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Showing posts from February, 2018

Method develpopment and validation of Itopride Hydrochloride and Rabeprazple Sodium in pharmaceutical dosage form by Reversed Phase High Performance Liquid Chromatography

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ABSTRACT: Itopride hydrochloride is a benzamide derivative in the class of prokinetic drugs . it has been approved for the symptomatic treatment of disorders like non-ulcer dyspepsia. chronic gastritis , diadetic gastro paresis or functional dyspepsia. the present study was designed to study the method of development in pharmaceutical dosage forms by reversed hplc . through developed validation method we can analyse the drug in reversed phase pharmaceutical dosage form by hplc. validation is a constant evolving process that starts before an instrument is placed on line and continuous long after method development and transferred. here a new hplc method for itopride hydrochloride and rabeprazole sodium was developed and validated the same. the best chromatographic seperation was performed on phenomenex c18 column and the uv detection wave length was set at 268nm . the mobile phase used was methanol : water : acetonitrile (50:40:10) . the retention time of itopride hydrochloride and r...

Design, development and characterization of orally disintegrating tablet of prochlorperazine maleate

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ABSTRACT: In Present work, orally disintegrating tablets of Prochlorperazine maleate were design with a view to enhance Patient compliance by direct compression method. In this method sodium starch glycolate, crospovidone and croscarmellose sodium use as superdisintegrant (2-8% w/w) along with microcrystalline cellulose (pH 102), directly compressible lactose (DCL-11) and sodium Saccharin to enhance mouth feel. The prepared batches of tablet were evaluated for hardness, friability, content uniformity, wetting time, water absorption ratio and in vitro dispersion time. Based on in vitro dispersion time (Approximately 21 to 30 s), two promising formulation were tested for in vitro drug release pattern in pH 6.8 phosphate buffer. Among the two promising formulation, the formulation containing 8% sodium starch glycolate and 8% crospovidone emerged as the overall best formulation (t50% 8-10 min) based on drug release characteristic in pH 6.8 phosphate buffer compared to commercial conven...

Synthesis of schiff base zinc metal complex (MAPIMP)2Zn and development of HPLC chromatographic method for its analysis

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ABSTRACT: A simple, fast and accurate method has been developed for the determination of (MAPIMP)2Zn by High Pressure Liquid Chromatography. The analysis was carried out on Waters 2695 separation module HPLC system with Waters 2487 Dual wavelength Absorbance detector. The column used was a stainless steel column of dimension 15 cm x 4.6 mm, packed with octadecylsilane bonded to porous silica ( Make : Neosphere 120-5-C18 Altima column is suitable ).The detector used was Ultraviolet ( UV ) detector. The validation of proposed method was also carried out. For more details PDF Link:   http://www.jocpr.com/articles/synthesis-of-schiff-base-zinc-metal-complex-mapimp2zn-and-development-of-hplc-chromatographic-method-for-its-analysis.pdf

Synthesis, molecular docking and ADME prediction of some pyridine and pyrimidine derivatives as anti-colorectal cancer drugs

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ABSTRACT: Thymidylate synthase is the important enzyme used to generate thymidine monophosphate (dTMP), which is subsequently phosphorylated to thymidine triphosphate for use in DNA synthesis and repair.. Thymidylate synthase inhibitors are chemical agents which inhibit the enzyme Thymidylate synthase and have potential as an anti-colorectal cancer chemotherapy. Pyridine and Pyrimidine derivatives are found to be the potent inhibitors of Thymidylate synthase enzyme were rapidly identified. The molecular modeling aspects of the pyridine and pyrimidine derivatives are also presented.  For more details PDF Link:  http://www.jocpr.com/articles/synthesis-molecular-docking-and-adme-prediction-of-some-pyridine-and-pyrimidine-derivatives-as-anticolorectal-cancer-dru.pdf

Simultaneous U.V. Spectrophotometric estimation of Lamivudine and Abacavir Sulphate in bulk and in tablet dosage form

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ABSTRACT: A Simultaneous ultraviolet spectrophotometric method has been developed for the analysis of LAM and ABA in the combined dosage form (Abamune-L). The method depends on the application of simultaneous equation to resolve the interference due to spectral overlapping. The analytical signals were measured at 270 and 289 nm using 0.1 N HCl as a solvent. Regression analysis of Beer's plot showed good correlation in a general concentration range of 5 to 30 µgml-1 with correlation coefficient (r= 0.9995; CV < 0.7022) for lamivudine, whereas abacavir concentration range 5 to 30µg/ml with correlation coefficient (r= 0.9992; CV <0.5151). These methods were validated with respect to accuracy, precision, linearity, limit of detection and quantification. The suggested procedures were successfully applied to the determination of these compounds in pharmaceutical preparations, with high percentage of recovery, good accuracy and precision.The results of analysis have been validate...

Design and in vitro evaluation of drug release and bioadhesive properties from bucoadhesive tablets of Glibenclamide for systemic delivery

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ABSTRACT: The buccal route has been used for many years to delivery drug which undergoes first pass metabolism within the oral mucosal cavity, the buccal region often attractive route of administration for local or systemic drug delivery. Due to its high potential a bioadhesive system place a major role in controlling drug release. Recent interest has been expressed in the delivery of drug via mucus membrane by the use of adhesive materials on which studies are been intensively undertaken. The objective of this work was to design a mucoadhesive tablet with a potential use in the treatment of Diabetes mellitus. A Bi-layered tablet (Core layered + Backing layered) containing Glibenclamide has been formulated. Carbopol-940, Polyvinylpyrrolidone (PVP), and Sodium corboxymethyl cellulose were used as polymer. Tablets were obtained through direct compression. Properties such as in vitro mucoadhesion, water uptake, surface pH, and drug release were evaluated. The core layer constituents we...

