Non-aqueous Oily Injectable Preservative Efficacy
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Solution Overview
Problem
Current injectable formulations, especially non-aqueous oily ones, face challenges in achieving high preservative efficacy against microorganisms, particularly when used in multi-dose applications, as traditional lipophilic preservatives often fail to maintain sterility effectively.
Innovation Solution
A non-aqueous injectable formulation combining a therapeutically effective amount of an active ingredient dissolved or suspended in oil with a hydrophilic excipient and a lipophilic preservative, where the hydrophilic excipient is non-phase separable from the oil, enhancing preservative efficacy by increasing the concentration of the preservative in the water phase.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If a lipophilic preservative is used alone in non-aqueous oily injectable formulation, then the formulation can maintain stability, but preservative efficacy against microorganisms is insufficient
Solution Approach 1:
The patent combines lipophilic preservative and hydrophilic excipient into a composite preservative system. The lipophilic preservative (e.g., phenol, cresol, benzyl alcohol) provides oil-phase stability while the hydrophilic excipient (e.g., propylene glycol, polyethylene glycol) creates a water-miscible phase that microorganisms require for growth. This composite approach achieves high preservative efficacy without requiring multiple separate components.
Solution Approach 2:
The patent optimizes the concentration ratio between lipophilic preservative and hydrophilic excipient to achieve phase compatibility. By adjusting parameters such as the amount of hydrophilic excipient (typically 0.1-10% w/v) and lipophilic preservative (typically 0.01-5% w/v), the formulation achieves both microorganism inhibition and physical stability without phase separation.
2Reliability
If hydrophilic excipient is added to increase preservative efficacy, then preservative ability improves, but phase separation may occur
Solution Approach 1:
The patent carefully controls the concentration parameters of hydrophilic excipient within specific ranges (typically 0.1-10% w/v) to prevent phase separation. By optimizing these parameters, the formulation maintains a single-phase system where the hydrophilic excipient enhances preservative efficacy without causing oil-water separation or affecting the stability of the active ingredient suspension.
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 formulation demonstrates significantly higher preservative efficacy, reducing bacterial and fungal counts by 3-4 logs within 6 hours to 7 days, ensuring the sterility and stability of the injectable over time, even in low water activity states.
Implementation Method 1
a lipophilic preservative combined with a hydrophilic excipient, which may exhibit higher preservative efficacy, compared to administration of the preservative alone
Data Source
AI summary
Disclosed herein is preferably a multi-dose type non-aqueous oily injectable formulation including; an active ingredient (drug) expressing therapeutic effects, which is dissolved, dispersed or suspended in a therapeutically effective amount, in oil. The disclosed non-aqueous oily injectable formulation may include; an oil-affinitive preservative, and a hydrophilic excipient non-phase separable from the oil-affinitive preservative when the excipient is mixed with the oil-affinitive preservative.