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Design and development of bilayer tablet for immediate and extended release of acarbose and metformin HCl
Meenakshi Joshi, Ruchi Tiwari, Gaurav Tiwari
July-December 2014, 5(2):93-108
The present investigation studied a novel Bilayer tablet having extended release (ER) system of metformin HCl (M.HCl) with Eudragit RS 100 and RL 100 and immediate release (IR) system of Acarbose with PVP K30 and PEG 6000 in different ratios using solvent evaporation technique. Solid dispersions (SDs) were characterized by Fourier Transform-Infra Red spectroscopy, Diffrential Scanning Calorimetry, X-Ray Diffractometry and Scanning Electron Microscopy. Selected SD system was subjected to Bilayer tablet preparation by direct compression. Compressed tablets were evaluated for physical parameters, drug release and stability. SEM studies suggested the homogenous dispersion of the drug in polymers. FT-IR studies confirmed the formation of hydrogen bonding between the drug and polymer. XRD and DSC suggested the amorphous nature of the drug in SDs. All tablet formulations showed compliance with pharmacopoeial standards. In-vitro dissolution kinetics followed the Higuchi model via a non-fickian diffusion controlled release mechanism after the initial burst release. Stability studies conducted for optimized formulation did not show any change in the physical properties, drug content and drug release. Bilayer tablets showed an IR effect to provide the loading dose of the drug, followed by ER effect for 12 h, indicating a promising potential of the M.HCl and Acarbose Bilayer tablet as an alternative to the conventional dosage form.
  2,505 709 -
Acute porphyria: The drug demon etiology
Sridharan Kannan, S Gowri
July-December 2015, 6(2):47-51
Drugs are one of the important factors that precipitate acute attacks in patients with porphyria. Various in vitro and preclinical animal models exist for determining porphyrogenicity of a drug, but these predictions are not very reliable. Ambiguities still remain with many drugs as to whether they are safe in patients with porphyria. An algorithm for determining the porphyrogenic potential using evidence from anectodotal reports, lipophilicity, affinity of a drug to the Cytochrome enzymes (CYP450), ability to induce or irreversibly inhibit either CYP450 2C9 or CYP450 3A4 and the ability to induce hepatic 5-aminolevulinate synthase has been devised. Management of an acute attack of porphyria involves symptomatic treatment and administration of haem arginate. Several international networks have been initiated that serve as good sources of information for the safe use of drugs to be used in porphyria.
  1,519 1,060 -
Stress degradation studies of Telmisartan and Metoprolol extended release tablets by a validated stability indicating reverse phase-high performance liquid chromatography method
Kabeer Ahmed Shaikh, Ashish Tanaji Patil
July-December 2014, 5(2):158-163
Background and Aim: A sensitive reverse phase high-performance liquid chromatographic method has been developed for the simultaneous determination of Telimisartan and Metoprolol in tablet dosage form. Materials and Method: The chromatographic separation was achieved on Inertsil ODS 3V, 150 x 4.6 mm, 5μ analytical column. Mobile phase consisting of mobile phase A- 0.05M sodium dihydrogen phosphate buffer pH 3.0 and mobile phase B-Acetonitrile, with gradient program time in min /Mobile phase B% 0/22, 4/45, 6/45,18/22, 20/22. Detector was set at 222nm. Results and Conclusion: The described method shows excellent linearity over a range of 80-2 μg mL−1 for Telmisartan and 100-4 μg mL−1 for Metoprolol. The correlation coefficient for Telmisartan is 0.9998 and Metoprolol is 0.9999. The proposed method was found to be suitable for determination of Telmisartan and Metoprolol in tablet dosage form. Forced degradation of the drug product was conducted in accordance with the ICH guideline. Acidic, basic, hydrolytic, oxidative, thermal and photolytic degradation was used to assess the stability indicating power of the method. The drug product was found to be stable in acid, oxidation, thermal and photolytic stress condition and found degradation in base hydrolysis stress condition.
  2,244 252 -
Screening of Indian medicinal plants for cytotoxic activity by Brine Shrimp Lethality (BSL) assay and evaluation of their total phenolic content
Mahesh Biradi, Kirankumar Hullatti
July-December 2014, 5(2):139-144
Objective: Plant-derived cytotoxic constituents and polyphenolic compounds have played an important role in the development of clinically useful anticancer agents. In this context, we have selected six Indian medicinal plants based on the literature claims and an attempt was made to evaluate the cytotoxic potential and total phenolic content (TPC) of their methanol extracts and fractions. Materials and Methods: Six plants have been selected for the study, namely, Artemisia absinthium Linn. (Asteraceae), Oroxylum indicum (Linn.) Vent. (Bignoniaceae), Heliotropium indicum Linn. (Boraginaceae), Amorphophallus sylvaticus (Roxb.) Kunth. (Araceae), Mimosa pudica Linn. (Mimosaceae), and Premna serratifolia Linn. (Verbenaceae). Authenticated plant materials were subjected to extraction with methanol by cold maceration and hot percolation methods. The extracts were fractionated into four fractions (F1, F2, F3, and F4). Preliminary phytochemical investigation was carried out for all extracts and fractions. All extracts and their fractions were subjected to cytotoxicity screening by brine shrimp lethality (BSL) bioassay. The plants with significant cytotoxicity were evaluated for TPC by using Folin-Ciocalteu reagent. Results: F1, F2, and F3 fractions of A. absinthium and P. serratifolia and F1 fraction of M. pudica have shown significant cytotoxicity (lethal concentration (LC 50 ) < 100 ppm) compared with other fractions. F1, F2, and F3 fractions of A. absinthium show the LC 50 values 32.52, 14.27, and 24.02, respectively; F1, F2, and F3 of P. serratifolia show LC 50 values 7.61, 4.01, and 10.91 and same for F1 fraction of M. pudica was 34.82 μg/ml, respectively. TPC was found to be significantly higher (39.11 mg gallic acid equivalent (GAE)/g) in P. serratifolia compared with other two plants. Conclusion: The cytotoxicity screening system confirmed the proposed anticancer plants used by traditional healers and literature claims.
