Aciclovir Topical Spray Formulation for Herpes Treatment
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Solution Overview
Problem
Current topical formulations of aciclovir for herpes treatment face challenges due to low water solubility, making it difficult to achieve a stable and effective concentration, and often cause skin irritation and infection risks during application.
Innovation Solution
A pharmaceutical composition in solution form using 9-(2-hydroxyethoxymethyl)guanine (aciclovir) with solvents, solubilizers, humectants, anti-itching agents, antioxidants, and demineralized water, formulated to be stable and non-irritating, applied via an atomizer to prevent rubbing and infection.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If aciclovir is formulated as a topical ointment or cream, then the drug can be applied to the skin, but the low water solubility of aciclovir makes it difficult to achieve stable and effective concentration
Solution Approach 1:
The patent changes the physical-chemical parameters of the formulation by using a hydrophobic solvent system (isopropyl myristate, isopropyl alcohol, white petrolatum) instead of water-based systems. This parameter change enables aciclovir to achieve adequate solubility and stability in the topical formulation despite its low water solubility, resolving the contradiction between formulation stability and active agent concentration.
2Ease of operation
If aciclovir is applied by rubbing onto the skin, then the drug can be distributed over the affected area, but this may cause additional infection and skin irritation
Solution Approach 1:
The patent replaces the mechanical rubbing action with a spray delivery system. The composition is applied by spraying onto the affected area, which eliminates the need for mechanical friction and contact that causes skin irritation and potential infection. This substitution maintains ease of operation while removing harmful effects.
3Reliability
If a topical formulation contains high concentration of aciclovir, then the curative effectiveness is improved, but the formulation becomes unstable due to low solubility
Solution Approach 1:
The patent creates a composite pharmaceutical formulation combining aciclovir with a specific matrix of hydrophobic solvents (isopropyl myristate, isopropyl alcohol, white petrolatum) and auxiliary ingredients. This composite system allows high concentration of aciclovir (5% w/w) to be maintained while ensuring formulation stability through the synergistic interaction of components that provide both solubility and physical stability.
Data Source
AI summary
A new presentation of an antiviral pharmaceutical composition in solution form comprising as an active agent, aciclovir in an amount of about 5% by weight; a solvent in an amount of from about 10 to 20% by weight; a solubilizing agent in an amount of from about 1.5 to 5.0% by weight; a humectant agent in an amount of from about 2 to 10% by weight; an anti-itching agent in an amount of from about 0.05 to 1.0% by weight; an antioxidant agent in an amount of from about 0.1 to 0.5% by weight and demineralized water in an amount of from about 20 to 80% by weight.