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Last Updated: September 22, 2021

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Claims for Patent: 4,910,021

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Summary for Patent: 4,910,021
Title: Targeted enternal delivery system
Abstract:A capsule for oral administration of a pharmaceutically active ingredient contains a pharmaceutical composition comprising the active ingredient, for example, a peptide, an absorption promoter and usually, a carrier. The absorption promoter is capable of enhancing absorption of the active ingredient from the intestine into the bloodstream. The capsule is coated with a film forming composition, which film is sufficiently insoluble at a pH below 7 as to be capable of protecting the capsule and its contents from the digestive juices until the capsule reaches a region below the upper part of the intestine, whereupon the coating and capsule are capable of eroding or dissolving to release the active ingredient for absorption into the bloodstream.
Inventor(s): Davis; John D. (Grossepointe Farms, MI), Touitou; Elka (Jerusalem, IL), Rubinstein; Ardon (Jerusalem, IL)
Assignee: R. P. Scherer Corporation (Troy, MI)
Application Number:06/934,741
Patent Claims:1. An orally administered enteric coated capsule for colonic absorption of a pharmaceutical composition contained therein comprising a capsule shell, an enteric coating, and a pharmaceutical composition;

said capsule shell being of either hard or soft and of the carbohydrate or gelatin type, containing said enteric coating thereon, and said pharmaceutical composition therein;

said enteric coating comprising a film forming composition that is sufficiently insoluble at a pH below 7 as to be capable of protection said capsule and said pharmaceutical composition contained therein from digestive juices below said pH 7, said film forming composition being sufficiently soluble at a pH above 7 as to be capable of permitting the erosion or dissolution of said capsule and the release of said pharmaceutical composition contained therein;

said pharmaceutical composition comprising an active ingredient and an absorption promoter, said active ingredient being a peptide or protein that is unsuited for absorption by any portion of a gastrointestinal tract wherein the pH is below 7, said absorption promoter enhancing absorption of said active ingredient in the colon and being selected from the group consisting of organic aromatic acids, their esters, amides and pharmaceutically acceptable salts thereof:

such that when said enteric coated capsule is orally administered, said capsule passes intact through the stomach and into the intestinal tract where it continues to pass intact until it encounters an environment having a pH above 7 in the distal intestine and/or colon, said environment eroding and/or dissolving said enteric coating thereby permitting the erosion and/or dissolution of said capsule shell thereunder and the release of said pharmaceutical composition contained within said capsule, whereupon a pharmaceutically effective amount of said active ingredient is colonically absorbed from said environment.

2. A capsule according to claim 1, wherein the active ingredient is a protein.

3. A capsule according to claim 2, wherein said protein is insulin or a pharmaceutically active fragment thereof.

4. A capsule according to claim 1, wherein the said peptide or protein is selected from the group consisting of gastrin, pentagastrin, calcitonin, human growth hormone, glucagon, adrenocorticotrophic hormone, leutinising releasing hormone, enkephalin, oxycotin, parathyroid hormone, thyrotropic releasing hormone and vasopressin.

5. A capsule according to claim 1, wherein said aromatic carboxylic acid or said salt thereof is salicylic acid, a substituted salicylic acid or a pharmaceutically acceptable salt thereof.

6. A capsule according to claim 5, wherein said substituted salicylic acid is a member of the group consisting of 5-methoxysalicylic acid; 5-methylsalicylic acid; 3-methylsalicylic acid; 5-tert-octylsalicylic acid; 3-tert-butyl-6methylsalicylic acid; 3,5-diisopropylsalicylic acid; 3-tert-butyl-5-methylsalicylic acid; 5-bromosalicylic acid; 3,5-diiodosalicylic acid; 3-methoxysalicylic acid; 5-octyloxysalicylic acid; 5-butoxysalicylic acid; and 5chlorosalicylic acid; and said pharmaceutically acceptable salt thereof is a sodium salt of any of the said acids.