  1,970 227 -
Cichorium intybus: A concise report on its ethnomedicinal, botanical, and phytopharmacological aspects
Sneha Das, Neeru Vasudeva, Sunil Sharma
January-June 2016, 7(1):1-12
Cichorium intybus L. (chicory) is a Mediterranean plant species belonging to the Asteraceae family. Chicory is gaining interests because of its culinary features, nutritional values and medicinal characteristics. C. intybus has been implemented in folk medicine from North Africa to South Asia for several 100 years. In Indian medicine, it has been used to treat fever, diarrhea, spleen enlargement, jaundice, liver enlargement, gout, and rheumatism. In China, it is valued for its tonic effects upon the liver and digestive tract. In Germany, chicory has been used as a folk medicine for everyday ailments. Thus, C. intybus is a plant of great economic potential due to high concentrations of fructooligosacharide, known as inulin, in its roots, used as a replacement ingredient for sugar and fat. The other various phytoconstituents reported in chicory are sucrose, cellulose, proteins, caffeic acid derivatives, flavonoids, polyphenols, carotenoids, anthocyanins, tannins, coumarins, sesquiterpene lactones, fatty acids, pectin, cholins, benzo-isochromenes, alkaloids, vitamins, amino acids, and minerals. The therapeutic investigations reveal that C. intybus is useful for maintaining normal health and has nematicidal, antihepatotoxic, antidiabetic, cardioprotective, antiallergic, antihyperlipidemic, anti-inflammatory, antineoplastic, calcium homeostater, bulking agent, immunostimulatory, prebiotic, protective against pancreatitis, antimicrobial, and antioxidant effects. This review encompasses botany, ethnomedicinal uses, phytoconstituents, pharmacological uses, and toxicity studies of C. intybus L.
  1,867 317 -
Assessment of locomotion behavior in adult Zebrafish after acute exposure to different pharmacological reference compounds
Pankaj Gupta, Shailaja B Khobragade, Vyas M Shingatgeri, Srinivisan M Rajaram
July-December 2014, 5(2):127-133
Objectives: The objective of the present study was to assess locomotor behavior of adult zebrafish after acute exposure to different pharmacological reference compounds. Materials and Methods: Adult zebrafish of 4-5-months-old were exposed to different concentrations of known reference compounds for 15 min. The test was conducted separately for each drug concentration as well as control. Locomotor activity parameters viz. distance travelled, speed, total mobile time, and total immobile time were recorded for each animal during the exposure period. Results: Out of 11 compounds tested, nine compounds showed decrease in locomotor behavior with significant changes in distance travelled, speed, total mobile time, and total immobile time. Caffeine exhibited biphasic response in locomotion behavior, while scopolamine failed to induce any significant changes. Conclusion: In view of the above findings, these results suggested that exposure of adult zebrafish with different known compounds produce the expected changes in the locomotion behavior; therefore, adult zebrafish can be used an alternative approach for the assessment of new chemical entities for their effect on locomotor behavior.
  1,797 316 -
Evaluation of antifungal activity of aqueous extracts of some medicinal plants against Aspergillus flavus, pistachio aflatoxin producing fungus in vitro
Sahar Omidpanah, Hamid Sadeghi, Mehdi Mohamadian Sarcheshmeh, Azadeh Manayi
July-December 2015, 6(2):66-69
Background: Contamination with aflatoxin, by Aspergillus flavus, is one the major challenges in agriculture and food industry. Preparation of organic products using natural components is widely considered these days. Aims: In this study, effects of aqueous extracts of five medicinal herbs, including thyme, senna, mentha, basil, and safflower on the growth of the A. flavus were investigated. Mterials and Methods: The extracts with different concentrations (200-800 µg/mL) and polyethylene glycol with the equal osmotic potential of plant extracts were added to the potato dextrose agar medium to evaluate fungus growth after 7 days using agar dilution method. Benomyl, a fungicide, was used as a positive standard. The tests were performed in triplicate, and the mean diameters of fungus growth were calculated as well. Results and Conclusion: All concentrations of the plants extracts significantly inhibited the fungus growth in comparison with each other and control treatments, while the extracts of thyme and safflower manifested the most effective prohibition compared to benomyl with minimum inhibitory concentration of 200 and 400 µg/mL, respectively.