Conductance and ion association studies of unsymmetrical electrolytes of complexes bromopentammine cobalt (III) halides and perchlorate in water at different temperatures

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ABSTRACT: Conductance of complexes bromopentammine cobalt (III) halides and perchlorate has been measured in water at different temperatures ( 25 c 35 c 0 → 0 ). The limiting equivalent conductance (Λ0 ) and ion association constant (KA) for complexes in water have been evaluated using Fuoss-Edelson equation. The influence of solvent on the solvation of ions has been discussed. Temperature variation of the association constant has been studied to evaluate the thermodynamic parameters.  For more details PDF Link:  http://www.jocpr.com/articles/conductance-and-ion-association-studies-of-unsymmetrical-electrolytes-of-complexes-bromopentammine-cobalt-iii-halides-an.pdf

Formulation and evaluation of Prednisolone tablet for colon targeted drug delivery system

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ABSTRACT The purpose of this study was to prepare prednisolone pH-dependent release tablets and evaluate their advantages as a colon targeted drug delivery system. prednisolone insoluble in water and unstable in gastric environment was formulated into pH-dependent tablets coated with combinations of two methacrylic acid copolymers Eudragit L100 and Eudragit S100. The influence of core tablet compositions, polymer combination ratios and coating levels on the in vitro release rate of prednisolone from coated tablets was investigated. The results showed that less than 10% drug was released in 0.1 N HCl within 2 hr, and about 90% of the drug was released in the pH 7.2 phosphate buffer within 6 hr. Colon drug delivery is advantageous in the treatment of colonic disease and oral delivery of drugs unstable or susceptible to enzymatic degradation in upper GI tract. In this study coated tablets that is resistant to gastric and small intestinal pH conditions but can be easily dissolved in co...

Enantiomeric separation in pharmaceutical analysis: A chromatographic approach

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ABSTRACT: Chirality plays a major role in biological processes, and the enantiomers of a bioactive molecule often possess different biological effects. For example, all pharmacological activity may reside in one enantiomer of a molecule, or enantiomers may have identical qualitative and quantitative pharmacological activity. In some cases, enantiomers may have qualitatively similar pharmacological activity, but different quantitative potencies. Since drugs that are produced by chemical synthesis are usually a mixture of enantiomers, there is a need to quantify the level of the isomeric impurity in the active pharmaceutical ingredient. Accurate assessment of the enantiomeric purity of substances is critical because isomeric impurities may have unwanted toxicological, pharmacological, or other effects. Such impurities may be carried through a synthesis and preferentially react at one or more steps and yield an undesirable level of another impurity. The determination of a trace enantio...

Comparative phytochemical and Isoperoxidase Studies on leaf and Leaves derived callus of Solanum anguivi Lam

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ABSTRACT: The present study was intended to produce a protocol for large scale production of callus and compare the phytochemical constituents and isoperoxidase profile of leaves and calli of Solanum anguivi Lam. Maximum percentage of friable callus (86.3 ± 0.94) proliferation was obtained on MS medium supplemented with 1.0 mg/l of 2, 4-D. The phytochemical study revealed that the high degree of steroids, alkaloids, phenolic compounds, flavanoids, tannins present in leaves derived calli and calli induced secondary calli. A total of 23 bands in seventeen different positions with seven activity regions (PRX1-7) were observed in the isoperoxidase enzyme system of Solanum anguivi. The leaves showed their uniqueness by the presence of following bands MW-Rf – 0.1250, 0.2125, 0.3250, 0.5000, 0.5750 and 0.6500. The primary calli expressed their individuality by the occurrence of MW-Rf 0.0875, 0.2875, 0.3625 and 0.5250. The MW-Rf 0.0750, 0.4500, 0.4875 and 0.5875 are present only in seconda...

Ultrasonic study of molecular interactions in some bio-liquids

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ABSTRACT: The velocity of ultrasonic wave of frequency 10 MHz has been measured by the ultrasonic Time Intervalometer using pulse echo overlap method, in the temperature range 100 to 550C, for the bio-liquids. Cinnamaldehyde, acrolein, acrylonitrile, methylmethacrylate, methanol, p-dioxane and cyclohexane. The relative strength of intermolecular interaction has been found to depend upon the presence of electron-donar and electron-accepter group. The ultrasonic parameters found useful in determining the relative strength of homo-molecular interaction in pure liquids. For more details PDF Link:  http://www.jocpr.com/articles/ultrasonic-study-of-molecular-interactions-in-some-bioliquids.pdf

In vitro cytotoxicity of Calotropis procera and Trigonella foenum graecum against human cancer cell lines

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ABSTRACT: Alcoholic whole plant extracts of Calotropis procera and Trigonella foenum graecum L. showed in vitro cytotoxicity against different human cancer cell lines such as lung, neuroblastima, liver and colon. Sulforhodamine B dye (SRB) assay was done for in vitro cytotoxicity test assay against five human cancer cell lines namely of lung (A-549), liver (Hep-2) colon (502713, HT29) and neuroblastima (IMR-32). Cannabis sativa and Trigonella foenum graecum L. showed more than 70% growth of in some cell lines 79% and 83% in Cannabis sativa and Trigonella foenum graecum L. respectively, against lung (A-549) cell line. In case of liver (Hep-2) cell lines, Cannabis sativa showed cytotoxic activity but Trigonella foenum graecum L extracts showed no activity. Colon 502713 cell lines were inhibited by the extracts of Trigonella foenum graecum L only. HT-29 liver human cancer line and IMR-32 neuroblastima cell lines showed cytotoxic inhibition by both plant extracts.  For more d...

