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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.
  4,178 2,716 -
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.
  2,580 2,777 -
Is depression an independent risk factor for the onset of Type 2 diabetes mellitus?
Harish Singh Parihar, Harivansh Thakar, Hongjun Yin, Shari Allen
July-December 2016, 7(2):75-80
Depression is one of the most common mental illnesses characterized by loss of pleasure, whereas diabetes is a metabolic disorder which leads to high serum glucose levels. Current literature supports the development of depressive symptoms in patients with chronic illnesses including diabetes. However, depression as a potential risk factor for diabetes has attracted a lot of attention for clinicians and researchers. It has been hypothesized that both diabetes and depression may be bidirectional in nature, and each may exacerbate the symptoms or play an important role in the development of the other. The most common association between them is the diagnosis of depression in Type 1 or Type 2 diabetes. As the matter of fact, diabetes has been reported to double the risk of depression. In this review article, we have summarized various scientific studies to evaluate the potential of depression as a risk factor for diabetes. MEDLINE search identified various articles assessing this hypothesis. Our review of literature indicate some support for depression as a risk factor for Type 2 diabetes however more clinical studies need to be performed to clarify the contribution of depression as an independent risk factor for diabetes and to check the diabetes epidemic from escalating at a higher rate.
  2,863 2,173 -
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.
  4,218 653 4
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.
  4,158 412 -
A review on the status of quality control and standardization of herbal drugs in India
Anju Dhiman, Kavita Sharma, Asha Sharma, Pawan Sindhu
July-December 2016, 7(2):107-112
Background: Most of the herbal medicines in the world originate from the developing countries. There are ample opportunities for these countries to expand their global export. The world market for botanical medicines including drug products and raw materials has been estimated to have an annual growth rate between 5% and 15%. Total global botanical drug market is estimated at US$62 billion and is expected to grow to the tune of US$5 trillion by the year 2050. In the USA alone, the usage of botanicals has been increased by 380% between the years 1990 and 1997. Materials and Methods: Ayurveda, the Indian system of medicine, is one of the ancient, yet living traditions that face a typical Western bias. Widespread and growing use of botanicals has created public health challenges globally in terms of quality, safety, and efficacy. Results and Discussion: The development of parameters for standardization and quality control of botanicals is a challenging task. Various regulatory authorities, research organizations, and botanical drug manufacturers have contributed in developing guiding principles and addressing issues related to the quality, safety, and efficacy. Conclusions: The present review describes the regulatory aspects of herbal drugs in India and various other countries.
  3,902 422 -
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.
  3,180 496 -
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.
  2,842 643 1
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.
  3,050 348 -
An ayurvedic formulation Sankat Mochan: A potent anthelmintic medicine
Khomendra Kumar Sarwa, Prabhat Kumar Vishwakarma, Vijendra Kumar Suryawanshi, Tilotma Sahu, Lokesh Kumar, Jaya Shree
January-June 2017, 8(1):13-16
Aim and Object: Sankat Mochan is an ayurvedic formulation used in the urban and rural area of India. This polyherbal formulation is used for general stomach problems including abdominal cramping and diarrhea. The present investigation evaluated the anthelmintic activity of an aqueous solution of an ayurvedic medicine Sankat Mochan. Materials and Method: Various concentrations (1%, 5%, and 10%) of medicine were used for anthelmintic activity on Pheretima posthuma. Piperazine citrate (10 mg/ml) was used as a reference standard and distilled water as a control. Result and Conclusion: The result showed that the Sankat Mochan possess anthelmintic activity more potent than that of piperazine citrate. Thus, Sankat Mochan may be used as a potent anthelmintic agent against helminthiasis.
  3,121 276 -
Strain improvement of Phaffia rhodozyma for astaxanthin production
Hina Nangia, Mojeer Hasan, Mohd. Azhar , Prakash Chandra Bhatt, Bibhu Prasad Panda
January-June 2016, 7(1):63-68
Objective: The aim of the present study is to evaluate and optimize different carbon sources at different temperatures in shake flask for cell growth and astaxanthin accumulation in ultraviolet (UV) mutant Phaffia rhodozyma. The focus is to make the process cost-effective and fruitful with higher productivity. Materials and Methods: Adaptive strain development was carried out so that the P. rhodozyma can give the best astaxanthin at a higher temperature (35°C), increasing the process economy. P. rhodozyma was cultivated with three broad spectrum antibacterial drugs - streptomycin, gentamycin, and ampicillin (200 μL) and with antifungal drug - fluconazole (200 μL) to determine the effect on yeast growth and astaxanthin production. Rice, cane juice, and sucrose were selected as carbon source and compared with dextrose at different fermentation temperatures - 22°C, 30°C, 33°C, and 35°C for astaxanthin production. Results: P. rhodozyma was resistant to antibiotic drugs inhibiting bacterial and fungal contaminants. Rice being more economical was selected as carbon source, but the strain was not able to utilize starch-rich substrate leading to its rejection. When P. rhodozyma was grown in cane juice, biomass is highest (OD 2.77) at 30°C and 610 nm wavelength, whereas astaxanthin productivity is highest (OD 2.64) in dextrose media at 30°C and 450 nm. Comparative metabolic and growth results for UV mutants showed significantly higher biomass and astaxanthin productivity in comparison to wild strain. Conclusion: The most efficient carbon source in terms of penny-pinching and astaxanthin productivity was found to be dextrose containing media at 30°C.