  1,571 382 1
Phytochemical evaluation of the ethanolic extracts of some Nigerian herbal plants
Enegide Chinedu, Arome David, Solomon F Ameh
January-June 2015, 6(1):11-14
Background: Herbs basically, are plants or plant parts employed due to their scent, medicinal properties or flavor. Herbal medicines have longed been used in the management and treatment of various ailments even before the arrival of modern medicine. Herbal medicines are still being used today, as it has even gained a new momentum in the field of medicine. Phytochemicals are responsible for eliciting definite physiological effects of various herbs in the body. In Nigeria, various plants are being used traditionally in the treatment of divers ailments. Some of these plants include Tapinanthus bangwensis, Tamarindus indica, Ocimum gratissimum, Allium sativum, Kigelia africana, Azadirachta indica, Solanum virginianum, Myrianthus serratus and Vernonia amygdalina. Though there have been claims of success in their traditional usage, it is however important to carry-out phytochemical assessment on them. Aim: The aim was to evaluate the phytochemical constituents of the ethanolic extract of these plants. Materials and Methods: The plant materials were extracted, and the plant extracts were screened for the presence of various phytochemical constituents such as alkaloids, steroids, glycosides, cardiac glycosides, flavonoids, carbohydrate, saponins, tannins and anthraquinones using the standard methods. Result: The experimental result revealed the presence of the various bioactive phytochemicals in the different plant extracts investigated. These phytochemicals were however present in different proportions in the various plant extracts. Conclusion: The experimental result vindicates the usage of these plants traditionally for medicinal purposes.
  1,458 243 -
Validated RP-HPLC-PDA method for simultaneous determination of Zidovudine, Lamivudine, and Nevirapine in pharmaceutical formulation
B Mohammed Ishaq, K Vanitha Prakash, G Krishna Mohan
January-June 2015, 6(1):27-32
Aim and Objectives: A simple, rapid, and sensitive high performance liquid chromatographic method with ultraviolet detection has been developed and validated according to the International Conference on Harmonization (ICH) guidelines for the quantitation and qualification of zidovudine (ZID), lamivudine (LAM), and nevirapine (NEV) in pharmaceutical dosage forms. Materials and Methods: The proposed method was based on the separation of the drugs in reversed phase mode using Water's C18 250 cm × 4.6 mm, 5 μ particle size column maintained at an ambient temperature. The optimum mobile phase consisted of Water: Methanol (70:30 v/v), pH adjusted to four with orthophosphoric acid (OPA). The flow rate of mobile phase was set 1.0 mL min -1 and photodiode array detection was performed at 275 nm with a total run time of 8 min which is very short for accurate analysis of simultaneous estimation of three analytes. The method was validated according to ICH guidelines. Results: The method was linear over the concentration range of 25-75 μg mL -1 with limit of quantifications (LOQ) of 13, 0.49, and 0.40 ng mL -1 for ZID, LAM and NEV respectively and limit of detection (LOD) of 4, 0.14, and 0.12 ng mL -1 for ZID, LAM and NEV respectively. Accuracy (% recovery studies) and precision values of both inter and intraday obtained from six different replicates for all the analytes ranged from 99.00% to 100.00% and % relative standard deviation of precision (assay) was between 0.64 and 1.28, respectively. All the three analytes and their combination drug product were exposed to thermal, photolytic, hydrolytic, reductive, oxidative and peroxide stress conditions and the stressed samples were analyzed by the proposed method. There were no interfering peaks from excipients, impurities or degradation products due to variable stress conditions and the proposed method is specific for the simultaneous estimation of ZID, LAM and NEV in the presence of their degradation products. Conclusion: The proposed method can be successfully applied in the quality control and stability samples of pharmaceutical dosage forms.
  1,493 195 -
Histopathological alterations in the vital organs of Indian Major Carps with parasitic infestation in fish farms West Bengal, India
Kurva Raghu Ramudu, Gadadhar Dash
January-June 2015, 6(1):38-43
The study was conducted to investigate the histological changes of vital organs such as kidney, gills and brain with the mixed infestation of parasites in Indian Major Carps (IMC). The parasites such as Myxobolus spp., Thelohanellus spp., Trichodina spp., Dactylogyrus spp., Gyrodactylus spp. and Nematodes were observed in three IMC. Several histological alterations were observed in the kidney of Catla catla, Labeo rohita and Cirrhinus mrigala, which includes vacuolar degeneration in the epithelium of renal tubules, focal areas of necrosis, proliferation of bowman's capsule and many cases the renal tubules lost its shape and canalculi formation was observed. The gills showed focal areas of necrosis, exacerbated swelling of gill arch, deposition of distinct black melanin pigmentation at the basal point of the gill arch, loss of primary and secondary lamellae, prominent vacuolar degeneration and formation of vacuoles. The presence of protozoan parasites in brain tissue resulted necrosis of the brain tissue, black pigmentation, vacuolization of myelin sheath of nerve fibers and common degenerative changes. Aims: To study histological changes of vital organs such as kidney, gills and brain with the mixed infestation of parasites in Indian Major Carps (IMC). Settings and Design: The organs fixed in 4% formalin are transferred to 50% ethyl alcohol and stored for further analysis. Materials and Methods: Histopathological analysis was made as described by Roberts. Statistical Analysis Used: Nil. Results: Described in text. Conclusions: The present study brings about conclusion that impact of mixed infestation of the parasites on their hosts was severe. Histopathological changes were observed in vital organs which might be due to toxins released by different parasites or physical damage of tissue with the presence of parasites.
