US4462991A
Expired / Lapsed
US
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Method of increasing oral absorption of polar bioactive agents
Assignee: Interx Research Corp
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Filing: 1982-06-11
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Granted: 1984-07-31
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Expires: 2002-06-11
Abstract
Abstract A method and drug form are provided for increasing the oral absorption of polar bioactive agents such as polypeptides by the oral administration of said polar bioactive agents in a suitable pharmaceutically accepted excipient to which has been added a hydroxyaromatic acid or salt as an adjuvant thereof. The adjuvant is present in the drug form in quantities sufficient to be effective in enhancing the rate of oral absorption of the polar bioactive agents.
Inventors
- 👤 Takeru Higuchi
- 👤 Toshiaki Nishihata
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 01:41
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/70; A61K31/33; A61K31/395; A61K31/495; A61K31/505; A61K31/519; A61K31/52; A61K31/60; A61K31/66; A61K45/00; A61K45/06; A61K47/00; A61K47/06; A61K47/08; A61K47/12; A61K47/20; A61K9/00; A61K9/20; A61K9/2004; A61K9/2013; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/27
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
152 words
A method for enhancing the rate of absorption of an orally administeredpolypeptide drug having 3 or more residues of amino acid and having a molecular weight of 4000 or less into the bloodstream, said method comprising the steps of preparing a drug form capable of being orally absorbed, said drug form comprising a therapeutically effective dosage amount of said polypeptide drug and an adjuvant of the formula: ##STR4## wherein R 1 is CO 2 H,--(CH 2 )--COOH, ##STR5## SO 3 H, or a pharmaceutically acceptable salt thereof wherein R 2 is OH, H, a lower alkoxy radical, a lower alkyl radical, a halo radical, or a tri-halo lower alkyl radical, and wherein y is an integer of 1 or 2; said adjuvant being present in said drug form in a sufficient amount to be effective in enhancing said oral absorption rate and administering said drug form orally to a warm blooded animal.
Claim 2
Independent Claim
152 words
A method for enhancing the rate of absorption of an orally administeredpolypeptide drug having 3 or more residues of amino acid and having a molecular weight of 4000 or less into the bloodstream, said method comprising the steps of preparing a drug form capable of being orally absorbed, said drug form comprising a therapeutically effective dosage amount of said polypeptide drug and an adjuvant of the formula: ##STR4## wherein R 1 is CO 2 H,--(CH 2 )--COOH, ##STR5## SO 3 H, or a pharmaceutically acceptable salt thereof wherein R 2 is OH, H, a lower alkoxy radical, a lower alkyl radical, a halo radical, or a tri-halo lower alkyl radical, and wherein y is an integer of 1 or 2; said adjuvant being present in said drug form in a sufficient amount to be effective in enhancing said oral absorption rate and administering said drug form orally to a warm blooded animal.
Claim 3
Dependent Claim
19 words
The method of claim 1 wherein said polypeptide drug is bradykinin, somatostatin, calcitonin, endorphin, secretin, oxytocin, TSH or Cyclo-(N-Me-Ala-Tyr-D-Trp-Lys-Val-Phe).
Claim 4
Dependent Claim
11 words
The method of claim 2 wherein said polypeptide drug is Cyclo-(N-Me-Ala-Tyr-D-Trp-Lys-Val-Phe).
Claim 5
Dependent Claim
26 words
The method of claim 1 wherein said adjuvant is sodium salicylate, sodium 5-methoxysalicylate, sodium-5-chlorosalicylate, sodium-5-bromosalicylate, 5-trifluorosalicylic acid, 3-t-butyl-5-methylsalicylic acid, sodium-5-t-octylsalicylate, sodium-3,5-diiodosalicylate, 5-n-butyoxysalicylic acid, or, 3-t-butyl-6-methylsalicylic acid.
Claim 6
Dependent Claim
16 words
The method of claim 1 wherein the adjuvant is salicylic acid, sodium salicylate, or sodium-5-methoxy salicylate.
Claim 7
Dependent Claim
118 words
An orally administered drug form comprising a therapeutically effective amount of a polypeptide drug having 3 or more residues of amino acids and having a molecular weight of 4000 or less and an adjuvant of the Formula ##STR6## wherein R 1 is CO 2 H,--(CH 2 )--COOH, ##STR7## or SO 3 H, or a pharmaceutically acceptable sodium or calcium salt thereof wherein R 2 is OH, H, lower alkoxy radical, a lower alkyl radical, a halo radical, or a tri-halo lower alkyl radical, and wherein y is an integer of 1 or 2; said adjuvant being present in said drug form in sufficient amount to be effective in enhancing the oral absorption rate of said polar bioactive agent.
Claim 8
Dependent Claim
118 words
An orally administered drug form comprising a therapeutically effective amount of a polypeptide drug having 3 or more residues of amino acids and having a molecular weight of 4000 or less and an adjuvant of the Formula ##STR6## wherein R 1 is CO 2 H,--(CH 2 )--COOH, ##STR7## or SO 3 H, or a pharmaceutically acceptable sodium or calcium salt thereof wherein R 2 is OH, H, lower alkoxy radical, a lower alkyl radical, a halo radical, or a tri-halo lower alkyl radical, and wherein y is an integer of 1 or 2; said adjuvant being present in said drug form in sufficient amount to be effective in enhancing the oral absorption rate of said polar bioactive agent.
Claim 9
Dependent Claim
21 words
The drug form of claim 6 wherein the said polypeptide drug is bradykinin, somatostatin, calcitonin, endorphin, secretin, oxytocin, TSH or Cyclo-(N-Me-Ala-Tyr-D-Trp-Lys-Val-Phe).
Claim 10
Dependent Claim
11 words
The drug form of claim 6 wherein said polypeptide is Cyclo-(N-Me-Ala-Tyr-D-Trp-Lys-Val-Phe).
Claim 11
Dependent Claim
27 words
The drug form of claim 6 wherein said adjuvant is sodium salicylate, sodium 5-methoxysalicylate, sodium-5-chlorosalicylate, sodium-5-bromosalicylate, 5-trifluorosalicylic acid, 3-t-butyl-5-methylsalicylic acid, sodium-5-t-octylsalicylate, sodium-3,5-diiodosalicylate, 5-n-butyoxysalicylic acid, or, 3-t-butyl-6-methylsalicylic acid.
Claim 12
Dependent Claim
17 words
The drug form of claim 6 wherein the adjuvant is salicylic acid, sodium salicylate or sodium-5-methoxy salicylate.
References Cited (Backward Citations)
FR2258171A1
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-07-31 | 1988-01-30 | 1988-07-31 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-07-31 | 1992-01-30 | 1992-07-31 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-07-31 | 1996-01-30 | 1996-07-31 | $7700.00 | Window Closed / Lapsed |