Abstract. Transdermal films of the furosemide were developed employing ethyl cellulose and hydroxypropyl methylcellulose as film formers. The effect of binary mixture of polymers and penetration enhancers on physicochemical parameters including thickness, moisture content, moisture uptake, drug content, drug-polymer interaction, and in vitro permeation was evaluated. In vitro permeation study was conducted using human cadaver skin as penetration barrier in modified Keshary-Chein diffusion cell. In vitro skin permeation study showed that binary mixture, ethyl cellulose (EC)/hydroxypropyl methylcellulose (HPMC), at 8.5:1.5 ratio provided highest flux and also penetration enhancers further enhanced the permeation of drug, while propylene glycol showing higher enhancing effect compared to dimethyl sulfoxide and isopropyl myristate. Different kinetic models, used to interpret the release kinetics and mechanism, indicated that release from all formulations followed apparent zero-order kinetics and nonFickian diffusion transport except formulation without HPMC which followed Fickian diffusion transport. Stability studies conducted as per International Conference on Harmonization guidelines did not show any degradation of drug. Based on the above observations, it can be reasonably concluded that blend of EC-HPMC polymers and propylene glycol are better suited for the development of transdermal delivery system of furosemide.

A series of 4-[4-(2, 4-dichloro-5-fluorophenyl)-6-(4-methoxyphenyl)pyrimidine-2-yl]-1-(arylaminocarbonyl/thiocarbonyl)semicarbazides was synthesized and their in vitro antibacterial activity was studied.In recent decades, the problems of multi-drug resistant microorganisms have reached alarming level in many countries around the world. Recent clinical reports published in the United State and European countries make an emphasis on increasing occurrence of meticillin-resistant S. aureus and other antibiotic-resistant human pathogenic microorganisms. Infections caused by those microorganisms pose a serious challenge to the medical community and need for an effective therapy has stimulated a search for novel antimicrobial agents. Chalcones are a class of privileged structure that have a wide range of biological properties [1] including anticancer [2], antimalarial [3 -4], antiviral [5], and antibacterial activities [6].Pyrimidine scaffold and its derivatives being components of a number of drugs are responsible for their biological, pharmaceutical and therapeutic activity [7]. Pyrimidine derivatives are attractive due to their pharmacological activity [8 -9] and possess antiviral [10], antitumor [11], antibacterial [12 -13], antihypertensive [14], and antituberculous properties [15]. Diaryl pyrimidine (DAPY'S) appears to be most effective against a wild type and various mutant strains of . In this work, we report the results of synthesis and biological assessment of some substituted pyrimidine derivatives. EXPERIMENTAL CHEMICAL PARTAll the reagents were of analytical grade and used directly. Melting points were determined in the open glass capillary and were uncorrected. Progress of the reaction was monitored by thin layer chromatography (TLC) using silica gel-G coated aluminum plates (0.5 mm thickness, Merck). Spots were visualized under UV radiation. All the components were purified by crystallization. Elemental analyses were carried out on PERKIN ELMER 2400. The IR spectra were recorded on BRUKER TENSOR Series using KBr pellets. 1 H NMR spectra were recorded on 300 MHz BRUKER ULTRASHIELD using DMSO-d 6 as a solvent and TMS as an internal reference and chemical shift values were expressed in d ppm. Table 1 and Table 2 present physicochemical and spectral data, respectively. 1-(2,4-Dichloro-5-fluorophenyl)-3-(4-methoxyphenyl)-2-propen-1-one (III).To a well stirred solution of 2,4-dichloro-5-fluoroacetophenone I (10.0 g, 0.048 mol) and 4-methoxybenzaldehyde II (6.53 g, 0.048 mol) in methanol (50 ml) 20% NaOH solution (10 ml) was added. The reaction mixture was stirred for 30 min at room temperature and left overnight. The progress of the reaction was monitored by TLC using toluene: acetone (8:2) as eluent. After completion of the reaction the mixture obtained was poured into ice-cold water, acidified, filtered and crystallized from ethanol to give III. Yield 70% (m.p. 120 -122°C). 2-Amino-4-(2,4-dichloro-5-fluorophenyl)-6-(4-methoxyphenyl)-pyrimidine (IV).A mixture of III (8.0 g, 0.024 mol), guanidine nitrate (4.39 ...

