Mechanical Characterization of Pharmaceutical Powders by Nanoindentation and Correlation with Their Behavior during Grinding.

Controlling the size of powder particles is pivotal in the design of many pharmaceutical forms and the related manufacturing processes and plants. One of the most common techniques for particle size reduction in the process industry is powder milling, whose efficiency relates to the mechanical properties of the powder particles themselves. In this work, we first characterize the elastic and plastic responses of different pharmaceutical powders by measuring their Young modulus, the hardness, and the brittleness index via nano-indentation.

Clinical pharmacology study of Bramitob, a tobramycin solution for nebulization, in comparison with Tobi.

Background And Objectives: To compare in vitro characteristics and pharmacokinetics of Bramitob, a preservative-free tobramycin solution for nebulization, and Tobi in patients with cystic fibrosis (CF) and Pseudomonas aeruginosa infection.

Methods: In vitro characteristics of Bramitob and Tobi were evaluated using Pari TurboBoy/LC Plus and the Systam 290 LS nebulizers. In the randomized, double-blind, two-way crossover pharmacokinetic study, 11 patients with CF received a single nebulized dose (300mg) of Bramitob or Tobi, separated by a 7-day washout period.

New basic esters of 2-phenyl-3-methyl-4-oxo-4H-1-benzopyran-8-carboxylic acid endowed with spasmolytic properties. Synthesis and pharmacological-pharmacokinetic evaluation.

In order to obtain new analogs of flavoxate endowed with higher stability and possibly higher potency, a new series of basic esters of 2-phenyl-3-methyl-4-oxo-4H-1-benzopyran-8-carboxylic acid (MFCA) has been prepared and investigated. Derivatives in which the structure of flavoxate was modified by branching and lengthening of the estereal alkyl chain were synthesized, together with the conformationally restricted N-piperidinyl derivatives. Esters containing in their structure various alicyclic tertiary amines which are present in natural or synthetic drugs endowed with spasmolytic properties, mainly of anticholinergic nature, were also prepared.

Synthesis and anticonvulsant activity of N-(benzoylalkyl)imidazoles and N-(omega-phenyl-omega-hydroxyalkyl)imidazoles.

A novel series of N-(benzoylalkyl)imidazoles and N-(omega-phenyl-omega-hydroxyalkyl)imidazoles was synthesized and evaluated for anticonvulsant activity in mice against maximal electroshock induced seizures. Some of the compounds showed an activity comparable to or better than phenytoin and phenobarbital. The N-[beta-[4-(beta-phenylethyl)phenyl]-beta-hydroxyethyl]imidazole (38) was selected for further studies; preclinical toxicology and additional efficacy evaluations are in progress.

[Condensation of N-alkyl-o-phenylendiamine with ethyl benzoylacetate].

By reaction in hot xylene of ethyl benzoylacetate with N-methyl-o-phenylenediamine (I a) and N-benzyl-o-phenylenediamine (I b) three five-membered ring compounds and one seven-membered ring compound were obtained. Compounds isolated were: 1-alkyl-2-phenacylbenzimidazoles (III), 1-alkyl-2-phenylbenzimidazoles (V), 1-alkyl-2-methylbenzimidazoles (VI) and 1-alkyl-4-phenyl-1,3-dihydro-2H-1,5-benzodiazepine-2-ones (IV). In the reaction with N-benzyl-o-phenylenediamine we isolated also the N-benzyl-2-benzoylacetamidoaniline (II b), which by further heating in xylene gave (IV b).