Intranasal Testosterone Gel Formulations for Sustained Release
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current testosterone replacement therapies for hypogonadism are limited by inefficiencies in delivering therapeutically effective amounts of testosterone, particularly through intranasal administration, which often result in inadequate plasma levels and convenience issues.
Innovation Solution
Development of novel 4% and 4.5% intranasal testosterone gel formulations designed for sustained release, administered topically in smaller volumes to the nasal cavity, with a novel titration method to determine optimal dosing regimens, ensuring effective testosterone levels are maintained.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional intranasal testosterone therapies are used, then administration is simplified, but plasma testosterone levels remain inadequate and therapeutic effectiveness is reduced
Solution Approach 1:
The patent changes the concentration parameter of testosterone in the intranasal gel formulation, using 4% and 4.5% concentrations to achieve adequate plasma levels. This parameter change resolves the contradiction by providing sufficient therapeutic substance while maintaining ease of intranasal administration.
Solution Approach 2:
The patent uses a composite gel formulation containing testosterone, oleoyl polyoxylglycerides, and castor oil. This composite material provides sustained release properties that maintain adequate plasma testosterone levels throughout the dosing interval, resolving the effectiveness issue while keeping administration simple.
2Quantity of substance
If larger volumes of testosterone gel are administered to achieve therapeutic levels, then plasma testosterone concentration improves, but patient convenience and ease of administration deteriorate
Solution Approach 1:
The patent optimizes the volume parameter by formulating concentrated gels (4% and 4.5%) that deliver therapeutic doses in small volumes (100-200 microliters per nostril). This resolves the contradiction by achieving adequate plasma concentration without requiring large, inconvenient application volumes.
Solution Approach 2:
The patent targets specific anatomical locations within the nasal cavity (superior nasal septum, superior lateral wall, or inferior nasal septum) for gel deposition. This localized application ensures efficient absorption in small volumes, maintaining convenience while achieving therapeutic plasma levels.
3Ease of operation
If intranasal testosterone gel is administered, then convenience and patient compliance improve, but irritation of the nasal mucosa may occur
Solution Approach 1:
The patent optimizes the concentration parameter of testosterone in the gel formulation (4% and 4.5%) to achieve therapeutic effectiveness while minimizing mucosal irritation. This parameter optimization resolves the contradiction by balancing convenience with reduced harmful effects on nasal tissue.
Solution Approach 2:
The patent uses a composite gel system with oleoyl polyoxylglycerides and castor oil that provides sustained release and reduces mucosal irritation compared to higher concentration formulations. This composite approach maintains convenience while minimizing harmful effects on the nasal mucosa.
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 formulations provide rapid and sustained absorption of testosterone, achieving therapeutic levels in hypogonadal men, improving symptoms associated with testosterone deficiency and offering a convenient, less-irritating administration method.
Implementation Method 1
The formulations provide rapid and sustained absorption of testosterone, achieving therapeutic levels in hypogonadal men
Implementation Method 2
4% and 4.5% intranasal testosterone gel formulations designed for sustained release
Data Source
AI summary
The present invention relates to pernasal testosterone bio-adhesive gel formulations for intranasal administration and testosterone replacement treatment methods for using the pernasal testosterone bio-adhesive gel formulations for providing sustained intranasal delivery of testosterone to testosterone deficient males to treat, for example, male subjects diagnosed with hypogonadism. The present invention is also concerned with a novel titration method to determine the appropriate daily treatment regimen, i.e., a BID or TID treatment regimen, to administer the intranasal gels of the present invention to treat hypogonadism or TRT.