International Journal of Pharmaceutical Sciences and Drug Research

178-182

Authors: D. Nagasamy Venkatesh1*, V. Swetha Priyanka1, K. Tulasi1, K. Kalyani1, Sheik Abid Ali1, Harikrishna Jilakara2

Proniosomes are solid colloidal particles which may be hydrated immediately before use to yield aqueous niosomes dispersions similar to those produced by more cumbersome conventional methods. The proniosomes minimize the problems associated with niosomes in terms of its physical stability such as aggregation, fusion and leaking. They also offer an additional convenience in transportation, distribution, storage, and dosing. The proniosomes derived niosomes are better than conventional niosomes in terms of their morphology, particle size, particle size distribution, and drug release. A slurry method was commonly used to produce proniosomes using maltodextrin as carrier. The time required to produce proniosomes by this simple method is independent of the ratio of surfactant solution to carrier material and appears to be a scalable process. The encapsulation efficiency of proniosomes is depends upon the amount of maltodextrin used in the process. The present review describes the method of preparation, characterization, applications of proniosomes as a potential drug delivery system.

189-192

Authors: Ravish Garg1*, Priti Girotra2, Shailendra Kumar Singh2, Dinesh Kumar3, S. K. Chakarvarti4

The track etch membranes has attracted the attention of researchers, as a kind of novel material, for their various applications such as precise separation of biological cells, detection of biomolecules and controlled drug release, especially for pharmaceutical and biomedical applications. In the present study, the efficacy of track etch membrane over goat skin for the Ex-vivo permeation of silver sulfadiazine gel has been investigated with the objective to evaluate track etch membrane as a surrogate for biological membrane owing to ethical issues and scarce availability of biological skins. The percent cumulative drug release from silver sulfadiazine gel using track etch membrane and goat skin were obtained as 18.18 % and 20.99 % respectively. The results obtained from track etch membrane and goat skin was similar with only a slight difference in percent drug diffusion which might be because of the lipids present in animal skin. Track etch membrane has the potential to mimic the animal skin for such ex-vivo drug diffusion studies with certain additional advantages such as sufficient mechanical strength and ruggedness. It can be efficiently reused and also surpasses the ethical issues involved with the use of biological membrane.

197-199

Authors: Pankaj Kumar*, Jennifer Fernandes, Abhishek Kumar

In order to develop relatively small molecules as pharmacologically active molecules, a series of novel oxazolidinones having benzothiazinen and their derivatives were synthesized, and characterized by IR, 1H NMR and Mass spectral studies. Various substituted oxazolidinones benzothiazinen were prepared by simple reflux in the presence of acetonitrile. Treatment of these oxazolidinones benzothiazinen deravatives with methanesulfonyl gives its sulphonates derivatives on further treatment with sodium azide and tri phenyl phosphine in acetic anhydride to give its acetamide derivatives. Further the synthesized compounds were evaluated for antibacterial activity against Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and antifungal activity against, Candida albicans and Aspergillus niger.

204-210

Authors: AL Castillo1*, JDA Ramos2, JL De Francia3, PF Quilala4, MU Dujunco5

Scabies is a contagious, parasitic skin infestation caused by Sarcoptes scabiei mite, which has the ability to regulate the host’s inflammatory and immune responses. It is a serious community health problem in many less-developed countries. A randomized, controlled, parallel, pilot clinical study was performed to investigate the immunomodulatory effect of the formulated Tinospora lotion in clinically diagnosed scabies-infected patients through Enzyme-Linked Immunosorbent Assay (ELISA) for Interleukin-1, Interleukin-6 and Interleukin-8 using blood serum samples. The pediatric patients were treated with Tinospora and Permethrin lotions for three consecutive days for two weeks. Blood extraction was performed before and after the second and fourth week of treatment period. Tinospora lotion significantly reduced the Interleukin-1 (IL-1) and Interleukin-6 (IL-6) levels from Day 14 to Day 28 (p=0.0002) comparable to Permethrin lotion (p<0.050). Permethrin efficiently decreased Interleukin-8 (IL-8) levels than Tinospora at Day 14 (p=0.0155). Down regulation of Interleukin 1, 6, and 8 levels in scabies infestation inhibits hyperkeratosis and infiltration of inflammatory cells into scabietic lesion. The modulation effect of the Tinospora lotion on interleukin levels reinforces its anti-scabies activity.

216-219

Authors: Nilutpal Sharma Bora*, Bibhuti Bhusan Kakoti, Partha Sarathi Bairy, Barnali Gogoi

The stem bark of Garcinia lanceifolia, a lesser known species of the genus Garcinia, was extracted with methanol after pretreatment with petroleum ether. The resultant extract was evaluated for its analgesic and anti-inflammatory potential using various models. The assays were carried out on adult male Wistar Albino rats. The analgesic activity was assayed by hot plate method and tail flick assay using Morphine sulphate as standard drug at a dose of 5 mg/kg body weight and the results were expressed as mean increase in latency after drug administration ± SEM. The anti-inflammatory activity was evaluated by Carrageenan-induced rat paw oedema model using Diclofenac sodium as standard drug at a dose of 100 mg/kg body weight. The results were expressed in terms of mean increase in paw volume ± SEM. The extract of the stem bark was given in doses of 250 mg/kg and 500 mg/kg body weight. All the doses were administered per orally. Results reveal that Garcinia lanceifolia Roxb. posseses remarkable analgesic and anti-inflammatory activities.

