Stabilizing Macrocyclic Lactones in Soft Chewable Veterinary Dosage Forms

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Solution Overview

Problem

Soft chewable veterinary dosage forms containing isoxazoline compounds and macrocyclic lactones face stability issues, leading to degradation products and content uniformity problems, which affect the shelf life and bioavailability of the macrocyclic lactones.

Innovation Solution

A soft chewable veterinary dosage form is developed, comprising a systemic insecticide, a forming agent, filler, liquid component, flavor, and an aggregate of physiologically active macrocyclic lactone, binder, and core material, where the macrocyclic lactone is stabilized through melt processing with the binder and core material to form a homogeneous aggregate, ensuring reduced degradation and improved stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If macrocyclic lactones are added to soft chewable veterinary formulation, then the spectrum of parasites controlled is broadened, but the macrocyclic lactones form significant degradation products and are not stable enough

Engineering Contradiction:

Improvespectrum of parasites controlledVSAvoidstability of macrocyclic lactone

Core Design Contradiction:

Adaptability or versatilityVSStability of the object's composition

Solution Approach 1:

A carrier substance is introduced as an intermediary between the macrocyclic lactone and the formulation matrix. This carrier substance forms a stable complex with the macrocyclic lactone, preventing its degradation while maintaining its parasiticidal activity. The carrier acts as a protective intermediary that allows the macrocyclic lactone to coexist stably with other formulation components.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite material system where the macrocyclic lactone is combined with specific carrier substances and formulation components to form a stable composite dosage form. This composite structure provides both the broadened parasite spectrum control and the stability needed for shelf life, as the composite material protects the macrocyclic lactone from degradation while maintaining its biological activity.

Inventive Principle:

Principle #40Composite materials

2Quantity of substance

If macrocyclic lactones are present in small amounts in soft chewable dosage form, then the dosage form can be formulated, but content uniformity becomes difficult to ensure

Engineering Contradiction:

Improveamount of macrocyclic lactoneVSAvoidcontent uniformity

Core Design Contradiction:

Quantity of substanceVSManufacturing precision

Solution Approach 1:

The dosage form is segmented into multiple components, with the macrocyclic lactone being incorporated into discrete units or particles that are then distributed throughout the formulation. This segmentation allows for better control and uniform distribution of the small amount of macrocyclic lactone, ensuring consistent content across multiple dosage units while maintaining the low concentration required for effective formulation.

Inventive Principle:

Principle #1Segmentation

3Duration of action of stationary object

If the shelf life of the dosage form is extended, then storage under harsh conditions is improved, but degradation products of macrocyclic lactones increase

Engineering Contradiction:

Improveshelf lifeVSAvoiddegradation products

Core Design Contradiction:

Duration of action of stationary objectVSObject-generated harmful factors

Solution Approach 1:

Stabilizing agents and protective formulations are incorporated into the dosage form in advance to prevent degradation before it occurs. These preliminary protective measures counteract the harmful effects of degradation by blocking degradation pathways or neutralizing degradation products, thereby extending shelf life without increasing harmful degradation products.

Inventive Principle:

Principle #9Preliminary anti-action

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 stabilization of macrocyclic lactones in the dosage form enhances their stability, reduces degradation products, and maintains bioavailability, allowing for longer shelf life and storage under harsh conditions without compromising content uniformity.

Implementation Method 1

an aggregate comprising (f1) one or more physiologically active macrocyclic lactone(s), (f2) binder, (f3) core material, wherein the core material (f3) is intimately associated with binder (f2) and physiologically active macrocyclic lactone (f1)

Methodology Applied

Scientific EffectMelt processing: Melting

Data Source

PatentUS20220323421A1Soft Chewable Veterinary Dosage Form

Publication Date: 2022.10.13 INTERVET INC

AI summary

The present application relates to a soft chewable veterinary dosage form comprising a systemic parasiticide as well as a physiologically active macrocyclic lactone and to a method for preparing said soft chewable veterinary dosage form.