  2,953 417 1
Comparative gas chromatography-mass spectroscopy, Fourier transform infrared spectroscopy, and high-performance liquid chromatography analysis of essential oils extracted using 4 methods from the leaves of Eucalyptus globulus L.
Yasmeen Khan, Hafizur R Ansari, Rinki , Rishika Chauhan, Ennus T Tamboli, Sayeed Ahmad
July-December 2016, 7(2):81-86
Background: Eucalyptus globulus L. (family, Myrtaceae) is one of the world's most widely planted genera. E. globulus L., commonly referred to as Tasmanian blue gum, is a fast growing, evergreen tree, native to Tasmania and South-East Australia. Apart from its extensive use in pulp industry, it is also produces Oleum Eucalypti (eucalyptus oil) that is extracted on commercial scale in many countries such as China, India, South Africa, Portugal, Brazil, and Tasmania, as a raw material in perfumery, cosmetics, food beverage, aromatherapy, and phytotherapy. Materials and Methods: Traditional hydrodistillation (HD), solvent extraction (SE), ultrasonication (US), and supercritical fluid extraction (SFE) were conducted for the extraction of essential oil from the leaves of E. globulus. Each oil was evaluated in terms of high-performance liquid chromatography (HPTLC) and Fourier transform infrared spectroscopy (FTIR) fingerprinting with qualitative and semi-quantitative composition of the isolated essential oil by gas chromatography-mass spectroscopy (GCMS), the extract yield of essential oil was 2.60%, 2.2%, 2.0%, and 3.6% v/w, respectively, for HD, SE, US, and SFE. Results: A total of 53 compounds were identified by GCMS. Comparative analysis indicated that SFE was favorable for extraction of monoterpene hydrocarbon, sesquiterpene hydrocarbon, and oxygenated sesquiterpene hydrocarbon. HD, SE, and US had certain advantages in the extraction of aliphatic saturated hydrocarbons organic acid and esters. Overlay, FTIR spectra of oil samples obtained by four extraction methods were superimposed with each other showing similar components. The maximum separation of compound seen at 254 nm and lesser at 366 nm by HPTLC fingerprinting which again showed superimposed chromatograms. Conclusion: It is concluded that different extraction method may lead to different yields of essential oils where the choice of appropriate method is very important to obtained more desired component with higher physiological activities.
  2,689 620 -
Solubility and stability enhancement of curcumin: Improving drug properties of natural pigment
MJ Ansari, Rabea Parveen
July-December 2016, 7(2):113-116
Aim: Water insolubility, low potency, and instability are inherent problems of several herbal medicines. Identity, strength, quality, and purity of herbal products are further compromised during manufacturing and storage. The aim of present work was to evaluate solubility and stability of curcumin, a pigment obtained from dried rhizomes of plant Cucrcuma longa. Materials and Methods: The stoichiometric ratios for inclusion complexation of curcumin with various cyclodextrins (CDs) were determined by phase solubility analysis. Grinding, kneading, and freeze-drying were employed to determine optimum complexation. Complexes were evaluated for drug inclusion, solubility, and stability. Results: Stability constants were 11200 M−1 , 1557 M−1 , 2858 M−1 , and 2206 M−1 for α-, β-, γ-CD, and dimethyl β-CD (DIMEB), respectively, thus indicating good complex formation. Theoretical amounts of curcumin in binary products were between 80% and 97% with a maximum of 96.8% in curcumin-β-CD freeze-dried product. The complexation resulted in a marked improvement in the solubility of curcumin up to 60, 55, 56, and 1500 folds by α-, β-, γ-CD, and DIMEB, respectively. Inclusion complexation protected the drug from hydrolytic degradations as only 20-40% degradation was observed at the end of 8 h as opposed to >70% for pure curcumin. Conclusion: A significant improvement in the solubility and stability was observed with curcumin-CD complex as compared to pure curcumin.
