Ivermectin Soft Gelatin Capsule Lipid Formulation
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Solution Overview
Problem
Ivermectin's insolubility and instability in aqueous environments pose challenges for formulating stable and bioavailable oral soft capsule formulations, leading to poor absorption and bioavailability, especially when administered with food.
Innovation Solution
A formulation using a lipid medium with medium chain triglycerides, a surfactant, and a co-surfactant, along with an antioxidant, to create a self-emulsifying system that enhances solubility and stability, allowing for effective bioavailability and rapid absorption of Ivermectin in soft capsules.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If Ivermectin is formulated in aqueous media, then it can be administered orally, but its absorption is poor and bioavailability is low
Solution Approach 1:
The patent changes the physical-chemical parameters of the formulation medium from aqueous to lipid-based (medium chain triglycerides), which fundamentally alters the solubility characteristics of Ivermectin and enables effective absorption while maintaining oral administration route
Solution Approach 2:
The patent introduces surfactants and co-surfactants as intermediary substances that facilitate the interaction between the lipid medium and the gastrointestinal environment, enabling proper absorption of Ivermectin while maintaining formulation stability
2Ease of manufacture
If Ivermectin is formulated in soft capsules, then it provides convenient oral delivery, but its instability in aqueous environments compromises formulation stability
Solution Approach 1:
The patent changes the chemical environment from aqueous to lipid-based (medium chain triglycerides), which eliminates hydrolysis and oxidation reactions that cause Ivermectin degradation, thereby ensuring formulation stability in soft capsules
Solution Approach 2:
The lipid medium creates an inert chemical environment that protects Ivermectin from degradation by water, oxygen, and other reactive species, maintaining formulation stability throughout shelf life
3Adaptability or versatility
If Ivermectin is administered with food, then it can be taken at any time, but absorption is hindered and bioavailability decreases
Solution Approach 1:
The patent changes the formulation from water-soluble to lipid-soluble (medium chain triglycerides), which enables Ivermectin to be absorbed effectively regardless of food presence, as the lipid medium is not interfered with by dietary components
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 ensures increased bioavailability and stability of Ivermectin, enabling its absorption at any time without food interference, with improved solubility and reduced risk of impurity formation, thus providing a stable and effective oral delivery system.
Implementation Method 1
A formulation using a lipid medium with medium chain triglycerides, a surfactant, and a co-surfactant, along with an antioxidant, to create a self-emulsifying system that enhances solubility and stability
Implementation Method 2
an antioxidant agent, to form a soft capsule for oral administration
Data Source
AI summary
The present invention relates to a formulation of Ivermectin in soft capsules. In particular, the present invention relates to a formulation of Ivermectin in soft capsules which allows proper absorption in water, allowing the drug to be consumed at any time. Ivermectin, as an insoluble active ingredient, according to the invention, can be formulated in a liquid solution without compromising its stability and without creating impurities to form a suitable soft gelatin capsule. Therefore, the invention comprises a formulation comprising Ivermectin in a lipid medium which includes a surfactant in combination with an oily solvent, a co-surfactant and an oxidant, to form a soft capsule comprising a collagen coating, a plasticiser and gelatin. The field of the invention relates to improving the bioavailability of insoluble drugs such as Ivermectin for delivery in oral soft gelatin capsule forms.