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   2009| January-March  | Volume 1 | Issue 1  
    Online since June 4, 2009

 
 
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INVITED ARTICLE
Microcrystalline cellulose as a versatile excipient in drug research
N Saigal, S Baboota, A Ahuja, J Ali
January-March 2009, 1(1):6-12
DOI:10.4103/0975-1483.51868  
Microcrystalline cellulose (MCC) has emerged as the most resourceful excipient of all times in drug research. Thanks to its profusion in terms of grades available for different needs and its physical properties that support a variety of functionality requirements especially for the most frequently used unit dosage forms. MCC can be used as a bulking agent, disintegrant, binder, lubricant, and glidant besides being a stability enhancer and a secondary suspending agent. It can be used in direct compression of most drugs and saves material, capital, equipment, and labor. Its ever increasing applications in drug research include its utility in immediate release (tablets and liquids) dosage forms, sustained release dosage forms (multiparticulates and matrix tablets), topical preparations, oral liquids, organoleptic enhancements as in chewable and mouth dissolving tablets, anti-reflux, and nutraceuticals. The review discusses these applications in sufficient detail citing examples and investigating the justifications for such functions.
  15,731 846 1
PHARMACEUTICS
Colon targeted drug delivery: Different approaches
S Jose, K Dhanya, TA Cinu, J Litty, AJ Chacko
January-March 2009, 1(1):13-19
DOI:10.4103/0975-1483.51869  
Oral colon-targeted drug delivery systems have recently gained importance for delivering a variety of therapeutic agents for both local and systemic administration- local treatment of a variety of colonic diseases as well as systemic absorption of proteins and peptides. Targeting of drugs to specific sites of action provides several advantages over non-targeting of drugs. The colon, as a site for drug delivery, is also beneficial for the treatment of diseases sensitive to circadian rhythms and delivery of poorly absorbable drugs. The successful targeted delivery of drugs to the colon via the gastrointestinal tract requires the protection of a drug from degradation and release in the stomach and small intestine and then ensures abrupt or controlled release in the proximal colon. This review will cover both past and present approaches for achieving colon specific drug delivery.
  6,943 1,354 3
PHARMACOGNOSY
Pharmacognostical studies and evaluation of anti-inflammatory activity of Ficus bengalensis linn
VV Patil, RB Pimprikar, VR Patil
January-March 2009, 1(1):49-53
DOI:10.4103/0975-1483.51879  
Pharmacognostical parameters for the leaves of Ficus bengalensis were studied with the aim of drawing the pharmacopoeial standards for this species: macroscopical and microscopical characters, physio-chemical constants, extractive values with different solvents, fluorescence analysis of dry powder, its reaction after treatment with chemical reagents under visible light, and UV light at 254 nm and 366 nm. Preliminary phytochemical studies on the Ficus bengalensis leaves were conducted. The determination of these characters will aid future investigators in their pharmacological analyses of this species. The anti-inflammatory effect of ethanolic and petroleum ether extracts of ficus bengalensis were evaluated in experimental animals. We have determined the anti-inflammatory activity of ethanolic and petroleum ether extracts of the bark of Ficus bengalensis by oral administration of doses of 300 and 600 mg/kg/day of body weight to healthy animals. The extracts were studied for their anti-inflammatory activity in carrageenan-induced hind paw edema in rats and the paw volume was measured plethysmometrically at 0 3h after injection. The ethanolic and petroleum ether extracts of Ficus bengalensis , significantly reduced ( P <0.05) carrageenan-induced paw edema in rats. The ethanolic and petroleum ether extracts showed a greater anti-inflammatory effect compared with the standard drug Indomethacin. The present results indicated the ethanolic extract of Ficus bengalensis exhibited more significant activity than petroleum ether in the treatment of inflammation.
