ARCHIVES(Journal of Harmonized Research in Pharmacy)


Title: EFFECT OF DIFFERENT TABLET DISNTEGRANTS ON PROCHLORPERAZINE MALEATE TABLETS
Author: Kuldeep Ganju*, Eisha Ganju
Keyword: Prochlorperazine maleate, disintegrant, magnesium stearate
Page No: 252-254
Abstract: The study is performed to determine the effect of selected superdisintegrants, Primellose and Primojel, on the Disintegration time (DT) of tablets of Prochlorperazine maleate. The molecule is an anti emetic and a high rate of disintegration would give faster pharmacological effect. 1%, 2% and 4% concentrations of the selected disintegrants were added and all other composites were kept constant. 4% Primellose gave the best result with a DT of 1 min 45 s. Key Words: Prochlorperazine maleate, disintegrant, magnesium stearate Download PDF


Title: IN -VIVO ANTI-TUMOUR ACTIVITY OF NOVEL IMIDAZO-[2,1 B]-1,3,4-THIADIAZOLE DERIVATIVES IN EHRLICH ASCITES CARCINOMA AND DALTON’S LYMPHOMA AS CITIES MODEL
Author: Pallavi K.J., S.V. Satyanarayana, B.S. Tippeswamy
Keyword: Imidazothiadiazoles; Ehrlich ascites carcinoma; Dalton`s lymphoma ascites; transforming growth factor-ß (TGF-ß) type 1 receptor.
Page No: 255-268
Abstract: Objective: To study the In-vivo antitumor activity of Novel Imidazo[2,1b]-1,3,4-thiadiazole derivatives on Ehrlich Ascites Carcinoma (EAC) and Dalton Ascites Lymphoma model.(DLA). Materials and Metho ds: The two novel imidazothiadiazole analogues ( Compound 4b, NSC:760239 and Compound 4c, NSC: 760240), in three different concentration were evaluated for their antitumor activity against Ehrlich Ascites Carcinoma (EAC) and two different concentrations were evaluated against Dalton’s ascites lymphoma (DLA), models. In EAC model increase in mean survival time of the drug was measured against control and standard (Levamisole) in mice. Their toxicity was assessed in normal, standard, and EAC bearing mice by measuring the drug induced changes in haematological parameters, In DLA model, the solid tumor volume, solid tumor weight, and % inhibition of the tumor weight of the drug treated over control and standard mice was measured. It is concluded that both the compounds showed dose dependent anticancer activity against control and standard Results: Both the molecules 4b and 4c showed dose dependent anticancer activity against control and standard. The compound 4b was more effective when compared to compound 4c mainly. Conclusion: from the observed results the compound 4b was more effective when compared to compound 4c. Keywords: Imidazothiadiazoles; Ehrlich ascites carcinoma; Dalton`s lymphoma ascites; transforming growth factor-ß (TGF-ß) type 1 receptor. Download PDF


Title: GUANINE-QUADRUPLEXES: BONDING, STRUCTURE AND BIOLOGICAL SIGNIFICANCE
Author: Ajay Kumar
Keyword: Guanine- Quadruplexes- structure, Quartet- bonding, G- quartet- stacking, quadruplex topology, G- quadruplex - Polymorphic Behavior, G-quadruplexes in human cell , Guanine Base Modifications- G Quartet.
Page No: 269-280
Abstract: The Guanine bases form non-canonical structures based on G-quartets was found in 1962. It is now well established that G-rich nucleic acids forms higher order structures called guanine quadruplexes . G-quadruplex structures show right-handed helicity due to hydrophobic stacking of two or more G-quartets. Little attention was paid to the of guanine tetrads structure and for more than 25 years this structure remained in search of functions. In this review the bonding in G-quartet, general features of quadruplex topology, structure and polymorphic behavior of G- quadruplex is described. In the quadruplex structure four guanines establish a cyclic array of hydrogen bonds from the Watson–Crick and the Hoogsteen bonding. A G-quartet is a planar association of four guanines held together by four central H-bonds between H1 of nitrogen and O6 of carbonyl group and also by four external H-bonds between H2 of amine and N7. Four guanine bases in a G-quartet can be brought together in monomer, dimmer or tetramer with parallel or antiparallel adjacent strands and structures can link up to provide different loop connectivities. The effect of guanine base modifications and metal cations on the G-guartets stability is described. The evidence of G-quadruplexes occurrence in human cells and anticipiated biological functions are highlighted. Key Words : Guanine- Quadruplexes- structure, Quartet- bonding, G- quartet- stacking, quadruplex topology, G- quadruplex - Polymorphic Behavior, G-quadruplexes in human cell , Guanine Base Modifications- G Quartet. Download PDF