224-228

Authors: Karunakar Hegde*, T. K. Deepak, K. K. Kabitha

The present study was designed to evaluate the hepatoprotective activity of leaves of Santalum album in experimentally induced liver injury by carbon tetrachloride and paracetamol. The levels of serum marker enzymes, bilirubin, total protein and antioxidant status were determined by measuring lipid peroxidation, glutathione, superoxide dismutase and catalase activity. Total wet weight and histopathological study of isolated liver was also carried out. The oral pre-treatment with hydroalcoholic extract of the leaves of S. album (200 and 400 mg/kg) showed significant hepatoprotective activity against CCl4 and paracetamol induced hepatotoxicity by decreasing the activities of serum marker enzymes, bilirubin and lipid peroxidation, and significant increase in the levels of glutathione, superoxide dismutase, catalase and protein in a dose dependent manner, which was confirmed by the decrease in the total weight of the liver and histopathological examinations. Data also revealed that the extract possessed strong antioxidant activity, which might leads to the promising hepatoprotective activity.

235-238

Authors: Abdullah Al Mamun, Tapas Kumar Shaha, Md. Murad Khan, Md. Shahidul Kabir*

The production of substandard drugs and use of inappropriate methods in manufacturing medical products in pharmaceutical industries may cause non-therapeutic effect in patients particularly in children. Hence this study was conducted to determine the microbiological quality of multivitamin and cough syrups of different brands sold in local pharmacy in Dhaka city. Microbiological analysis was carried out using spread plate technique on different culture media including nutrient agar, mannitol salt agar, MacConkey agar, mFC agar, TCBS agar and SS agar for the determination of total viable bacteria, Staphylococcus aureus, Escherichia coli, total coliforms, Vibrio cholerae, Salmonella spp. and Shigella spp. respectively from eleven multivitamin and twelve cough syrups. The results revealed that 50% of the cough syrup and 91% of the multivitamin syrup showed compliance with the official requirement of microbiological quality as they did not show any growth or their microbiological count is within the USP permissible limit (<102 cfu/ml). While the major contaminants in cough syrup were Staphylococcus aureus (75%), Escherichia coli (17%) and total coliforms (42%), multivitamin syrup (9%) contained only Staphylococcus aureus. Other pathogens like Vibrio cholerae, Salmonella spp. and Shigella spp. could not be detected in both cough and multivitamin syrups. Although most of the multivitamin syrup (91%) samples are free from potential microbial threat, some of the cough syrup (75%) samples are contaminated with pathogenic bacteria. Hence potential safety measurement should be taken during the production and use of cough syrups to maintain the microbiological quality.

243-245

Authors: Łukasz Czubak*, Alina Krygier, Bożena Tejchman-Małecka

Cleaning validation is an integral operation of good manufacturing practice in pharmaceutical industry. The aim of this study was to validate simple analytical method for detection of 2-propanol residue in equipment, which is likely contaminated with 2-propanol, usually used in the production area. The gas chromatography with flame ionization detection (GC-FID) method was validated on a GC system using DB-FFAP capillary column at the flow rate of 4.9 mL/min. The calibration curve was linear over concentration range from 2.8µg/mL to 110.7µg/mL with a correlation coefficient equal to 0.99981. The detection limit (LOD) and quantitation limit (LOQ) were 1.1µg/mL and 2.8µg/mL, respectively. The simplicity of gas chromatography method makes it useful for routine analysis of 2-propanol residue and is an alternative to corresponding methods.

250-252

Authors: Sanagapati Manasa1*, Dhanalakshmi K1, Nagarjuna Reddy G1, Sreenivasa S2

In the present study, two analytical methods were developed for the estimation of Dapagliflozin in API. Method A: RP-HPLC method, Method B: UV spectroscopic method. In method A, the drug showed linearity in the range of 25-150µg/ml with a correlation coefficient (r2) of 0.999, where as in method B, the linearity range was found to be 1-5µg/ml with a correlation coefficient of (r2) 0.999. Both the methods were validated for different validation parameters such as linearity, accuracy, precision, detection limit, quantitation limit, robustness and ruggedness and the results were found to be within the acceptance limits as per the guidelines of International Conference on Harmonization (ICH).

85-89

Authors: Sara Fatima*, Sobia Noor, Mohammed Maazuddin, Ayesha Fatima

Hormone replacement therapy (estrogens with or without progestogens) is widely used medication therapy worldwide for alleviating post menopausal symptoms. The association of Hormone replacement therapy (HRT) and risk of cancers leads to many studies. A lot of controversial results regarding the risk of cancers arises which leads to many questions that are still unanswered and can be cleared by further extensive research. There is considerable uncertainty among general practitioners to balance the beneficial and harmful effects of long term HRT particularly regarding the risk of cancers (breast, ovarian, endometrial, colorectal, lung cancers, lymphoma’s and leukaemia’s). The goal of HRT is not only to normalize the follicle stimulating hormone value, but rather to use the minimum effective dosage to suppress vasomotor reactions, treat urogenital atrophy, prevent trabecular and cortical bone loss, and reduce cardiac risk. Use of HRT should be individualized for risks and benefits of each patient that is being taken into consideration.

