Topical and transdermal administration of peptidyl drugs with hydroxide-releasing agents as skin permeation enhancers
First Claim
1. A method for enhancing the flux of a peptidyl drug through a body surface of an individual so as to achieve therapeutically effective blood levels thereof, the method comprising administering a peptidyl drug and a predetermined amount of a hydroxide-releasing agent to the body surface of the individual, wherein the predetermined amount of the hydroxide-releasing agent is effective to provide a pH in the range of approximately 8.5 to 13 at the localized region of the body surface, during drug administration, and wherein the peptidyl drug and hydroxide-releasing agent are present in a formulation and the amount of hydroxide-releasing agent in the formulation applied to the body surface is the total of (a) the amount required to neutralize any acidic species in the formulation plus (b) an mount equal to approximately 0.25 wt. % to 7.0 wt. % of the formulation.
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Accused Products
Abstract
A method is provided for increasing the permeability of skin or mucosal tissue to a topically or transdermally administered pharmacologically or cosmeceutically active peptide, polypeptide or protein. The method involves use of a specified amount of a hydroxide-releasing agent, the amount optimized to increase the flux of the peptide, polypeptide or protein through a body surface while minimizing the likelihood of skin damage, irritation or sensitization. Formulations and drug delivery devices employing hydroxide-releasing agents as permeation enhancers are provided as well.
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Citations
50 Claims
- 1. A method for enhancing the flux of a peptidyl drug through a body surface of an individual so as to achieve therapeutically effective blood levels thereof, the method comprising administering a peptidyl drug and a predetermined amount of a hydroxide-releasing agent to the body surface of the individual, wherein the predetermined amount of the hydroxide-releasing agent is effective to provide a pH in the range of approximately 8.5 to 13 at the localized region of the body surface, during drug administration, and wherein the peptidyl drug and hydroxide-releasing agent are present in a formulation and the amount of hydroxide-releasing agent in the formulation applied to the body surface is the total of (a) the amount required to neutralize any acidic species in the formulation plus (b) an mount equal to approximately 0.25 wt. % to 7.0 wt. % of the formulation.
Specification