An Advanced Twin-Screw Granulation Technology: The Use of Non-Volatile Solvents with High Solubilizing Capacity

Overview

Journal AAPS PharmSciTech

Publisher Springer

Specialty Pharmacology

Date 2024 Jul 31

PMID 39085532

Authors

Siva Satyanarayana Kolipaka

Laura Andrade Junqueira

Steven Ross

Vivek Garg

Md Sadeque Hossein Mithu

Saumil Bhatt

Dennis Douroumis

Affiliations

Soon will be listed here.

Abstract

Purpose: Twin-screw wet granulation (TSWG) is a manufacturing process that offers several advantages for the processing of water-insoluble active pharmaceutical ingredients (APIs) and has been used for increasing the solubility and dissolution rates. Here we introduce a novel TSWG approach with reduced downstream processing steps by using non-volatile solvents as granulating binders.

Methods: Herein, TSWG was carried out using Transcutol a non-volatile protic solvent as a granulating binder and dissolution enhancer of ibuprofen (IBU) blends with cellulose polymer grades (Pharmacoat 603, Affinisol™, and AQOAT).

Results: The physicochemical characterisation of the produced granules showed excellent powder flow and the complete transformation of IBU into the amorphous state. Dissolution studies presented immediate release rates for all IBU formulations due to the high drug-polymer miscibility and the Transcutol solubilising capacity.

Conclusions: Overall, the study demonstrated an innovative approach for the development of extruded granules by processing water-insoluble APIs with non-volatile solvents for enhanced dissolution rates at high drug loadings.

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