Unlocking Drug Amorphization: Continuous, Solvent-free Twin Screw Granulation

Can you please present yourself and your domiciled astatine Thermo Fisher Scientific?

My sanction is Margarethe Richter, Pharma Application Specialist astatine Thermo Fisher Scientific. I create and trial caller pharmaceutical applications for our extruders, helping customers standard their processes. I activity pinch a scope of techniques, from basking melt extrusion and copy screw granulation to divers dosage forms.

Why is supplier amorphization important successful pharmaceutical development?

Amorphization is simply a awesome method for enhancing a drug’s bioavailability. Many caller molecules are ample and poorly soluble. By converting them to an amorphous state, they dissolve much easy successful h2o and permeate biologic membranes much readily, benefiting efficacy.

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What are nan existent techniques for achieving amorphous supplier states?

Two communal techniques are spray drying and basking melt extrusion. In spray drying, some nan API and excipient are dissolved successful a solvent, which is past evaporated to nutrient an amorphous powder. While effective, this method tin time off down solvent residues and poses handling challenges. Hot melt extrusion, connected nan different hand, eliminates nan request for solvents but relies connected heat-stable APIs and excipients to forestall molecular degradation.

How does mesoporous silica connection a caller way to amorphization?

Mesoporous silica provides an innovative pathway to amorphization by stabilizing nan supplier wrong its porous structure. In this method, nan API is milled together pinch mesoporous silica, allowing nan supplier to stay successful an amorphous authorities arsenic it becomes embedded successful nan silica’s pores. This process intends that we don't request to usage power and solvents, minimizing nan consequence of degradation and contamination. However, accepted shot milling, often utilized to harvester nan materials, is inherently slow, batch-based, and challenging to standard for large-scale manufacturing.

Can copy screw granulation (TSG) beryllium adapted for this silica‑based amorphization?

Yes. We group up a co-rotating copy screw extruder successful granulation mode, utilizing an unfastened tube pinch nary die. The mechanical shear from nan screws efficaciously collapsed down nan silica. Testing pinch a medium-grade alloy setup confirmed that nan silica–API blend was successfully fragmented.

How did you verify nan process achieved afloat amorphization?

We utilized differential scanning calorimetry (DSC) to observe crystalline pouring points and X‑ray diffraction (XRD) to cheque for remaining crystallinity. We ran challenging 50:50 silica:API blends and besides captured SEM images that confirmed particle size simplification and nonaccomplishment of crystals.

What are nan advantages of utilizing TSG for this process?

TSG offers continuous processing pinch elastic formulation integration via aggregate provender ports. This setup enabled accelerated screening of screw configurations and process parameters—adjusting provender rates and screw speeds on‑the‑fly without restarting batches. Only customizing nan screw creation requires little downtime.

How captious is screw configuration?

Extremely. High‑shear, high‑energy mixing is basal to part crystals and beforehand absorption into silica pores. We optimized configurations to present nan basal mechanical energy, arsenic elaborate successful our published data.

About Margarethe Richter

Margarethe Richter is simply a Pharma Application Specialist astatine Thermo Fisher Scientific, focusing connected pharmaceutical processes via copy screw and basking melt extrusion technologies. She holds a grade successful Pharmaceutical Sciences.

At Thermo Fisher, Margarethe has spearheaded projects advancing solvent-free supplier amorphization and worked intimately pinch partners specified arsenic Grace connected silica‑based formulations. Her published activity successful MDPI explores continuous twin screw granulation for amorphous supplier delivery, contributing valuable insights into scalable pharmaceutical manufacturing.

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