IJPAR | International Journal of Pharmacy and Analytical Research

International Journal of Pharmacy and Analytical Research

ISSN: 2320_2831

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  1. Method development and validation of simultaneous estimation of hydrochlorothiazide and triamterene in combined tablet dosage form by RP-HPLC methodDownload Article

    Dr.A.Yasodha, A.Chandramouli, G.Venkataih, A.Sivakumar
    • Article Type: Research Article
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    • Pages (001-017)
    • No of Download = 581

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    A new simple, accurate, rapid and precise isocratic high performance liquid chromatographic (HPLC) method was developed and validated for the determination of Hydrochlorothiazide (HTZ), and Triamterene (TMT) in tablet formulation. The optimized conditions comprises of column Purospher ®STAR C18 250 mm x 4.6 mm I.D; 5 μm with a flow rate of 1.0 mL/min, 0.05 M Phosphate buffer, methanol and acetonitrile mixture was used as mobile phase in the ratio 55:35:10 v/v at a detection wavelength 270 nm. Retention times of HTZ and TMT were found to be 3.49 min, and 4.68 min with a tailing factor 1.25, 1.27 and 4704, 4841 as theoretical plates respectively which are within the limits. All the parameters were validated according to the ICH guidelines and found to be within limits. Limit of detection (LOD) and Limit of quantification (LOQ) were estimated from the signal-to-noise ratio. The LOD values of HTZ and TMT were found to be 0.089 and 0.251 µg/mL respectively. HTZ and TMT LOQ’s were found to be 0.27, and 0.78µg/mL respectively. Linearity ranges for HTZ, and TMT were 2-10 µg/mL, and 3-15 µg/mL respectively. Percent recovery study values of HTZ and TMT were found to be within 98-102 %. This new method was successfully developed and validated as per ICH guidelines, can be utilized for the quantitative estimation of HTZ and TMT in pharmaceutical dosage forms.

  2. RP-HPLC method development and validation of RilpivirineDownload Article

    Dr.A.Yasodha, J. Rani, G.Venkataih, A.Sivakumar
    • Article Type: Research Article
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    • Pages (018-038)
    • No of Download = 952

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    A simple, accurate, rapid, and stability-indicating RP-HPLC method for a Rilpivirine has been developed and subsequently validated in commercial tablets. The proposed HPLC method utilizes Develosil ODS HG-5 RP C18, 5µm, 15cmx4.6mm and mobile phase consisting of ACN : Acetate buffer (pH=4.0) = 65:35 (v/v) at a flow rate of 1.0 ml/min. Quantitation was achieved with UV detection at 260nm. The method was validated in terms of accuracy, precision, linearity, limits of detection, limits of quantitation, and robustness. This optimized method has been successively applied to pharmaceutical formulation and no interference from the tablet excipients was found. Rilpivirine drug products were subjected to acid, base, neutral hydrolysis, oxidation, dry heat, and photolytic stress conditions and the stressed samples were analyzed by the proposed method. As the proposed RP-HPLC method could effectively separate the drugs from its degradation products, it can be employed as stability-indicating method for the determination of instability of these drugs in bulk and pharmaceutical dosage form.

  3. Physicochemical standardization, phytochemical screening, TLC profiling and GC-MS study of Buddleja asiaticaDownload Article

    Raja S and Ramya I
    • Article Type: Research Article
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    • Pages (039-052)
    • No of Download = 351

