CA2439570A1 - In-situ gel formation of pectins - Google Patents

In-situ gel formation of pectins Download PDF

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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
Application number
CA002439570A
Other languages
French (fr)
Other versions
CA2439570C (en
Inventor
Yawei Ni
Kenneth M. Yates
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Carrington Laboratories Inc
Original Assignee
Carrington Laboratories, Inc.
Yawei Ni
Kenneth M. Yates
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Carrington Laboratories, Inc., Yawei Ni, Kenneth M. Yates filed Critical Carrington Laboratories, Inc.
Publication of CA2439570A1 publication Critical patent/CA2439570A1/en
Application granted granted Critical
Publication of CA2439570C publication Critical patent/CA2439570C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A61K9/0024Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial 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.

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.
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.
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.
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.
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.
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.
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 %.
CA2439570A 2001-02-28 2002-02-27 In-situ gel formation of pectins Expired - Fee Related CA2439570C (en)

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

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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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