Thyroid Hormone Dry Powder Inhalation Carrier Stability

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Solution Overview

Problem

Current dry powder compositions for inhalation of thyroid hormones, particularly those using lactose monohydrate as a carrier, are not stable due to lactose's reducing sugar nature, which is incompatible with thyroid hormones, leading to instability and unsuitability for inhalation.

Innovation Solution

Development of dry powder compositions using non-reducing sugars or sugar alcohols like trehalose, raffinose, mannitol, and isomaltitol as single carriers for thyroid hormone drugs, with micronized particle sizes optimized for inhalation, eliminating the need for additional excipients and enhancing stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If lactose monohydrate is used as a carrier for thyroid hormone dry powder compositions, then the composition can be formulated for inhalation, but the stability of the thyroid hormone deteriorates due to lactose's reducing sugar nature

Engineering Contradiction:
Improveformulation capabilityVSAvoidthyroid hormone stability
Core Design Contradiction:
Ease of manufactureVSStability of the object's composition

Solution Approach 1:

The patent changes the chemical parameter of the carrier from a reducing sugar (lactose) to a non-reducing sugar or sugar alcohol (trehalose, raffinose, mannitol, or isomaltitol). This parameter change eliminates the chemical incompatibility with thyroid hormones while maintaining the carrier's physical properties necessary for inhalation formulation.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent replaces the commonly used lactose carrier with alternative carriers that provide superior stability. Although these alternatives may be slightly more expensive, they eliminate the need for additional stabilizing excipients and provide long-term stability without degradation, effectively replacing multiple components with a single superior carrier.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

2Stability of the object's composition

If multiple excipients are added to stabilize thyroid hormone in dry powder composition, then the stability improves, but the composition complexity increases

Engineering Contradiction:
Improvethyroid hormone stabilityVSAvoidcomposition complexity
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The patent extracts and eliminates the need for multiple stabilizing excipients by selecting a carrier (non-reducing sugar or sugar alcohol) that inherently provides stability. This removes unnecessary components from the formulation, simplifying the composition while maintaining or improving stability.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The selected carrier performs multiple functions simultaneously: it serves as the inhalation carrier, provides structural support for particle formation, ensures proper flow properties, and most importantly, provides chemical stability to the thyroid hormone without requiring additional stabilizing agents.

Inventive Principle:
Principle #6Universality (Multi-functionality)

3Ease of manufacture

If thyroid hormone is administered orally, then the absorption is affected by food and drug interactions, but the formulation is simpler

Engineering Contradiction:
Improveformulation simplicityVSAvoidabsorption consistency
Core Design Contradiction:
Ease of manufactureVSReliability

Solution Approach 1:

The patent uses the non-reducing sugar or sugar alcohol carrier as an intermediary that enables pulmonary delivery of the thyroid hormone. This intermediary route (inhalation through respiratory mucosa) bypasses the gastrointestinal tract and its interactions with food and drugs, providing consistent and reliable absorption while maintaining formulation simplicity.

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentUS11786460B2Pharmaceutical dry powder composition for inhalation comprising a thyroid hormone
Publication Date: 2023.10.17 TSETI IOULIA

AI summary

The invention relates to dry powder compositions, suitable for inhalation through an appropriate inhalation device, comprising a thyroid hormone drug and a non-reducing sugar or sugar alcohol as a single carrier. The preparations of the invention show higher stability than the corresponding ones with lactose monohydrate, a commonly used carrier for dry powder preparations.