INDO AMERICAN JOURNAL OF PHARMACEUTICAL SCIENCES

1352-1365

Authors: Wagh Supriya R1 , Arsul Vilas A2 , Gadade Deepak D1 ,Rathi Pavan B1

The objective of present study was to improve the dissolution rate of Acyclovir. The major drawback of Acyclovir is its low aqueous solubility that delays its absorption and has poor oral bioavailability (15-30%). Solubility was increased by solid dispersion technique using a water soluble carrier, Kollidon VA64 (VA64), Soluplus (SOL) and Eudragit EPO (EPO). The solid dispersions were prepared by solvent evaporation method. The prepared solid dispersions showed an enhancement in dissolution rate and solubility compared to API. In vitro release profiles of all SDs were comparatively evaluated. Faster dissolution was exhibited by solid dispersion containing 1:4 ratio of drug: Eudragit EPO. The prepared solid dispersion was subjected for % practical yield, drug content, infrared (IR) spectroscopic, differential scanning calorimetry (DSC). FT‐IR spectra and DSC revealed no chemical incompatibility between drug and polymer. The solid dispersion in drug: Eudragit EPO (1:4, w/w) was relatively stable at 40 °C/75% RH conditions for at least 3 month. Key words: Solid dispersions, carriers, solubility enhancement, poorly soluble drugs, bioavailability

1371-1381

Authors: G. Bhavani, S.S. Hussain, S. Laxmi Prasanna, A. Ashok Kumar*

The article aims at developing a rapid, sensitive, accurate, precise and linear stability indicating Reverse Phase High Performance Liquid Chromatographic (RP-HPLC) assay method and validate as per ICH guidelines for the estimation of Balofloxacin in tablets. The optimized method employs a reverse phase column, Phenomenex Kinetex C18 (250X4.6mm;5μ), a mobile phase of Potassium dihydrogen phosphate buffer (pH 2.5):acetonitrile in the proportion of 50:50 v/v, flow rate of 0.6ml/min and a detection wavelength of 220 nm using a UV detector. Optimized method separated all the forced degradant impurities from the drug peak. Linearity of the method was 15-45μg/ml. Intra day and Inter day precision were exemplified by relative standard deviation of 1.09 and 1.17% respectively. Percentage mean recovery was found to be in the range of 90‐110, during accuracy studies. The limit of detection (LOD) and limit of quantitiation (LOQ) was found to be 247.9ng/ml and 751.2ng/ml respectively. Keywords: Balofloxacin, stability indicating HPLC, validation.

1393-1398

Authors: Sheth Chintan*, Prakasha Kaggere Jayaramu*, Rohini R Maralihallia

Some new acryloyl chromene-4-one derivatives were synthesized by Claisen-Schmidt condensation of 2-hydroxy acetophenone and benzaldehyde to form Chalcones which on further oxidative cyclization gives Flavone. Further on acetylation of Flavone, compound obtained was reacted with different substituted benzaldehyde to give acryloyl chromone-4-one derivatives. CN (1–10). The Characterization of newly synthesized compounds done on the basis of UV, IR, 1HNMR, 13CNMR, Mass spectral data. All the synthesized compounds were evaluated for their anti-inflammatory and antitubercular activity. Keywords: chromene-4-one derivatives, Flavones, Spectral data, Anti-inflammatory activity, Antitubercular activity.

1408-1422

Authors: Bandi Bhavani* , Pavan Kumar Chadalawada1 .

The aim of the present research work, Clofibrate a BCS class II Anti-hyperlipidemic drug belongs to fibrate class was formulated as solid dispersions by using various hydrophilic carriers to enhance the solubility, dissolution rate and oral bioavailability. Kneading technique is used to prepare solid dispersions of Clofibrate. Solid state characterization of solid dispersions is done by Differential Scanning Calorimetry, FourierTransform Infrared spectrometry and X-ray powder Diffraction studies, Scanning electron microscopy. The solid dispersions can be evaluated by in-vitro dissolution studies. To develop the solid oral dosage form (Tablets) with Clofibrate solid dispersions. To study the physical parameters of tablets prepared by direct compression, which includes hardness, friability, weight variation, and disintegration. To estimate the % drug content in the solid dispersions and the fabricated formulations. To evaluate the drug release from the tablets by in-vitro dissolution studies and to compare in-vitro dissolution profile of fabricated formulation with marketed formulation. Key words: FT-IR, SEM Studies, Clofibrate, Hydroxyl propyl -Cyclodextrin, - Cyclodextrin, Solid dispersion, BCS class II Anti-hyperlipidemic drug.

1437-1440

Authors: Asif Husain*, Mohammad Maaz , Aftab Ahmad , Shah Alam Khan

We describe herein the in vitro anthelmintic activity of di/trisubstituted 3-arylidene-5-(biphenyl-4-yl)-2(3H)- furanones against two species of earthworms i.e. Pheretima posthuma and Perionyx excavatus. The anthelmintic activity was determined by noting the mean paralyzing and death times of the worms due to furanone derivatives at a concentration of 2mg/mL. All the tested compounds displayed moderate to good anthelmintic activity but compounds 1 and 5 were found to be the most potent against Perionyx excavatus and Pheretima posthuma, respectively. These exhibited significant anthelmintic activities against both types of worms and the results were comparable to reference drug albendazole. Keywords: Furnaone, Pheretima posthuma, Perionyx excavatus, Anthelmintic

1453-1459

Authors: Sunita Patil , P Rajiv , Rajeshwari Sivaraj

Silver nanoparticles are being used in numerous fields for their optical, conductive, antioxidant anticancer and antibacterial properties. Green synthesis of silver nanoparticles is a simple and reliable method over chemical, physical and mechanical methods. The leaf extract of Aegle marmelos was successfully used for the synthesis of silver nanoparticles. Use of the silver nanoparticles in the field of biomedicine is rapidly growing because of their high efficacy and low toxicity. With respect to biological and clinical applications, silver nanoparticles has ability to control and manipulate the accumulation of nanoparticles inside a cell can provide sensitivity towards diagnosis and therapeutic efficacy. Here the antioxidant property of silver nanoparticles studied by performing 1,1-diphenyl- 2-picryl hydrazyl radical, nitric oxide and hydrogen peroxide scavenging assay. While cytotoxicity of the biogenic silver nanoparticles studied by performing the MTT assay. The result obtained for biogenic silver nanoparticles shows the dose dependent increase in antioxidant activity and it is comparable with standard ascorbic acid. Silver nanoparticles exhibits cytotoxic activity against A-431 squamous cell carcinoma cell lines. This potential to silver nanoparticles may impart form capping agent from leaf extract. Study of the anticancer mechanism of biogenic silver nanoparticles is the further way of research in coming future. Keywords: Biogenic silver nanoparticles, antioxidant, cytotoxicity, squamous cell carcinoma, A431 cell lines.