7
- KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 claims 6
- PYMYPHUHKUWMLA-UHFFFAOYSA-N 2,3,4,5-tetrahydroxypentanal Chemical compound OCC(O)C(O)C(O)C=O PYMYPHUHKUWMLA-UHFFFAOYSA-N 0.000 claims 6
- FHVDTGUDJYJELY-UHFFFAOYSA-N 6-{[2-carboxy-4,5-dihydroxy-6-(phosphanyloxy)oxan-3-yl]oxy}-4,5-dihydroxy-3-phosphanyloxane-2-carboxylic acid Chemical compound O1C(C(O)=O)C(P)C(O)C(O)C1OC1C(C(O)=O)OC(OP)C(O)C1O FHVDTGUDJYJELY-UHFFFAOYSA-N 0.000 claims 6
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims 6
- 102000008186 Collagen Human genes 0.000 claims 6
- 108010035532 Collagen Proteins 0.000 claims 6
- 229920002307 Dextran Polymers 0.000 claims 6
- 108010010803 Gelatin Proteins 0.000 claims 6
- 229920002230 Pectic acid Polymers 0.000 claims 6
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims 6
- 239000002671 adjuvant Substances 0.000 claims 6
- 229940072056 alginate Drugs 0.000 claims 6
- 235000010443 alginic acid Nutrition 0.000 claims 6
- 229920000615 alginic acid Polymers 0.000 claims 6
- 239000007864 aqueous solution Substances 0.000 claims 6
- 239000002775 capsule Substances 0.000 claims 6
- 229920006184 cellulose methylcellulose Polymers 0.000 claims 6
- 229920001436 collagen Polymers 0.000 claims 6
- 229960005188 collagen Drugs 0.000 claims 6
- 229960002086 dextran Drugs 0.000 claims 6
- 239000000032 diagnostic agent Substances 0.000 claims 6
- 229940039227 diagnostic agent Drugs 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- 239000000839 emulsion Substances 0.000 claims 6
- 239000000499 gel Substances 0.000 claims 6
- 229920000159 gelatin Polymers 0.000 claims 6
- 239000008273 gelatin Substances 0.000 claims 6
- 229940014259 gelatin Drugs 0.000 claims 6
- 235000019322 gelatine Nutrition 0.000 claims 6
- 235000011852 gelatine desserts Nutrition 0.000 claims 6
- 229920002674 hyaluronan Polymers 0.000 claims 6
- 229960003160 hyaluronic acid Drugs 0.000 claims 6
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 6
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 6
- FZWBNHMXJMCXLU-BLAUPYHCSA-N isomaltotriose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1OC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)[C@@H](OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C=O)O1 FZWBNHMXJMCXLU-BLAUPYHCSA-N 0.000 claims 6
- 108020004707 nucleic acids Proteins 0.000 claims 6
- 102000039446 nucleic acids Human genes 0.000 claims 6
- 150000007523 nucleic acids Chemical class 0.000 claims 6
- 239000010318 polygalacturonic acid Substances 0.000 claims 6
- 108090000765 processed proteins & peptides Proteins 0.000 claims 6
- 108090000623 proteins and genes Proteins 0.000 claims 6
- 102000004169 proteins and genes Human genes 0.000 claims 6
- 239000011780 sodium chloride Substances 0.000 claims 6
- 159000000000 sodium salts Chemical class 0.000 claims 6
- 239000003826 tablet Substances 0.000 claims 6
- 229940124597 therapeutic agent Drugs 0.000 claims 6
- 150000001768 cations Chemical class 0.000 claims 5
- 230000008020 evaporation Effects 0.000 claims 1
- 238000001704 evaporation Methods 0.000 claims 1
- 230000002459 sustained effect Effects 0.000 claims 1
- 235000002961 Aloe barbadensis Nutrition 0.000 abstract 1
- 244000186892 Aloe vera Species 0.000 abstract 1
- 238000009472 formulation Methods 0.000 abstract 1
- 238000001879 gelation Methods 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
- A61K9/0024—Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
Abstract
In-situ gelation of a pectic substance. Composition, method of preparation, and method of use of a pectin in-situ gelling formulation for the delivery and sustained release of a physiologically active agent to the body of an animal.