Comparative conformational, structural and vibrational study on the molecular structure of tyrosine and L-DOPA using density functional theory

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ABSTRACT: A brief conformational, structural and vibrational study has been performed on the molecular structure of two well known amino acids tyrosine and L-DOPA. The equilibrium geometry, harmonic vibrational frequencies, infrared intensities and Raman scattering activities were calculated by the Density Functional B3LYP method employing 6-311G(d,p) as the basis set and the vibrational studies were interpreted in terms of potential energy distribution (P.E.D.). The internal coordinates were optimized repeatedly to maximize the P.E.D. contributions. A detailed interpretation of the infrared and Raman spectra of tyrosine and L-DOPA is reported in the present work. The similarities and differences between the vibrational spectra of the two molecules studied have been highlighted. The calculations are in agreement with experiment. The thermodynamic calculations related to the title compounds were also performed at B3LYP/6-311G(d,p) level of theory. The FT-Raman and FT-IR spectra of ty...

Inhibition effect of methanolic extract of Atractylis serratuloides on the corrosion of mild steel in H2SO4 medium

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ABSTRACT:  The inhibitive properties of the methanolic extracts of three parts of Atractylis serratuloides towards the corrosion of type API 5L X52 steel in 15% H2SO4 was evaluated by weight loss method and polarization technique. The results showed that extracts are a good inhibitor for the steel in this medium. The corrosion inhibition efficiency increases with increasing extracts concentration. Potentiodynamic polarization results revealed that the studied inhibitors behave as mixed type. For more details PDF Link:   http://www.jocpr.com/articles/inhibition-effect-of-methanolic-extract-of-atractylis-serratuloides-on-the-corrosion-of-mild-steel-in-h2so4-medium.pdf

Synthesis and characterization of some divalent transition metal complexes with tellurium containing 10-membered tetraazamacrocyclic ligands

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ABSTRACT  : A new series of 10-membered tellurium containing tetraazamacrocyclic complexes, [ML1Cl2], [ML2Cl2] and [ML3Cl2], where [M = Mn(II), Co(II), Cu(II); L1 , L2 and L3 = 10-membered tellurium containing tetraazamacrocyclic ligands] have been prepared via the template condensation of 1,2-diaminoethane and diaryltellurium dichlorides, R2TeCl2, (R = phydroxyphenyl, 3-methyl-4-hydroxyphenyl, p-methoxyphenyl) in the presence of metal chlorides. These complexes have been characterized by elemental analyses, conductivity, magnetic susceptibility measurements, infrared, electronic absorption and proton magnetic resonance spectra. An octahedral geometry has been assigned to all the metal complexes. Keywords: tellurium containing, tetraazamacrocycles, diaryltellurium dichlorides, 1,2- diaminoethane, template condensation, metal complexes. For more details PDF Link :  http://www.jocpr.com/articles/synthesis-and-characterization-of-some-divalent-transition-metal-complexe...

Study of Degrading Some Petroleum Cuts by Bacteria

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ABSTRACT:  Degradation of polycyclic aromatic hydrocarbon were studied by using the bacteria pseudomonas sp. isolated from soil contaminate with oil. The yield of microbial cells reaches a maximum at pH value of 7 for five different phenanetherene concentration media (5-25) mg/ml. At temperature of 32oC, the growth was activated established metabolism within five days. Higher biomass concentration obtained with time of 22.5 min for initial substrate concentrations of 25 mg / ml. The change of cell growth and substrate concentration with time is directly proportional to time while substrate concentration decreases exponentially with time. These results analytically confirmed that the bacteria undergoes Monod's Kinetics. The order of degrading phenanthrene is obvious when a limiting substrate ( 5 or 10 mg/ml ) is been used , the degradation processes are rather sluggish than those observed in ( 20 or 25 mg/ml ). First order curve fitting was determined that the statistical software...

Method development and validation of Irbesartan using LCMS/MS: Application to pharmacokinetic studies

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ABSTRACT A simple, accurate liquid chromatography with tandem mass spectrometry (LC/MS-MS) method has been developed and validated in human plasma. The method employed liquid-liquid extraction. Samples containing Irbesartan were chromatographed on a Hypersil gold column (C18, 5µm, 100 x 4.6 mm) at a temperature of 40°C. The isocratic mobile phase composition was a mixture of 2 mM ammonium formate (pH 4.0) / methanol (20:80 v/v), which was pumped at a flow rate of 0.5 mL / min with split ratio of 20:80.The retention time under these chromatographic conditions was found to be 2.20 minutes with run time 2.82 minute. Ethyl acetate & n-Hexane (80:20, v/v) was found to be good extracting and produced a satisfactory chromatogram. The developed LC/MS-MS method was found to be selective, simple, sensitive, accurate and linear for the analysis of Irbesartan in human plasma. The retention time and inturn run time was very short, hence required less mobile phase for the method, making it mor...

Cancer pathogenesis caused by xenoestrogens of environment and food contaminants: A Review

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ABSTRACT:   The environmental and food contaminants, including therapeutic agents (e.g, antibiotics, antihypertensive drugs, etc.) and oestrogenic endocrine disruptors (xenoestrogens or xenobiotic chemicals), which mediate the oestrogens may lead to the development of cancer. Oestrogens and their metabolites are involved in the cancer pathogenesis of breast, uterus, ovary, pituitary gland, testicle, liver, kidney and bone marrow. Xenoestrogens that can cause cancer include polychlorinated biphenyl congeners, pesticides, food-related mycotoxin zearalenone and its derivatives, ultraviolet screen, some metals, fungicides, algicides, oestrogens, retinoids, pyrethroid insecticides, pentachlorophenol, β-hexachlorocyclohexane, etc. Diet has influence on cancer development, and several compounds, either present as dietary components or contaminants or formed during food processing, may play a role in cancer risk. All these can adversely interfere with the physiological functions of oestr...

