Phospholipid-steroid ocular formulation reduces intraocular pressure
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Solution Overview
Problem
Intravitreal corticosteroid injections for conditions like macular edema and uveitis are effective but associated with significant side effects such as infectious endophthalmitis, retinal detachment, and increased intraocular pressure due to repetitive administration, necessitating a reduction in side effects.
Innovation Solution
A pharmaceutical composition combining a lipid cake mixture of phospholipids and cholesterol with a steroid solution, where the total amount of phospholipids is less than 2.5 umol per 50 ul, reducing side effects compared to compositions with higher phospholipid amounts, and is administered for ocular delivery to treat ophthalmic diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If intravitreal corticosteroid injection is administered to treat macular edema and uveitis, then therapeutic efficacy is improved, but side effects such as increased intraocular pressure, corneal edema, and opacity occur
Solution Approach 1:
The patent changes the chemical composition parameters of the injection formulation by incorporating phospholipids at controlled concentrations (0.1-10% w/v) alongside corticosteroids. This parameter modification reduces side effects like increased intraocular pressure and corneal damage while preserving therapeutic efficacy for treating macular edema and uveitis
Solution Approach 2:
The invention creates a composite pharmaceutical formulation combining corticosteroids with phospholipids (such as phosphatidylcholine, phosphatidylethanolamine, phosphatidylserine, or phosphatidic acid). This composite material approach allows the formulation to deliver therapeutic benefits while reducing harmful side effects through the synergistic interaction between the two components
2Duration of action of stationary object
If repetitive intravitreal injection is performed to maintain optimal corticosteroid concentration, then therapeutic effect is maintained, but complications such as infectious endophthalmitis, retinal detachment, and traumatic cataract increase
Solution Approach 1:
The patent employs phospholipid-based formulations that dynamically interact with ocular tissues, providing sustained drug release and extended therapeutic duration. This reduces the frequency of repetitive injections needed, thereby lowering the risk of injection-related complications while maintaining effective corticosteroid levels
Solution Approach 2:
Phospholipids act as intermediary carriers that facilitate prolonged retention and controlled release of corticosteroids in the ocular environment. This intermediary mechanism extends the duration of therapeutic action, reducing the need for frequent re-injection and associated complications
3Stability of the object's composition
If high concentration of phospholipids is used in the composition, then stability and retention in vitreous humor are improved, but side effects are increased
Solution Approach 1:
The patent optimizes the phospholipid concentration parameter within a specific range (0.1-10% w/v, preferably 0.5-5% w/v) to achieve the desired balance. This parameter optimization ensures sufficient stability and retention in the vitreous humor while avoiding the side effects associated with excessively high phospholipid concentrations
Data Source
AI summary
The present invention relates to pharmaceutical compositions comprising a combination of a lipid cake mixture comprising one or more phospholipids, with or without cholesterol, and a steroid solution comprising an ocular steroid, derivative thereof, a pharmaceutically acceptable salt thereof or a prodrug thereof, wherein the total amount of the phospholipid in the said composition is about 0.1 umol to less than about 2.5 umol per 50 ul of pharmaceutical composition and the side effects of the ocular steroid are reduced. The pharmaceutical composition is preferably administered by ocular route to treat ophthalmic diseases.