  1,476 194 -
Formulation and evaluation of sustained release matrix tablets of pioglitazone hydrochloride using processed Aloe vera mucilage as release modifier
Manoj Choudhary, Tushar Salukhe, Aditya Ganeshpurkar, Vikas Pandey, Nazneen Dubey, Divya Bansal
January-June 2015, 6(1):5-10
Background: Natural gums and mucilage which hydrates and swells on contact with aqueous media are used as additives in the formulation of hydrophilic drug delivery system. Aim: The purpose of this study was to develop a new monolithic matrix system for complete delivery of Pioglitazone hydrochloride (HCl), in a zero-order manner over an extended time period using processed Aloe vera gel mucilage (PAG) as a release modifier. Materials and Methods: The matrices were prepared by dry blending of selected ratios of polymer and ingredients using direct compression technique. Physicochemical properties of dried powdered mucilage of A. vera were studied. Various formulations of pioglitazone HCl and A. vera mucilage were prepared using different drug: Polymer ratios viz., 1:1, 1:2, 1:3, 1:4, 1:5 for PAG by direct compression technique. Results: The formulated matrix tablets were found to have better uniformity of weight and drug content with low statistical deviation. The swelling behavior and in vitro release rate characteristics were also studied. Conclusion: The study proved that the dried A. vera mucilage can be used as a matrix forming material for controlled release of Pioglitazone HCl matrix tablets.
  1,323 244 -
Anti-inflammatory and antinociceptive activity of vanillin
Junaid Niazi, Narinderpal Kaur, Rajesh K Sachdeva, Yogita Bansal, Vikas Gupta
July-December 2014, 5(2):145-147
Objective: Vanillin is known to have antimutagenic, anti-invasive, and metastatic suppression potential. Antinociceptive property in acetic acid and antioxidant and hepatoprotective properties in carbon tetrachloridetreated rats have also been demonstrated. Objective of this study is to evaluate the anti-inflammatory and antinociceptive activity of vanillin. Materials and Methods: The drugs and fine chemicals were purchased from Sigma Aldrich, Ranbaxy, India and MS Pharmaceuticals, India. Experimental Rats were assigned to groups of six animals each and anti-inflammatory activity was evaluated using carrageenan induced rat paw aedema and anti-nocicetion was done using tail flick method. Carrageenan-induced paw edema was used to evaluate pre and post anti-inflammatory activity and tail flick method was used in the evaluation of antinociceptive activity. Two-way analysis of variance (ANOVA) followed by Student's t-test was used for statistical analysis in both the studies. Results: There was significant decrease in the paw volume at 50 and 100 mg/kg doses of vanillin when compared with control group. Meanwhile, an increase in percentage maximum possible effect (MPE) was seen by same doses of vanillin. Conclusion: It has been concluded from the findings that vanillin possesses the anti-inflammatory and antinociceptive effect by virtue of its antihistaminic and central analgesic activity, respectively.
  1,337 224 -
Modulation of solubility and dissolution of furosemide by preparation of phospholipid complex
Mona Semalty, Prateeksha Badoni, Devendra Singh, Ajay Semalty
July-December 2014, 5(2):172-176
Aim: The aim of this study is to improve the solubility and dissolution of furosemide (a potent high ceiling diuretic used for the treatment of hypertension and a Class IV drug that is low solubility and low permeability drug as per the Biopharmaceutical Classification System) by preparing its phospholipid complexes or pharmacosomes. Materials and Methods: Furosemide was complexed with phosphatidylcholine in four different molar ratios (1:1, 1:2, 1:3 and 1:4) by conventional solvent-evaporation technique. The pharmacosomes prepared were evaluated for drug content, solubility, X-ray powder diffraction (XRPD) and in-vitro dissolution study. Results: Pharmacosomes of furosemide showed high drug content ranging from 88.30% to 100%. XRPD studies confirmed the formation of phospholipid complex and the amorphization of drug in the complex. The water solubility was found to be increased up to six-fold in the complexes. The octanol solubility also increased in the complexes indicating the probable increase in permeability. The in-vitro dissolution profile of the prepared complexes was found to be much better than furosemide. Conclusion: It was concluded that the phospholipid complexes can be effectively used for improving the solubility, dissolution, permeability and hence the bioavailability of furosemide like Class IV drugs.