  4,363 586 3
PHARMACOLOGY
Anti-inflammatory activity of methanolic extracts of Dillenia indica L. leaves
SB Yeshwante, AR Juvekar, DM Nagmoti, SS Wankhede, AS Shah, RB Pimprikar, DS Saindane
January-March 2009, 1(1):63-66
DOI:10.4103/0975-1483.51885  
The anti-inflammatory activities of the methanol extract of Dillenia indica Linnaeus (Family Dilleniaceae) leaves were observed in various experimental models related to inflammation to provide some evidence for its traditional use. Anti-inflammatory activity was observed in carrageenan-induced edema and acetic acid-induced capillary permeability. The methanol extract showed significant ( P <0.01) anti-inflammatory activity in the paw edema test and acetic acid-induced capillary permeability at 200 mg/kg and 400 mg/kg. The extract at 100 mg/kg showed significant ( P <0.05) activity in acid-induced permeability. These findings support the folkloric use of Dillenia indica in diseases related to inflammatory conditions.
  3,884 373 1
PHARMACEUTICAL CHEMISTRY
Synthesis and characterization of 2, 5-disubstituted-1, 3, 4-oxadiazoles as potential anti-inflammatory agents
K Ilango, P Valentina, N Umarani, T Kumar
January-March 2009, 1(1):72-76
DOI:10.4103/0975-1483.51882  
The aim of this study was to design, synthesize, and investigate the in vivo anti-inflammatory activity of some novel 2, 5-disubstituted - 1, 3, 4-oxadiazole derivatives. Ethyl-4-acetamido phenoxy acetate (I) was prepared by the condensation of ethyl chloroacetate with starting material p-acetamidophenol in the presence of dry acetone and anhydrous potassium carbonate. Hydrazinolysis of (I) with hydrazine hydrate results in the formation of 4-acetamidophenoxy acetyl hydrazide (II), which on cyclisation with various substituted aromatic carboxylic acids in the presence of phosphorous oxychloride affords various 2, 5-disubstituted - 1, 3, 4-oxadiazole derivatives (IIIa-IIIi). The newly synthesized compounds were characterized by IR, 1 HNMR, and MS spectral data. The titled compounds were screened for in vivo anti- inflammatory activity using the carrageenan-induced paw edema method. A few of them manifested promising activity when compared with the standard drug Diclofenac sodium.
  3,781 464 1
PHARMACEUTICS
Development and evaluation of gelatin microspheres of tramadol hydrochloride
JB Jeevana, G Sunitha
January-March 2009, 1(1):24-27
DOI:10.4103/0975-1483.51871  
To develop formulations for effective management of chronic pain without side effects associated with NSAIDs and COX-2 antagonists, Tramadol hydrochloride, an opioid antagonist, was encapsulated within Gelatin microspheres for controlled delivery for longer periods. The microspheres were prepared using a single emulsion technique and were investigated. Tramadol hydrochloride could be encapsulated into Gelatin microspheres with an entrapment efficiency of 97.2%. Spherical, transparent, and free-flowing microspheres were obtained. Scanning electron microscopy revealed the spherical structures under the magnification of 200 m. The FTIR and DSC analysis indicated the stability and compatibility of the drug in gelatin microspheres. The microspheres were in the suitable particle size range of 20 to 160 m. The drug was released continuously for a period of 12 hrs with a maximum release of 99.79%.
  3,334 452 1
PHARMACEUTICAL ANALYSIS
Quantitative estimation of ascorbic acid by HPTLC in different varieties of amla
GS Chakraborthy
January-March 2009, 1(1):82-85
DOI:10.4103/0975-1483.51878  
Medicinal plants provide good remedies for human diseases and play a vital role in our day-to-day lifes. Phyllanthus emblica Linn family- Euphorbiaceae, commonly known as amla, is an important household fruit. The anti-ascorbic agent Vitamin C is a very effective antioxidant constituent present in amla. It is considered to be the richest source of Vitamin C. The determination of ascorbic acid in this fruit was done by thin layer chromatography (TLC) and qualitative test. Thus, it was quantified using the High Performance Thin Layer Chromatography (HPTLC) method in different varieties of fruit collected from different geographical regions. The method was carried out in TLC precoated aluminium plates with silica gel 60 GF as stationary phase. The solvent system was Ethanol: Acetic Acid (9.5:0.5 v/v) with the Rf value of 0.76 0.03). Quantitative analysis was carried out in the absorbance at 254 nm. The linearity regression analysis for the calibration showed r= 0.992 and 0.986 with respect to peak area and height in the concentration range of 0.5-5.0 g per spot. The highest content of ascorbic acid was found in the bigger variety collected from Shirpur. The method developed can be used for a routine analysis of ascorbic acid in crude drugs as well as in herbal and pharmaceutical dosage form containing amla as an ingredient.