The pectin can be isolated from Aloe vera.
The pectin can be isolated from Aloe vera.
Claims (75)
1. A composition for the sustained release of a physiologically active agent in an animal, the composition comprising:
the physiologically active agent; and a pectic substance in an amount effective to gel in situ in the animal.
the physiologically active agent; and a pectic substance in an amount effective to gel in situ in the animal.
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, oil/water emulsion, adjuvant, tablets, or capsules.
4. The composition of claims 1, wherein the pectic substance comprises a calcium-reactive pectin.
5. The composition of claim 1, wherein the pectic substance comprises a low methoxyl pectin.
6. The composition of claim 1, wherein the pectic substance comprises a polygalacturonic acid.
7. The composition of claim 1, wherein the pectic substance comprises an Aloe pectin.
8. The composition of claim 1 further comprising a monovalent cation.
9. The composition of claim 1 further comprising a sodium salt.
10. The composition of claim 2, wherein the composition has a pH from about 2 to about 10.
11. The composition of claim 1 further comprising a thickener.
12. The composition of claim 11, wherein the thickener comprises CMC, HPMC, collagen, gelatin, dextran, hyaluronic acid, or alginate.
13. The composition of claim 1, wherein the physiologically active agent comprises a pharmacologically active substance, a therapeutic agent, a diagnostic agent, a peptide, a nucleic acid, or a protein.
14. The composition of claim 1, wherein, based on the total weight of the composition, the physiologically active agent ranges from about 0.01 % to about 90 %.
15. A composition for the sustained release of a physiologically active agent in an animal, the composition comprising:
the physiologically active agent;
a carrier;
a pectic substance in an amount effective to gel in situ in the animal.
the physiologically active agent;
a carrier;
a pectic substance in an amount effective to gel in situ in the animal.
16. The composition of claim 15, wherein the carrier comprises water, saline, buffered aqueous solution, oil/water emulsion, adjuvant, tablets, or capsules.
17. The composition of claim 15, wherein the pectic substance comprises a calcium-reactive pectin.
18. The composition of claim 15, wherein the pectic substance comprises a low methoxyl pectin.
19. The composition of claim 15, wherein the pectic substance comprises a polygalacturonic acid.
20. The composition of claim 15, wherein the pectic substance comprises an Aloe pectin.
21. The composition of claim 15 further comprising a monovalent cation.
22. The composition of claim 15 further comprising a sodium salt.
23. The composition of claim 15, wherein the composition has a pH from about 2 to about 10.
24. The composition of claim 15 further comprising a thickener.
25. The composition of claim 24, wherein the thickener comprises CMC, HPMC, collagen, gelatin, dextran, hyaluronic acid, or alginate.
26. The composition of claim 15, wherein the physiologically active agent comprises a pharmacologically active substance, a therapeutic agent, a diagnostic agent, a peptide, a nucleic acid, or a protein.
27. A composition for the sustained release of a physiologically active agent in an animal, the composition comprising:
the physiologically active agent;
a carrier;
an Aloe pectic substance in an amount effective to gel in situ in the animal.
the physiologically active agent;
a carrier;
an Aloe pectic substance in an amount effective to gel in situ in the animal.
28. The composition of claim 27, wherein the carrier comprises water, saline, buffered aqueous solution, oil/water emulsion, adjuvant, tablets, or capsules.
29. The composition of claim 27, wherein the pectic substance comprises a calcium-reactive pectin.
30. The composition of claim 27, wherein the Aloe pectic substance comprises a low methoxyl pectin or a polygalacturonic acid.