  1,349 208 -
Development and validation of reverse phase-high performance liquid chromatographic method for simultaneous estimation of naproxen sodium and esomeprazole magnesium trihydrate
Sampath Saravanan, Thomas Sudha, Bachu Surendra
July-December 2014, 5(2):109-114
Background: Naproxen sodium (NAP) is a non steroidal anti-inflammatory drug and Esomeprazole magnesium trihydrate (ESO) is a proton pump inhibitor. Aim: A high performance liquid chromatographic method was developed and validated for the quantitative determination of naproxen (NAP) sodium and esomeprazole (ESO) magnesium trihydrate. The different analytical parameters such as linearity, precision, accuracy, limit of detection and limit of quantification were determined according to the International conference harmonization (ICH) Q2B guidelines. Materials: Chromatography was carried out by isocratic technique on a reversed phase C18 base deactivated silanol hypersil column with mobile phase and optimized depending upon the polarity of the molecules. Results: The calibration curves were linear (r2 > 0.9997) over the concentrations 20-120 μg/mL for NAP sodium and 0.8-4.8 μg/mL for ESO magnesium trihydrate. The method was accurate and precise with recoveries in the range of 99.48-99.98% for the two drugs and relative standard deviation less than 2%. No chromatographic interferences from the tablet excipients were found. Conclusion: The proposed method was highly sensitive, precise and accurate. Hence the method was successfully applied for the reliable quantification of active pharmaceutical ingredients content in house prepared tablet formulation of NAP sodium and EOS magnesium trihydrate.
  1,332 219 -
Spectrophotometric method for simultaneous estimation of atazanavir sulfate and ritonavir in tablet dosage form
Disha A Patel, Bhavini N Patel, Chhaganbhai N Patel
January-June 2015, 6(1):1-4
Background: Ritonavir (RTV) and atazanavir sulfate (ATV) are protease inhibitor and RTV mostly used as a booster for increasing the bioavailability of other protease inhibitors like ATV. Aims: Quality assessment of the new dosage form of RTV and ATV i.e., tablets is very essential and hence this work deals with to develop sensitive, simple and precise method for simultaneous estimation of ATV and RTV in tablet dosage form by absorbance correction method. Materials and Methods: The present work was carried out on Shimadzu Ultraviolate(UV)-1700 double beam spectrophotometer with 1 cm path length supported by S Shimadzu, model-1700(Japan), UV-Probe software, version 2.31 was used for spectral measurements with 10 mm matched quartz cells. Standard ATV and RTV were supplied by Cipla Pharmaceutical Ltd. Methanol was purchased from Finar Chemicals Pvt. Ltd. Results and Conclusion: The λmax or the absorption maxima for ATV and RTV were found to be 279 and 240 nm, respectively in methanol as solvent. The drugs follow Beer-Lambert's law in the concentration range 30-90 and 10-30 μg/mL for ATV and RTV, respectively. The percentage recovery was found to be 100-100.33% and 100-101.5% for ATV and RTV, respectively. The method was validated for different parameters as per the International Conference for Harmonization Guidelines.
  1,283 250 -
Functional characterization and expression of folate receptor-α in T47D human breast cancer cells
J Renukuntla, S Shah, S.H.S. Boddu, AD Vadlapudi, RK Vadlapatla, D Pal, Ashim K Mitra
July-December 2015, 6(2):52-61
Purpose: The objective of this study was to investigate the functional and molecular expression of a carrier mediated system responsible for folate uptake in breast cancer (BC) (T47D) cells and to delineate the mechanism of intracellular regulation of this transport system. Materials and Methods: [ 3 H]-folic acid uptake was studied in T47D cells with respect to time, pH, temperature, sodium and chloride ion dependency. Inhibition studies were conducted in the presence structural analogs, vitamins, metabolic and membrane transport inhibitors. [ 3 H]-folic acid uptake was also determined with varying concentrations of cold folic acid. Uptake kinetics was studied in the presence of various modulators of intracellular regulatory pathways; calcium-calmodulin, protein kinases A and C (PKA and PKC) and protein tyrosine kinase (PTK). Molecular evidence was studied by qualitative and quantitative polymerase chain reaction (PCR) and Western blot analysis. Results: Linear increase in [ 3 H]-folic acid uptake was observed over 30 min. The process followed saturation kinetics with an apparent K m of 11.05 nM, V max of 1.54 * 10−8 μmoles/min/mg proteins and K d of 9.71 * 10−6 /min for folic acid. Uptake process was found to be dependent on pH, sodium ions, chloride ions, temperature and energy. Uptake was inhibited in the presence of structural analogs (cold folic acid, methyltetrahydro folate and methotrexate), but structurally unrelated vitamins did not show any effect. Membrane transport inhibitors such as SITC, DIDS, probenecid and endocytic inhibitor colchicine significantly inhibited the [ 3 H]-folic acid uptake process. PKA, PTK and Ca 2+ /calmodulin pathways positively regulate the uptake process. Reverse transcriptase polymerase chain reaction (RT PCR) analysis had shown mRNA expression of folate receptor (FR)-α at 407 bp. Quantitative polymerase chain reaction analysis showed significantly higher FR-α mRNA levels in T47D cells compared to MCF-7 cells and Western blot analysis confirmed the FR-α protein expression at 37 kDa. Conclusions: This work demonstrated the functional characterization and molecular presence of FR-α in the T47D cell line. The high expression of FRs in T47D human breast carcinoma cells supports their validity as molecular therapeutic targets in BC.