Photocatalytic Degradation of diazinic ring- containing azo dye (Direct Yellow 12) by Photo-Fenton Reagent

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ABSTRACT: Photocatalytic decolourization of dyes using AOP is a new concern among researchers since it offers an attractive method for decolorization of dyes and breaks them into simple mineral form. The oxidation using Fenton Reagent has been found to be a promising treatment method for the effective decolorization and degradation of dyes. A detailed investigation of photodegradation of Direct Yellow-12 (DY12) using H2O2/Fe+2 has been carried out. Results indicate that dye degradation is dependent on concentration of Dye (DY12), photocatalyst (Fenton reagent), H2O2 and pH of the experimental solutions. The optimum conditions for the photobleaching of dye had been established. The kinetics of degradation of the dye in the dilute aqueous solutions follows first order kinetics. The results indicated that the treatment of the dye by Photo-Fenton reagent was efficient at optimum conditions. For more details PDF Link:   http://www.jocpr.com/articles/photocatalytic-degradation-of...

Synthesis and antimicrobial screening of some new N3-substituted derivatives of quinazolin-4(3H)one

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ABSTRACT: Quinazolin-4-one-3-yl-propan-2-one (2) was prepared by N-alkylation of Quinazolin-4(3H)one 1. The treatment of compound 2 with hydrazine hydrate yielded hydrazine derivative (3), which on condensation with variously substituted aryl aldehydes gave the corresponding hydrazones (4). Compound 3 on reaction with phenyl isocyanate and phenyl isothiocyanate transformed into the corresponding carbamates and thiocarbamates (5) respectively. Compound 3 also gave a tricyclic compound (6) when refluxed in presence of ammonium acetate and acetic acid, while hydrazone derivative (7) when treated with dehydroacetic acid. Keywords: Quinazoline, chloroacetone, hydrazones. For more details PDF Link :  http://www.jocpr.com/articles/synthesis-and-antimicrobial-screening-of-some-new-n3substituted-derivatives-of-quinazolin43hone.pdf

Noble metal catalysts for monolithic converters

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ABSTRACT Catalytic combustion of pollutants released from the vehicular exhaust is one of the best methods to decrease their concentration before their release to the atmosphere. The catalyst help to bring about the reduction of these pollutants at a much lower temperature as compared to homogenous combustion reactions. In this paper a review about the noble metal catalysts used for gasoline vehicles is carried out. These noble metal catalysts although expensive and limited in supply are the best option for reduction of the pollutants hydrocarbons, carbon monoxide and oxides of nitrogen released from the vehicular exhaust. For more details PDF Link:  http://www.jocpr.com/articles/noble-metal-catalysts-for-monolithic-converters.pdf

Synthesis and antibacterial evaluation of some hydrazones of flavanoid derivative

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ABSTRACT :  In an effort to synthesize potent anti-bacterial agents, few hydrazones of Flavanol derivatives have been synthesized and screened for in vitro anti-bacterial activity against 25 strains of Gram –ve and Gram +ve pathogenic bacteria. The chemical structures of compounds were established by IR, NMR spectra and elemental analysis. The synthesized compounds have shown inhibitory effect (MIC< 392 µg/ml) against few pathogenic bacterial strains and also posses activity against Methicillin-resistant Staphylococcus aureus strain because of presence of carbonyl region and hydroxyl group. For more details PDF Link :  http://www.jocpr.com/articles/synthesis-and-antibacterial-evaluation-of-some-hydrazones-of-flavanoid-derivatives.pdf

Development and validation of a UV spectrophotometric method for the estimation of torsemide in bulk and in tablet dosage form

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ABSTRACT: A simple and cost effective spectrophotometric method described is based on use of 0.1N sodium hydroxide solution in which the drug is completely soluble, is used as a solvent. The drug has an absorption maximum at 290 nm and obeys Beer’s Lambert law in the concentration range 1– 25µg ml-1. The absorbance was found to increase linearly with increasing concentration of torsemide, which is corroborated by the calculated correlation coefficient value of 0.9999(n=6). The apparent molar absorptivity is1.896x103 L mol-1 cm -1. The slope and intercept of the equation of the regression line are 3.4 ×10-2 and 11.2x10-2 respectively. The optimum experimental parameters for the reaction have been studied. The validity of the described procedure was assessed. Statistical analysis of the results has been carried out revealing high accuracy and good precision. The proposed method was successfully applied to the determination of torsemide in pharmaceutical formulations. For more...

Efficient production of Alpha – amylase from agro residues using Bacillus subtilis

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ABSTRACT: Two different agro residues were screened for alpha- amylase production using the Gram positive rod, Bacillus subtilis. Supplementation with different nitrogen and carbon source favoured the increased enzyme yield by submerged fermentation. Maximum enzyme yield titre was expressed as units as per micro mole of glucose yields. The objective of this study is to select a suitable strain for the production of amylase, screening of different agricultural by products as substrates for maximum enzyme production, application of different combinations of these substrates for enzyme production and optimization of cultural conditions for the production of amylase. Enzyme yield of Wheat bran and Rice bran were 51.04 ± 0.54 IU/g and 12.42 ± 0.15 IU/g respectively at the time of 40hr incubation at 37˚C of which the wheat bran (WB) was proved as the best substrate source.  For more details PDf Link:  http://www.jocpr.com/articles/efficient-production-of-alpha--amylase-from...

