Bilastine Eye Drop Composition Using β-Cyclodextrin and Gelling Agents

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Solution Overview

Problem

There is a lack of an enabling disclosure for ophthalmic pharmaceutical compositions containing high concentrations of bilastine suitable for once-daily administration, as existing formulations fail to provide effective and stable solutions, and bilastine is often compared unfavorably to olopatadine in terms of potency and duration of action.

Innovation Solution

An ophthalmic pharmaceutical composition comprising at least 0.4% w/v bilastine, a β-cyclodextrin, and a pharmaceutically acceptable water-soluble gelling agent, with a pH range of 4 to 9, which ensures complete dissolution of bilastine and provides prolonged ocular efficacy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If high concentration of bilastine is formulated in ophthalmic composition, then ocular efficacy is improved, but bilastine precipitation occurs

Engineering Contradiction:

Improveocular efficacyVSAvoidbilastine precipitation

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent uses cyclodextrins as intermediary molecules to solubilize bilastine. The cyclodextrin forms an inclusion complex with bilastine, where the hydrophobic cavity of cyclodextrin accommodates the bilastine molecule, preventing precipitation while maintaining high concentration (0.4% w/v) in the ophthalmic solution.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent modifies the chemical environment by adjusting pH to specific ranges (pH 4-9) and optimizing cyclodextrin concentration to prevent bilastine precipitation. These parameter changes ensure complete dissolution of bilastine at therapeutic concentrations while maintaining solution stability during storage and administration.

Inventive Principle:

Principle #35Parameter changes

2Reliability

If frequent dosing is required for effective symptom relief, then therapeutic efficacy is improved, but patient compliance deteriorates

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidpatient compliance

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent achieves continuous therapeutic action through once-daily dosing by optimizing the formulation to maintain effective drug concentration throughout the day. The cyclodextrin-bilastine complex provides sustained release and prevents precipitation, ensuring continuous efficacy without requiring multiple daily administrations, thereby improving patient compliance.

Inventive Principle:

Principle #20Continuity of useful action

3Ease of manufacture

If conventional excipients are used in bilastine formulation, then manufacturing simplicity is improved, but formulation stability deteriorates

Engineering Contradiction:

Improveformulation simplicityVSAvoidformulation stability

Core Design Contradiction:

Ease of manufactureVSStability of the object's composition

Solution Approach 1:

The patent replaces conventional excipients with cyclodextrins as the key stabilizing agent. Cyclodextrins serve as both solubilizers and stabilizers, eliminating the need for complex preservative systems and pH adjustment agents while maintaining formulation stability. This approach simplifies manufacturing by using a single multifunctional ingredient that prevents precipitation and maintains solution stability.

Inventive Principle:

Principle #24Intermediary (Mediator)

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 achieves unexpected increases in ocular efficacy and stability, allowing for once-daily administration without precipitation, addressing the limitations of previous formulations.

Implementation Method 1

an ophthalmic pharmaceutical composition comprising at least 0.4% w/v bilastine, or a pharmaceutically acceptable salt or solvate thereof, wherein the bilastine or salt or solvate thereof is completely dissolved in the aqueous ophthalmic pharmaceutical composition; at least one β-cyclodextrin

Methodology Applied

Scientific EffectInclusion complex formation: Solvation

Implementation Method 2

at least one pharmaceutically acceptable water-soluble gelling agent or an acceptable salt thereof, selected from the group consisting of hyaluronic acid, Gellan gum, guar gum, locust bean gum, alginic acid, povidone, kappa-carrageenan, alginate gum, dextran, dextran sulfate, chitosan and mixtures thereof

Methodology Applied

Scientific EffectGel formation: Gel

Data Source

PatentUS20260027099A1Ophthalmic compositions comprising bilastine, a beta-cyclodextrin and at least one gelling agent

Publication Date: 2026.01.29 FAES FARMA SA

AI summary

The disclosure relates to an aqueous ophthalmic pharmaceutical composition including: a) at least 0.4% w/v of bilastine, of formulaor a pharmaceutically acceptable salt or solvate thereof, wherein the bilastine salt or solvate thereof is completely dissolved in the pharmaceutical composition; b) at least one β-cyclodextrin; and c) at least one pharmaceutically acceptable water-soluble gelling agent; and wherein the pH is comprised between 4 and 9. Use of the composition is described for the treatment and/or prevention of conditions mediated by H1 histamine receptor, such as allergic disorders or diseases. The treatment and/or prevention of allergic conjunctivitis is described.