L-.alpha.-amino acids as transdermal penetration enhancers
AssigneeAmerican Home Products Corporation
InventorsPramod P. Sarpotdar, James L. Gaskill, Robert P. Giannini, Charles R. Daniels
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AssigneeAmerican Home Products Corporation
InventorsPramod P. Sarpotdar, James L. Gaskill, Robert P. Giannini, Charles R. Daniels
Estimating the term…
The disclosed invention provides methods and compositions ulilizing L-.alpha.-amino acids for enhancing the rate of penetration through the skin of both topical medicaments and of drugs employed for systemic administration. Fifteen L-.alpha.-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, .alpha.-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.
A pharmaceutical composition for transdermal administration of a steroidal contraceptive, comprising a steroidal contraceptive and an amount of an L-.alpha.-amino acid, selected from Tryptophan, Alanine, Proline, Serine, Cysteine, Glycine, Isoleucine, Leucine, Valine and .alpha.-Aminobutyric Acid, Norvaline and Norleucine, effective to enhance the penetration of said steroidal contraceptive through the skin, dispersed in a transdermally effective carrier.
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-.alpha.-amino acid, selected from Tryptophan, Alanine, Proline, Serine, Cysteine, Glycine, Isoleucine, Leucine, Valine, .alpha.-Aminobutyric Acid, Norvaline and Norleucine effective to enhance the penetration of said steroidal contraceptive through the skin.
Dependencies are inferred from the claim text.