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US3961041A Expired / Lapsed US ⏱️ 0.0 years remaining

Effervescent enteric coated L-dopa formulation and method of using the same

Assignee: Interx Research Corp
•
Filing: 1975-04-10
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Granted: 1976-06-01
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Expires: 1995-04-10
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Abstract

Abstract Therapeutic levels of L-DOPA are achieved by orally administering a pharmaceutical effervescent-enteric coated tablet comprising:

Inventors

  • 👤 Kenji Nishimura
  • 👤 Mikio Arai
  • 👤 Kunihiro Sasahara
  • 👤 Takashi Nitanai

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 04:18
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/21; A61K31/215; A61K31/185; A61K31/19; A61K31/195; A61K38/00; A61K38/04; A61K9/00; A61K9/0002; A61K9/0007; A61K9/20; A61K9/28; A61K9/2806; A61K9/2833; A61K9/2853; A61K9/286; A61K9/2866

Claims Analysis

Total Claims: 9
Claim 1
Independent Claim 225 words
A pharmaceutical effervescent enteric-coated tablet for oral administration to a warm-blooded animal which permits release and absorption of L-DOPA in the area of the upper portion of the small intestine thereof comprising a tableted admixture of: a. a member selected from the group consisting of L-DOPA, 3,4-diacetyloxy-L-phenylalanine or a pharmaceutically acceptable acid addition salt thereof, 3,4-dipivalyloxy-L-phenylalanine or a pharmaceutically acceptable acid addition salt thereof, 3,4-dihydroxy-L-phenylalanine methyl ester or a pharmaceutically acceptable acid addition salt thereof, 3,4-diacetyloxy-L-phenylalanine methyl ester or a pharmaceutically acceptable acid addition salt thereof, 3,4-dihydroxy-L-phenylalanine benzyl ester or a pharmaceutically acceptable acid addition salt thereof, 3,4-diacetyloxy-L-phenylalanine benzyl ester or a pharmaceutically acceptable acid addition salt thereof, glycyl-3,4-diacetyloxy-L-phenylalanine methyl ester or a pharmaceutically acceptable acid addition salt thereof, 3,4-dipivalyloxy-N(1-methyl-2-acetylvinyl)-L-phenylalanine pivalyloxy methyl ester, the alkali metal salt of 3,4-dipivalyloxy-N(1-methyl-2-acetylvinyl)-L-phenylalanine, the alkali metal salt of 3,4-diacetyloxy-N(1-methyl-2-acetylvinyl)-L-phenylalanine, N-formyl-3,4-dipivalyloxy-L-phenylalanine, N-formyl-3,4-dipivalyloxy-L-phenylalanine-pivalyloxymethyl ester, N-formyl-3,4-diacetyloxy-L-phenylalanine, the alkali metal salt of N-formyl-3,4-diacetyloxy-L-phenylalanine, glycyl-3,4-diacetyloxy-L-phenylalanine or a pharmaceutically acceptable acid addition salt thereof, 3,4-diacetyloxy-L-phenylalanylglycine or a pharmaceutically acceptable acid addition salt thereof, 3,4-dihydroxy-L-phenylalanyl-3,4-dihydroxy-L-phenylalanine or a pharmaceutically acceptable acid addition salt thereof, 3,4-diacetyloxy-L-phenylalanyl-3,4-diacetyloxy-L-phenylalanine methyl ester or a pharmaceutically acceptable acid addition salt thereof, and 3,4-diacetyloxy-L-phenylalanyl-3,4-diacetyloxy-L-phenylalanine benzyl ester or a pharmaceutically acceptable acid addition salt thereof, b. a non-toxic pharmaceutically acceptable inert diluent, c. a non-toxic pharmaceutically acceptable effervescent couple acid and base, and d. a non-toxic pharmaceutically acceptable enteric coating over said entire tableted admixture.
Claim 2
Dependent Claim 225 words