  3,185 501 1
PHARMACOGNOSY
Study on the areca nut for its antimicrobial properties
Reena R Nelson Anthikat, A Michael
January-March 2009, 1(1):42-45
DOI:10.4103/0975-1483.51874  
This study evaluates the antibacterial, antifungal, and antiviral properties of the areca nut in vitro using isolated organisms. A variety of human and veterinary isolates, both gram positive and gram negative, were tested against areca nut extract by measuring the growth of the organisms using the spectrophotometric method. It was found that both gram negative and gram positive organisms were susceptible to the areca nut extract. The concentration needed for 100% inhibition of growth was found to be 3.3-7 g/ml for gram negative organisms and 16 g/ml for gram positive bacteria. The extract was also found to inhibit the growth of Candida albicans at a concentration of 16 g/ml and inhibited aflatoxin production by Aspergillus flavus . The extract was also found to inhibit the viral growth of the New Castle Disease Virus (NDV) and Egg Drop Syndrome Virus (EDS) grown in embryo cultures. These results indicate that betel nut chewing may have significant disinfective properties.
  2,883 265 -
GENERAL
Emerging opportunities in pharma industry
D Jha, K Jasubhai, MS Tomar
January-March 2009, 1(1):3-5
DOI:10.4103/0975-1483.51867  
Almost every pharmaceutical graduate, during the tenure of his/her study, is in a dilemma when it comes to choosing the professional field. Conventional jobs related to formulation, synthetic chemistry, analytical research, microbiology, marketing and sales are evergreen and well known, but there are some newer opportunities with tremendous potential which need to be talked about. There are upcoming jobs in the fields of clinical research, regulatory affairs and intellectual property rights. These are prospering at a very high rate and can give rise to a sea of opportunities in the coming years. The demands of these fields are continuously growing because of stringent regulatory requirements and a big pool of talented scientists to address these issues. The word 'outsourcing' also has a significant impact on the pharmaceutical industry. The lower economic costs, a vast pool of skilled workers and a large demographic variation of patient population favor the winds of change. Big pharmaceutical houses in the developed countries are keen on outsourcing their production and research to developing countries like China, India and Malaysia to increase the margin of their profits by lowering their research and filing costs. This in turn is a boon for the Indian pharmaceutical industry and is giving rise to the concept of contract manufacturing and contract research among the Indian counterparts. The outcome: strategic alliances between both Indian firms and foreign based companies and Indian companies entering the domain of contract research.
  2,418 564 -
PHARMACOGNOSY
Pharmacognostical studies of Bauhinia variegata linn root
DK Golwala, LD Patel
January-March 2009, 1(1):36-41
DOI:10.4103/0975-1483.51873  
The present study deals with the macroscopical and microscopical studies of Bauhinia variegata Linn root. Some distinct and different characters were observed with sections of young, thick and very old and thick roots. The anatomy of the root was studied by taking transverse section. Secondary phloem and secondary xylem were seen distinctly. Secondary phloem had fairly wide rays, dense masses of phloem fibers and radial rows of phloem elements. Secondary xylem had much wider, thin-walled vessels which were either solitary or in radial multiples. The xylem fibers constituted gelatinous type and normal type. Calcium oxalate crystals were predominantly prismatic type. Powder microscopical examination showed presence of xylem parenchyma cells, xylem fibers and vessel elements. Physicochemical parameters and preliminary phytochemical studies of the root powder were also carried out. The present study on pharmacognostical investigation of B. variegata L. root might be useful to supplement information in regard to its identification parameters assumed significantly in the way of acceptability of herbal drugs in present scenario lacking regulatory laws to control quality of herbal drugs.
