Skin permeation enhancer compositions using sucrose esters

• US 4,865,848 A
• Filed: 02/26/1987
• Issued: 09/12/1989
• Est. Priority Date: 02/26/1987
• Status: Expired due to Term

• Current Assignee: ALZA Corporation (Johnson & Johnson)
• Original Assignee: ALZA Corporation (Johnson & Johnson)
• Inventors: Cheng, Yu-Ling, Gale, Robert M., Sanders, Harold F., Sugihara, Edna
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): HORNE, LEON
• Application Number:
  US07/019,442
• Time in Patent Office: 929 Days
• Field of Search: 424/448, 424/449, 514/946, 514/947
• US Class Current: 424/449
• CPC Class Codes: A61K 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• CPC Class Codes: A61K 9/7053 obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
• CPC Class Codes: A61K 9/7076 the adhesive comprising ingredients of undetermined constitution or reaction products thereof, e.g. rosin or other plant resins
• CPC Class Codes: A61K 9/7084 Transdermal patches having a drug layer or reservoir, and one or more separate drug-free skin-adhesive layers, e.g. between drug reservoir and skin, or surrounding the drug reservoir; Liquid-filled reservoir patches

Abstract

A method for enhancing the transdermal flux of a transdermally deliverable drug through intact skin is described in which the drug is delivered simultaneously with sucrose monolaurate or a mixture of sucrose esters of coconut fatty acids, which is predominantly sucrose monolaurate. Preferred embodiments of therapeutic systems for delivering the drug and the sucrose ester employ a matrix containing drug at a concentration above saturation.

Claims

1. A method for enhancing the transdermal flux of a biologically active agent through intact skin which comprises placing a source of said agent in agent transmitting relationship to said intact skin in the presence of a permeation enhancing amount of a permeation enhancer consisting essentially of a sucrose monolaurate mixed with sucrose esters of coconut fatty acids.

2. The method of claim 1 wherein the source of said agent contains agent in excess of its saturation concentration in said source.

3. In a method for transdermally administering a biologically active agent by permeation through skin which comprises:

(a) placing a source of said agent and a permeation enhancer therefor in agent and permeation enhancer transmitting relationship to said skin, and

(b) maintaining said source in contact with said skin for a period of time sufficient to produce a beneficial effect;

the improvements wherein said permeation enhancer consists essentially of a material selected from the group consisting of sucrose monolaurate mixed with sucrose esters of coconut fatty acids.