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US4692433A Expired / Lapsed US ⏱️ 0.0 years remaining

Method and composition for regulating serum calcium levels of mammals

Assignee: University of California
•
Filing: 1985-08-01
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Granted: 1987-09-08
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Expires: 2005-08-01
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Abstract

Abstract Method for regulating serum calcium levels in mammals by orally administering a composition which includes a polypeptide hormone such as parathyroid hormone (PTH) or calcitonin. The polypeptide hormone is protected from destruction in the digestive tract by encapsulation in liposomes. The liposome preferably includes a cationic amphiphilic agent so that the surface of the liposome has a net positive charge. Agents for enhancing the action of the liposome encapsulated hormones are also disclosed.

Inventors

  • 👤 Karl Y. Hostetler
  • 👤 Leonard J. Deftos

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-26 11:40
CPC Classifications
A; A61; A61K; A61K38/00; A61K38/16; A61K38/17; A61K38/22; A61K38/23; A61K38/29; A61K9/00; A61K9/10; A61K9/127

Claims Analysis

Total Claims: 25
Claim 1
Independent Claim 53 words
A method for regulating blood calcium levels in a mammal which comprises: orally administering to said mammal a blood calcium-regulating effective amount of a composition consisting essentially of an aqueous solution of a polypeptide hormone selected from the group consisting of parathyroid hormone and calcitonin, said polypeptide hormone being encapsulated in a liposome.
Claim 2
Independent Claim 53 words
A method for regulating blood calcium levels in a mammal which comprises: orally administering to said mammal a blood calcium-regulating effective amount of a composition consisting essentially of an aqueous solution of a polypeptide hormone selected from the group consisting of parathyroid hormone and calcitonin, said polypeptide hormone being encapsulated in a liposome.
Claim 3
Dependent Claim 13 words
A method according to claim 1 wherein said polypeptide hormone is parathyroid hormone.
Claim 4
Dependent Claim 18 words
A method according to claim 2 wherein said polypeptide hormone is the hPTH 1-34 fragment of parathyroid hormone.
Claim 5
Dependent Claim 12 words
A method according to claim 1 wherein said polypeptide hormone is calcitonin.
Claim 6
Dependent Claim 37 words
A method according to claim 1 wherein said liposome contains from about 1 to 20 molar percentage of an alkylamine having the general formula C n H 2n+1 NH 2 , where n is 12 to 20.
Claim 7
Dependent Claim 11 words
A method according to claim 5 wherein said alkylamine is stearylamine.
Claim 8
Dependent Claim 34 words
A method according to claim 1 including the additional step of administering salicylate, salicylamide, acetylsalicylate or methylsalicylate to said mammal to improve the blood calcium-regulating action of said polypeptide hormone encapsulated in said liposome.
Claim 9
Dependent Claim 23 words
A method according to claim 1 wherein said liposome is made from phospholipids selected from the group consisting of phosphatidylcholine, dimyristoylphosphatidylcholine and dipalmitoylphosphatidylcholine.
Claim 10
Dependent Claim 69 words
A composition for use in oral administration in mammals to regulate blood calcium levels, said composition consisting essentially of a polypeptide hormone selected from the group consisting of parathyroid hormone and calcitonin, said polypeptide hormone being encapsulated in a liposome, said liposome containing from about 1 to 20 molar percentage of an alkylamine having the general formula C n H 2n+1 NH 2 ,where n is 12 to 20.
Claim 11
Dependent Claim 69 words
A composition for use in oral administration in mammals to regulate blood calcium levels, said composition consisting essentially of a polypeptide hormone selected from the group consisting of parathyroid hormone and calcitonin, said polypeptide hormone being encapsulated in a liposome, said liposome containing from about 1 to 20 molar percentage of an alkylamine having the general formula C n H 2n+1 NH 2 ,where n is 12 to 20.
Claim 12
Dependent Claim 13 words
A composition according to claim 9 wherein said polypeptide hormone is parathyroid hormone.
Claim 13
Dependent Claim 12 words
A composition according to claim 9 wherein said polypeptide hormone is calcitonin.
Claim 14
Dependent Claim 20 words
A composition according to claim 9 wherein said polypeptide hormone is the hPTH 1-34 amino acid fragment of parathyroid hormone.
Claim 15
Dependent Claim 11 words
A composition according to claim 9 wherein said alkylamine is stearylamine.
Claim 16
Dependent Claim 23 words
A composition according to claim 9 wherein said liposome is made from phospholipids selected from the group consisting of phosphatidylcholine, dimyristoylyphosphatidylcholine and dipalmitoylphosphatidylcholine.
Claim 17
Dependent Claim 30 words
A method according to claim 1 including the additional step of administering aprotinin to said mammal to improve the blood calcium-regulating action of said polypeptide hormone encapsulated in said liposome.
Claim 18
Dependent Claim 13 words
A method according to claim 4 wherein said polypeptide hormone is salmon calcitonin.
Claim 19
Dependent Claim 13 words
A composition according to claim 11 wherein said polypeptide hormone is salmon calcitonin.
Claim 20
Dependent Claim 82 words
A composition for oral administration in mammals to regulate blood calcium levels, said composition comprising: a polypeptide hormone selected from the group consisting of parathyroid hormone and calcitonin, said polypeptide hormone being encapsulated in a liposome, said liposome containing from about 1 to 20 molar percentage of an alkylamine having a general formula C n H 2n+1 NH 2 , where n is 12 to 20; and a pharmaceutically acceptable aqueous buffer solution have a pH of between about 4.0 and 8.0.
Claim 21
Dependent Claim 82 words
A composition for oral administration in mammals to regulate blood calcium levels, said composition comprising: a polypeptide hormone selected from the group consisting of parathyroid hormone and calcitonin, said polypeptide hormone being encapsulated in a liposome, said liposome containing from about 1 to 20 molar percentage of an alkylamine having a general formula C n H 2n+1 NH 2 , where n is 12 to 20; and a pharmaceutically acceptable aqueous buffer solution have a pH of between about 4.0 and 8.0.
Claim 22
Dependent Claim 20 words
A composition for oral administration according to claim 18 wherein cysteine is added to said buffer solution as a preservative.
Claim 23
Dependent Claim 39 words
A composition for oral administration according to claim 18 wherein aprotinin, salicylate, salicylamide, acetylsalicylate or methylsalicylate is added to said buffer solution in an amount sufficient to improve the calcium-regulating action of said polypeptide hormone encapsulated in said liposome.
Claim 24
Dependent Claim 15 words
A composition for oral administration according to claim 18 wherein said polypeptide hormone is calcitonin.
Claim 25
Dependent Claim 14 words
A composition for oral administration according to claim 18 wherein said alkylamine is stearylamine.

References Cited (Backward Citations)

US4151276A Cited
US4241051A Cited
US4342826A Cited
US4459295A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1990-09-07 1991-03-09 1991-09-08 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1994-09-07 1995-03-09 1995-09-08 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1998-09-07 1999-03-09 1999-09-08 $7700.00 Window Closed / Lapsed

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