Conductivity of Poly (Vinylmercaptobenzothiazole) Iodine Complex

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ABSTRACT: A non-conjugated polymer poly (vinylmercaptobenzothiazole) (PVMBT) shows semi conducting properties in presence of electron acceptor-iodine. The enhancement of conductivity is presumably due to the formation of charge transfer (CT) complexes between iodine and the lone pair of the nitrogen atom of the polymer. This CT complex is characterized through FTIR, UV, ESR, electrical conductivity measurement and dependence of conductivity on temperature. The thermal properties of PVMBT have also been studied with the help of DSC and TGA. For more details PDF Link:   http://www.jocpr.com/articles/conductivity-of-poly-vinylmercaptobenzothiazole-iodine-complex.pdf

Antimicrobial Activity of Earthworm Extracts

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ABSTRACT:  Earthworm plays a major role in the proper functioning of the soil ecosystem. It acts as scavenger and helps in recycling of dead and decayed plant material by feeding on them. Earthworm increases the soil fertility and is often referred to as a farmer’s friend. Earthworms have been used in medicine for various remedies. In the present investigation, various solvent extracts of an earthworm, Eudrilus eugeniae were prepared and antimicrobial activity of these extracts were determined by well diffusion method. It was found that 95% ethanol extract of earthworm was potent antibacterial agent against Streptococcus pyogens and antifungal agent against Candida albicans. Petroleum ether extract showed maximum potency against Staphylococcus aureus in comparison to Streptococcus pyogens. Petroleum ether extract was found to possess maximum antifungal activity against Aspergillus niger in comparison to Candida albicans. Against E. coli, ethanol and petroleum ether extract posse...

Pressure dependence of Gruneisen parameter of some transition metals

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ABSTRACT: Comparison of seismic velocities in mantle metals under mantle conditions with seismic data is the first step towards constraining mantle chemistry. The calculation, however, is uncertain due to lack of data on certain physical properties. The Grüneisen parameter ( γ ) is of much importance regarding to the physical properties of mantle metals, because it sets limitations on the thermo elastic properties of the lower mantle and core at different compression ratio.The Grüneisen parameter of ten transition metals; Mo, Cd, Co, Zn, La, Cu, Ag, Au, Fe and Hf have been calculated using three equation of states viz; Brennan Stacey EOS, Shanker EOS and Vinet EOS, taking isothermal bulk modulus and its first pressure derivative into the consideration. On the basis of calculations it is concluded that, except for Hf, the Shanker EOS is the best for calculating Gruneisen parameter at both high and low compression ranges for transition metals, where as Vinet EOS is applicable at high ...

Pharmacological Profile of Benzoxazines: A Short Review

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ABSTRACT Benzoxazine and its derivatives are used in organic synthesis for building natural and designed synthetic compounds and they have been frequently utilized as suitable skeletons for the design of biologically active compound. This review covers updated information on the most active benzoxazine derivatives that have been reported to show considerable pharmacological actions such as antimicrobial, antimycobacterial, anti-diabetic, antihypolipidaemic, and antidepressant. It can act as an important tool for chemists to develop newer benzoxazine derivatives that may prove to be better agents in terms of efficacy and safety. For more details PDF Link:  http://www.jocpr.com/articles/pharmacological-profile-of-benzoxazines-a-short-review.pdf

Antidiabetic activity of leaves of Spinacia oleracea Linn. in Alloxaninduced diabetic rats

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ABSTRACT: To evaluate the hypoglycaemic activity of ethanolic and aqueous extract of Spinacia oleracea in normal and alloxan induced diabetic rats. The ethanolic and aqueous extract of leaves of spinacia oleraceae were orally tested at the dose of (200&400mg\kg) for hypoglycaemic effect in normal and alloxan-induced diabetic rats. In addition, changes in body weight, serum cholesterol, triglyceride assessed in the aqueous and ethanolic extract treated diabetic rats, were compared with diabetic control and normal animals histopathological observations during 12 days treatment were else evaluated. Ethanolic and aqueous extract of spinacia oleraceae produced a significant reduction in fasting blood glucose levels in the normal and significant reduction in fasting blood glucose levels in the alloxan-induced diabetic rats significant differences were observed in serum lipid profiles (Cholesterol and triglyceride) and changes in body weight by both ethanolic and aqueous treated diabet...

Synthesis, Anti-Tumor, Anti-Diabetic, and Anti- Asthmatic Activitives of Some Novel Benzimidazole Derivatives

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ABSTRACT: A series of novel substituted benzimidazole derivatives by the condensation of different diamines with anthranilicacid were synthesized. The subsequent reactions of the benzimidazole derivatives were reacted with different aromatic acid chlorides to get tetrazole moieties. These compounds were screened for their potential anti-cancer, anti-diabetic, anti-tumor and anti- asthmatic properties, which exhibited some authentic results towards testing organism invitro and invivo studies. For more details PDf Link:  http://www.jocpr.com/articles/synthesis-antitumor-antidiabetic-and-anti-asthmatic-activitives-of-some-novel-benzimidazole-derivatives.pdf

Antimicrobial Activity Of Thiosemicarbazone Derivatives Of Lawsone And Its Nickel Complexes

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ABSTRACT: Thiosemicarbazone derivative at 1 and 2 position of the Biologically important Lawsone ( 2- hydroxy-1,4-naphthalenedione ) have been synthesized. This possesses a powerful chelating ability, appreciable analytical utility and significant biological activity. Metal complexes of TSCND with Ni(II) metal have been synthesized and studied with the help of spectral analysis and elemental analysis. The antimicrobial activity of the ligands and their metal complexes against bacteria and fungus has been carried out. It is found that the metal complexes have higher activities than those of free ligands. For more details PDF Link:  http://www.jocpr.com/articles/antimicrobial-activity-of-thiosemicarbazone-derivatives-of-lawsone-and-its-nickel-complexes.pdf

Microwave assisted synthesis of some 5-pyridyl-2-[(N-substituted phenyl) thioacetamido]-1,3,4-oxadiazoles as antibacterial and antioxidant agents

Several substituted 1,3,4-oxadiazole exhibit antibacterial, antimicrobial pesticidal, anti-mycobacterial, anti-inflammatory and anti-fungal activities. Recently microwave assisted synthesis has attracted the researcher throughout the world for its less time consumption, minimum usage of solvents and increased yield of the compounds. The present investigation was to synthesize the title compounds 5-pyridyl-2-[(N-substituted phenyl) thioacetamido]-1,3,4- oxadiazoles (4a-g) by conventional and microwave methods and evaluate their antibacterial and antioxidant activities. It is well known that free radicals play an important role in the inflammatory process. PDF