  2,399 435 -
PHARMACOLOGY
Protective effect of polyherbal formulation on simvastatin hepatotoxicity in rats
J Vaghasiya, S Rathod, Y Bhalodia, R Manek, S Malaviya, N Jivani
January-March 2009, 1(1):57-62
DOI:10.4103/0975-1483.51883  
Objective: This study was designed to assess the effect of polyherbal formulation (PHF) on simvastatin hepatotoxicity in rats and to assess the possibility of co-administration of PHF along with hepatotoxic drugs. Methods: Hepatotoxicity in rats was induced by simvastatin (20 mg/kg p.o. for 30 days) and the protective effect of PHF (0.25 ml/kg/p.o. and 0.5 ml/kg/p.o. either along with drug or followed by inducing hepatotoxicity) was identified by estimating marker enzymes for liver function such as aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, and g glutamic transpeptidase; oxidative stress markers such as lipid peroxidation, reduced glutathione, super oxide dismutase, and catalase; and protein profile such as total bilirubin, direct bilirubin, total albumin, and total protein. A histopathological study was also carried out to confirm hepatotoxicity. Results and Discussions: Simvastatin hepatotoxicity was characterized by a significant increase in oxidative stress along with marker enzymes of liver function and depletion of proteins. Administration of PHF either along with simvastatin or followed by inducing hepatotoxicity significantly improved the level of marker enzymes for liver function, oxidative stress, and protein profile. Conclusion: The study suggests a protective role of PHF on simvastatin hepatotoxicity and it can be utilized to treat hepatotoxicity with long-term clinically useful drugs.
  2,011 336 -
Gastroprotective effect of medicinal plants from Chapada do Araripe, Brazil
Gerlania de Oliveira Leite, Antonia Rosangela Soares Penha, Glauberto Quirino da Silva, Aracelio Viana Colares, Fabiola Fernandes Galvao Rodrigues, Jose Galberto Martins Costa, Andre Luiz Herzog Cardoso, Adriana Rolim Campos
January-March 2009, 1(1):54-56
DOI:10.4103/0975-1483.51881  
Gastric ulcer is a serious gastrointestinal disorder that requires a well targeted therapeutic strategy. A number of drugs are available for the treatment of gastric ulcer, but clinical evaluation has shown incidence of relapses, side effects, and drug interactions. The search for novel molecules has been extended to herbal drugs that offer better protection and decreased relapse. The essential oils from Croton zehntneri (EOCZ) and Vanillosmopsis arborea (EOVA), the oil from Caryocar coriaceum pulp (OCC), the latex from Himatanthus drasticus (LHD), and the extract from Stryphnodendron rotundifolium (ESR) obtained from Chapada do Araripe, Cearα (Brazil) have been evaluated for cytoprotetive activity on ethanol-induced ulcer formation in mice. EOCZ, EOVA, OCC, and ESR were administrated by gavage at doses of 200 and 400 mg/kg and LDH, by the same way, at 0.2 and 0.4 mL/animal (n=8). Following 60 min, mice were given 0.2 mL of ethanol (96%) by gavage. Thirty minutes after the administration of ethanol, all groups were sacrificed and the gastric ulcer index was calculated by planimetry. Preliminary results suggest that all the plants tested showed significant activity. EOVA (6.471.91%*), OCC (8.862.45%*) and ESR (1.500.30%**) were the most active. Data are expressed as means.e.m. of the lesioned area (%) and were analyzed by ANOVA and Student-Newman-Keuls test (* P <0.05 and ** P <0.01 vs. control). Phytochemical screening showed the presence of tannins, terpenes, and essential fatty acids, thus suggesting that these substances may be involved in the observed antiulcer activity.