  1,155 339 3
In vitro α-glucosidase and α-amylase inhibition by aqueous, hydroalcoholic, and alcoholic extract of Euphorbia hirta L.
Manjur Ali Sheliya, Rayhana Begum, Kolappa Krishna Pillai, Vidhu Aeri, Showkat Rasool Mir, Abuzer Ali, Manju Sharma
January-June 2016, 7(1):26-30
Background: Euphorbia hirta L. (Euphorbiaceae), commonly known as Dudhani, is distributed in the warm region of India and China. Traditionally, it is used in respiratory and gastrointestinal disorders. In addition, the antidiabetic property of the plant was also reported in the literature. This study was designed to evaluate the effect of aqueous, hydroalcoholic, and methanolic extracts (MEHs) of E. hirta on α-glucosidase and α-amylase in vitro. Materials and Methods: Aqueous, hydroalcoholic, and MEHs of E. hirta were prepared as per application program interface. In α-glucosidase activity, α-glucosidase (0.1 μ/mL) and substrate, 2.5 mM p-nitrophenyl-α-D-glucopyranoside was used; absorbance was recorded at 405 nm. In α-amylase activity, α-amylase solution (1.0 μ/mL) and substrate, 0.25% starch were used, and absorbance was measured at 540 nm. The IC50values were calculated by linear regression. Results: All the extracts showed α-glucosidase inhibitory activity comparable to acarbose with MEH having highest inhibitory activity among tested extracts. The observed IC50values were 213.63, 146.9, 78.88, and 8.07 μg/mL for aqueous, hydroalcoholic, MEH, and acarbose, respectively. All the extracts have shown mild α-amylase inhibitory activity compared to acarbose. Lineweaver–Burk plot has shown that the MEH is a mixed noncompetitive inhibitor for α-glucosidase enzyme. Conclusion: The results from this in vitro study clearly indicated that MEH of E. hirta had strong inhibitory activity against α-glucosidase and mild inhibitory activity against α-amylase. It can be used for management of postprandial hyperglycemia with lesser side effects, and provide a strong rationale for further animal and clinical studies.
  1,308 156 -
Formulation variable study and optimization of taste masked mouth dissolving tablets using design of experiment
Vijay Sharma, Lalit Singh
January-June 2015, 6(1):20-26
Background: Aim of present work is to prepare and optimized mouth dissolving tablets (MDTs) by using tasteless complex of levocetirizine. Materials and Methods: Formulation and optimization of tablets was done by using computer optimization technique. Formulated taste masked complex of drug was characterized by taste evaluation, percentage drug loading, thermal analysis and X-ray diffraction pattern. Optimization of MDTs was done by considering concentration of binder (polyvinylpyrrolidone [PVP] K30) and super-disintegrant (Kyron T-314) as independent variables whereas wetting time (WT), friability (Fr) and amount of drug release in 15 m (Q 15 ) as dependent variables. Response surface plots and contour plots were drawn, and optimum formulations were selected by feasibility and grid searches. Result and Discussion: By using 3 2 central composite design (CCD) optimized batch was obtained for which value of independent variable, PVP K30 (X1) and Kyron T-314 (X2) was 15 mg and 21 mg respectively and for dependent response, that is, Fr, WT and Q 15 to be 0.42%, 11.8 s. and 91.16% respectively. Validation of optimization study indicated very high degree of prognostic ability of response surface methodology (RSM). By analyzing the observed value to predicted value for Fr, WT and Q 15 the regression coefficient value was found to be 0.950, 0.961 and 0.957. Linearity of plot concluded that desired predicted response of all check-point batches were close to the predicted values and show the validity of data. Conclusion: Hence, optimized formulated batches were formulated by proper balancing of concentration of independent variables to attain desired dependent response using 3 2 CCD. Thus, 3 2 CCDs is an efficient tool in optimization experiments. High degree of outcome obtained using RSM concludes that 3 2 CCD is quite efficient in optimizing drug delivery systems that exhibit nonlinearity in response.
  1,287 167 -
Learning and memory enhancing activity of Ficus carica (Fig): An experimental study in rats
Meera Sumanth, K Mamatha
July-December 2014, 5(2):123-126
Objective: The study aimed to assess the learning and memory enhancing activity of the ethanolic fruit extract of Ficus carica in rats using elevated plus maze (EPM), Hebb-William maze (HWM) and Morris water maze (MWM). Materials and Methods: Wistar rats (100-150 g) of either sex, were divided into 5 groups (n = 6). Group I (control) animals received vehicle, Group II (scopolamine control) animals received scopolamine (0.4 mg/kg i.p), Groups III and IV animals received ethanolic fruit extract of F. carica (200 mg/kg and 400 mg/kg p.o) and Group V animals received piracetam (400 mg/kg i.p) for 27 days. The rats of Groups III-V were injected with a single dose of scopolamine (0.4 mg/kg i.p) on 19 th and 27 th day. Assessment of transfer latency (TL), time taken to reach reward chamber (TRC) and swim latency (SL) was done on 19 th and 27 th day using EPM, HWM and MWM, respectively. The data was analyzed by one-way Analysis of Variance followed by Dunnett's test. P ≤ 0.05 was considered to be significant. Results: Ethanolic fruit extract of F. carica decreased TL, TRC and SL in comparison to scopolamine treated rats. Conclusion: The fruit of F. carica enhanced learning and memory activity.