7. A capsule according to claim 1, wherein the absorption promoter is selected from the group consisting of homovanillic acid; 2,5-dihydroxy-benzoic acid; 2,4-dihydroxybenzoic acid; 5-methoxy-2-hydroxy-phenylsulfonic acid; guaicolsulfonic acid; 2-hydroxyphenylacetic acid; 2-hydroxyphenyl-methanesulfonic acid; 5-trifluoromethyl-2-hydroxybenzoic acid; 2-hydroxy-3-methoxy-benzoic acid; and the sodium salt of any of the said acids.

8. A capsule according to claim 2, wherein the absorption promoter is selected from the group consisting of 5-methoxysalicylic acid; salicylic acid; 2,5-dihydroxybenzoic acid; 2,4-dihydroxybenzoic acid; 3-methylsalicylic acid; 5-methylsalicylic acid; 5-tert-octylsalicylic acid; 3-tert-butyl-6-methylsalicylic acid; 3,5-diisopropylsalicylic acid; 3-tert-butyl-5-methylsalicylic acid; 5-bromosalicylic acid; 3,5-dibromosalicylic acid; 5-iodosalicylic acid; 3,5-diiodosalicylic acid; 2-hydroxy-phenylacetic acid; 5-trifluoromethyl-2-hydroxybenzoic acid; 3-methoxysalicylic acid; 5-octyloxysalicylic acid; 5-butoxysalicylic acid; 5-chlorosalicylic acid; 2-hydroxy-3-methoxybenzoic acid; and the sodium salt of any of the said acids

9. A capsule according to claim 1, wherein said capsule shell comprises a gelatin composition.

10. A capsule according to claim 1, wherein the film forming composition comprises a mixture of anionic acrylic copolymers derived from at least one monomer selected from acrylic and methacrylic acids and methyl acrylates.

11. A capsule according to claim 10, wherein the mixture of acrylic copolymers comprises a first said copolymer being derived from acrylic and methacrylic acid esters with a low content of quaternary ammonium groups, the molar ratio of the said quaternary ammonium groups: the said ester groups being about 1:40, and having a mean molecular weight of about 150,000, and a second said copolymer being derived from methacrylic acid and methyl methacrylate, the molar ratio of free carboxyl:ester groups being about 1:2, and having a mean molecular weight of about 135,000, the said first and second copolymers being present in the mixture in a proportional amount of 2:3 respectively.

12. A capsule according to claim 10, wherein the mixture of acrylic copolymers comprises a first said copolymer being derived from acrylic and methacrylic acid esters with a low content of quaternary ammonium groups, the molar ratio of the said quaternary ammonium groups: the said ester groups being about 1:40, and having a mean weight of about 150,000, a second said copolymer being derived from methacrylic acid and methyl methacrylate, the molar ratio of free carboxyl:ester groups being about 1:2, and having a mean molecular weight of about 135,000, and a third said copolymer being derived from methacrylic acid and methyl methacrylate, the molar ratio of free carboxyl:ester groups being about 1:1 and having a mean molecular weight of about 135,000, the said first, second and third copolymers being present in the mixture in a proportional amount of 1:1:3respectively.

Summary for Patent: ⤷  Free Forever Trial

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Italy77186Nov 29, 1985

Details for Patent 4,910,021

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Nps Pharms Inc NATPARA parathyroid hormone INJECTABLE;INJECTION 125511 001 2015-01-23 ⤷  Free Forever Trial R. P. Scherer Corporation (Troy, MI) 2007-03-20 RX Orphan search
Nps Pharms Inc NATPARA parathyroid hormone INJECTABLE;INJECTION 125511 002 2015-01-23 ⤷  Free Forever Trial R. P. Scherer Corporation (Troy, MI) 2007-03-20 RX Orphan search
Nps Pharms Inc NATPARA parathyroid hormone INJECTABLE;INJECTION 125511 003 2015-01-23 ⤷  Free Forever Trial R. P. Scherer Corporation (Troy, MI) 2007-03-20 RX Orphan search
Nps Pharms Inc NATPARA parathyroid hormone INJECTABLE;INJECTION 125511 004 2015-01-23 ⤷  Free Forever Trial R. P. Scherer Corporation (Troy, MI) 2007-03-20 RX Orphan search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

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