JPTRM Vol. 2 No. 1 (May 2014)
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Item Synthesis, antimicrobial evaluation and QSAR studies of p-amino benzoic acid derivatives(Chitkara University Publications, 2014-05) Meeta; Pradeep Kumar; Balasubramanian NarasimhanA series of Schiff bases (1-16) and esters (17-27) of p-amino benzoic acid (PABA) was synthesized and its in vitro antimicrobial potential was evaluated by using tube dilution method. Compound 11 was found to be most promising antibacterial agent (pMICbs = 2.11 μM/ml) having antibacterial potential comparable to standard drug norfloxacin (pMICbs = 2.61 μM/ml) and may be taken as a lead compound for the development of novel antibacterial agents. QSAR analysis indicated that electronic parameters, total energy (Te) and energy of lowest unoccupied molecular orbital (LUMO) were found dominant in explaining the antimicrobial activity of synthesized compounds.Item Estimation of Total Phenols and Flavonoids in Selected Indian Traditional Plants(Chitkara University Publications, 2014-05) Deepak Kumar; Anupam Jamwal; Reecha Madaan; Suresh KumarTraditionally, aerial parts of Abies pindrow Royle (Himalayan Fir; Pinaceae); Abies webbiana Lindl. (Talispatra; Pinaceae); Cephalandra indica Naud. (Ivy Gourd; Cucurbitaceae) and roots of Calotropis gigantea (L.) Dryand (Giant Milkweed; Asclepiadaceae) have been used in the Indian systems of medicine for the treatment of various ailments. But no systematic phytochemical work has ever been carried out on these potential plants. Thus, it was planned to estimate total phenols and flavonoids content in methanol extract, ethyl acetate fraction (EAF) and remaining methanol extract (RME) of selected plants. Properly identified plants were defatted with petroleum ether, and then separately extracted in a Soxhlet apparatus with methanol. The methanol extract of each plant was partitioned by ethyl acetate solvent to obtain EAF of respective plant. The total phenols and flavonoids contents were estimated using standardized procedures. Quantitative determination of total phenols and total flavonoids was done using standard curve of gallic acid (linearity: 20 to 120 mg/ml; r2 = 0.995) and quercetin (linearity: 30 to 180 mg/ml; r2 = 0.997), respectively. EAF of selected plants contained higher content of phenols and flavonoids, where as lowest content was observed in RME of plants. The content of total phenols and flavonoids in selected plants were found to be in order of C. indica > A. webbiana > A. pindrow > C. gigantea. The available literature reveals that polyphenols have been reported to possess varied pharmacological activities. As selected Indian plants contain polyphenols as major class of phytoconstituents, it is suggested that these constituents may be responsible for their medicinal uses.Item Receptor Identification: Advances in Ligands and Transmitters Discovery(Chitkara University Publications, 2014-05) Sandeep Arora; Govindrajan Raghavan; Avaneesh KumarReceptor identification is an integral part of drug discovery and development. By the beginning of the next millennium, the search for the natural ligands of the orphan G-protein-coupled receptors will lead to the discovery of so many new peptides that it may well double their present number. It has recently become evident that all types of chemical messengers, hormones and transmitters act through membrane receptors which constitute our largest superfamily of proteins, i.e. the G protein-coupled receptors. The development of targeted therapies has revolutionized the treatment of various chronic diseases. Receptors have well-conserved regions that are recognized and activated by hormones and neurotransmitters. These ligands are peptides, lipids or biogenic amines, and act as transmitter molecules. Identification of orphan receptors include screening, binding and reverse engineering that help to find out cysteinyl leukotriene CysLT1 and Cys T2, hepatointestinal leukotriene B4, motilin, Ghrelin, Growth hormone-releasing peptide and growth hormone secretagogue receptor and many more. Techniques involved in screening of receptors include low stringency hybridization followed by PCR-derived approaches helps to discover various orphan g protein couple recptors (oGPCR). The discovery of the oGPCR represents a hallmark in neuroscience research, and the exploitation of its numerous physiological and pathophysiological functions is a promising avenue for therapeutic applications.Item Pharmacogenomics: Applications in Drug Discovery and Pharmacotherapy(Chitkara University Publications, 2014-05) Hitesh Chopra; Sandeep Kumar; Vandana; Sandeep AroraPharmacogenomics is the scientific study which explains individual variability of drug