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Fundação para a Ciência e a Tecnologia

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Publications

Drug-excipient and drug-drug mixtures : a pathway for the production of co-amorphous entities

Publication . Costa, Nuno F. da; Fernandes, Ana Isabel; Pinto, João F.

2018-06-20Conference object

Open access

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

Restricted access

Development of an at-line method to monitor the conversion of amorphous into crystalline Olanzapine, in dry blends of wet masses

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

2019-03-25Conference object

Open access

Comparison of the co-amorphization ability of Olanzapine with amino, carboxylic and sulfonic acids

Publication . Bastos, Ana C.; Costa, Nuno F.; Fernandes, Ana I.; Pinto, João F.

2019-03-25Conference object

Open access