95-101

Authors: Kinjal R. Shah1, Sunita A. Chaudhary2, Tejal A. Mehta1*

Polymers are tools used in novel drug delivery system to modify the drug release of pharmaceutical dosage form. Polyox is hydrophilic polymer made of non-ionic homopolymer of ethylene oxide. Polyox is popular for its film forming, binding, lubricating, mucoadhesive, viscosity imparting property in pharmaceuticals. Polyox are available in various grades based on its molecular weight. Lower molecular weight Polyox are widely used for immediate drug release based on erosion properties of the polymer like quick dissolving film and high molecular weight Polyox are used to retard the drug release based on swelling and erosion properties of the polymer in controlled release, sustained release, extended release, buccal films, ocular inserts, ocular gels, osmotic tablets and so on. Polyox plays an important role in design of a novel drug delivery system for both highly and poorly soluble drug due to its multifunctional property. This review is detailed on Polyox its advantages, disadvantages, salient feature, mechanism, stability and application in pharmaceutical dosage form.

109-113

Authors: Uzondu AL*, Nwadike KN, Okoye EI

The study was aimed at investigating the effects of Brachystegia gum (BG)-egg albumin (EA) mixture as binding agent on the qualities of metronidazole tablets. BG and EA were mixed at different ratios to generate fifteen binder mixtures (F1-F15), from which F1-F5, F6-F10 and F11-F15 were used at 2%, 4% and 6% w/w respectively to formulate metronidazole granules by wet granulation. The granules after micromeritic characterization were subsequently compressed into tablets. Quality control tests conducted on the tablets include: hardness, friability, weight uniformity and dissolution studies. Results reveal that granules flow rates ranged from 3.02 g/s (F4) to 4.73 g/s (F1); angle of repose ranged from 29.06° (F12) to 35.93° (F3); Carr’s index values were between 7.49% (F9) and 25.43% (F12), while Hausner’s ratio ranged from 1.08 (F9) to 1.34 (F12). Tablet hardness values were between 3.65±0.47 (F2) and 5.95±0.60 (F11). Tablets friability values were of magnitude ranging from 0.84 (F11) t0 21.73 (F1). The result of weight variation test revealed that only four batches (F4, F6, F9 and F15) met compendia specifications. Among the metronidazole tablet formulations, those containing binder at 2% w/w released the highest amount of drug, giving up to 90% drug release in 6 h. The least amount of metronidazole was released by tablets formulated with binders at 6% w/w from which only about 30% of drug was released in 6 h. The BG-EA mixture was found useful in imparting slow release profile on metronidazole tablets, which is desirable for some tablet formulations.

120-123

Authors: Shailesh Kumar1*, Onkar Nath2, Sumit Govil2, A. N. Pathak1

Pyruvate dehydrogenase protein is a part of cellular respiration which helps in maintaining glucose and energy level (ATP) in the cells for their normal functioning. Initially it was reported that Brugia pahangi is a nematode causing filarial infections in animals like dogs and cats. But, in the recent studies, Brugia pahangi is also found to cause filarial infections in Humans, in Kuala Lumpur, Malaysia. By targeting the cellular respiration of this worm this filarial infections can be treated. The three dimensional structure of pyruvate dehydrogenase in B. pahangi will help to target cellular respiration more efficiently. The comparative modeling approach based software Modeller9.13 is used to model three dimensional structure of pyruvate dehydrogenase. The modeled structure was evaluated by Procheck, VADAR, Process, ProSA tools. The Physiochemical properties of this protein are analyzed by APD2 and Protparam software. Enzymatic Cleavage site of this protein is identified by Peptide cutter tool. Active sites in modeled structure are identified by Pocket finder tool for drug targets. The modeled structure, properties and active sites of this protein will help to design lead molecules which can treat the filarial infections in humans. The structure will also help to understand the working of pyruvate dehydrogenase in better and efficient manner by identifying the protein interaction networks in Brugia pahangi.

128-131

Authors: M. J. Neethu*, Shakkeela Yusuf

A series of novel pyrazoline derivatives of vanillin were synthesized. The hydroxyl group in vanillin was masked by converting into methyl vanillin. The methyl vanillin was allowed to condense with different acetophenone derivatives gave chalcone derivatives and finally cyclized with thiosemicarbazide to form the pyrazoline derivatives of vanillin. Docking studies were carried out against anti-inflammatory cyclooxygenase receptor and anticancer farnesyl transferase receptor. Majority of the synthesized compounds showed good fitting with the active site of all the docked targets. The synthesized compounds had shown significant anti inflammatory and anticancer activities.

137-139

Authors: Kodia M1, Trébissou Jonhson Noel D2*, Crezoit Yapo A3, Eyangoh S4, Asse H5

The aqueous extract of a plant coded OBAYOKOU (Moringa oleifera ) has been tested on the healing of ulcers in children under 15 years, two lots of 15 children each were made all presenting clinical forms of Buruli ulcer. The aqueous plant extract of Moringa oleifera was added to the food supply given to Lot B (lot of experimental subjects) at a rate of 330 ml per meal per child for six weeks. Children of Lot A (control Lot) received normal diet without Moringa oleifera. The results of this study have shown that children in (lot B) in addition to the normal diet received 330 ml of Moringa oleifera per meal, had a higher rate of healing than Lot A (Witness Lot) who received only normal diet. Thus, the rate of healing of ulcers with M. oleifera (24 mm) is superior to healing without M. oleifera (10 mm) after six weeks. This study shows that we can overcome Buruli ulcer with medicinal plants that is abundantly available in Africa. It also shows that it is necessary to conduct research on a wider range of fractions of Moringa oleifera to improve the activity of antimycobacteriennes molecules in the aqueous extract of Moringa oleifera.

