Spray-Dried Triptan Powders for Pulmonary Delivery

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Solution Overview

Problem

Current treatments for migraine, particularly those involving sumatriptan, often face challenges in delivering the drug effectively to the pulmonary system for rapid relief, as existing formulations may not provide stable and efficient pulmonary administration.

Innovation Solution

Development of stable, spray-dried particle formulations of triptans like sumatriptan or their pharmaceutically acceptable salts, designed for pulmonary delivery, which include specific particle size and density characteristics, and combinations with phospholipids, salts, and excipients to optimize deposition in the respiratory tract.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If triptan is formulated for pulmonary delivery, then rapid relief from migraine symptoms is achieved, but formulation stability and effective pulmonary administration are compromised

Engineering Contradiction:
Improveonset of actionVSAvoidformulation stability
Core Design Contradiction:
SpeedVSReliability

Solution Approach 1:

The patent changes the physical and chemical parameters of the triptan formulation by converting it into a spray-dried particulate form with specific characteristics (particle size 1-10 μm, amorphous or crystalline structure, specific surface area 0.5-5.0 m²/g). This parameter transformation enables both rapid pulmonary delivery and formulation stability, resolving the contradiction between speed of action and reliability.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite particulate formulation combining triptan with pharmaceutically acceptable excipients, carriers, and stabilizers. This composite structure maintains drug stability while enabling effective pulmonary delivery, thus resolving the contradiction between formulation stability and rapid onset of action.

Inventive Principle:
Principle #40Composite materials

2Manufacturing precision

If particle size is reduced for better pulmonary deposition, then deposition efficiency is improved, but manufacturing complexity increases

Engineering Contradiction:
Improveparticle size controlVSAvoidformulation complexity
Core Design Contradiction:
Manufacturing precisionVSDevice complexity

Solution Approach 1:

The patent replaces complex mechanical particle size control methods with a spray-drying process that inherently produces particles of the desired size range (1-10 μm) through controlled atomization and rapid drying. This substitution simplifies manufacturing while achieving the required precision in particle size control for optimal pulmonary deposition.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

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 formulations enable effective pulmonary delivery of triptans, providing rapid relief from migraine symptoms by ensuring optimal deposition in the respiratory tract, thereby improving treatment efficacy.

Implementation Method 1

spray-dried particles (also referred to herein as 'powders' or 'dry powders') comprising the triptan or pharmaceutically acceptable salt thereof

Methodology Applied
Scientific EffectAerosol: Aerosol

Implementation Method 2

dispersing the powder by breath actuation of the patient

Methodology Applied
Scientific EffectDispersion: Dispersion (of waves)

Data Source

PatentUS10034857B2Triptan powders for pulmonary delivery
Publication Date: 2018.07.31 CIVITAS THERAPEUTIC INC
  • US10034857B2 patent drawing

AI summary

The invention provides stable, spray-dried, particle formulations containing a triptan, preferably sumatriptan, or a pharmaceutically acceptable salt thereof, which are useful for pulmonary administration to the respiratory tract of a patient for the treatment of disease.