No abstract

(10 examples, yields not given) are synthesized and evaluated for their antimicrobial activities. Derivatives (VIIIa), (VIIId) show good antibacterial activities and compound (VIIIe) displays good antifungal activity against C. albicans. -(SHAH*, S. H.; PATEL, P. S.; J. Indian Chem.

A new series of 4-(4-hydroxyphenyl)-3-chloro-1-{4-[5-(substituted phenyl)-1-phenyl-4,5dihydro-pyrazol-3-yl]phenyl}azetidin-2-one were synthesized by reacting 3-chloro-1-{4-[3-(substituted-phenyl)prop-2-enoyl]phenyl}-4-(4-hydroxyphenyl)azetidin-2-one (0.01 M) and phenyl hydrazine (0.01 M) in presence of acetic acid (glacial). All these compounds were characterized by means of their IR, 1 H NMR, spectroscopic data and microanalysis. All the synthesized products were evaluated for their antimicrobial activity. All the compounds were tested for their antibacterial and antifungal activities by broth dilution method.

Elementary osmotic pumps (EOP) are well known for delivering moderately soluble drugs at a zero order rate. A push-pull osmotic system was developed and commercialized for poorly water-soluble drugs [Procardia XL (Nifedipine), Glucotrl XL (Glipizide)]. However, the technology is complex comprising of bilayer compression and the suspension of drug formed in the core has more viscosity and has to withstand the osmotic pressure within the tablet, for which the membrane must be thicker than that of EOP. The aim of the present study was to develop a solid dispersion based EOP system for a poorly water-soluble drug, nifedipine and deliver it in a zero order fashion over an extended period of time. Solid dispersions were prepared by hot melt technique using Poloxamer-188 at various ratios of drug and polymer (1:1, 1:5 and 1:10, on weight basis) and investigated for solubility study. Formation of complex and decrease in crystallinity was confirmed from differential scanning calorimetry (DSC) and X-ray crystallography (XRD) study. Core tablets using solid dispersions were prepared and coated with cellulose acetate and PEG-400. An orifice was drilled manually to create passage for drug release. The system was optimized for amount of osmogent, membrane weight gain, amount of plasticiser and diameter of the orifice, to achieve desired release profile. The osmotic system was found to deliver nifedipine at a zero order rate for 20 h. The drug release from the developed formulation was independent of pH and agitational intensity.

Mucoadhesive buccal films of rivastigmine were prepared by the solvent casting technique using HPMC K15M, sodium alginate, glycerine, and Eudragit RL100. Arranged films assessed for weight variation, thickness, % drug substance, % moisture loss, % moisture take-up, folding endurance, in-vitro medicament release, and Fourier transform Infrared spectroscopy (FTIR). The films showed a controlled release (CR) over 8 h. The preparation observed to be a worthy candidate for the development of buccal patches for therapeutic purposes. Drug-polymer compatibility considers FTIR demonstrated no contradiction between the medicament and the polymers. The optimized formulation found F7 indicated drug release 85% at the end of 8 h. Thinking about the correlation coefficient (R2) values got from the kinetic equations, the drug release from the formulations F1-F8 has discovered zero-order release mechanism. It can be concluded that oral buccal patches of rivastigmine, for treatment of Alzheimer’s and Parkinson’s disease, can be formulated. The study suggests that rivastigmine can be conveniently administered orally in the form of buccal patches, with the lesser occurrence of its side effects and improved bioavailability.