145-153

Authors: P. Prabhu, M. Muralidhar*

A novel isocratic reverse phase high performance liquid chromatographic (RP-HPLC) method was developed for the determination of purity of Irbesartan drug substance in bulk samples and its pharmaceutical dosage forms in the presence of its impurities. This method is capable of separating related impurities along with Irbesartan. This method can be also be used for the estimation of assay of Irbesartan in drug substance as well as in single tablet formulation. Two impurities were detected in drug sample by HPLC analysis. The chromatographic conditions were optimized using an impurity-spiked solution. MS and IR method was used for the identification of impurities. The structure of the impurities were confirmed as 2-Cyano-4'-bromomethyl biphenyl and 2-n-butyl-1, 3-diazaspiro [4, 4]-non-1-ene-4-one. The method was subsequently validated for the determination of Irbesartan and its related compounds, as per ICH guidelines, for accuracy, precision, linearity and range, selectivity, limit of detection, limit of quantification and robustness. The LOD for Irbesartan, Impurity 1 and Impurity 2 was found to be 18.51µg/ml or ppm, 16.033µg/ml or ppm and 16.069µg/ml or ppm respectively while LOQ was found to be 56.098µg/ml or ppm, 48.587µg/ml or ppm and 48.69µg/ml or ppm respectively.

160-163

Authors: AJG Yaya1, RD Feumba2, T Emmanuel3*, AT Tchinda1, M Fredérich5, J Oben6, JT Mbafor4

The aim of this study was to isolate, to characterize secondary metabolites from methanolic extract of the root woods of Erythrina droogmansiana and to assess the antioxidant activity of the crude extract and isolated compounds. The phytochemical study led to the isolation of 3-(3’,4’-methelenedioxyphenyl)-2,3-epoxypropanol (1), asperphenamate (2) and three flavonoids namely genistein, diadzein and 4’,5,7-trihydroxy-8-prenylisoflavone. These compounds were characterized using their 1H NMR, 13C NMR, HMBC, HSQC, COSY, mass spectral and the literature. To evaluate antioxidant activity of crude extract and isolated compounds, the radical scavenging (DPPH) and Ferric Reducing Ability Power (FRAP) were performed using ascorbic acid as standard. Compounds 1 and 2 showed moderate radical scavenging potential with IC50 value of 3.14 and 3.31 mg/ml respectively, and moderate reducing power ability with value of 0.14±0.01 mgAAE/mg and 0.21±0.01 mgAAE/mg respectively. The more active compound was genistein (3) with IC50 value of 1.96 mg/ml for the DPPH radical scavenging potential and 0.24±0.02 mgAAE/mg for its ability to reduce iron.

169-173

Authors: S. Usha Rani1, M.Chitra1, Mallika Jainu2*

Wattakaka volubilis (Linn) is used as a phytomedicine for liver diseases. In the present study the effect of methanolic extract of Wattakaka volubilis powder was carried out against the Aluminium toxicity in rat model. Various doses of Wattakaka volubilis extract (100, 200, 400 mg/kg/b.w) was given orally for 30 days to Aluminum sulphate toxicity exposed rats. They were observed each hour for 24 h and each day for 30 days for any changes in behavioural activity and mortality. Clinical observation, body weight, organ weight, biochemical enzymatic analysis and histological examination were carried out. The extract was found to possess hepatoprotective activity in a dose dependent manner and the effect was comparable with silymarin, a standard drug. The extract significantly reduce the toxicity of Aluminium sulphate caused in liver due to the presence of phytoconstituents such as alkaloids, sterols, tannins, triterpenoids and flavonoids which are known hepatoprotectant.

01-11

Authors: M. Rousse, N. Cucuat, C. Janicot, R. Shrivastava*

Pharyngitis is primarily a viral infection of the respiratory tract, followed by secondary bacterial invasion due to weakening of local defenses. Influenza A and rhinoviruses are principally involved, the influenza virus having much higher pathogenicity, however, than rhinoviruses which usually cause the common cough and cold without severe damage to the respiratory mucosa. Following initial infection, the virus enters the cells only for multiplication and almost all virulent virus particles subsequently produced are shed onto the throat surface. From the throat surface, the virions infect new healthy cells, damaging the throat mucosa, and creating a favorable ground for secondary bacterial colonization which is the cause of almost all symptoms of throat infection (sore throat, strep throat). The virus’ complex structure, its constant mutation, the variety of its surface glycoproteins, as well as the role of topical proteases helping virus entry and virus – bacteria symbiosis must all be taken into account in designing an effective treatment, acting on multiple parameters. As most viruses and all bacteria are present on the throat’s outer lining, treatment should be designed to act topically on the surface of the pharynx, which also minimizes side effects. Until 2012, no topical antiviral drugs were available and almost all treatment strategies were directed to relieve only the symptomatic manifestations of throat infections. Anti-influenza vaccination is still considered the best preventive measure, while the use of intracellular virus inhibitors is strictly limited to severe cases as they were not found to be very effective once throat infection is established. The recent development of non-specific topical virus glycoprotein inhibitors, incorporated in a filmogen glycerol solution for an increased duration of action, represents a breakthrough yet relatively simple scientific approach for the treatment of viral throat infections accompanied by secondary bacterial infection. In this review, we analyze the whole process of viral throat infection, virus – bacteria interactions on the throat surface, currently available treatments and their drawbacks, and this innovative therapeutic approach consisting in virus glycoprotein inhibitors in an osmotic solution, destined to totally change the future treatment of throat infections.

