Process for the Production of Spray-Freeze-Dried Particles and Particles Produced Accordingly

Simple SummaryContent extracted from patent full text and abstract with AI.

The invention provides a method for making spherical, spray-freeze-dried pharmaceutical particles with excellent flowability and mechanical stability. It involves preparing a solution of an active pharmaceutical ingredient (API) with a specific solvent, spraying this solution into a very cold environment to quickly freeze droplets, and then drying them through sublimation (either under vacuum or at atmospheric pressure). The process is optimized by using certain solvents and solid contents, allowing for the production of amorphous or partially crystalline, porous particles even with compounds that are poorly soluble in water.

Use CasesContent extracted from patent full text and abstract with AI.

• Preparation of powder forms of poorly water-soluble or thermolabile drugs for oral, nasal, buccal, or injectable delivery.
• Manufacturing inhalable pharmaceutical powders for pulmonary drug delivery.
• Production of rapid-dissolving tablets or reconstitutable suspensions for patients who have swallowing difficulties.
• Creation of stable protein or peptide drug powders with enhanced storage and handling properties.
• Formulation of drugs with improved dissolution rates and bioavailability, such as painkillers (e.g., Celecoxib), antibiotics (e.g., chloramphenicol), or cannabinoid mixtures for medicinal purposes.
• Processing of plant extracts into well-flowing powder mixtures containing multiple active ingredients (e.g., cannabis extracts).

BenefitsContent extracted from patent full text and abstract with AI.

• Enables gentle drying of thermolabile (heat-sensitive) drugs, preserving their activity.
• Improves the flowability and handling of pharmaceutical powders, facilitating accurate dosing and manufacturing.
• Allows for the use of lipophilic and poorly water-soluble drugs by dissolving them in non-aqueous solvents like tert-butanol.
• Produces spherical, porous particles with enhanced dissolution rates compared to crystalline forms, potentially increasing the effectiveness of the medication.
• Yields amorphous or partially crystalline structures with good mechanical stability, which can simplify further processing (e.g., tableting).
• The process is adaptable to a variety of active ingredients, excipients, and end-use requirements, including highly complex formulations like protein drugs or combination therapies.
• Can be used for continuous production, supporting large-scale pharmaceutical manufacturing.

Technical Classifications (CPCs)

Inventors & Applicants

Patent Abstract

The invention relates to a method for producing spray-freeze-dried pharmaceutical particles, comprising the following steps: a) providing a solution comprising at least a pharmaceutical active ingredient and a solvent, b) spraying the solution into a cold environment, whereby solidified droplets are obtained, and c) removing the solvent by means of atmospheric sublimation or vacuum freeze drying, whereby spherical spray-freeze-dried particles are obtained. In step a), the solvent is selected from tert-butanol, dimethyl sulfoxide, water and mixtures thereof, and the solution has a solids content in the range of ≥ 1.5% to ≤ 60%, in relation to the total volume of the solution (m/V). In step b), drops having an average diameter in the range of ≥ 30 μm to ≤ 700 μm are produced. The drops are sprayed into an environment having a temperature in the range of ≥ -100 °C to ≤ 20 °C.