Composition of dexibuprofen transdermal hydrogel
Inventors
BERGMAN, Jeffrey Stuart • DEVARAJAN, Sampathkumar • RAMALINGAM, Selvakumar • PALANISAMY, Anandsenthil Vel
Assignees
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Publication Number
US-10085939-B2
Publication Date
2018-10-02
Expiration Date
Abstract
Stable non-alcoholic transdermal hydrogel of dexibuprofen was prepared by using a simple manufacturing process, and the experimental trials showed that the pH modifying agent, antioxidant and water miscible solvent are the essential excipients to obtain stable non-alcoholic transdermal hydrogel of dexibuprofen. The dexibuprofen hydrogel prepared using carbopol as a gelling polymer produced an opaque gel, whereas hydrogel prepared using hyroxypropyl methylcellulose (HPMC) as a gelling polymer produced a transparent gel. There was no significant changes observed with respect to physical description, pH, assay and particularly to the related substance values when the hydrogels were subjected to the stability study at accelerated condition (40° C./75% RH) for 3 months in laminated tubes.
Core Innovation
The invention relates to a transdermal hydrogel composition comprising dexibuprofen formulated as a stable, non-alcoholic hydrogel. The composition is designed for transdermal delivery and includes dexibuprofen and excipients that control pH and oxidative stability while maintaining a hydrogel system.
A key aspect is the inclusion of a pH modifying agent and an antioxidant, together with water miscible solvents to provide stability. The antioxidant is sodium metabisulfite, the pH modifying agent is sodium hydroxide, and the hydrogel further comprises polyethylene glycol and propylene glycol.
The hydrogel system uses a defined combination of gelling agents and a permeation enhancer. The gelling agents are selected as HPMC K4M or hydroxy ethyl cellulose, together with HPMC E5 and poloxamer 188, and the permeation enhancer consists of diethylene glycol monoethyl ether.
Claims Coverage
The independent claim provides a transdermal hydrogel composition with a defined loading of dexibuprofen, a three-gelling-agent combination, a specific permeation enhancer, and specified excipient classes. The independent claim centers on inventive features that collectively define the composition.
Defined dexibuprofen loading for transdermal hydrogel
The composition consists essentially of, by weight %, 1% to 15% dexibuprofen.
Three gelling agents combination
The composition comprises 0.5% to 30% of a combination of three gelling agents, where the first gelling agent is selected from one of HPMC K4M and hydroxy ethyl cellulose, the second gelling agent is HPMC E5, and the third gelling agent is poloxamer 188.
Diethylene glycol monoethyl ether permeation enhancer
The composition comprises 0.1% to 20% of a permeation enhancer consisting of diethylene glycol monoethyl ether.
Sodium hydroxide pH modifying agent
The composition comprises sodium hydroxide.
Sodium metabisulfite antioxidant
The composition comprises 0.05% to 5% of an antioxidant consisting of sodium metabisulfite.
Two water miscible solvents
The composition comprises two water miscible solvents consisting of polyethylene glycol and propylene glycol.
Preservative and soothing agent with water to 100%
The composition comprises one or more preservative, one or more soothing agent, and water to total 100%.
Overall, the claim coverage focuses on a composition definition where transdermal hydrogel performance is supported by the combination of dexibuprofen at a defined loading, a defined three-gelling-agent system, diethylene glycol monoethyl ether as the permeation enhancer, and specified stabilizing components including sodium hydroxide, sodium metabisulfite, polyethylene glycol, propylene glycol, preservative, and soothing agent.
Stated Advantages
The formulation is reported as stable.
Stability results indicate no significant changes in physical appearance, pH, assay, or related substances under the reported storage conditions.
HPMC-based gels are reported to be transparent, and carbopol-based gels are reported to be opaque.
Documented Applications
Transdermal delivery.
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