20-25

Authors: Swaroopa. A, C. Aparna*, Prathima Srinivas

The aim of the present study was to develop microemulsion gel of Satranidazole for the treatment of periodontitis. The objective was to increase the solubility of Satranidazole, a lipophilic drug and to enhance depth of penetration of the drug into the periodontal pocket for efficacious treatment of periodontitis. Pseudo ternary phase diagrams were constructed to determine the region of existence of microemulsions prepared using cosurfactant titration method. The formulations were developed using isopropyl myristate, tween 80, ethanol; oleic acid, tween 80, propylene glycol; oleic acid, cremophor RH 40, ethanol. Optimization of formulations was done based on in vitro diffusion studies. The microemulsion was gelled using carbopol 940 as the gelling agent. The formulations were evaluated for pH, viscosity, percent transmittance, centrifugation (phase separation), and characterized by scanning electron microscopy, particle size, zeta potential and polydispersity index. The formulation inhibited the growth of micro organism, Salmonella typhimurium which indicates that the formulation could be used to treat periodontal infection.

31-37

Authors: P. Padmanabhan*, S. N. Jangle

Oxidative stress in mammals results from imbalance between generation of free radicals and the rate of their suppression by antioxidant. Hepatotoxicity may result as an effect of excessive free radical formation due to exogenous chemicals or metabolic reactions. D-Galactosamine (D-GalN) is a well known hepatotoxicant. Herbal medicines have been utilized to manage hepatotoxicity according to recent trends. In the present study Herbal Preparation or HP-4 is a combination of 80% alcoholic extract of leaves of Aloe vera, Bacopa monniera, Moringa oleifera and rhizome of Zingiber officinale has been utilized to study its efficacy on mice model of D-GalN hepatotoxicity. D-GalN hepatotoxicity induces liver injury closely resembling human viral hepatitis with necrosis, inflammation and regeneration. Evidenced by biochemical and histopathological studies it is concluded that polyherbal formulation HP-4 offered a synergistic protection due to the phytochemicals present which provide hepatoprotective activity induced by D-GalN hepatotoxicity.

41-47

Authors: Thonda.V.S.S.Swaroop*, Suddhasatwa Banerjee, Handral. M

This research was performed to characterize the neuroprotective effect of ethanolic extract of Dalbergia sissoo leaves in 3-Nitropropionic acid induced neurotoxic rats. The ethanolic extract of Dalbergia sissoo leaves was administered orally at different doses (300 and 600 mg/kg) to neurotoxic rats. During treatment psychopharmacological parameters were recorded, 24 hours after experiment antioxidant profiles from brain isolate were estimated and histopathology of brain was performed. The ethanolic extract significantly attenuated behavioral alterations, oxidative damage, mitochondrial dysfunction, and striatal/hippocampus damage in 3-Nitropropionic acid treated rats. These results suggest that ethanolic extract of Dalbergia sissoo leaves may have potential therapeutic value in the treatment of some neurological disorders, probably by its anti-inflammatory, antioxidant and estrogenic properties.

52-59

Authors: Lisina K. V*, Shanmughavel Piramanayagam

Thymoma is a tumor originating from the epithelial cells of the thymus. Thymoma is an unusual tumor, best known for its association with the neuromuscular disorder myasthenia gravis. When diagnosed, thymomas may be removed surgically. In the rare case of a dangerous tumor, chemotherapy may be used. Health and medicinal applications of tender coconut product get research interest in recent years. The application of edible coconut part is due to the different natural components present in it. This research paper aimed to know the main reported components of coconut i.e., tender coconut water and coconut Petiole for its inhibitory activity against Thymoma. We have chosen target proteins for Thymoma viz RasP21 protein (PDB ID: 4FSS), AKT-1 (PDB ID: 3O96) and BCL-2 (PDB ID: 4AQ3) for our study, it was predicted to be expressed in Thymoma. Docking is frequently used to predict the binding orientation of small molecule drug candidates to their protein targets in order to in turn predict the affinity and activity of the small molecule. Docking study of the target protein was done with natural compounds derived from coconut. The coconut palm (also, cocoanut), Cocos nucifera, is a member of the family Arecaceae (palm family). It is the only accepted species in the genus Cocos. The term coconut can allude to the whole coconut palm, the seed, or the fruit, which, botanically, is a drupe, not a nut. Chemical constituents found in extracts of entire coconut palm. Phytochemicals screened for Glide HTVS docking showed good interaction with the target. The antitumor compound that yielded a fitness score of more than -5 and good toxicity value were further subjected to Molecular dynamics simulation (MDS). L-Histidine can be a good drug considering their binding affinity, glide energy, glide score and toxicity and that could be a potential target for Thymoma. The docking and ADME studies were performed using Schrödinger Suite.

