Equine Pergolide Transdermal Solvent Formulation
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Solution Overview
Problem
Current pergolide formulations for treating Equine Cushing's Disease face challenges such as poor palatability, variability in dosing, instability, and difficulty in administration, particularly with oral and transdermal patch formulations, which result in subtherapeutic plasma levels and administration issues in equines.
Innovation Solution
A transdermal non-patch formulation of pergolide or its salt, utilizing a solvent system that includes dimethyl sulfoxide, N-methylpyrrolidone, and other solvents to achieve solubility of 5 mg/ml or higher, allowing for prolonged systemic absorption through deposition in the stratum corneum, providing consistent and therapeutic plasma concentrations with reduced dosing frequency and ease of administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If oral tablets are used for pergolide administration, then the drug can be delivered to equines, but the tablets have poor palatability, large size, and require forceful swallowing which complicates administration
Solution Approach 1:
The patent replaces the mechanical oral tablet administration system with a transdermal delivery system that uses chemical penetration through the skin. This eliminates the need for forceful swallowing and mechanical insertion of large tablets into the equine's mouth, directly resolving the administration difficulty while maintaining effective drug delivery.
Solution Approach 2:
The patent introduces a transdermal patch as an intermediary delivery mechanism between the pergolide drug and the equine's systemic circulation. This intermediary system bypasses the problematic oral administration route by using the skin as a penetration pathway, thereby improving ease of administration without requiring forceful swallowing.
2Reliability
If transdermal patches are used for pergolide delivery, then non-invasive dosing and steady drug delivery are achieved, but the patches may be damaged, consumed, or not reproducibly absorbed by equines
Solution Approach 1:
The patent modifies the physical and chemical parameters of the pergolide formulation by using different solvents, penetration enhancers, and adhesive systems optimized for equine skin. These parameter changes create a more durable and stable patch formulation that resists damage and consumption by equines while maintaining reliable transdermal absorption and consistent systemic exposure.
Solution Approach 2:
The patent employs composite material structures in the transdermal patch, combining multiple layers including drug reservoirs, penetration enhancers, adhesives, and protective barriers. This composite construction enhances the patch's resistance to damage and consumption by equines while ensuring reliable drug delivery and reproducible systemic exposure.
3Ease of operation
If compounded oral suspensions are used for pergolide, then administration is easier than tablets, but the formulations show variation in dosages, poor stability, and inconsistent potency
Solution Approach 1:
The patent replaces the compounded oral suspension system with a manufactured transdermal patch system. This substitution eliminates the compounding variability and stability issues inherent in oral formulations by using a controlled manufacturing process that ensures consistent drug concentration, stability, and potency in each patch application.
Solution Approach 2:
The patent performs preliminary formulation development and stability testing during the manufacturing process to ensure each transdermal patch contains the correct dosage and maintains stability throughout its shelf life. This preliminary action prevents the dosage variation and instability problems that occur with compounded oral suspensions by establishing quality control before the product reaches the equine.
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 transdermal formulation achieves therapeutic plasma concentrations with reduced dosing frequency, improved administration ease, and stability, overcoming limitations of oral and patch formulations, ensuring effective treatment of Equine Cushing's Disease with consistent potency and reduced side effects.
Implementation Method 1
A transdermal non-patch formulation of pergolide or its salt, utilizing a solvent system that includes dimethyl sulfoxide, N-methylpyrrolidone, and other solvents to achieve solubility of 5 mg/ml or higher
Implementation Method 2
Through what is believed to be deposition of pergolide in the stratum corneum of an equine followed by prolonged systemic absorption
Implementation Method 3
utilizing a solvent system that includes dimethyl sulfoxide, N-methylpyrrolidone, and other solvents to achieve solubility of 5 mg/ml or higher, allowing for prolonged systemic absorption through deposition in the stratum corneum
Data Source
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AI summary
This invention provides transdermal non-patch pergolide formulations useful for the treatment of disease in an equine. The invention also provides methods for treating a disease in an equine by administering a formulation of the invention to an equine.