Title: ANTI-PARKINSONISM ACTIVITY OF SARACA ASOCA BY HALOPERIDOL INDUCED MODEL
Author: C. Velmurugan*, K.Sapura, G. Indira Priyadarshini, S. Vijaya Kumar, B. Sasivardhan Reddy & M. Akmal Ali Baig
Keyword: haloperidol, Saraca asoca, dopamine, Catatonic score, in-vivo antioxidant.
Page No: 281-295
Abstract: Aim: The present study was designed to investigate the effects of different extracts of leaves of Saraca asoca in haloperidol induced Parkinsonism experimental model. Methods: Swiss albino mice of ei ther sex, weighing about 20-25 gm were used. Anti parkinsonism activity was done by haloperidol induced model using catalepsy score by Hole board test and catatonic score by block model and also evaluated in-vivo antioxidant, estimation of dopamine, nor adrenaline, adrenaline from brain tissue and histopathalogical studies of brain. Results: The extracts of AESA, MESA & WESA at doses (200 mg/Kg, p.o.) revealed the anti-parkinsonism activity while the PESA non significant to Parkinsonism control. The anti-parkinsonism activity was confirmed by Catatonic score, Head dip, number of line crossing, anti-oxidant enzyme level, LPO, histology of brain and level of monoamines like dopamine etc. at the dose levels of (200 mg/Kg, p.o.). The extracts MESA & WESA significantly decreased the Catatonic score and increased the head dip & number of line crossing. The dopamine, nor adrenaline and adrenaline significantly increased with extracts treated group except PESA at a dose of 200 mg/kg. Extracts MESA & WESA (200 mg/Kg, p.o.) has shown significant morphological changes when compared to haloperidol administered group. Conclusion: The results of the present work suggested that the MESA & WESA has a potent antiparkinsonism activity. Key words: haloperidol, Saraca asoca, dopamine, Catatonic score, in-vivo antioxidant. Download PDF


Title: EVALUATION OF HEPATOPROTECTIVE EFFECT OF LENZITUS BETULINA AGAINST PARACETAMOL INDUCED HEPATIC DAMAGE IN RATS
Author: C. Sundaramoorthi, R. Jayaraman, Johnson, Vipul, Riyas, Kamal Kumar Dhariya*
Keyword: Lenzites betulina, paracetamol, Hepatoprotective effect, lipid peroxidation, Mushroom.
Page No: 296-304
Abstract: In present work preliminary phytochemical analysis and pharmacological evaluation methanolic extract of lenzitus betuline (MELB) was done. Phytochemical analysis was done for lenzitus betulina. Agai nst toxicity produced by administering a combination of antipyretic drugs in paracetamol (PCM) 200mg/kg each for 21 days in male Wister rats. MELB was administered in two graded doses 0f 200 and 400mg/kg orally. Hepatoprotective effect of MELB WAS evident in the doses of 200 and 400 mg/kg as there was a significant decrease in SGOT, SGPT, ALP, Total and direct bilirubin levels treated groups in comparison to only induced groups without treatment. The reverse condition is seen in total protein level. The glutathione content and the activity of antioxidant enzyme such as superoxide dismutase, catalase, glutathione peroxidise and glutathione reductase were estimated in liver which shows that treatment with mushroom extract brought the enzyme levels close to normality. Histopathology of the liver section of the animals with the MELB further confirms the hepatoprotective activity. Key Words: Lenzites betulina, paracetamol, Hepatoprotective effect, lipid peroxidation, Mushroom. Download PDF


Title: STUDIES ON MIXED SOLVENCY CONCEPT IN FORMULATION DEVELOPMENT OF ORAL SOLUTION (SYRUP) OF POORLY WATER SOLUBLE DRUGS
Author: Love Kumar Soni, Shailendra Singh Solanki, Rajesh Kumar Maheshwari
Keyword: Solubility, Aceclofenac, Aqueous oral solution, Mixed solvency, Nsaids. Polyethylene glycol, Sodium citrate.
Page No: 305-315
Abstract: Application of the mixed solvency has been employed in the present research work to develop the oral solution (syrup) formulations of poorly water soluble drugs aceclofenac (as model drug). Due to t he low water solubility of aceclofenac in water, an attempt was made to enhance the solubility of drug by adding cost effective additives (combination of solubilizers as mixed solvent system) which could increase the solubility as well as stabilized the developed oral solution (syrup) formulation. On the basis of solubility studies mixed solvent oral solution formulations of aceclofenac were developed. Formulations were characterized by FTIR and Raman spectroscopy. Various properties of solution such as pH, viscosity, specific gravity and refractive index were also studied. The physical and chemical stability studies were carried out to examine the physical and chemical stability of an optimal oral solution (syrup) formulation of aceclofenac. All the formulations were physically, chemically and microbiologically stable for more than three months. Keywords: Solubility, Aceclofenac, Aqueous oral solution, Mixed solvency, Nsaids. Polyethylene glycol, Sodium citrate. Download PDF