31. The composition of claim 27 further comprising a monovalent cation.
32. The composition of claim 27 further comprising a sodium salt.
33. The composition of claim 27, wherein the composition has a pH of from about 2 to about 10.
34. The composition of claim 27 further comprising a thickener.
35. The composition of claim 34, wherein the thickener comprises CMC, HPMC, collagen, gelatin, dextran, hyaluronic acid, or alginate.
36. The composition of claim 27, wherein the physiologically active agent comprises a pharmacologically active substance, a therapeutic agent, a diagnostic agent, a peptide, a nucleic acid, or a protein.
37. A method for preparing a composition for the sustained release of a physiologically active agent in an animal, comprising:
dissolving a pectic substance in a carrier to give a pectic solution or dispersion, wherein the amount of the pectic substance is effective to gel in situ in the animal;
adding the physiologically active agent to the pectic solution or dispersion to give the composition.
dissolving a pectic substance in a carrier to give a pectic solution or dispersion, wherein the amount of the pectic substance is effective to gel in situ in the animal;
adding the physiologically active agent to the pectic solution or dispersion to give the composition.
38. The method of claim 37, wherein the carrier comprises water, saline, buffered aqueous solution, oil/water emulsion, adjuvant, tablets, or capsules.
39. The composition of claim 37, wherein the pectic substance comprises a calcium-reactive pectin.
40. The composition of claim 37, wherein the pectic substance comprises a low methoxyl pectin.
41. The method of claim 37, wherein the pectic substance comprises a polygalacturonic acid.
42. The method of claim 37, wherein the pectic substance comprises an Aloe pectin.
43. The method of claim 37 further comprising adding a monovalent cation to the composition.
44. The method of claim 37 further comprising adding a sodium salt to the composition.
45. The method of claim 37, wherein the composition has a pH of from about 2 to about 10.
46. The method of claim 37 further comprising adding a thickener to the composition
47. The method of claim 46, wherein the thickener comprises CMC, HPMC, collagen, gelatin, dextran, hyaluronic acid, or alginate.
48. The method of claim 37, wherein the physiologically active agent comprises a pharmacologically active substance, a therapeutic agent, a diagnostic agent, a peptide, a nucleic acid, or a protein.
49. The method of claim 37, wherein, based on the total weight of the composition, the physiologically active agent ranges from about 0.01 % to about 90 %.
50. A method for preparing a relatively dry composition for the sustained release of a physiologically active agent in an animal, comprising:
dissolving a mixture of a pectic substance and a physiologically active agent in a carrier to give a solution of dispersion, wherein the amount of the pectic substance is effective to gel in situ in the animal;
removing volatile components in the carrier to give the relatively dry composition.
dissolving a mixture of a pectic substance and a physiologically active agent in a carrier to give a solution of dispersion, wherein the amount of the pectic substance is effective to gel in situ in the animal;
removing volatile components in the carrier to give the relatively dry composition.
51. The method of claim 50, wherein the carrier comprises water, saline, buffered aqueous solution, oil/water emulsion, adjuvant, tablets, or capsules.
52. The method of claim 50, wherein the pectic substance comprises a calcium-reactive pectin.
53. The method of claim 50, wherein the pectic substance comprises a low methoxyl pectin.
54. The method of claim 50, wherein the pectic substance comprises a polygalacturonic acid
55. The method of claim 50, wherein the pectic substance comprises an Aloe pectin.
56. The method of claim 50 further comprising adding a monovalent cation to the solution or dispersion.
57. The method of claim 50 further comprising adding a sodium salt to the solution or dispersion.
58. The method of claim 50 further comprising adding a thickener to the solution or dispersion.
59. The method of claim 58, wherein the thickener comprises CMC, HPMC, collagen, gelatin, dextran, hyaluronic acid, or alginate.
