Efficient drug development of oseltamivir capsules based on process control, bioequivalence and PBPK modeling.

Oseltamivir phosphate is used to treat influenza. For registration of a generic product, bioequivalence studies are crucial, however, studies can sometimes replace the conventional human pharmacokinetic. To assess whether the dissolution profile is comparable with the release, physiologically based pharmacokinetic absorption models (PBPK) are being used.

Challenging identification of polymorphic mixture: Polymorphs I, II and III in olanzapine raw materials.

Olanzapine (OLZ), a drug for the treatment of schizophrenia, presents in more than 60 crystal forms. Polymorphs I, II and III were reported, however, the preparation conditions for pure II and III have not been reported. Polymorph IV was reported but this form is actually polymorph II described at different temperature.

Vibrational spectroscopic and Hirshfeld surface analysis of carvedilol crystal forms.

The drug carvedilol, used to treat cardiovascular conditions, is known to exist in distinct crystalline forms. Polymorphs II and III and the hydrate are characterized by variations in their molecular packing and conformation. This study deals with the spectroscopic (supported by quantum chemistry calculations) characterization of carvedilol structures.

Efavirenz Dissolution Enhancement IV-Antisolvent Nanocrystallization by Sonication, Physical Stability, and Dissolution.

Efavirenz is a fundamental drug in the HIV therapy; however, it has a low bioavailability due to low water solubility. Particle nanonization should enhance its dissolution and therefore its bioavailability. Nanocrystallization is a promising technique for preparing drug nanocrystals.

Efavirenz dissolution enhancement III: Colloid milling, pharmacokinetics and electronic tongue evaluation.

Efavirenz (EFV), a non-nucleoside reverse transcriptase inhibitor (NNRTI), is part of first-line therapy for the treatment of human immunodeficiency virus type 1 infection (HIV-1/AIDS). This drug shows relatively low oral absorption and bioavailability, as well as high intra- and inter-subject variability. Several studies have shown that treatment failure and adverse effects are associated with low and high EFV plasma concentrations, respectively.

Evaluation and correlation of the physicochemical properties of carvedilol.

Carvedilol is an antihypertensive drug with non-selective blockade (moderate selectivity for β1 and β2 adrenoceptors) and vasodilating properties due to α receptor blockade. Its molecule has one chiral centre; therefore, the drug has two enantiomers. Furthermore, it presents different polymorphs depending on the synthesis route and crystallization procedure.

Galenic approaches in troubleshooting of glibenclamide tablet adhesion in compression machine punches.

This study aimed to examine the adhesion of glibenclamide 5 mg tablets to the tools of compression machines. This problem is not commonly reported in the literature, since it is considered as tacit knowledge. The starting point was the implementation of three technical alternatives: changing the parameters of compression, evaluating the humidity of the powder blend and the manufacturer of the lubricant magnesium stearate.

Further study of (+/-)-mefloquinium chloride solvates. Crystal structures of the hemihydrate and monohydrate of (+/-)-mefloquinium chloride, from data collected at 120 K.

The crystal structure of a monohydrate of (+/-)-mefloquinium chloride, (+/-)-[MEFHCl.(H(2)O)], has been obtained from data collected at 120 K. Further details of the crystal structure of a hemihydrate, (+/-)-[MEFHCl*(1/2)(H(2)O)], previously determined at room temperature, are also reported from data collected at 120 K.