  1,254 197 -
Total protein in gingival crevicular fluid as indicators of periodontal disease activity: A clinico biochemical analysis
Arati C Koregol, Shobha P More, Savita C Koregol, Nagaraj Kalburgi
January-June 2015, 6(1):15-19
Background: Gingival crevicular fluid (GCF) is regarded as a promising medium for detection of markers of periodontal disease activity. Very few investigators have examined concentration of total protein in GCF, but most results are not in agreement to one another. Aim: This study was undertaken to quantitatively estimate total protein concentration of GCF in gingivitis and periodontitis and to find reliability of these as diagnostic markers of disease activity. This will indicate the stage of disease activity, help in early diagnosis, prevention and treatment of periodontal diseases. Materials and Methods: Study included patients between 18 and 55 years, divided into two groups: Gingivitis (Group-I) and periodontitis (Group-II). Using volumetric micro capillary pipette 1 μl GCF was collected for quantitative analysis of total protein using spectrophotometry. Results: The concentration of total protein in GCF and their significant correlation with gingival index, pocket depth measurements, reflects the clinical status of gingival and periodontal tissues. Conclusions: Estimation of proteins may be used as potential diagnostic markers of active disease status in periodontal tissues and to predict effective methods of prevention and treatment.
  1,236 212 -
In-vitro antimicrobial screening and molecular docking studies of synthesized 2-chloro-N-(4-phenylthiazol-2-yl)acetamide derivatives
Rahmat Ali, Suresh Kumar, Obaid Afzal, Sandhya Bawa
July-December 2015, 6(2):79-87
Introduction: Glucosamine-6-phosphate (GlcN6P) synthase biosynthetic pathway has been identified as potential targets for the development of new antimicrobial agents. Aim: A series of 2-chloro-N-(42-phenylthiazol-25-yl)acetamide derivatives (3a-r) was synthesized and evaluated their antimicrobial activity. Materials and Methods: The 2-chloro-N-(Para substituted phenylthiazol-25-yl) acetamide (2a-c) were synthesized by stirring intermediates (1a-c) with 2-chloroacetylchloride in dichloromethane in the presence of K2CO3. The intermediate (2a-c) were further reacted with different secondary amine such as pyrrolidine, N-methyl piperazine, N-ethyl piperazine, thiomorpholine, morpholine, piperidine etc in ethanol in presence of TEA Triethylamine (TEA) to get desired compounds (3a-r). Compounds were characterized by a spectroscopic technique such as Fourier transform infraredFTIR, 1 H-NMR, 13 C-NMR, and mass spectrometry. The synthesized thiazole derivatives (3a-r) were screened for anti-bacterial and anti-fungal activity against Escherichia coli, Staphylococcus aureus NCTC 6571, Pseudomonas aeruginosa NCTC 10662, CandidaC. albicans (MTCC-183), AspergillusA. niger (MTCC 281) NCTC 10418 and AspergillusA. flavus (MTCC 277). Result and Conclusion: The results of anti-bacterial screening revealed that among all the screened compounds, eight compounds viz. 3b, 3c, 3d, 3e, 3i, 3j, 3k, and 3p showed moderate to good anti-bacterial and antifungal activity having minimum inhibitory concentration (MIC) between 6.25- and 25 µg/ml. While compound 3d showed the most promising antibacterial activity against E. coli and S. aureus, while the compound 3j showed promising antifungal activity with MIC value 6.25 µg/ml against C. albicans, A. niger and A. flavus. In addition, all these eight potential molecules were also examined for possible binding on enzyme GlcN6Pglucosamine-6-phosphate synthase by molecular docking studies on (PDB ID 1JXA).
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Antibacterial potency of Ziziphus mauritiana (Fam-Rhamnaceae) roots
Sukirti Upadhyay, Ankita Mishra, Srishti Srivastava, Prashant Upadhyay, AK Ghosh, Vijender Singh
January-June 2015, 6(1):44-46
Background: Ziziphus mauritiana is a well known herb generally its fruit is used in stomach ailments or infections.The genus Ziziphus is known for its antimicrobial potency. Material and Methods: Here Z. mauritiana roots were taken for conducting experiments in various bacterial strains for evaluating its antibacterial potency by disc diffusion method. The minimum inhibitory concentration and zone of inhibition were also determined. The mode of action was determined by leakage of nucleic acid and its determination by UV spectrometry. Results: The root extract of Z.mauritiana posses excellent antibacterial activity against as the activity is well compared with standard drug ciprofloxacin. The mode of action of the extract was bactericidal. Conclusion: Effective and safe herbal antibiotic may be produced in the future by root extract of Z.mauritiana.