60. The method of claim 50, wherein the physiologically active agent comprises a pharmacologically active substance, a therapeutic agent, a diagnostic agent, a peptide, a nucleic acid, or a protein.
61. The method of claim 50, wherein, based on the total weight of the composition, the physiologically active agent ranges from about 0.01 % to about 90 %.
62. The method of claim 50, wherein the step of removing volatile components of the carrier comprises evaporation.
63. A method for sustained releasing a physiologically active agent in an animal, comprising:
dissolving a pectic substance in a carrier to give a pectic solution or dispersion, wherein the amount of the pectic substance is effective to gel in situ in the animal;
adding the physiologically active agent to pectic solution or dispersion to give a composition;
administering the composition to the animal.
dissolving a pectic substance in a carrier to give a pectic solution or dispersion, wherein the amount of the pectic substance is effective to gel in situ in the animal;
adding the physiologically active agent to pectic solution or dispersion to give a composition;
administering the composition to the animal.
64. The method of claim 63, wherein the carrier comprises water, saline, buffered aqueous solution, oil/water emulsion, adjuvant, tablets, or capsules.
65. The method of claim 63, wherein the pectic substance comprises a calcium-reactive pectin.
66. The method of claim 63, wherein the pectic substance comprises a low methoxyl pectin.
67. The method of claim 63, wherein the pectic substance comprises a polygalacturonic acid.
68. The method of claim 63, wherein the pectic substance comprises an Aloe pectin.
69. The method of claim 63 further comprising adding a monovalent ration to the composition.
70. The method of claim 63 further comprising adding a sodium salt to the composition.
71. The method of claim 63, wherein the composition has a pH of from about 2 to about 10.
72. The method of claim 63 further comprising adding a thickener to the composition
73. The method of claim 72, wherein the thickener comprises CMC, HPMC, collagen, gelatin, dextran, hyaluronic acid, or alginate.
74. The method of claim 63, wherein the physiologically active agent comprises a pharmacologically active substance, a therapeutic agent, a diagnostic agent, a peptide, a nucleic acid, or a protein.
75. The method of claim 63, wherein, based on the total weight of the composition, the physiologically active agent ranges from about 0.01 % to about 90 %.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US09/795,897 | 2001-02-28 | ||
US09/795,897 US6777000B2 (en) | 2001-02-28 | 2001-02-28 | In-situ gel formation of pectin |
PCT/US2002/005974 WO2002067897A2 (en) | 2001-02-28 | 2002-02-27 | In-situ gel formation of pectins |
Publications (2)
Publication Number | Publication Date |
---|---|
CA2439570A1 true CA2439570A1 (en) | 2002-09-06 |
CA2439570C CA2439570C (en) | 2012-04-24 |
Family
ID=25166729
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CA2439570A Expired - Fee Related CA2439570C (en) | 2001-02-28 | 2002-02-27 | In-situ gel formation of pectins |
Country Status (8)
Country | Link |
---|---|
US (1) | US6777000B2 (en) |
EP (1) | EP1372606A2 (en) |
JP (2) | JP2005506284A (en) |
KR (1) | KR20030088440A (en) |
CN (1) | CN1256080C (en) |
AU (1) | AU2002306603A1 (en) |
CA (1) | CA2439570C (en) |
WO (1) | WO2002067897A2 (en) |
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2001
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2002
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2008
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US20020119941A1 (en) | 2002-08-29 |
JP2005506284A (en) | 2005-03-03 |
CN1256080C (en) | 2006-05-17 |
JP2009029824A (en) | 2009-02-12 |
CN1531419A (en) | 2004-09-22 |
US6777000B2 (en) | 2004-08-17 |
CA2439570C (en) | 2012-04-24 |
WO2002067897A2 (en) | 2002-09-06 |
AU2002306603A1 (en) | 2002-09-12 |
EP1372606A2 (en) | 2004-01-02 |
WO2002067897A3 (en) | 2003-05-01 |
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