67-69

Authors: K. Govinda Rao, Dipankar Chakraborty*

Present study circumspects synthesis of some novel 2-substituted analogues of Benzimidazole and their spectral characterization by means of UV, IR and 1H NMR. The compounds were screened for antibacterial activity against standard strains of both Gram positive and Gram negative bacteria. Results obtained establish compounds KD1 and KD2 to be significantly responsive against different bacterial strains and as such these compounds can pave the way for development of potent antibacterial agents.

75-77

Authors: R. Vijayalakshmi1, P. Sandya2, M. Poorna Chandra Rao3, M. D. Dhanaraju1*

The combination of Perindopril (PRN) and Losartan (LRN) is used in the management of hypertension. The present work was focused on the development of RP-HPLC method for the estimation of perindopril and losartan in binary mixtures. The separation was performed on LUNA C18 column at 210 nm by isocratic elution. Methanol and phosphate buffer (pH 6.8) in the ratio of 85:15 with a flow rate of 0.8 ml/min at ambient temperature was found to be suitable for chromatographic separation. Perindopril and losartan exhibits linearity in the ranges of 200-500 and 30-80 µg/mL respectively. The proposed method evidenced the absence of chromatographic interference by pharmaceutical excipients. Separation of the mixtures was proved to be good from the resolution of the peaks. Validation and recovery studies were performed and the results proved the method to be suitable for routine analysis.

82-84

Authors: Y.Kranthi Kumar, K.Vanitha Prakash*, Mogili Swetha

A simple, economical, precise, reliable and reproducible visible Spectrophotometric method has been developed for the estimation of Tapentadol in bulk as well as in tablet formulations. This method is based on the formation of Blood red colored chromogen with2, 2 -bipyridyl which shows maximum absorption at λ max 520 nm. The absorbance-concentration plot is linear over the range 50-250µg/mL. Results of analysis were validated statistically. Recovery studies were also performed. The proposed method is economical, accurate precise and sensitive for the estimation of Tapentadol in bulk drug and its formulation.

133-140

Authors: Priti Girotra, Shailendra Kumar Singh*

Katira gum, a natural polysaccharide resembles guar gum in chemical composition and is susceptible to degradation by colonic microflora. Azathioprine is used in the treatment of inflammatory bowel disease, ulcerative colitis and Crohn’s disease. Present investigation was undertaken to design Katira gum oral colon targeted matrix tablets containing azathioprine, in order to maximize its therapeutic efficacy. Central composite design (software design expert v. 8.0.7.1) was employed to optimize the formulation for maximum drug release in colon. The optimized batch tablets obtained were further coated by Eudragit S100 to minimize the drug release in upper part of GIT. The uncoated matrix tablets released around 20-50% of the drug in the physiological environment of stomach and small intestine but released all its contents in the colon. The coated optimized formulation exhibited a release of only 5-35% in stomach and small intestine and almost all drug in simulated colonic dissolution media. The drug release kinetics followed Korsmeyer-Peppas model, indicating the drug release mechanism through combined diffusion and erosion mechanism. The results suggested that Katira gum can be a good carrier for colon targeting owing to its moderate viscosity, biocompatibility and biodegradability which could be successfully degraded by the microbial flora in the colon.

146-151

Authors: Preethi N*, Sujatha S

A novel type of elementary osmotic pump [EOP] tablet for efficient delivery of poorly water-soluble drug, glipizide has been designed. Drug release from the system, called Swellable Elementary Osmotic Pump [SEOP], is through a delivery orifice in the form of a very fine dispersion, ready for dissolution and absorption. SEOP tablets were prepared by compressing the mixture of micronized drug and excipients into convex tablet. The effect of wetting agent, swelling agent, osmotic agent and hydrophobic plasticizer on the release rate were investigated. The release behavior of glipizide from different formulations of this dosage forms were studied at pH 6.8 for a period of 24 hours. The drug release profile from osmotic devices showed that the type of polymer in the core formulation can markedly affect the drug release. When the amount of HPMC E50-LV was increased from 30 to 60 mg, decrease in drug release was observed. Increasing the amount of wetting agent to an optimum level of 45 mg significantly increased the release rate and improved zero order release pattern of glipizide. Increasing the concentration of Dibutylphthalate [DBP-30%] in the semi permeable membrane of the device retarded the release rate of glipizide but gave best results at the 20% concentration. Based on the SEM studies, optimized orifice diameter was found to be 500µm. Compared with the marketed Glipizide extended release tablet; GF2 gave the best release rate for 24 hours. The bioavailability studies for glipizide SEOP and Glipizide extended release tablet was carried out in albino rabbits and there was a good in-vivo and in-vitro correlation for GF2 as shown by the higher Cmax and AUC values. Thus a novel SEOP was successfully formulated for glipizide to achieve zero order drug release over a period of 24 hours.

