Posted by admin on Jan 1, 2012 in |
In order to explore the antihistaminic and anthelmintic activity associated with piperazine framework, several 1-benzhydryl piperazine derivatives and 1- benzhydryl piperazine acyl derivatives were synthesized. Their chemical structure was characterized and confirmed by H1 nuclear magnetic resonance (NMR), Fourier-transform infrared (FTIR). The target compounds were synthesized by the nucleophilic substitution reaction of 1-benzhydryl piperazine with various acyl chlorides. The intermediate (AT-1) was prepared by reaction of benzhydryl chloride and piperazine in presence of anhydrous potassium carbonate in N-N dimethylformamide. Further 1-benzhydrylpiperazine was reacted with various acyl chloride in presence of triethylamine in dichloromethane afforded target compounds (AT5 -9). The anthelmintic activity of compounds were evaluated by Garg and Atal method while antihistaminic activity was evaluated by in- vitro guinea pig...
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Posted by admin on Jan 1, 2012 in |
Various approaches have been used to retain the dosage form in the stomach as a way of increasing the gastric residence time (GRT), including floatation systems; high-density systems; mucoadhesive systems; magnetic systems; unfoldable, extendible, or swellable systems; and superporous hydrogel systems. The aim of this study was to prepare and evaluate floating microspheres of Pioglitazone hydrochloride for the prolongation of gastric residence time. The microspheres were prepared by emulsion solvent diffusion-evaporation method using Eudragit S-100. A full factorial design was applied to optimize the formulation. Preliminary studies revealed that the concentration of polymer and stirring speed significantly affected the characteristics of floating microspheres. The optimum batch of microspheres exhibited some rough surfaces with good flow and packing properties, prolonged sustained drug release, remained buoyant for more than 10 hrs, high entrapment efficiency upto 89%w/w. Scanning electron microscopy confirmed the hollow structure with particle size in the order of 270 µm. The studies revealed that decrease in particle size of the microspheres increase the drug release from the floating microspheres....
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Posted by admin on Jan 1, 2012 in |
The present study attempt to evaluate the physicochemical and phytochemicals parameters of Capparis zeylanica leavesbelong to family Caparadaceae is a climbing shrub found in through out India. The plant is used in folk medicine to treat, rheumatism, abdominal ulcers and hernia, swelling, itching, hepatitis, liver tonic, insect poisoning and anti-inflammatory. But there is no standardization work reported on Capparis zeylanica leaves. Physicochemical parameters, preliminary characterization and phytochemical analysis were carried out. There finding will be useful to words establishing quality control parameters for the standardization of the plant...
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Posted by admin on Jan 1, 2012 in |
The extraction of active compounds from plants is one of the most critical steps in the commercial development of natural products for medicinal and health benefits. In view of the large number of plant species potentially available for study, it is essential to have efficient systems for the rapid and efficient extraction of phytochemicals for further investigation on their properties. The present study involves the use of microwave and ultrasonication as methods to extract phytochemicals from the fruits of Terminalia chebula. The effect of the extraction methods were studied by determining the total phenolic content, tannin content and the antioxidant activity of the extracts. The total phenolic content, tannin content and the antioxidant activity were determined by the Folin Ciocalteau method, Indigo carmine method and the DPPH free radical scavenging assay method respectively. The study revealed a 17.6% increase in the yield of phenolics and a 14% increase in the tannin content of the microwave extracts. A 20.6% increase in the antioxidant activity of the microwave extract was also...
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Posted by admin on Jan 1, 2012 in |
Ibuprofen, a widely prescribed anti-inflammatory and analgesic drug belongs to class II under BCS and exhibit low and variable oral bioavailability due to its poor aqueous solubility. Solid dispersion of ibuprofen in Starch 1500, a modified starch and polyvinyl pyrrolidone (PVP K 30) was investigated to enhance the dissolution rate and to develop ibuprofen tablets with fast dissolution characteristics. The individual and combined (interaction) effects of Starch 1500 and PVP K 30 on the dissolution rate of ibuprofen solid dispersions and tablets were evaluated in a series of 22 – factorial experiments. Solid dispersions and tablets of ibuprofen were formulated employing selected combinations of Starch 1500 and PVP K 30 as per 22 – Factorial design and were evaluated. The individual and combined effects of Starch 1500 and PVP on the dissolution rate of solid dispersions as well as tablets were highly significant (P<0.01). Solid dispersion of ibuprofen in Starch 1500 enhanced the dissolution rate of ibuprofen by 1.40 fold. Addition of PVP K30 to the solid dispersion in...
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