  2,092 212 5
PHARMACEUTICS
Buoyant microspheres of famotidine: An approachable dosage form for gastric treatment
AK Jain, CP Jain
January-March 2009, 1(1):20-23
DOI:10.4103/0975-1483.51870  
The present study involves the preparation and evaluation of buoyant microspheres using famotidine as a model drug for prolongation of gastric retention time. The microspheres were prepared by the solvent evaporation method using different polymers i.e., acrycoat S100 and cellulose acetate. The size or average diameter (d avg ) characterized by optical microscopic method and surface morphology (internal texture) was recognized by the scanning electron microscopic method, which showed that fabricated microspheres were spherical with a smooth surface. The presence of pores was detected; this indicated leaching of the drug during the dissolution without gelation of polymeric surface. Effects of the stirring rate during preparation and polymer concentration on the size of microspheres and drug release were also observed by in vitro drug release kinetic studies. The prepared microspheres exhibited prolonged drug release (18 h). The cumulative release of famotidine significantly decreased with increasing polymer concentration ( P < 0.05). The increased density of the polymer matrix at higher concentrations resulted in an increased diffusional path length. This may decrease the overall drug release from the polymer matrix. Furthermore, smaller microspheres are formed at a lower polymer concentration and have a larger surface area exposed to dissolution medium, giving rise to faster drug release that remained buoyant for more than 12 h. The mean particle size increased and the drug release rate decreased at higher polymer concentrations. No significant effect of the stirring rate during preparation on drug release was observed. In vitro studies demonstrated diffusion-controlled drug release from the microspheres.
  1,874 430 -
PHARMACOGNOSY
Natural products as regulators of progenitor cells: Role in cardiovascular regenerative medicine
AHS Kumar, BG Hynes, KK Mueen Ahmed
January-March 2009, 1(1):28-35
DOI:10.4103/0975-1483.51872  
The cellular network in vasculature is predominantly composed of two distinct cell types i.e., endothelial and smooth muscle cells, which along with the connective tissue and extracellular matrix govern the tone and function of the blood vessels. In response to vascular injury, progenitor cells are mobilized from local niece, peripheral circulation, or bone marrow in order to contain the inflammatory process in progress and/or repair the damaged vasculature. The progenitor cells are reported to play a significant role in the repair of vascular disorders. A variety of cytokine-chemokine interplay are shown to precisely regulate the mobilization, homing, and differentiation of progenitor cells as a consequence to the vascular injury and enable restoration of vascular structure and function. The cytokine-chemokine interplay and factors leading to impairment of the progenitor cell dynamics are complex cascades, which govern the regenerative capacity of vascular progenitors, thus negatively modulating the development of atherosclerosis or other vascular diseases. These complex cascades provide an opportunity for identifying novel diagnostic markers and therapeutic targets for combating vascular diseases. However, many challenges remain in understanding dynamics of progenitor cells origin, mobilization, homing, and differentiation. Recent studies have reported the potential of natural products to mimic the role of cytokines in modulating the vascular progenitor function. Furthermore, some natural products have been shown to restore the defective progenitor cell function, thus promoting the vascular repair process. In this review, we provide a basic background on vascular progenitor biology and highlight the untapped potential of natural products to positively modulate the progenitor biology.
  1,959 209 -
PHARMACEUTICAL MANAGEMENT
Effective tools of pharma counseling
KR Vinod, S Sandhya
January-March 2009, 1(1):90-93
DOI:10.4103/0975-1483.51875  
Pharma counseling is an important tool for any community pharmacist. With a 110 crore population, there is a tremendous opportunity for Pharma counselling on the Indian subcontinent. This could highlight a new beginning and recognition for pharmacists. Alas, this opportunity is not being explored properly. This article gives in-depth information on how to implement and improve a community pharmacy and serve our society better.
  1,922 229 -
PHARMACEUTICAL CHEMISTRY
Licofelone- novel analgesic and anti-inflammatory agent for osteoarthritis: An overview
K Gaur, ML Kori, LK Tyagi, V Singh, RK Nema, P Tripathi, CS Sharma
January-March 2009, 1(1):67-71
DOI:10.4103/0975-1483.51884  
Licofelone (2-[6-(4-chlorophenyl)-2, 2-dimethyl-7-phenyl-2, 3-dihydro-1H-pyrrolizin-5-yl] acetic acid) is the first member of a new class of analgesic and anti-inflammatory drugs acting by dual mechanism inhibiting both cyclooxygenase (COX) and 5-lipooxygenase (5-LOX). Inhibition of 5-LOX may reduce the gastrointestinal toxicity associated with other non steroidal anti-inflammatory drugs (NSAIDs), which only inhibit cyclooxygenase (COX). It has been evaluated for the treatment of osteoarthritis (OA), the most common form of arthritis. It has been found to be significantly effective in Phase III clinical trials conducted on patients of osteoarthritis. The present review describes the pharmacological and clinical developments of licofelone as a dual inhibitor for COX and 5-LOX.
