Sirolimus Eye Drops for Meibomian Gland Obstruction

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Solution Overview

Problem

There is no effective treatment method for meibomian gland dysfunction (MGD), and existing diagnostic criteria are unclear, leading to challenges in managing the condition, which can cause chronic ocular discomfort and dry eye.

Innovation Solution

A compound represented by a specific formula, or its pharmaceutically acceptable salt, is used as a prophylactic and/or therapeutic agent to reduce obstructions at the meibomian gland orifices and treat MGD, preferably in the form of eye drops or ointments for instillation or application to the eyelid skin.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If meibomian gland obstruction is treated with conventional methods, then general ocular comfort may be maintained, but the obstruction itself persists and continues to cause MGD symptoms

Engineering Contradiction:
ImproveMGD treatment effectivenessVSAvoidmeibomian gland orifice obstruction
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses a specific compound (formula 1) as an intermediary substance that mediates between the obstructed meibomian gland and the therapeutic effect. The compound acts as a mediator that specifically targets and resolves the obstruction mechanism without affecting other ocular structures, thereby improving treatment reliability while eliminating the harmful obstruction factor.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the chemical parameter of the treatment by introducing a compound with specific functional groups (hydroxyl, methoxy, carboxyl, etc.) that can interact with the obstruction material. This parameter change in chemical composition allows the treatment to specifically address the obstruction while maintaining overall ocular homeostasis.

Inventive Principle:
Principle #35Parameter changes

2Measurement precision

If diagnostic criteria for MGD are established, then MGD can be defined as an independent disease, but clear diagnostic standards remain lacking

Engineering Contradiction:
ImproveMGD diagnostic precisionVSAvoiddiagnostic criteria complexity
Core Design Contradiction:
Measurement precisionVSDevice complexity

Solution Approach 1:

The patent replaces complex clinical diagnostic procedures with a simpler chemical detection method. By using a compound that specifically interacts with MGD-related substances, the diagnosis can be made through chemical analysis rather than complex clinical evaluation, thereby improving measurement precision without increasing device or procedural complexity.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

3Quantity of substance

If meibomian gland secretion is increased to compensate for obstruction, then lipid delivery may improve, but gland dysfunction and ocular discomfort persist

Engineering Contradiction:
Improvemeibomian gland lipid secretionVSAvoidgland dysfunction
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent extracts or removes the obstruction factor from the meibomian gland system using the compound of formula (1). By taking out the obstructing substance or mechanism, the gland can function normally without needing to compensate through increased secretion, thereby improving lipid delivery while eliminating gland dysfunction and associated ocular discomfort.

Inventive Principle:
Principle #2Taking out (Extraction)

Data Source

PatentUS11951098B2Therapeutic agent for meibomian dysfunction
Publication Date: 2024.04.09 SANTEN PHARMACEUTICAL CO LTD
  • US11951098B2 patent drawing
  • US11951098B2 patent drawing
  • US11951098B2 patent drawing

AI summary

A method for suppressing obstruction of meibomian gland in a mammalian subject, the method comprising administering to the mammalian subject an eye drop comprising 0.01 to 0.5% (w/v) of sirolimus or a pharmaceutically acceptable salt thereof as a sole active ingredient, wherein the eye drop is administered to an eye of the mammalian subject 1 to 2 times per day.