Ivacaftor Oral Liquid Solution for Solubility and Flexible Dosing
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Solution Overview
Problem
Existing solid dosage forms of ivacaftor, such as tablets and granules, are difficult for pediatric and geriatric patients to swallow, leading to issues with compliance and incomplete dosing, particularly in patients with physical disabilities or swallowing complications.
Innovation Solution
Development of a stable oral liquid solution of ivacaftor comprising specific excipients like Polyethylene Glycol 400, Hydrogenated Castor Oil, Sucralose, Sodium Lauryl Sulfate, Methyl Parahydroxybenzoate, Butylated Hydroxy anisole, and a flavoring agent, which enhances bioavailability and provides a flexible dosage form for easier administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If solid dosage forms (tablets and granules) are used for ivacaftor administration, then the drug can be manufactured and stored easily, but pediatric and geriatric patients have difficulty swallowing leading to poor compliance and incomplete dosing
Solution Approach 1:
The patent changes the physical state of the dosage form from solid (tablets/granules) to liquid solution. This parameter change fundamentally alters the administration method, allowing the drug to be easily administered to patients who cannot swallow solids, thereby improving compliance while maintaining reliable drug delivery
Solution Approach 2:
The patent introduces specific excipients as intermediaries to enable liquid formulation. Polyethylene Glycol 400 and Hydrogenated Castor Oil act as solubilizing agents that mediate between the poorly water-soluble ivacaftor API and the aqueous environment, enabling creation of a stable liquid solution that is easy to administer
2Ease of operation
If ivacaftor is formulated in oral liquid solution, then patient compliance and ease of administration are improved, but the drug's low aqueous solubility presents formulation challenges
Solution Approach 1:
The patent creates a composite formulation system combining ivacaftor with specific excipients (Polyethylene Glycol 400, Hydrogenated Castor Oil, Sodium Lauryl Sulfate). This composite approach allows the poorly water-soluble drug to be formulated as a stable liquid solution by leveraging the solubilizing properties of the excipient combination
Solution Approach 2:
The excipients serve as intermediaries that bridge the incompatibility between ivacaftor's low aqueous solubility and the liquid dosage form requirement. These substances facilitate drug dissolution and stabilization in the liquid medium without compromising formulation stability
3Reliability
If conventional solid dosage forms are used, then formulation stability is easier to maintain, but bioavailability is significantly reduced compared to liquid formulations
Solution Approach 1:
The patent changes the dosage form parameter from solid to liquid, which fundamentally improves bioavailability. The liquid solution allows for better drug dissolution and absorption in the gastrointestinal tract, enhancing the body's ability to utilize the medication while maintaining formulation stability through careful excipient selection
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 oral liquid solution offers higher bioavailability and improved patient compliance, particularly in pediatric, geriatric, and institutionalized patients, ensuring complete dosing and rapid absorption from the gastrointestinal tract.
Implementation Method 1
The oral liquid solution comprises Polyethylene Glycol 400 and Hydrogenated Castor Oil as excipients which enhance the bioavailability of ivacaftor
Implementation Method 2
Sodium Lauryl Sulfate is included in the formulation to enhance the dissolution and absorption of ivacaftor
Implementation Method 3
Methyl Parahydroxybenzoate and Butylated Hydroxy anisole are added as antioxidants to prevent drug degradation
Data Source
AI summary
The present invention provides a stable oral liquid solution composition comprising ivacaftor or a pharmaceutically acceptable salt or solvate thereof and a solvent system selected from the group consisting of Polyethylene Glycols 400 and / or Hydrogenated Vegetable Oil used individually or in combination thereof. The invention also provides a method for treating or lessening the severity of cystic fibrosis is provided.