  1,885 185 -
PHARMACOGNOSY
GC-MS analysis of propolis of Indian origin
N Kumar, KK Mueen Ahmed, R Dang, TN Shivananda, K Das
January-March 2009, 1(1):46-48
DOI:10.4103/0975-1483.51876  
More than 300 constituents have been identified in different propolis samples. This study investigated the composition of ethanolic extracts of propolis samples collected from the Gujarat zone. A gas chromatography-mass spectrometry was carried out on a Agilent GC-MS 5975 under electron impact ionization (70 eV). The chromatographic column for the analysis was done by the HP5MS capillary column (30 m x 0.25 mm internal diameter). The carrier gas used was helium at a flow rate of 1 ml/min. The oven temperature was 100C to 280C with a constant increase of 10C. Propolis samples were analyzed with the column held initially at 60C for 2 min and then increased to 230C with a 2C/ min heating ramp and then kept at 230C for 3 min. Finally, the temperature was increased to 280C with a 3C/min heating ramp. The injection was performed in split mode at 220C. Sample volumes of 1 μl were injected and analyzed by GC-MS. The following compounds were identified for the first time in the propolis sample: p-coumeric acid, Benzyl cinnamate, 4-pentanoic acid, and Ferulic acid. The main type of the compound identified was fatty acids derivatives. Similar results were found by Silici, et al . [5] for the turkey propolis.
  1,853 215 -
EDITORIAL
The launch of J Young Pharm
KK Mueen Ahmed
January-March 2009, 1(1):1-1
DOI:10.4103/0975-1483.51866  
  1,667 371 3
PHARMACEUTICAL CHEMISTRY
QSAR analysis on β-carboline as antitumor agent
P Valentina, K Ilango, K Yamuna, D Purushothaman, A Samyuktha Rani
January-March 2009, 1(1):77-81
DOI:10.4103/0975-1483.51880  
A quantitative structure activity relationship (QSAR) study on β-Carboline derivatives as an anti-tumor agent was performed with 30 compounds of β-Carboline derivatives on different cancer cell lines from reported work. Molecular modeling studies were performed using ChemBioDraw Ultra 11.0. The sketched structures were subjected to energy minimization and the lowest energy structure was used to calculate the physiochemical properties. The regression analysis was carried out using a computer program called Valstat. The best models were selected from the various statistically significant equations. From the derived QSAR model, it can be concluded that the cytotoxic activity of β-carboline derivatives is strongly influenced by the thermodynamic and electronic nature of the substituents.
  1,742 204 -
PHARMACEUTICAL MANAGEMENT
Prophylaxis in migraine management
M Sonal Sekhar, TP Aneesh, S Sathianarayanan, K JinyVarghese, DT Vasudevan, KG Revikumar
January-March 2009, 1(1):86-89
DOI:10.4103/0975-1483.51877  
A migraine is the most common cause of severe, recurring headache. With the recent advances in our understanding of migraine, it can be effectively treated and even prevented. Prophylactic treatment of migraines is indicated when patients have three or more severe migraine attacks a month that interfere with quality of life or when attacks are prolonged and symptomatic medication used alone is not satisfactory. The major objective of migraine prophylactic therapy is optimizing the patient's ability to function normally by reducing the frequency, duration, and intensity of attacks. The major migraine preventive therapies include β-blockers, calcium-channel blockers, and tricyclic medications. Preventive treatment should be tailored to individual patient needs. This requires that patient and healthcare professionals understand the rationale and participate actively in decisions regarding therapeutic intervention.
  1,594 168 1
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