  2,949 296 -
Significance of molecular markers in pharmacognosy: A modern tool for authentication of herbal drugs
Karishma Chester, Ennus T Tamboli, Sarvesh K Paliwal, Sayeed Ahmad
July-December 2016, 7(2):96-106
Quality evaluation of herbal preparation is an elementary requirement of industry and other association dealing with Ayurvedic and herbal products. The growing use of botanical products now a days is forcing to assess these agents and to develop standards of quality and produce. An attempt has been made through this article to highlight the use of molecular markers for botanicals with special reference to Indian herbal medicine. As the desire for herbal-based products becomes ingrained in our society but standardization of botanicals offers many obstacles like the controversial identity of various plants, deliberated adulteration of plant material, ensuring quality is much more than discovery, specification, and process control. It also includes awareness of every aspect of a manufacturing process from research to shipping. Extensive research on DNA-based molecular markers is in progress for its great utility in the herbal drug analysis and widely used for the authentification of plant species of medicinal importance. DNA markers are reliable for information as the genetic composition is unique for each species and is not affected by age, physiological conditions, as well as environmental factors. DNA markers offer several advantages over conventional phenotypic markers, as they provide data that can be analyzed objectively.
  2,862 275 -
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.
  2,720 397 1
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.
  2,260 841 7
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.
  2,657 349 -
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.
  2,627 372 2
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.
  2,244 709 -
Characterization of Arachis hypogaea L. oil obtained from different extraction techniques and in vitro antioxidant potential of supercritical fluid extraction extract
Rishika Chauhan, Iftekhar Ahmad, Yasmeen Khan, Ennus Tajuddin Tamboli, Sayeed Ahmad
July-December 2016, 7(2):87-91
Aim: The present investigation was aimed to characterize the fixed oil of Arachis hypogaea L. using five different extraction methods: Supercritical fluid extraction (SFE), ultrasound assistance extraction, soxhlet extraction, solvent extraction, and three phase partitioning method. Materials and Methods: The SFE conditions (temperature, pressure, and volume of CO 2) were optimized prior for better yield. The extracted oils were analyzed and compared for their physiochemical parameters, high-performance thin layer chromatography (HPTLC), gas chromatography-mass spectrometry (GC-MS), and Fourier transform infrared spectrometry (FT-IR) fingerprinting. Anti-oxidant activity was also determined using DPPH and superoxide scavenging method. Results: The main fatty acids were oleic, linoleic, palmitic, and stearic acids as obtained by GC-MS. HPTLC analysis revealed the presence of similar major components in chromatograms. Similarly, the pattern of peaks as obtained in FT-IR and GC-MS spectra of same oils by different extraction methods was superimposable. Conclusion: Analysis reported that the fixed oil of A. hypogaea L. is a good source of unsaturated fatty acid, mainly n-6 and n-9 fatty acid with a significant antioxidant activity of oil obtained from SFE extraction method.
  2,648 252 -
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.
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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.
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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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Antibiotic susceptibility pattern of Salmonella enterica serovar typhi and Salmonella enterica serovar paratyphi A with special reference to quinolone resistance
Shoorashetty Manohar Rudresh, T Nagarathnamma
July-December 2015, 6(2):70-73
Background and Objectives: Typhoid fever is endemic in India. Extensive use of first-line antibiotics has led to the emergence of multi-drug resistant (MDR) Salmonella typhi. Ciprofloxacin has become empirical therapy of choice against MDR salmonellae. Recent year's emergence of low-level ciprofloxacin resistance in salmonellae resulted in delayed response and serious complications. Nalidixic acid (NA) screen test is used as surrogate marker for detection low-level ciprofloxacin resistance. In this study, we evaluated prevalence of MDR and low-level ciprofloxacin resistant S. typhi and Salmonella paratyphi A. Materials and Methods: A total of 50 blood culture isolates of S. typhi and S. paratyphi A were tested for antibiotic susceptibility according to Clinical Laboratory Standards Institute (CLSI) method. Minimal inhibitory concentration (MIC) to ciprofloxacin was carried out by E-test and agar dilution method. Results: Among the 50 salmonella isolates, 80% were S. typhi and 20% were S. paratyphi A. MDR was found in 2% S. typhi. NA resistant salmonellae showed ciprofloxacin MIC ranging from 0.25 to 0.75 μg/ml. One isolate of S. typhi showed ciprofloxacin MIC of 32 μg/ml and was also resistant to ceftriaxone. NA screen test for low-level ciprofloxacin resistance was 100% sensitive and 97.9% specific. Interpretation and Conclusion: NA resistant isolates should be tested for ciprofloxacin MIC to decide therapeutic options. The current CLSI breakpoints may have to be re-evaluated for salmonellae.
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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.
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