Veterinary DSI Composition for Rapid Mucosal Drug Absorption
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Solution Overview
Problem
Existing therapeutic methods for animals, such as equines, bovines, canines, felines, and porcines, face challenges including rapid onset and short duration of activity, variability in bioavailability, instability of active ingredients, high inactive material content, and risks of infection and side effects from injectable and oral formulations.
Innovation Solution
Development of veterinary pharmaceutical compositions for direct systemic introduction (DSI) using bovine gelatin, mannitol, and surfactants, which dissolve rapidly in non-keratinous tissues to provide quick absorption into the bloodstream, minimizing inactive materials and avoiding gastric metabolism, with formulations like omeprazole achieving rapid disintegration and high systemic availability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If injectable formulations are used to provide rapid onset of activity, then the onset speed is improved, but the risk of infection at injection sites increases and cleanliness is difficult to ensure outside clinical settings
Solution Approach 1:
The patent introduces a mucosal membrane as an intermediary route for drug delivery. Instead of direct injection into the bloodstream or oral administration, the composition is applied to mucosal membranes (oral, nasal, vaginal, rectal) which serve as an intermediate absorption pathway, allowing rapid systemic uptake without breaking the skin barrier and thus avoiding infection risk while achieving fast onset
Solution Approach 2:
The patent replaces the mechanical injection process (needles, syringes, skin penetration) with a non-invasive application method. The composition is applied topically to mucosal surfaces where it dissolves and absorbs directly into the bloodstream, substituting the mechanical injection system with a dissolution-absorption system that eliminates infection hazards
2Ease of operation
If conventional oral formulations are used, then the ease of administration is improved, but the bioavailability varies considerably due to digestive system characteristics and food content
Solution Approach 1:
The patent uses mucosal membranes as an intermediary absorption site that bypasses the gastrointestinal tract. By applying the composition to mucosal surfaces (particularly buccal, sublingual, or nasal mucosa), the drug absorbs directly into the bloodstream through the rich vascular supply of these membranes, avoiding degradation by gastric acid and enzymes, and eliminating the variability introduced by food content and digestive characteristics
Solution Approach 2:
The patent extracts the active ingredient from the gastrointestinal environment entirely. Instead of relying on oral absorption through the stomach and intestines, the formulation is designed to dissolve and absorb at mucosal membranes, effectively removing the drug delivery process from the variable digestive system and placing it in the more controlled mucosal absorption environment
3Ease of operation
If oral formulations are used to administer active ingredients, then the ease of administration is improved, but the active ingredient stability deteriorates due to pH and digestive materials in the stomach
Solution Approach 1:
The patent introduces mucosal membranes as an intermediary pathway that protects the active ingredient from the harsh gastric environment. The composition dissolves at the mucosal surface where pH is more neutral and digestive enzymes are absent, allowing the active ingredient to remain stable and absorb directly into the bloodstream without exposure to degrading conditions in the stomach
Solution Approach 2:
The patent extracts the drug delivery process from the gastrointestinal tract entirely. By targeting mucosal membranes instead of the stomach and intestines, the formulation removes the active ingredient from exposure to gastric acid, pepsin, and other digestive materials that cause degradation, while maintaining ease of administration through non-invasive application
4Reliability
If conventional oral or injectable formulations are used, then the therapeutic effect is achieved, but the amount of inactive material (carriers and excipients) administered increases significantly
Solution Approach 1:
The patent fundamentally changes the formulation parameters by designing a composition with dramatically reduced excipient content. Instead of conventional formulations requiring large amounts of carriers, binders, and fillers to achieve appropriate dosage form properties, the invention uses a minimal excipient approach where the active ingredient constitutes the majority of the composition, enabled by the unique dissolution and absorption characteristics of mucosal membrane delivery
Solution Approach 2:
The patent extracts and removes unnecessary excipients from the formulation. By utilizing the natural dissolution properties of the active ingredient in mucosal fluids and the high absorption capacity of mucosal membranes, the formulation eliminates the need for numerous carriers and excipients that would otherwise be required to maintain dosage form integrity and deliver adequate doses through conventional routes
5Speed
If injectable formulations are used to provide rapid onset, then the onset speed is improved, but the duration of action is limited to a single peak and relatively short period
Solution Approach 1:
The patent achieves continuous useful action through sustained dissolution and absorption at the mucosal membrane site. As the composition dissolves in mucosal fluids over time, the active ingredient is continuously released and absorbed into the bloodstream, creating a sustained therapeutic effect rather than a single rapid peak followed by rapid elimination. This continuous supply mechanism extends the duration of action while maintaining rapid onset characteristics
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 DSI compositions offer faster onset of therapy, reduced side effects, improved bioavailability, and more accurate dosing, allowing for shorter withdrawal times and safer administration with minimal stress for both the animal and handler.
Implementation Method 1
dissolve rapidly in non-keratinous tissues to provide quick absorption into the bloodstream
Data Source
AI summary
Veterinary pharmaceutical compositions for direct systemic introduction, also known as DSI pharmaceutical compositions. One veterinary pharmaceutical composition for direct systemic introduction includes about 10-17 dry mass % bovine gelatin; about 10-17 dry mass % mannitol; about 0-1 dry mass % of a surfactant; and about 65-80 dry mass % of the active pharmaceutical ingredient which is a proton pump inhibitor. A method of manufacturing a veterinary pharmaceutical composition for direct systemic introduction includes combining one or more pharmacologically inactive compounds to form a first solution; using one or more surfactants to form a second solution; adding an active pharmaceutical ingredient to the second solution to form a first mixture; adding the first solution to the first mixture to form a pre-formulation; freezing the pre-formulation; and lyophilizing the pre-formulation.