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Effect of aqueous and alcoholic extract of Sesbania sesban (Linn) Merr. root on glycemic control in streptozotocin-induced diabetic mice
Manjusha Choudhary, Neha Aggarwal, Nitesh Choudhary, Pankaj Gupta, Vikaas Budhwaar
July-December 2014, 5(2):115-122
Aim: The present study was carried out to investigate the hypoglycemic effects of the aqueous and ethanolic extracts of Sesbania sesban (SS) (Merr.) roots, which is widely used in inflammation, fever, ulcers, leucoderma and diabetes in various parts of India. Materials and Methods: SS extracts were administered orally at doses (500 and 1000 mg/kg) to normal and streptozotocin (STZ) induced Type-2 diabetic mice. The fasting blood glucose (FBG), biochemical parameters in serum viz., blood glucose, serum insulin, cholesterol, triglyceride (TG), high-density lipoprotein (HDL) cholesterol, urea, creatinine and total protein, change in body weight, internal organs weight, food intake, water intake and glycogen level in liver were performed for the evaluation of hypoglycemic effects. Results: Both doses of aqueous and ethanolic SS extracts caused a marked decrease of FBG in STZ induced Type-2 diabetic mice. Both extracts decreased the cholesterol, TG, urea, creatinine level and increased the insulin, HDL cholesterol and total protein level. Decrease in body weight and glycogen level induced by STZ was restored. Increase in water and food intake induced by STZ was decreased. Conclusions: The results suggest that aqueous and ethanolic extracts of SS may have hypoglycemic potential for the Type-2 diabetes and support the traditional use of the roots of plant as a hypoglycemic agent.
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A green analytical method for the simultaneous analysis of cefixime trihydrate and ambroxol HCl based on ultraviolet derivative spectroscopy
Ceema Mathew, Suman Naik Bhukya, Ajitha Makula, R Sathesh Babu Puvvadi
July-December 2015, 6(2):74-78
Context: Until date, there is no reported derivative spectrophotometric method for the combination of cefixime trihydrate (CEF) and ambroxol HCl (ABH). So an urgent need was felt to develop an ultraviolet (UV) derivative spectroscopic method, which reduces the cost of analysis on comparing with high-performance liquid chromatography or high-performance thin layer chromatography method. Aims: To develop and validate an economical and ecofriendly derivative spectroscopic method that avoids the use of organic solvents for simultaneous quantification of both the drugs. Materials and Methods: A simple method based on the derivative spectrophotometric method at zero crossing wavelengths has been developed for the simultaneous quantification of CEF and ABH. As the method depends on hydrotropic dissolution, 0.1N urea is used as the solvent, and it yields an economical and ecofriendly method. Two wavelengths 253 nm (zero crossing point (ZCP) for CEF) and 306 nm (ZCP for ABH) were selected for the quantification of ABH and CEF respectively. Results: The first derivative amplitude-concentration plots were linear over the range of 5-35 μg/ml and 3-10.5 μg/ml with detection limits of 0.187 and 0.0937 μg/ml and quantification limits of 0.625 and 0.312 μg/ml for CEF and ABH respectively. The percentage recovery was within the range between 99.05% and 102%. The % relative standard deviation for precision and accuracy of the method was found to be <2%. Conclusion: The proposed method was found to be simple, accurate and precise and can be successfully applied to the routine quality control analysis of studied drugs in their tablet formulations.
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Quality control analysis of Safoof-e-Pathar phori: Antiurolithiatic formulation
Wasim Ahmad, Washim Khan, Masood S Khan, Mohd Mujeeb , SM Arif Zaidi, Sayeed Ahmad
January-June 2016, 7(1):20-25
Aim: Safoof-e-Pathar phori (SPP), a Unani polyherbomineral formulation used for antilithiatic activity. The present study involves standardization of SPP to assess the quality. SPP were subjected to pharmacognostic studies, physiochemical properties, phytochemical analysis, high-performance thin layer chromatography (HPTLC), high-performance liquid chromatography (HPLC), and gas chromatography-mass spectrometry (GC-MS) fingerprint profile to set the standards, which can be used as reference of quality by herbal industries for its preparation and human use. Materials and Methods: The quality control of SPP has been carried out as per the AYUSH and WHO guidelines. The HPTLC fingerprinting has been done using chloroform: ethyl acetate (9:2, v/v) for petroleum ether extract, chloroform: toluene: ethyl acetate (7:2:4, v/v/v) for chloroform extract and for methanol extract petroleum ether: ethyl acetate (9:2, v/v) was used as mobile phase. HPLC was carried out using mobile phase consisted of acetonitrile and water in the ratio of 50:50 (v/v) for the methanolic extract. GC-MS fingerprinting profile has been carried out using hexane extract. Result: SPP was subjected to qualitative estimation of phytochemicals using standard methods, which revealed the presence of various bioactive components such as anthraquinone glycosides, carbohydrates, resins, proteins, flavonoids, phenolics, tannins, and terpenoids. The quantitative estimation of total phenolics and flavonoid content showed 0.44 mg/g and 1.02 mg/g, respectively. The HPTLC fingerprint showed presence of number of compounds for extracts at different Rfvalues. However, HPLC fingerprinting showed presence of 23 well-separated compounds and GC-MS showed presence of 22 compounds. Conclusion: The quality control parameters in present study reveal complete standardization profile of SPP for the 1st time, which would be of immense value in checking quality of developed formulation for human use.
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