targets and to explore the genetic basis for such changes. With the completion of human genomic study, clear relation could now be established between the drug response in relation to a person’s genome. Pharmacogenomics, also known as personalized medicine, uses the person’s genome to determine the dose and dosage regimen, so that therapy could be optimized. As with the techniques like DNA microarray technologies person’s response to a therapy can be predicted and new therapies could be assigned. In the present review, the current technologies, and past significance has been discussed.Item Dementia: An Overview(Chitkara University Publications, 2014-05) Nitin Bansal; Milind ParleDementia is a neurodegenerative disorder characterized by progressive and continuous loss of cognitive functions. The neuropsychiatric symptoms include apathy; agitation and depression. As the disorder progresses, the patient gradually becomes dependent on others to perform routine daily activities. Various underlying diseases or disorders are the root cause of the syndrome of dementia. Each of these disorder or disease is characterized by a specific signs and symptoms in combination with a presumed underlying neuropathology. Alzheimer’s disease is the most prevalent cause of dementia. The second most prevalent cause is vascular dementia. In this review, the clinical types, pathophysiology and pharmacotherapy is summarized.Item Sustained Release Solid Dispersions of Pentoxyfylline: Formulation and Optimization(Chitkara University Publications, 2014-05) Sandeep Kumar; Manju Nagpal; Kalpana Nagpal; Gitika Arora DhingraObjective: The purpose of the study is to formulate and optimize sustained release solid dispersions of pentoxyfylline using a combination of eudragit polymers and ethyl cellulose. Methods: Solid dispersions were formulated by solvent evaporation method.Preliminary batches were formulated using various drug to polymer ratio; with eudragit S100 and L100 (1:1 to 1:5 ratio), and with ethyl cellulose(1:1 to 1:3 ratio) and evaluated for solubility analysis. Based on results of preliminary batches, Box Behnken design was further applied and three factors (X1- concentration of Eudragit S100, X2- concentration of Eudragit L100, X3- concentration of Ethyl Cellulose) were selected with three levels (+1, 0, -1). Multiple linear regression was applied to generate polynomial equations and statistical evaluation. Prepared solid dispersions were investigated for sustained release properties via in vitro dissolution studies. Fourier transform infrared spectroscopic analysis (FTIR), X-ray diffraction analysis (X-RD), Differential scanning calorimetry (DSC) studies were carried out to evaluate drug polymer interactions. Scanning Electron Microscopy (SEM) analysis of optimized solid dispersion was carried out to evaluate surface morphology of the particles. Results: Batch F5 showed maximum sustained release (65.46% in 24 h) characteristics out of all solid dispersions. DSC studies indicated drug integrity when mixed with the polymeric carriers. FTIR and X-RD studies also ruled out any drug polymer interaction. A change in crystalline habit was observed in solid dispersion particles (F5 batch) as seen in SEM micrographs. Polynomial mathematical model generated using multiple regression analysis was found to be statistically significant (p<0.05). Conclusion: Release retarding effect was found to be dependent on polymer concentration. Therefore, an optimized combination may lead to better sustaining effect.Item Formulation, Optimization and Evaluation of Sustained Release Microspheres using Taguchi Design(Chitkara University Publications, 2014-05) Sukhbir Singh; Sandeep Arora; Neelam; Dharna AllawadiThe aim of present study is to prepare microspheres of eudragit RL 100 loaded with Nefopam Hydrochloride by single emulsion solvent evaporation technique. Taguchi L9 orthogonal array design has been used to optimize the composition and operating conditions for preparation of formulations. Nine batches (F1-F9) were prepared by taking three independent variables (X1- drug: polymer ratio, X2- stirring speed and X3- stirring time) at three levels (+1, 0, -1). Response variables studied for batches (F1-F9) were mean particle size (μm) (Y1), drug entrapment efficiency (% w/w) (Y2) and drug loading (% w/w) (Y3). Drug- polymer compatibility study was carried out by DSC and FTIR spectroscopy and indicates no physicochemical interaction. Microspheres were analyzed for morphological characteristics, mean particle size, drug entrapment efficiency, drug loading and in-vitro drug release. Percentage cumulative drug release for optimized batch F5 was found to be 85.421 ± 0.054 and followed higuchi model for release of drug.