Title: NATURAL PRODUCTS: AN IMPORTANT LEADS FOR ANTICANCER DRUG DISCOVERY
Author: Dr. S.P.Dhanabal, Dr. Namrita Lall, N.Pavithra*, M.V.N.L. Chaitanya
Keyword: Drug discovery, Bioprospecting, anticancer, traditional health practitioners.
Page No: 316-328
Abstract: Plants have played a significant role in maintaining human health and improving the quality of human life from many years. In recent times, focus on plant research has increased all over the world a nd a large body of evidence has collected to show immense potential of medicinal plants used in various traditional systems. There are many herbs, which are used to treat cardiovascular problems, liver disorders, cancer and many disorders. In any cancer drug discovery program, a paradigm based on ethnobotanical and ethnopharmacological data would be more economical and beneficial in identifying potential anticancer molecules than mass screening of plant species. Therefore, this review strives to describe the literature on the traditional plants/potent molecules those have been proved to have anticancer activity and to provide an important platform to accelerate the anticancer drug discovery process. The plants were selected for this review based on Literature survey was performed via electronic search using pub med and Google, also based on the field survey and discussion with South Indian traditional health practitioners(THPS). The present review focuses on the important traditional plants which are having good anticancer potential can be a good bioprospecting tools for novel anticancer drug discovery. Hence the current review is focused on the important ethnopharmacological uses of important plants. Keywords: Drug discovery, Bioprospecting, anticancer, traditional health practitioners. Download PDF


Title: SOLUBILITY ENHANCEMENT OF A POORLY AQUEOUS SOLUBLE DRUG USING SOLID DISPERSION TECHNIQUE
Author: Rubendra Kurmi*, Dinesh Kumar Mishra, Nitin Dubey, Dinesh Kumar Jain
Keyword: BCS Class II, Solubility, Carriers, Solid dispersion, Physical mixing, Solvent evaporation.
Page No: 329-336
Abstract: The purpose of present work was to enhance the solubility and dissolution rate of Valsartan by solid dispersion technology employing various carriers such as sodium starch glycolate (SSG), Mannitol. Solid dispersions were prepared by physical mixing and solvent evaporation method. Various ratios of drug and carriers were used in the preparation in the ratio of 1:1, 1:1.5, 1:2, 1:2.5 and 1:3, 1:3.5. All the SD prepared was found to be fine free flowing powders and the drug content was uniform in all batches. The results of the disintegration test revealed that FT5 has faster disintegration within (5.3 min.) Keywords: BCS Class II, Solubility, Carriers, Solid dispersion, Physical mixing, Solvent evaporation. Download PDF


Title: CORDYCEPS SINENSIS (YARSAGUMBA): A PROMISING CATERPILLER MUSHROOM
Author: Pritesh Paliwal*, Divya Barua, Praful D. Bharadia
Keyword: Pritesh Paliwal*, Divya Barua, Praful D. Bharadia
Page No: 337-343
Abstract: Cordyceps sinensis has been described as a medicine in old Chinese medical books and Tibetan medicine. It is a rare combination of a caterpillar and a fungus and found at altitudes above 4500m in Si kkim. Traditional healers and local people of North Sikkim recommend the mushroom, i.e., Yarsa gumba, Keera jhar (C. sinensis) for all diseases either as a single drug or combined with other herbs. The present study was undertaken to collect information regarding the traditional uses of cordyceps in Sikkim. It was found that most local folk healers/traditional healers use cordyceps for the treatment of 21 ailments.Download PDF


Title: BENZOTRIAZOLES: A VALUABLE INSIGHT INTO RECENT DEVELOPMENTS AND BIOLOGICAL ACTIVITIES
Author: Mohammad Rizwan Khan* and Love Kumar Soni
Keyword: Benzotriazoles; Antifungal; Antitubercular; Anticancer; Antiviral; Anticonvulsant; Anti-inflammatory; Antidepressant; Antimalarial
Page No: 344-352
Abstract: In recent years, heterocyclic compounds, analogs, and derivatives have attracted strong interest due to their useful biological and pharmacological properties. The small and simple benzotriazole nuc leus is present in compounds aimed at evaluating new entities that possess anti-microbial, anti-tumor, antitubercular, anti-convulsant, anti-depressant, antimalarial, and anti-inflammatory activities. Benzotriazoles display a broad range of biological activities and are found in many potent, biologically active compounds. So far, modifications of the benzotriazole ring have proven highly effective with improved potency and lesser toxicity. The present review highlights the recently synthesized benzotriazoles possessing important biological activities. Key Words: Benzotriazoles; Antifungal; Antitubercular; Anticancer; Antiviral; Anticonvulsant; Anti-inflammatory; Antidepressant; Antimalarial Download PDF