SYNTHESIS AND BIOLOGICAL EVALUATION OF THE DERIVATIVES OF 1,3,5-TRIAZIN-2,4-DIONES AND THEIR FUSED ANALOGUES.

Ph.DDOCTOR OF PHILOSOPH

Effect of citric acid and polymer blend on characteristics of ofloxacin floating matrix tablets by factorial design

The present investigation deals with the development of floating matrix tablet containing Ofloxacin, to prolong the gastric residence time, thereby effective in eradication of Helicobacter pylori from the gastric mucosa. A 32 factorial design was employed to formulate floating matrix tablet selecting polymer blend ratio [hydroxypropyl methylcellulose (HPMC) / sodium carboxymethylcellulose (SCMC)] and content of citric acid as independent variables. Time required for 50 % of drug release (t50 %), percentage drug release at 8 h (Q8), floating duration (h) and diffusion exponent (n) were selected as dependent variables. Multiple regression analysis with two way ANOVA revealed statistically significant effect of the two independent variables on the responses studied (P 8 varied from ~ 76 % to ~100 % whereas t50 % ranged from 1.7 h to 3.7 h. The kinetics of drug release fitted best to Higuchi diffusion controlled model.Colegio de Farmacéuticos de la Provincia de Buenos Aire

4-Carbethoxy-1-[4-(N,N-dimethylamino)benzoyl]thiosemicarbazide

The mol­ecular structure of the title compound, C13H18N4O3S, (systematic name: ethyl N-{2-[4-(dimethyl­amino)benzo­yl]hydrazinethio­carbon­yl}carbamate) is stabilized by intra­molecular N—H⋯O=C hydrogen bonding arranged in an S(6) graph-set motif. In the crystal, inversion dimers connected via inter­molecular N—H⋯S=C hydrogen bonds [R 2 2(8) graph-set motif] form sheets parallel to the (21) plane. Dimers are also formed by the mol­ecules via weak inter­molecular N—H⋯S=C hydrogen bonds [R 2 2(10) graph-set motif] connecting the sheets

Pharmaceutical strategies to extend pulmonary exposure of inhaled medicines

Pulmonary administration route has been extensively exploited for the treatment of local lung diseases such as asthma, chronic obstructive pulmonary diseases and respiratory infections, and systemic diseases such as diabetes. Most inhaled medicines could be cleared rapidly from the lungs and their therapeutic effects are transit. The inhaled medicines with extended pulmonary exposure may not only improve the patient compliance by reducing the frequency of drug administration, but also enhance the clinical benefits to the patients with improved therapeutic outcomes. This article systematically reviews the physical and chemical strategies to extend the pulmonary exposure of the inhaled medicines. It starts with an introduction of various physiological and pathophysiological barriers for designing inhaled medicines with extended lung exposure, which is followed by recent advances in various strategies to overcome these barriers. Finally, the applications of the inhaled medicines with extended lung exposure for the treatment of various diseases and the safety concerns associated to various strategies to extend the pulmonary exposure of the inhaled medicines are summarized