Palatable Oral Dosage Formulation for Stable Multi-Drug Deworming
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Solution Overview
Problem
Existing veterinary oral formulations face challenges with drug solubility, bioavailability, palatability, stability, toxicity, efficacy, resistance, and compliance due to the inclusion of poorly soluble and labile active agents like moxidectin and praziquantel, which are also unpalatable and obnoxious.
Innovation Solution
The formulation involves coating praziquantel granules with a physiologically acceptable polymer matrix and co-granulating moxidectin to create stable granulates, which are then combined with other actives and excipients to form a tablet, masking taste and ensuring stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If active agents like moxidectin and praziquantel are included in oral formulations, then parasiticidal efficacy is improved, but palatability deteriorates due to unpalatable and obnoxious taste
Solution Approach 1:
The formulation is segmented into multiple granulate types, with each granulate containing specific active agents combined with excipients. This segmentation allows different functional components to be optimized independently while maintaining overall efficacy and palatability.
Solution Approach 2:
Excipients serve as intermediaries between the active agents and the animal patient. These excipients mask the unpalatable taste of moxidectin and praziquantel while facilitating delivery, thus resolving the contradiction between maintaining efficacy and improving palatability.
2Reliability
If multiple active agents are incorporated to broaden parasiticidal spectrum, then efficacy against various parasites is improved, but formulation complexity increases
Solution Approach 1:
Multiple active agents (isoxazoline, moxidectin, praziquantel) are merged into a single oral dosage form containing multiple granulate types. This combining approach broadens the parasiticidal spectrum while presenting a unified formulation to the patient, reducing operational complexity despite the multifunctional composition.
Solution Approach 2:
The oral dosage form achieves multi-functionality by incorporating actives that target different parasite classes (ectoparasites, gastrointestinal nematodes, flukes, tapeworms). A single formulation performs multiple parasiticidal functions, eliminating the need for separate treatments and simplifying the overall treatment regimen.
3Reliability
If active agents are included at effective doses, then parasiticidal activity is improved, but solubility and bioavailability problems worsen
Solution Approach 1:
The formulation utilizes parameter changes in the physical and chemical properties of the system by incorporating specific excipients that modify the solubility environment. These excipients change the dissolution parameters to enhance the bioavailability of poorly soluble actives like moxidectin and praziquantel while maintaining effective parasiticidal doses.
Data Source
AI summary
Palatable oral dosage formulations are provided including an effective amount of an isoxazoline parasiticidal agent, an avermectin, and a pyrazinoisoquinoline, and optionally one or more additional active ingredients, such as a tetrahydropyrimidine.