alterado para: “Assessment of the stability of drugs in the amorphous and co-amorphous form in extrudates, pellets and tablets designed to circumvent drugs’ alterado para: “Assessment of the stability of amorphous and coamorphous as micro and nanoparticles of drugs in extrudates, pellets and tablets designed to circumvent drug’s poor water solubility’ Production, characterization and assessment of the stability of amorphous and coamorphous drugs as micro and nanoparticles in extrudates, pellets and tablets designed to circumvent drugs’ poor water solubilities

Research Project

alterado para: “Assessment of the stability of drugs in the amorphous and co-amorphous form in extrudates, pellets and tablets designed to circumvent drugs’ alterado para: “Assessment of the stability of amorphous and coamorphous as micro and nanoparticles of drugs in extrudates, pellets and tablets designed to circumvent drug’s poor water solubility’ Production, characterization and assessment of the stability of amorphous and coamorphous drugs as micro and nanoparticles in extrudates, pellets and tablets designed to circumvent drugs’ poor water solubilities

Funder

Fundação para a Ciência e a Tecnologia

Organizational Unit

Publications

Sulfonic acid derivatives in the production of stable co-amorphous systems for solubility enhancement

Publication . Costa, Nuno F. da; Santos, Inês A.; Fernandes, Ana I.; Pinto, João F.

"Co-amorphization is a promising approach to stabilize drugs in the amorphous form. Olanzapine, a poorly water-soluble drug was used in this study. Sulfonic acids (saccharin, cyclamic acid and acesulfame), free and in salt forms, were used as co-formers and compared with carboxylic acids commonly used in the preparation of co-amorphous systems. Several manufacturing techniques were tested, and the co-amorphous systems characterized by differential scanning calorimetry, X-ray powder diffraction, thermogravimetry and Fourier-transform infrared spectroscopy. Free sulfonic acids produced co-amorphous systems with the drug, unlike their salts. Spectroscopy data suggests the formation of salts between olanzapine and the sulfonic acids, used as co-formers. The co-amorphous system produced with saccharin by solvent evaporation, showed the most notable solubility enhancement (145 times). The stability of amorphous and co-amorphous olanzapine systems was assessed upon exposure to stress conditions during storage. Amorphized olanzapine readily reconverted back to the crystalline form while sulfonic acids:olanzapine co-amorphous were stable for up to 24 weeks in low/medium humidity conditions (11-75% RH). Results highlight the potential advantages offered by sulfonic acids as co-formers to produce stable and more soluble co-amorphous olanzapine."

2022-12Journal article

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