158-164

Authors: Phyllis Elsie Dadzeasah, Charles Ansah*

Spathodea campanulata, well known for its traditional medicinal uses was investigated for hepatoprotective activity against acetaminophen-induced hepatic damage in mice. Six groups of mice were pre-treated with 100, 300 and 625 mg/kg of the aqueous extract of Spathodea campanulata stem bark, N-acetyl cysteine (300 mg/kg; p.o) or distilled water for 5 days before they were intoxicated with a single dose of acetaminophen (600 mg/kg; p.o). Alanine aminotransferase, Aspartate aminotransferase and total protein levels were measured in serum, glutathione peroxidase, superoxide dismutase and total cytochrome P450 levels were measured in liver homogenate and liver histology was also observed on liver sections. Total liver cytochrome P450 levels in Spathodea campanulata extract, distilled water, ketoconazole or phenobarbital-treated animals were also measured. Significant hepatoprotection was obtained against liver damage induced by acetaminophen as evident from decreased serum levels of Aspartate transaminase, Alanine transaminase and increased levels of total protein in the combined acetaminophen and extract treated groups and the acetaminophen and N-acetylcysteine-treated groups compared to the acetaminophen only controls. The decrease in serum antioxidant enzymes; glutathione peroxidase and superoxide dismutase levels caused by acetaminophen was significantly reversed by the extract. The results correlated well with the histopathology of liver from treated and control animals. The extract also caused considerable inhibition of total CYP450, the enzymes involved in the activation of acetaminophen. The present results indicate that Spathodea campanulata protects the liver against acetaminophen-induced hepatotoxicity by enhancing antioxidant protection capacity and interfering with the bio-activation of acetaminophen.

170-174

Authors: N. Shruthila, Priya Narayan, D. Jagadeesh Kumar, H. G. Nagendra*

The aggregation of Amyloid beta peptides is considered as one of the causative events in the pathogenesis of Alzheimer’s disease (AD). Polyphenols present in different plant sources, which have acclaimed therapeutic values, are known to inhibit the formation of Amyloid fibrils. Hence, docking studies with different polyphenols were carried out to appreciate their binding modes and plausible molecular interactions. The results reveal a consensus pattern of association, exhibiting that all the ligands preferentially dock to the metal coordinating residues in the peptide fragments. In fact, the metal interacting geometries in the Aβ segments are known to be implicated in aggregation events. Further, due to non-specific binding, these polyphenols are expected to have a competitive inhibitory efficacy over a range of amyloid peptide fragments. Thus, these findings suggest that the polyphenolic compounds could become promising lead molecules that aid in the development of inhibitors and neuroprotectors towards prevention of amyloid fibril formations and AD.

179-183

Authors: S. Dhanure, A. Savalia, S. K. Nayak*, A. K. Das, S. K. Kotha, A. K. Patra

The bioequivalence between test and reference Tramadol and Paracetamol (37.5 + 325 mg) tablets was determined in 36 healthy subjects after a single dose in a randomized crossover study under fasting condition. Plasma concentrations were monitored over a period of 24 hour after the drug administration by validated LC/MS/MS analytical method. The pharmacokinetic parameters Cmax, AUC0-t, AUC0-∞, AUC0-t / AUC0-∞, Tmax, Kel and t½ were determined from plasma concentration time profile of both formulations and found to be acceptable. The calculated pharmacokinetic parameters were compared statistically to evaluate bioequivalence between the test and reference products. The analysis of variance did not show any significant difference between the two formulations and 90 % confidence intervals for the ratio of Cmax (92.29 -104.18 %), AUC0-t (99.52 - 104.11 %) and AUC0-∞ (99.05 - 104.22 %) for tramadol and Cmax (93.56 - 110.27 %), AUC0-t (96.37 - 102.70 %) and AUC0-∞ (97.22-103.28 %) for paracetamol test and reference products were within the 80 – 125 % interval, satisfying the bioequivalence criteria the US Food and Drug Administration Guidelines. These results indicate that the test and the reference products of Tramadol and Paracetamol are bioequivalent.

187-193

Authors: OO Johnson1*, GA Ayoola1, T Adenipekun2

The synergistic effect in the antimicrobial activity of the volatile oil blend from Garlic clove (Allium sativum) and tangerine fruits (Citrus reticulata) were investigated and compared to antimicrobial activity when the individual volatile oils were used alone. The volatile oils were extracted by steam distillation using Clevenger hydrodistillator apparatus and each oil was tested for antimicrobial activity, while equal volume of these oils were blended and tested for antimicrobial activity. The microorganisms used include, Staphylococcus aureus isolate, Escherichia coli isolate, Pseudomonas aeruginosa, Salmonella typhi, Candida albicans isolate, Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922 and Candida albicans ATCC 90028. The Minimum Inhibitory Concentrations (MICs) ranged from 9.31×10-13 – 7.88 mg/ml for garlic oil, 0.16 – 2.66 mg/ml for tangerine oil and 5.95×10-31 – 1.24 mg/ml for the essential oil blend. Minimum Inhibitory Concentration indicated that the Garlic oil and Tangerine oil blend was better at inhibiting the tested microorganisms than the individual oils except for Escherichia coli ATCC 25922 and Staphylococcus aureus ATCC 25923. The Gas Chromatography-Mass Spectrometry revealed Trisulphide, di-2-propenyl (30.32%) as the major component in the garlic oil extract and 3-Cyclohexene-1-methanol, alpha 4-trimethyl (33.38%) in the tangerine oil. While the equal volume of the oil blend also revealed Trisulphide, di-2-propenyl (15.92%) and 3-Cyclohexene-1-methanol, alpha.4-trimethyl (12.02%) as the major constituents though in lower concentrations. Hence, the more potent antimicrobial properties demonstrated by the oil blend can be exploited further with a view to generate new effective antimicrobial compounds.

