US4732892A
Expired / Lapsed
US
⏱️ 0.0 years remaining
L-α-amino acids as transdermal penetration enhancers
Assignee: Wyeth LLC
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Filing: 1985-07-12
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Granted: 1988-03-22
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Expires: 2005-07-12
Abstract
Abstract The disclosed invention provides methods and compositions ulilizing L-α-amino acids for enhancing the rate of penetration through the skin of both topical medicaments and of drugs employed for systemic administration. Fifteen L-α-amino acids were tested and found to enhance the rate of penetration of levonorgestrel through hairless mouse skin. These were Tryptophan, Glutamic Acid, Glycine, Proline, Alanine, Serine, Arginine, Aspartic Acid, Leucine, Isoleucine, Cysteine, Valine, α-Aminobutyric Acid, Norvaline and Norleucine. The effect of pH on the rate of penetration of the various amino acids was also examined and found to be unpredictable overall.
Inventors
- 👤 Pramod P. Sarpotdar
- 👤 James L. Gaskill
- 👤 Robert P. Giannini
- 👤 Charles R. Daniels
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 15:42
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0014; A61K31/00; A61K31/185; A61K31/19; A61K31/195; A61K31/33; A61K31/395; A61K31/40; A61K31/403; A61K31/404; A61K31/405; A61K31/56; A61K31/565; A61K47/00; A61K47/06; A61K47/16; A61K47/18; A61K47/183; A61K47/20
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
56 words
A pharmaceutical composition for transdermal administration of a steroidal contraceptive, comprising a steroidal contraceptive and an amount of an L-α-amino acid, selected from Tryptophan, Alanine, Proline, Serine, Cysteine, Glycine, Isoleucine, Leucine, Valine and α-Aminobutyric Acid, Norvaline and Norleucine, effective to enhance the penetration of said steroidal contraceptive through the skin, dispersed in a transdermally effective carrier.
Claim 2
Dependent Claim
56 words
A pharmaceutical composition for transdermal administration of a steroidal contraceptive, comprising a steroidal contraceptive and an amount of an L-α-amino acid, selected from Tryptophan, Alanine, Proline, Serine, Cysteine, Glycine, Isoleucine, Leucine, Valine and α-Aminobutyric Acid, Norvaline and Norleucine, effective to enhance the penetration of said steroidal contraceptive through the skin, dispersed in a transdermally effective carrier.
Claim 3
Dependent Claim
20 words
A pharmaceutical composition for transdermal administration of claim 1 in which the steroidal contraceptive includes Levo-norgestrel, Ethinyl Estradiol or 17-Beta-estradiol.
Claim 4
Dependent Claim
24 words
A pharmaceutical composition for transdermal administration of claim 1 in which the L-α-amino acid is selected from Valine, Cysteine, Isoleucine, Leucine and α-Aminobutyric Acid.
Claim 5
Dependent Claim
18 words
A pharmaceutical composition for transdermal administration of claim 1 in which the transdermally effective carrier comprises a matrix.
Claim 6
Independent Claim
78 words
A method for enhancing the rate of penetration through the skin of a steroidal contraceptive contained in a pharmaceutical composition for transdermal administration, said composition comprising such steroidal contraceptive dispersed in a transdermally effective carrier, said method characterized in including in said transdermal composition an amount of an L-α-amino acid, selected from Tryptophan, Alanine, Proline, Serine, Cysteine, Glycine, Isoleucine, Leucine, Valine, α-Aminobutyric Acid, Norvaline and Norleucine effective to enhance the penetration of said steroidal contraceptive through the skin.
Claim 7
Independent Claim
78 words
A method for enhancing the rate of penetration through the skin of a steroidal contraceptive contained in a pharmaceutical composition for transdermal administration, said composition comprising such steroidal contraceptive dispersed in a transdermally effective carrier, said method characterized in including in said transdermal composition an amount of an L-α-amino acid, selected from Tryptophan, Alanine, Proline, Serine, Cysteine, Glycine, Isoleucine, Leucine, Valine, α-Aminobutyric Acid, Norvaline and Norleucine effective to enhance the penetration of said steroidal contraceptive through the skin.
Claim 8
Dependent Claim
16 words
A method of claim 5 in which the steroidal contraceptive includes Levo-Norgestrel, Ethinyl Estradiol or 17-Beta-estradiol.
Claim 9
Dependent Claim
20 words
A method of claim 5 in which the L-α-amino acid is selected from Valine, Cysteine, Isoleucine, Leucine and α-Aminobutyric Acid.
Claim 10
Dependent Claim
14 words
A method of claim 5 in which the transdermally effective carrier comprises a matrix.
References Cited (Backward Citations)
US3527864A
Cited
US3787571A
Cited
US3989816A
Cited
US4258037A
Cited
US4409233A
Cited
US4362737A
Cited
US4537776A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1991-03-22 | 1991-09-21 | 1992-03-22 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-03-22 | 1995-09-21 | 1996-03-22 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-03-22 | 1999-09-21 | 2000-03-22 | $7700.00 | Window Closed / Lapsed |