Ophthalmic Depot Preparation Solvent System for Stable Spherical Shape
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Solution Overview
Problem
Existing ophthalmic depot preparations face challenges in forming a stably spherical depot shape regardless of administration site or conditions, leading to inconsistent sustained release of drugs.
Innovation Solution
An ophthalmic depot preparation comprising benzyl benzoate and/or benzyl alcohol, polyethylene glycol, and/or dimethylsulfoxide, with a volume ratio of 75:25 to 25:75 and a total concentration of 50%(w/w) or more, which consistently forms similar spherical depots and achieves sustained drug release across different administration sites and conditions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If conventional depot preparations are used, then drug release is achieved, but the depot shape becomes randomly unstable and varies by administration site
Solution Approach 1:
The patent changes the physical-chemical parameters of the solvent system by specifying a volume ratio of 75:25 to 25:75 between benzyl benzoate/benzyl alcohol and polyethylene glycol/dimethylsulfoxide, with total amount of 50%(w/w) or more. This parameter optimization enables the formation of stable spherical depots with consistent drug release profiles across different administration sites including vitreous humor, anterior chamber, and subconjunctival spaces.
Solution Approach 2:
The patent employs a composite solvent system combining benzyl benzoate and/or benzyl alcohol with polyethylene glycol and/or dimethylsulfoxide in specific proportions. This composite formulation creates a balanced system that forms stable spherical depots while maintaining adaptability to various ocular administration sites and conditions.
2Duration of action of stationary object
If depot formation is achieved, then sustained drug release is possible, but the release consistency varies with administration conditions
Solution Approach 1:
The patent optimizes the concentration parameter by setting the total amount of benzyl benzoate/benzyl alcohol and polyethylene glycol/dimethylsulfoxide at 50%(w/w) or more, with a volume ratio of 75:25 to 25:75. This parameter control ensures reliable and consistent drug release profiles over extended periods regardless of administration site or conditions.
3Shape
If solvent composition is optimized for stable depot formation, then spherical shape is achieved, but formulation complexity increases
Solution Approach 1:
The patent uses a composite solvent system of benzyl benzoate/benzyl alcohol combined with polyethylene glycol/dimethylsulfoxide in specific ratios. This composite approach achieves stable spherical depot formation through the synergistic interaction of components while maintaining a relatively simple two-component formulation structure.
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 ophthalmic depot preparation ensures stable and prolonged pharmacological effects by maintaining consistent depot formation and drug release, enhancing safety and efficacy regardless of administration site or conditions.
Implementation Method 1
an ophthalmic depot preparation containing benzyl benzoate and/or benzyl alcohol and polyethylene glycol and/or dimethylsulfoxide
Implementation Method 2
a preparation in which a depot is formed at a site where a pharmaceutical agent is injected and a drug is gradually released from that site
Data Source
Figure 1
AI summary
The present invention relates to an ophthalmic depot preparation comprising benzyl benzoate and/or benzyl alcohol and polyethylene glycol and/or dimethylsulfoxide, wherein the volume ratio of benzyl benzoate and/or benzyl alcohol to polyethylene glycol and/or dimethylsulfoxide in the ophthalmic depot preparation is 75:25 to 25:75, and the total amount of benzyl benzoate and/or benzyl alcohol and polyethylene glycol and/or dimethylsulfoxide contained is 50%(w/w) or more.