A series of urea and thiourea derivatives of s-triazine have been developed based on high yielding nucleophilic substitution of 2,4,6-trichloro-1,3,5-triazine by 4-hydroxy coumarin, cyclopropylamine and ammonia at suitable conditions. These were further treated with various substituted aryl isocyanate and aryl isothiocyanate. All the synthesized compounds were evaluated for their antibacterial activities against various Gram-positive and Gram-negative strains of bacteria. A few compounds showed good to superior in vitro antibacterial activity against S.aureus, B.subtilis, E.coli and P.aeruginosa respectively. The new synthesized compounds were characterized using IR, 1 H-NMR and elemental analysis.

No abstract

Satellite communication systems operating at Ka band and Ku band frequencies must affect the problem of propagation impairments which includes fading due to rain, clouds, snow for obtaining the required performance. Rain affects the signal most and involved is absorption & scattering. Auto-Regressive Integrated Moving Average (ARIMA) model is used to generate and predict the time series values for rain attenuation. The predicted values obtained for different window size of the ARIMA model and analysis is done in terms of error matrix

No abstract

Aim: Brexpiprazole (BPZ) is a typical antipsychotic drug used for the treatment of schizophrenia and depression. It is classified under BCS class-II with low aqueous solubility and high intestinal permeability. In the present investigation, a solid dispersion of BPZ was prepared to improve the solubility. A transdermal patch was optimized using the central composite design to control the delivery of BPZ. Place and Duration of Study: The formulation was prepared and characterized at K. B. Institute of Pharmaceutical Education and Research, Gandhinagar, Gujarat, India during January 2021 to September 2021. Methodology: A solid dispersion of BPZ was prepared using PEG 6000.A transdermal patch of BPZ was prepared and optimized using central composite design. Independent variables were fixed as ratio of RLPO: RSPO=2:1 (X1) and conc. of plasticizer (Triacetin) %W/W of polymer (X2). Dependent variables were fixed as folding endurance% (Y1) and cumulative % drug release at 24, 48, 72 and 96 hrs respectively (Y2-Y5) for the optimization of transdermal patch of SD of BPZ. Optimized formulation was characterized fully for its safety and efficacy using ex- vivo permeation study, skin irritation study and stability study. Result: The tensile strength of optimized patch was 2.1±0.045 Kg/cm2. The thickness and hardness of patch was 0.0478±0.025 and 80.54±2.64gm/mm. The moisture content and moisture uptake values were 5.2%±0.36 and 6.21±0.24% respectively. Drug content was found to be 99.41±2.64%. The flux value obtained from BRX-SD-TP was 0.06 µg/cm2h. The flux was very proximal to the desired flux value. Prepared formulation was non-irritant and stable. Conclusion: From the findings it can be concluded that BRX-SD-TP was successfully developed for treatment of Schizophrenia.

In the current investigation, some newer triazines merged benzothiazole hybrids were subjected to molecular properties prediction, drug-likeness, lipophilicity and solubility parameters determination using Molinspiration, Molsoft and ALOGPS 2.1 softwares. Amongst ten proposed analogues only seven therapeutic candidates were chosen on the basis of Lipinski's "Rule of Five". Selected title compounds were synthesized by cyclizing 3-chloroaniline and potassium thiocyanate in presence of bromine yielded the corresponding 2-amino benzothiazole synthon, which on further treatment with different substituted aromatic aldehydes afforded Schiff's bases. The later one condensed with phenyl isothiocyanate gave triazine merged benzothiazole analogues (4a-4j). The structural 1 confirmation of the target compounds were established on the basis of IR, HNMR and Mass spectral analysis and subjected to in-vitro anti-inflammatory and anti-oxidant screening. Compound 4c and 4g showed pronounced antioxidant and ant-inflammatory activity respectively. The phenyl ring of triazine bearing -OH and -OCH exhibited good biological activity and their predicted drug-likeness model score also found to be convincing among the series. MATERIALS AND METHODS General:All the reagents and chemicals used were of analytical grade. Melting points were determined by open capillary tube method and are uncorrected. The progress of reaction and purity of the products were monitored by TLC and spots were located by UV chamber and iodine vapour.