Design development and evaluation of extended release tablets of Alfuzosin hydrochloride

Alfuzosin hydrochloride(HCl) was formulated as oral extended release matrix tablets using polymers like sodium alginate, ethyl cellulose( EC), hydroxyl propyl methyl cellulose (HPMC K100) and hydrogenated castor oil (HCO).Matrix tablets were prepared by wet granulation method. Tablets were prepared with drug to polymer ratios 1:5, 1:10, 1:15 and 1:20.The formulated tablets were evaluated for various physicochemical parameters by official procedures. The in vitro release study of the matrix tablets were carried out in 0.1N HCl for 2hrs at pH 1.2 and pH 6.8 buffer for the next 22 hours. Based on drug release rate, polymers can be arranged as sodium alginate > EC >HPMC >HCO. Among all the polymers HCO was most suitable to design the extended release formulation of alfuzosin HCl. Analysis of drug release mechanism indicated that the drug release from the matrix tablets was found to be non fickian obeying zero order kinetics. PDF

Pharmacoeconomical comparison of bare metal stent and drug eluting stent

Coronary artery disease (CAD) is the leading cause of death and disability world over. To achieve PCI; either bare metal stent (BMS) or drug eluting stent (DES) are used. The objective of the present retrospective study was to evaluate pharmacoeconomics between BMS (Driver TM) and DES (Endeavor TM) in patients who underwent coronary angioplasty. 20 patients underwent PCI between December 2007 and June 2009 at The Heart Care Clinic, Ahmedabad, out of which 10 patients were implanted with Zotarolimus Eluting Stent (ZES) and 10 were implanted with BMS. Both groups had similar demographics and risks factors. Follow-up was conducted. In pharmaco economics cost and effectiveness in terms of quality of life (Seattle Angina Questionnaires) and quality adjusted life years (QALY) was analyzed. Cost (in Indian Rupees) of BMS and DES was 96225±34732 and 152967±39086 (p <0.0001*), respectively. Effectiveness in term of QALY (Quality adjusted Life Year gained) was 1.58±0.33 in BMS group patien...

Formulation and in-vitro evaluation of floating capsules of Loratadine

The present work focuses on the development of hydrodynamically balanced delivery system of loratadine as a single unit floating capsules. Sustained release floating capsules for loratadine were fabricated using drug:polymer ratio of 1:4. The hydrocolloids were used in different proportions using 32 full factorial design and formulations were prepared. These formulations were optimized on the basis of buoyancy, matrix integrity, duration of floating and in vitro drug release. All the nine formulations showed good buoyancy and matrix integrity. The duration of floating was more than 12 h for all formulations. In vitro drug release study of these formulations indicated controlled release of loratadine and about 90 percent drug was released at the end of 12 h. PDF

UV-spectrophotometric method development and validation for estimation of Galantamine Hydrobromide in tablet dosage form

Two innovative, new, simple and low cost UV-spectrophotometric and first order derivative methods were developed and validated for estimation of Galantamine Hydrobromide in bulk drug and tablet dosage form. Galantamine Hydrobromide was estimated at 289 nm in Distilled Water. In first order derivative, it showed amplitude at 284.8 nm and λminima = 290.4 nm with 286.4 nm as zero crossing point (ZCP). In both the methods linearity was found to be in the range of 20-100 µg/ml; for UV spectrophotometric method (y = 0.007x - 0.002, r² = 0.999) and for first order derivative spectrophotometric method (Y=0.0012 x+0.00045; r2=0.999), respectively. These methods were analyzed and validated for various validation parameters according to USP guidelines. The quantitation limits were found to be 0.50 and 1.54 µg/ml, for UV-Spectrophotometric method and 3.3 and 10 µg/ml for the 1st order derivative method. The proposed methods were successfully applied for the determination of Galantamine Hydrobrom...

Solid phase extraction of copper, cadmium and lead in environmental samples FAAS using activated carbon modified with 5-(4-dimethyl aminobenzyledeneamino)-2-hydroxy benzoic acid

Sensitive and selective preconcentration procedure was developed for the determination of trace Cu(II), Cd(II) and Pb(II) ions in environmental samples. 5(4-dimethyl aminobezyledeneamino) 2-hydroxy benzoicacid modified with activated carbon was prepared and used as new solid phase extractor. Adsorbed metal ions were eluted with 10ml of 3N HNO3 at a flow rate of 2 ml/min. The concentration of metal ion determined by flame atomic absorption spectrometry (FAAS). Different factors including pH of the sample solutions, effect of sample volume, the amount of modified activated carbon, type and volume of eluent were examined. The proposed method was applied to the determination of metal ions in water samples and soil samples with satisfactory results (recoveries range from 96 to 99%). PDF

Synthesis and biological screening of picric acid & p-amino phenol derivatives for anti-microbial activity

The treatment of infectious diseases still remains an important and challenging problem because of a combination of factors including emerging infectious diseases and the increasing number of multi-drug resistant microbial pathogens with particular relevance for Gram positive bacteria. Bacteria are among the oldest living organisms on earth and are very small. Because the bacteria structure is so minute, it can only be seen through a microscope. Bacteria are commonly found in the ground, water and in other living organisms. While some types of bacteria can cause diseases and become harmful to the environment, animals and humans, others offer benefits that we likely could not live without. Some types of bacteria can attack plants, causing diseases like leaf spot and fire blight. PDF

Synthesis and spectroscopic characterization of copper (II) metal complexes of a 16 membered pentaaza (N5) bis (macrocyclic) complexes

