Prostaglandin Ophthalmic Composition Stabilization
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Solution Overview
Problem
Prostaglandin derivatives, used to treat elevated intraocular pressure, are unstable when stored in polyethylene containers due to absorption or adsorption, leading to drug loss and sorption issues, which affects their stability and efficacy.
Innovation Solution
Formulating prostaglandin derivatives with polyethylene glycol hydroxystearate and adding a small amount of oil, such as castor oil, to create a stable ophthalmic composition that reduces sorption to polyethylene containers and maintains stability at room temperature without irritation to the ocular mucosa.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If prostaglandin derivatives are stored in polyethylene containers, then dispensing in small volumes is enabled, but drug loss due to absorption and adsorption occurs
Solution Approach 1:
The patent introduces a surfactant as an intermediary substance between the prostaglandin derivative and the polyethylene container. The surfactant adsorbs onto the container surface first, creating a protective layer that prevents the drug from directly interacting with and being absorbed by the polyethylene material, thereby reducing drug loss while maintaining dispensing capability
Solution Approach 2:
The patent modifies the chemical environment by adding surfactants that change the surface properties of the polyethylene container. This parameter change in surface chemistry reduces the affinity between the polyethylene and the prostaglandin derivative, minimizing adsorption and drug loss
2Reliability
If prostaglandin derivatives are formulated with surfactants to reduce sorption, then stability in polyethylene containers is improved, but formulation complexity increases
Solution Approach 1:
The patent systematically evaluates and optimizes surfactant parameters including type, concentration, and hydrophilic-lipophilic balance (HLB) value. By identifying specific optimal ranges for these parameters, the formulation achieves stable drug-container interaction without requiring overly complex multi-component systems
Solution Approach 2:
The surfactant acts as a simple intermediary that provides the necessary stabilizing function through its amphiphilic nature, allowing the formulation to achieve reliability without adding significant complexity to the overall system
3Reliability
If oil is added to reduce sorption, then drug stability is improved, but ocular irritation may occur
Solution Approach 1:
The patent carefully controls the concentration parameter of oil in the formulation, maintaining it within a specific low range that is sufficient to reduce sorption but below the threshold that would cause ocular irritation. This parameter optimization allows the formulation to gain stability benefits while avoiding harmful effects
Solution Approach 2:
The patent uses surfactants as intermediaries that enable the use of small amounts of oil without direct contact between the oil and ocular tissues. The surfactant forms a protective interface that allows the oil to perform its stabilizing function while preventing irritation
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The composition significantly reduces sorption of prostaglandin derivatives to polyethylene containers, maintains stability and efficacy, and is non-irritating, effectively lowering intraocular pressure and reducing ocular pigmentation.
Implementation Method 1
The composition comprises a prostaglandin derivative, polyethylene glycol hydroxystearate and a pharmaceutically acceptable vehicle. The prostaglandin derivatives are known to be unstable either because of absorption or adsorption or degradation, when stored in polyethylene containers.
Implementation Method 2
U.S. patent application US20060100288 (herein after referred to as '288) discloses an oil in water type emulsion, which comprises colloid particles having an oily core surrounded by an interfacial film
Data Source
AI summary
The present invention relates to a pharmaceutical composition suitable for ophthalmic use comprising one or more prostaglandin derivatives or salts, a stabilizing amount of polyethylene glycol hydroxystearate and pharmaceutically acceptable vehicle.