84-87

Authors: Ruchika Nandha*

Lidocaine, a known local anaesthetic agent has been demonstrated to possess significant efficacy in managing asthma due to its anti inflammatory and direct spasmolytic actions. Various clinical studies have been conducted to assess the role of Lidocaine in asthma management with convincing results showing reduction in steroid dose or discontinuation of steroid therapy associated with improvement in quality of life, marking this old drug as a novel efficacious, fast and safe addition in armamentarium of anti asthma drugs. Inhaled Lidocaine when given alone causes biphasic effect on bronchi with initial bronchoconstriction followed by bronchodilatation. Treatment with combination inhalers, containing Lidocaine and a long-acting β2- agonist seems the safer and more reliable alternative to minimise adverse effects of initial reflex bronchoconstriction caused by inhaled Lidocaine. This review elucidates the available evidence on efficacy and safety of inhaled Lidocaine after analyzing various clinical studies. Searches of pubmed, Cochrane database, Medscape, Google and clinicaltrial.org were made for terms like Lidocaine and bronchial asthma.

96-100

Authors: Sunakar Panda*, D. L. Singh, S. K. Nayak

Some 1-Nicotinoyl-4-aryl-3-methyl 3a, 4-dihydropyrazole [3, 4c] pyrazoles were synthesised and their inclusion complexes were prepared with β-cyclodextrin. The compounds and their inclusion complexes were characterised by the study of their physical and spectral properties. The determination of stability constant of inclusion complexes and other thermodynamic parameters such as change in free energy, change in enthalpy and change in entropy, suggested the inclusion complex formation to be thermodynamically allowed. Further, the compounds and their inclusion complexes were screened for antibacterial activities against Escherichia coli (MTCC 40), Bacillus subtilis (MTCC 441), Staphylococcus aureus (MTCC 87) and Proteus vulgaris (MTCC 426). It was found that that the formation of inclusion complex causes an increase in antibacterial activity.

105-107

Authors: Singh Sunil*, Choudhary Nisha, Rai Jyoti, Inamullah, Sharma Surabhi, Yadav Ajit Kumar, Gautam Hemendra, Chaturvedi Shashank, Agrawal Vipin Kumar

A simple, sensitive and precise isocratic ultra performance liquid chromatographic method for the analysis of Lansoprazole has been developed, validated and used for the determination of compounds in commercial pharmaceutical products. The separation was carried out isocratically on a C18 column utilizing a mobile phase consisting of methanol: water (80:20 v/v) at a flow rate of 1.0 mL/min with UV detection at 284 nm. The retention time of Lansoprazole was found to be 3.905 min. The described method was linear over a concentration range of 50-30 μg/ml (r2 =0∙998) for the assay of Lansoprazole. Results of analysis were validated statistically. The results of the study showed that the proposed RP-UPLC method is simple, rapid, precise and accurate, which is useful for the routine determination of Lansoprazole in tablet dosage form and in its pharmaceutical dosage forms.

113-119

Authors: J Sojitra1, P Dave1, K Pandya2*, V Parikh2, P Patel2, G Patel2

Standardization of Ayurvedic formulations is an important step for the establishment of a consistent biological activity, chemical profile, or simply a quality assurance program for production and manufacturing of herbal drugs. WHO specifies guidelines for the assessment of the safety, efficacy and quality of herbal medicines as a prerequisite for global harmonization. Hence it is very essential to ensure that each packet sold in the market is standardized. In this research work, a polyherbal formulation (PHF), Caspa Drops has been taken to establish its standardization level using various physico-chemical parameters. For raw material various parameters such as pH, Moisture content, ash values, HPTLC fingerprinting, assays of marker compounds etc. were carried out to confirm their quality and potency. The presence of the raw materials in the finished product was carried out with the aid of sophisticated instruments. Study results revealed that product was well standardized at selected analytical parameters. All the tests were carried out in triplicates after which their SD was calculated. All the raw materials as well as finished product were found free from heavy metal and microbial contaminants.

125-128

Authors: Renjana P. K.*, John E. Thoppil

Cytotoxic and genotoxic effects of methanolic extract of the roots of Strobilanthes heyneanus Nees have been studied on the root meristem cells of Allium cepa. Roots of A. cepa were exposed to different concentrations (0.01%, 0.05%, 0.1% and 0.5%) of the extract for ½, 1, 2 and 3 h. Mitotic index and chromosomal aberrations in the treated cells were analysed. Distilled water has been used as control. Mitotic index val¬ues were decreased with increasing concentrations and longer treatment durations compared to the control (p < 0.05) in dose and time dependent manner. Additionally, different abnormal mitotic figures were observed in all treatments. Among these abnormalities were nuclear and chromosome lesions, anaphase bridges, C-mitosis, pulverization, stathmo-anaphases, diagonal orientation, chromosome fragments etc. The total percentage of aberrations generally increased with increasing concentrations of the extract and longer durations of exposure. The observations of the present study are a clear indication of clastogenic and non-clastogenic property of the extract, which is evident from the direct actions on the chromosomes and manifestation of spindle abnormalities.