Copper (II) complexes were synthesized with 1,1’-diphenyl, and 1,1’-diphenyl methane– bis(8,10-dimethyl-1,3,7,11,15-pentaazacyclohexadeca-7,11-diene) a tetradentate ligand (L) and characterized by elemental analysis, molar conductance measurements, IR, electronic and EPR spectral studies. The molar conductance measurements of all the complexes in DMF solution correspond to non-electrolytic nature for (ML)2RX4 complexes,1:4 electrolytes for (ML)2RY4 . Thus the complexes may be formulated by [(ML)2RX4 ] and [(ML)2R]Y4 respectively [where M = Cu (II), R = (C6H4NH2 ) 2 , (C6H4NH2 ) 2CH2 ., X= Cl, CH3COO, NO3 - and Y = ClO4 - . All the complexes are of the high-spin type and found to have six-coordinated octahedral geometry except the complexes of perchlorate which were four coordinate and square planar in geometry. PDF

Stability study of O/W emulsions using zeta potential

Emulsions are widely used as medicinal and cosmetic delivery systems on account of general observations that emulsified materials normally possess the properties being exhibited by its bulk components. In order to widen scope of application of the conclusions drawn, o/w emulsions covering almost all routes of administration were considered for the study. These included parenteral emulsion, oral Emulsion and topical emulsion. Zeta potential including zeta deviation and peak position, and effective particle size of the emulsions including Z-average diameter, poly dispersity index and peak position were studied using a Zeta sizer (Malvern instrument). Employing Laser Doppler Electrophoresis and dynamic light scattering technique, Zeta potential and particle size distribution of the droplet as a function of time can be determined, which was done in this paper. Zeta potential is used to study the chemistry involved in determining whether or not an emulsion will remain stable in the enviro...

Synthesis and biological activity of 8-chloro-[1,2,4]triazolo [4,3-a]quinoxalines

8-Chloro-1-substituted-[1,2,4]triazolo[4,3-a]quinoxalines 6 underwent facile condensation with various hydrocarbon derivatives in the presence of TEBAC in acetonitrile was refluxed and afforded corresponding 8-chloro-1,4-substituted-[1,2,4]triazolo[4,3-a]quinoxaline derivatives 7aj. Their chemical structures were characterized using IR, H1 NMR and Mass spectral studies. All the above compounds were screened for anti-microbial activity, anti-oxidant activity and their bioassay showed them to possess significant antimicrobial activity and anti-oxidant activity. PDF

Synthesis, Antibacterial and invitro Antioxidant Activity of 2,3-Substituted Quinazolin-4(3H)-ones

Quinazolinone and their derivatives have been studied extensively for various biological activities such as anti-inflammatory, antimicrobial, antitumor, antioxidant and anti-HIV activity. Schiff bases have also been exploited extensively for antimicrobial and antioxidant activities. In the present investigation various quinazolinone amines have been clubbed with five membered heterocyclic aldehydes to obtain the title compounds. All the synthesized compounds have been screened for their antibacterial activity against S.aureus, B.subtilis, E.coli and K.pneumonia and invitro antioxidant activity by 1,1-diphenyl-2,2-picryl hydrazyl free radical (DPPH) method. PDF

Synthesis and spectroscopic studies of tetradentateschiff base complexes of Cu(II), Ni(II), Mn(II) and Co(II

Cu(II), Ni(II), Mn(II) and Co(II) complexes were synthesized with bis(salicylaldehyde)malonyldihydrazone a tetradentate ligand (L) and characterized by elemental analysis, molar conductance measurements, magnetic susceptibility, IR, electronic and EPR spectral studies. Metal(II) salts react with Schiff base ligand in 1:1 molar ratio. The ligand and its complexes are stable at room temperature and all of them are nonhygroscopic also. The elemental analysis for carbon, hydrogen and nitrogen were performed by micro analytical methods. Apart from this, the geometry of the newly synthesized compounds has been explained based on their elemental analysis, molar conductivity and spectral data. The molar conductance measurements of all the complexes in DMF solution correspond to electrolytic nature for the complexes except Mn(II) complexes. PDF

Carbon Nanotubes in Pharmaceutical Nanotechnology: An introduction to Future Drug Delivery System

Recent discoveries indicate that the materials are bought down in sizes in the range 1-100nm, these exhibits unique electrical, optical, chemical and pharmaceutical properties. Methods have now been established to obtain the monodispersed nanocrystals of various metallic and semi conducting materials, single walled and multiwalled nanotubes of carbon and other metallic and non metallic materials together with organic nanomaterials such as nanostructures composites with tailored functionalities. Carbon nanotubes (CNTs) have great impact on the development of newer methodologies and devices useful for the analysis and the detection of various types of chemicals. The detection sensitivity can be increased many folds. The extraordinary properties of carbon nanotubes have led to demonstration of several applications of CNTs. But commercial realization of these CNTs and CNTs based devices require consistent quality of CNTs and these should be free of any impurity. Such demanding requiremen...

UV- Spectrophotometric determination of Ceftazidime in pure and pharmaceutical formulation

A simple sensitive spectrophotometric method in UV region has been developed for the determination of Ceftazidime in bulk dosage form. The solution of ceftazidime in 0.1N HCl shows maximum absorbance at 261nm, beer’s law was obeyed in the concentration range of 2-10 µg ml-1. The absorbance was found to increase linearly with increasing concentration of ceftazidime, which is corroborated by the calculated correlation coefficient value of 0.9981. The slope and intercept of the equation of the regression line are 0.0465 and 0.0007 respectively. The analysis were validated statistically and its recovery studies result of percentage shows that the method was not affected by the presence of excepients which proves suitability of the developed method for the routine estimation of ceftazidime bulk and solid dosage form. This method were extended to pharmaceutical formulations and there no interference from excepients and diluents. The proposed methods are economical and sensitive for the est...

