Dobesilic Acid Ophthalmic Ointment for Posterior Segment Delivery
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Solution Overview
Problem
Current methods for treating posterior segment eye diseases face challenges due to ocular barriers, leading to low bioavailability and invasive treatment options with significant risks, particularly for highly polar or hydrophilic drugs like calcium dobesilate monohydrate, which are quickly oxidized and have limited absorption across the corneal epithelium.
Innovation Solution
Topical administration of dobesilic acid and its pharmaceutically acceptable salts, such as calcium dobesilate and etamsylate, directly onto the eye surface, allowing these compounds to bypass anterior segment barriers and achieve higher bioavailability in the posterior segment, where they can exert vasoprotective, antioxidant, and anti-inflammatory effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If intravitreal injection is used to treat posterior segment eye diseases, then drug bioavailability is maximized, but the risk of blinding complications and retinal detachment increases
Solution Approach 1:
The patent uses the conjunctival sac as an intermediary reservoir to accumulate drug before it gradually permeates through the cornea and other ocular barriers. This mediates between the need for high drug concentration and the need to avoid invasive procedures, allowing sustained drug release directly into the eye without intravitreal injection
Solution Approach 2:
The patent applies drug-containing ointment to the conjunctival sac before the drug needs to reach the posterior segment. This preliminary placement allows the drug to gradually permeate through ocular barriers over time, achieving therapeutic concentrations in the vitreous cavity without direct intravitreal injection
2Ease of operation
If topical administration is used for anterior segment disease, then the treatment is non-invasive, but drug residence time is limited due to blinking and tear film turnover
Solution Approach 1:
The patent uses an ointment formulation that forms a semi-solid film on the ocular surface, which is more stable and longer-lasting than aqueous eye drops. This ointment film persists through blinking and tear turnover, maintaining drug availability for prolonged periods
Solution Approach 2:
The ointment is applied preliminarily to the conjunctival sac, creating a reservoir that slowly releases drug over time. This preliminary placement ensures continuous drug availability despite blinking and tear film turnover that would otherwise rapidly clear aqueous formulations
3Ease of operation
If highly polar drugs like calcium dobesilate monohydrate are topically administered, then the treatment is non-invasive, but absorption across the corneal epithelium is limited due to oxidation and hydrophilicity
Solution Approach 1:
The patent changes the physical state of the drug from a highly soluble crystalline form to an ointment formulation with different release characteristics. This formulation modification allows the polar drug to be delivered through the ocular surface by altering how the drug is presented and released, overcoming the limitation of corneal permeation for highly polar substances
Solution Approach 2:
The ointment base acts as an intermediary vehicle that facilitates the delivery of highly polar drugs like calcium dobesilate monohydrate through the corneal epithelium. The ointment formulation protects the drug from premature oxidation and provides a sustained release mechanism that overcomes the rapid clearance and poor absorption issues of topical polar drugs
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
This approach enables effective treatment of posterior segment eye diseases with higher bioavailability and reduced side effects compared to systemic or invasive intravitreal injections, as dobesilic acid salts remain active and effective in the posterior segment for an extended period, providing therapeutic benefits without the risks associated with invasive treatments.
Implementation Method 1
They topically administered, they pass through cornea, conjunctiva and sclera, but also overcome the barrier of iris and lens
Implementation Method 2
CDO is the monohydrate of calcium salt of dobesilic acid... CDO is a compound that can be easily oxidized to calcium 3,6-dioxocyclohexa-1,4-diene-1-sulfonate and thus it is highly unstable
Data Source
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AI summary
The invention relates to a new therapeutic approach for treatment and/or prevention of a disease of the posterior segment of the eye, in particular for retinal and optic nerve pathologies. Dobesilic acid and/or a pharmaceutically acceptable salt,or an ester of any of the acid or the salt,are proposed for use topically administered onto eye surface. There are also disclosed new compositions comprising dobesilic acid and/or a pharmaceutically acceptable salt,or an ester of any of the acid or the salt, adapted for performing the treatment and/or prevention of diseases of the posterior segment of the eye.