A pharmaceutical effervescent enteric-coated tablet for oral administration to a warm-blooded animal which permits release and absorption of L-DOPA in the area of the upper portion of the small intestine thereof comprising a tableted admixture of: a. a member selected from the group consisting of L-DOPA, 3,4-diacetyloxy-L-phenylalanine or a pharmaceutically acceptable acid addition salt thereof, 3,4-dipivalyloxy-L-phenylalanine or a pharmaceutically acceptable acid addition salt thereof, 3,4-dihydroxy-L-phenylalanine methyl ester or a pharmaceutically acceptable acid addition salt thereof, 3,4-diacetyloxy-L-phenylalanine methyl ester or a pharmaceutically acceptable acid addition salt thereof, 3,4-dihydroxy-L-phenylalanine benzyl ester or a pharmaceutically acceptable acid addition salt thereof, 3,4-diacetyloxy-L-phenylalanine benzyl ester or a pharmaceutically acceptable acid addition salt thereof, glycyl-3,4-diacetyloxy-L-phenylalanine methyl ester or a pharmaceutically acceptable acid addition salt thereof, 3,4-dipivalyloxy-N(1-methyl-2-acetylvinyl)-L-phenylalanine pivalyloxy methyl ester, the alkali metal salt of 3,4-dipivalyloxy-N(1-methyl-2-acetylvinyl)-L-phenylalanine, the alkali metal salt of 3,4-diacetyloxy-N(1-methyl-2-acetylvinyl)-L-phenylalanine, N-formyl-3,4-dipivalyloxy-L-phenylalanine, N-formyl-3,4-dipivalyloxy-L-phenylalanine-pivalyloxymethyl ester, N-formyl-3,4-diacetyloxy-L-phenylalanine, the alkali metal salt of N-formyl-3,4-diacetyloxy-L-phenylalanine, glycyl-3,4-diacetyloxy-L-phenylalanine or a pharmaceutically acceptable acid addition salt thereof, 3,4-diacetyloxy-L-phenylalanylglycine or a pharmaceutically acceptable acid addition salt thereof, 3,4-dihydroxy-L-phenylalanyl-3,4-dihydroxy-L-phenylalanine or a pharmaceutically acceptable acid addition salt thereof, 3,4-diacetyloxy-L-phenylalanyl-3,4-diacetyloxy-L-phenylalanine methyl ester or a pharmaceutically acceptable acid addition salt thereof, and 3,4-diacetyloxy-L-phenylalanyl-3,4-diacetyloxy-L-phenylalanine benzyl ester or a pharmaceutically acceptable acid addition salt thereof, b. a non-toxic pharmaceutically acceptable inert diluent, c. a non-toxic pharmaceutically acceptable effervescent couple acid and base, and d. a non-toxic pharmaceutically acceptable enteric coating over said entire tableted admixture.
Claim 3
Dependent Claim 10 words
The tablet of claim 1, wherein said diluent is talc.
Claim 4
Dependent Claim 27 words
The tablet of claim 1, wherein said effervescing agent is a member selected from the group consisting of tartaric acid, citric acid, citric anhydride, and phthalic acid.
Claim 5
Dependent Claim 14 words
The tablet of claim 1, wherein said carbon dioxide releasing agent is sodium bicarbonate.
Claim 6
Dependent Claim 24 words
The tablet of claim 1, wherein said enteric coating is a member selected from the group consisting of cellulose acetate phthalate and hydroxypropylmethylcellulose phthalate.
Claim 7
Dependent Claim 23 words
The tablet of claim 5, wherein said hydroxypropylmethylcellulose phthalate is a member selected from the group consisting of hydroxypropylmethylcellulose phthalate-50 and hydroxypropylmethylcellulose phthalate-45.
Claim 8
Dependent Claim 14 words
The tablet of claim 1, further comprising microcrystalline cellulose as a dry binding agent.
Claim 9
Dependent Claim 39 words
A method for orally inducing higher therapeutic blood levels of L-DOPA in a warm-blooded animal as compared to those blood levels obtained from administering conventional enteric-coated L-DOPA tablets to said animal comprising: administering thereto, the tablet of claim 1.

References Cited (Backward Citations)

US3131123A Cited
FR2116256B1 Cited
US3891696A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1979-06-01 1979-12-01 1980-06-01 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1983-06-01 1983-12-01 1984-06-01 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1987-06-01 1987-12-01 1988-06-01 $7700.00 Window Closed / Lapsed

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