Topical and transdermal administration of peptidyl drugs using hydroxide releasing agents as permeation enhancers
First Claim
1. A method for enhancing the flux of a peptidyl drug through a body surface, comprising administering the peptidyl drug to a localized region of a human patient'"'"'s body surface in combination with a hydroxide-releasing agent applied to the body surface in a predetermined amount effective to enhance the flux of the drug through the localized region of the body surface without causing damage thereto, and effective to provide a pH in the range of approximately 8.5 to 11.5 at the localized region of the body surface, during drug administration, 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 amount equal to approximately 0.25 wt. % to 25.0 wt. % of the formulation.
6 Assignments
0 Petitions
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.
128 Citations
54 Claims
- 1. A method for enhancing the flux of a peptidyl drug through a body surface, comprising administering the peptidyl drug to a localized region of a human patient'"'"'s body surface in combination with a hydroxide-releasing agent applied to the body surface in a predetermined amount effective to enhance the flux of the drug through the localized region of the body surface without causing damage thereto, and effective to provide a pH in the range of approximately 8.5 to 11.5 at the localized region of the body surface, during drug administration, 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 amount equal to approximately 0.25 wt. % to 25.0 wt. % of the formulation.
Specification