Design, Development and Formulation of Antiacne Dermatological Gel

In the present study, Adapalene gels were prepared using CMC Na, HPMC, HPC, Carbomer and combinations of cellulose derivatives; as base and PluronicPE-6200 as penetration enhancer for the treatment of Acne. The gels were evaluated for drug content, viscosity determination, in vitro permeation (Nylone-66) and stability studies. The drug content of the gels was found to range from 98-105.7 %. The viscosity of the gels ranged between 7100-83144 cps. . In-vitro diffusion profile of Adapalene gel (optimized formula F-22) obtained in ethanol with water (80:20) indicate that 40.33% drug release found within 6 hrs. while 35.22% of marketed preparation. Although the difference is insignificant, the percentage release of drug was found to increase in the following order of the polymer composition: Carbopol-980> Carbopol-940> Carbopol-934> HPC > SODIUM CMC> HPC+SODIUM CMC > METHYL CELLULOSE > HPMC > HPC+HPMC. Further the formulation F-22 was found to be stable at acceler...

Medicinal uses and health benefits of Honey: An Overview

Honey is highly nutritious, it has traces of minerals and vitamins not to mention the antioxidants which destroy free radicals and delay ageing. In short, it is a safe and wholesome food for old, children and adults. Although not an herb, honey is a plant by-product and used medicinally around the world. Honey is also an energizer, helping workers and athletes overcome fatigue and regain energy. Children, young and old can alike take honey, without worrying any side effects. Honey is a multivitamin tonic, has antibacterial properties and has antioxidants. Nausea, cough, cold etc can be treated by taking honey with a tsp of tulsi (basil) leaf juice. Asthmatic persons can also benefit from taking honey everyday. Ayurveda acknowledges honey as a wonder medicine capable of providing longevity. Osteoporosis is another condition, which can be prevented by taking honey regularly. Modern researches have underpinned the wonderful effects of honey, proving honey to be effective against advance...

Preparation and characterization of pectin pellets of Aceclofenac for colon targeted drug delivery

The present study objective was to develop novel colon specific drug delivery systems for aceclofenac using pectin as a microbially degradable polymeric carrier and to coat the optimized batches with a pH dependent polymeric coating solution containing Eudragit L 100 and S 100 (1:4). Pellets containing four proportions of pectin were prepared. The pellets were evaluated for physicochemical properties, drug content, dissolution, water uptake & erosion characteristics, in vitro drug release studies. The amount of aceclofenac released from the pectin pellets at different time intervals was estimated by UV spectrophotometric method at 275nm. Eudragit coated pectin pellets prevented release of the aceclofenac in the physiological environment of stomach and small intestine depending on the proportion of pectin used in the formulation. The dissolution profile and in vitro release kinetics showed that pectin pellets were promising for controlled delivery of the drug. The findings of the ...

Leucotrienes and Its Biological Activities: A Review

Leucotrienes have attracted the attention of physician, medicinal chemist and pharmacist for its versatile biological activities.The present review highlights physiological and pathophysiological aspects of Leucotrienes. Leukotrienes, together with the prostaglandins and other related compounds, are derived from 20 carbon (eicosa) fatty acids that contain double bonds (enoic). They are formed from the breakdown of arachidonic acid, a polyunsaturated 20 carbon fatty acid. In its esterified form, arachidonic acid is bound to the phospholipids of the cell membranes. Both immunological and non-immunological stimuli can release arachidonic acid from membrane phospholipids by activating phospholipase A2.There is wide scope of Leukotrienes in therapeutic efficacy against many diseases, hence in this regard the review is outlined to collect the data of history of Leukotrienes releated to its molecular study, structure, pathophysiology and application. it is very interesting and note worthy t...

Design, synthesis and biological evaluation of benzoxazole derivatives as new antiinflammatory agents

New series of methyl 2-(arylideneamino) benzoxazole -5-carboxylate derivatives were synthesized by the reaction of Schiff bases of methyl 2-aminobenzoxazole-5-carboxylate with appropriate aromatic aldehydes. The chemical structures of the synthesized compounds were confirmed by means of IR, 1HNMR, mass spectral analysis. Further, the synthesized compounds (SH1-SH9) were screened for antiinflammatory activity by using Carrageenan – induced paw edema rat model. The results showed that, compounds SH1-SH3 and SH6-SH8 were significantly (p <0.0001) reduced the inflammation there by showed a promising antiinflammatory activity; where as the compound SH5 moderately reduced the inflammation. Only the two compounds i.e SH4 and SH9 showed very poor anti-inflammatory activity towards Carrageenan – induced paw edema rat. PDF

Synthesis and antimicrobial activity of some new chalcones and flavones containing substituted naphthalene moiety

Seven new chalcones and flavones containing substitued naphthalene nucleus in their structure were synthesized and the structures of these compounds were confirmed by spectral data. The newly synthesized compounds were screened for antibacterial activity against Escherichia coli and Stahylococcus aureus. PDF

Synthesis, characterization and bioactivities of Ni(II) and Co(II) complexes of benzyloxybenzaldehydethiosemicarbazone

Ni(II) and Co(II) complexes of benzyloxybenzaldehydethiosemicarbazone(L) were prepared and characterized by their physical, spectral and analytical data. The newly synthesized metal complexes have a composition of [M(L)2X2], where M= Co(II) or Ni(II) and X= Cl. The electronic spectral studies show an octahedral geometry around Ni(II) and Co(II) complexes. The IR spectral data suggest the involvement of sulphur and azomethane nitrogen in coordination with the central metal ion. In order to evaluate the biological activity of the ligand and its metal, complexes have been screened for their antibacterial and antifungal activity against bacterial species like – B.subtilis and S.aureus(Gram-positive bacteria) and E. coli, P. aeruginosa and P. vulgaris (Gram-negative bacteria) and also fungal species like- Microsporumgypseum, Teloschistes villous, Aspergillus fumigates and Candida albicans. The results of antimicrobial studies clearly show that the process of chelation dominantly affects t...