Biodegradable penetration enhancers with multiple hydrophilic moieties

US7514574B2 · kind B2 · utility

Inventor

• Ooi Wong · Fremont, US

Key dates

• Filing date: Aug 6, 2004
• Grant date: Apr 7, 2009
• Expiry date: Aug 6, 2024

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K47/16
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Design of new, safe and effective biodegradable agents, which can cover a wide range of drug molecules in the transdermal permeation and other membranes absorption of physiologically active agents are disclosed. Biodegradable agents includes compounds having a multiple hydrophilic moiety groups which are water loving groups with general chemical structures provide for contributing the penetration enhancement characteristics such as glycolic group and N-alkyl substituted amino acidic group and a lipophilic moiety and also in contributing the balanced lipophilicity of the compounds such as long chain alkyl group are disclosed. More particularly, compounds with R1, and R2, as the steric hindered but can significantly affect the hydrolytic and enzymatic degradation or stability of the biodegradable enhancers. With these physical chemical features, the disclosed compound can influence the efficacy, toxicity, irritation, duration of action of the enhancers, and the reversibility of the skin, and the stability of the enhancers. The substituents also affect the final lipophilicity of the enhancers as the compounds will have higher partition coefficient values.