In Situ Co-Amorphization of Olanzapine in the Matrix and on the Coat of Pellets.

In situ amorphization is a promising approach, considered in the present work, to enhance the solubility and dissolution rate of olanzapine, while minimizing the exposure of the amorphous material to the stress conditions applied during conventional processing. The production of pellets by extrusion/spheronization and the coating of inert beads were investigated as novel methods to promote the co-amorphization of olanzapine, a poorly water-soluble drug, and saccharin. Samples were characterized using differential scanning calorimetry, X-ray powder diffraction, Fourier-transform infrared spectroscopy and scanning electron microscopy, and dissolution and stability testing.

Amorphous and Co-Amorphous Olanzapine Stability in Formulations Intended for Wet Granulation and Pelletization.

The preparation of amorphous and co-amorphous systems (CAMs) effectively addresses the solubility and bioavailability issues of poorly water-soluble chemical entities. However, stress conditions imposed during common pharmaceutical processing (e.g.

Sulfonic Acid Derivatives in the Production of Stable Co-Amorphous Systems for Solubility Enhancement.

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.

Downstream Processing of Amorphous and Co-Amorphous Olanzapine Powder Blends.

The work evaluates the stability of amorphous and co-amorphous olanzapine (OLZ) in tablets manufactured by direct compression. The flowability and the compressibility of amorphous and co-amorphous OLZ with saccharin (SAC) and the properties of the tablets obtained were measured and compared to those of tablets made with crystalline OLZ. The flowability of the amorphous and mostly of the co-amorphous OLZ powders decreased in comparison with the crystalline OLZ due to the higher cohesiveness of the former materials.

The Precision and Accuracy of 3D Printing of Tablets by Fused Deposition Modelling.

Tablet manufacture by fused deposition modelling (FDM) can be carried out individually (one tablet printed per run) or as a group (i.e., 'multiple printing' in one run) depending on patient's needs.

Measurement of the amorphous fraction of olanzapine incorporated in a co-amorphous formulation.

Amorphous and co-amorphous formulations have been used to enhance the solubility and bioavailability of poorly water-soluble drugs. However, during handling and/or storage amorphous solids present inherent instability and overtime recrystallize back into their crystalline counterpart. The development of tools capable of quantifying and monitoring the recrystallization of amorphous materials is required to ensure the delivery of solid dosage forms with improved performance.

Are the binary typology models of alcoholism valid in polydrug abusers?

Objective: To evaluate the dichotomy of type I/II and type A/B alcoholism typologies in opiate-dependent patients with a comorbid alcohol dependence problem (ODP-AP).

Methods: The validity assessment process comprised the information regarding the history of alcohol use (internal validity), cognitive-behavioral variables regarding substance use (external validity), and indicators of treatment during 6-month follow-up (predictive validity).

Results: ODP-AP subjects classified as type II/B presented an early and much more severe drinking problem and a worse clinical prognosis when considering opiate treatment variables as compared with ODP-AP subjects defined as type I/A.

The burden of cyclothymia on alcohol dependence.

Background: The relationship between cyclothymic temperament and alcoholism remains insufficiently explored.

Methods: A sample of 125 alcohol-dependent patients diagnosed according to DSM-IV-TR criteria (APA, 2000) was recruited from a clinical setting. Cyclothymic temperament was diagnosed according to the Portuguese version of the Akiskal and Akiskal (2005) temperament scale.