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    Background Buddleja asiatica is a deciduous shrub traditionally used as an antipyretic, antimalarial and abortifacient. The present study was designed to perform physicochemical standardization and to examine the presence of various phytoconstituents by phytochemical screening and gas chromatography-mass spectroscopy method. Methods Evaluation of organoleptic characters and physicochemical parameters were carried out according to WHO guidelines. Various extracts (petroleum ether, chloroform, ethyl acetate and methanol) were subjected to standard phytochemical screening methods. Different phytoconstituents in the extracts were analyzed by thin layer chromatography (TLC). Further, gas chromatography mass spectroscopy (GC-MS) study of ethanol extract was performed in Scion 436-GC Bruker instrument. Results The values of standardization parameters were found to be 19.25 ± 0.33% w/w, 07.36 ± 0.07 % w/w, 03.35 ± 0.06 % w/w, 25.75±1.13% w/w and 01.85± 1.12 % w/w for loss on drying, total ash, acid insoluble ash, water soluble extractive and swelling index respectively. In phytochemical screening, petroleum ether extract revealed the presence of saponins, steroids and terpenoids whereas chloroform extract confirmed the presence of alkaloids and saponins. Ethylacetate extract proved the presence of glycosides, phenolic compounds, tannins and steroids. Further, major constituents like glycosides, phenols, tannins, steroids, saponins, tannins flavonoids, carbohydrates and proteins were present in methanol extract. TLC analysis confirmed the presence of steroids in ethyl acetate extract and terpenoids & flavonoids in methanol extract. GC-MS analysis exhibited the presence of main constituents such as carbohydrates (myoinositol-4-c-methyl), terpenoids(6-epi-shyobunol), fatty acid (dibutyl phthalate) and steroids (stigmasterol) in ethanol extract. Conclusion The results of standardization parameters ensure quality and purity of Buddleja asiatica crude drug. Phytochemical, TLC and GC-MS studies indicate the presence of significant constituents like steroids, terpenoids and flavonoids in different extracts. Further experimental designs to isolate active constituents and examine their pharmacological aspects are highly recommended

  4. RP-HPLC method development and validation of citalopram in pharmaceutical dosage formDownload Article

    Dr.A.Yasodha, Sumayya Shahnaz , G.Venkataih, A.Sivakumar
    • Article Type: Review Article
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    • Pages (053-073)
    • No of Download = 1705

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    A simple, sensitive, precise and Reverse phase high performance liquid chromatographic method has been developed for the quantitative analysis of Citalopram drug present in drug substance. A suitable HPLC having a gradient system equipped with manual injector, UV detector is used for this work. The HPLC separation was achieved on HITACHI L2130 with D Elite 2000 software with Isocratic with UV-Visible detector (L2400).C18 Develosil ODS HG-5 RP 150 mm x 4.6 mm 5 µm particle size and column temperature 25ºc used as stationary phase. The mobile phase used in this analysis consists of a mixture of Phosphate Buffer 0.01M potassium dihydrogen phosphate (pH adjusted to 3.0 with ortho phosphoric acid ) and acetonitrile in the ratio of 60:40. Stock sample is prepared by using acetonitrile. Working sample used is about 10 ppm. Flow rate maintained is about 1.0 ml/minute and wavelength is about 229nm. Sample colour is ambient. Injection volume injected about 20 µL with run time 10 minutes. The proposed method provided linear responses within the concentration range 10 ppm for Citalopram LOD and LOQ values for the active substance were 0.04 and 0.12 µg/mL respectively. Regression equations for the drug substance is about 0.994 in all cases. The precision of the method was demonstrated using intraday and inter day assay % RSD values which were in acceptance limit (≤ 2%) in all instances. The proposed method was found to be accurate, precise, reproducible and specific and it can also be used for routine quality control analysis.

  5. RP-HPLC method development and validation of capecitabine in pharmaceutical dosage formDownload Article

    Dr.A.Yasodha, J. Parvathi1, G.Venkataih, A.Sivakumar
    • Article Type: Research Article
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    • Pages (074-092)
    • No of Download = 700

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    A simple, accurate, rapid, and stability-indicating RP-HPLC method for a Capacetabine has been developed and subsequently validated in commercial tablets. The proposed HPLC method utilizes Shimadju ODS (C8) RP Column, 150 mm x 4.6 mm. and mobile phase consisting of a mixture of Buffer (0.01 M potassium dihydrogen phosphate & pH adjusted to 2.2 with ortho phosphoric acid) and Methanol in a ratio of 40:60 Quantitations was achieved with UV detection at 260 nm. The method was validated in terms of accuracy, precision, linearity, limits of detection, limits of quantitation, and robustness. This optimized method has been successively applied to pharmaceutical formulation and no interference from the tablet excipients was found. Capecitabine drug products were subjected to acid, base, neutral hydrolysis, oxidation, dry heat, and photolytic stress conditions and the stressed samples were analyzed by the proposed method. As the proposed RP-HPLC method could effectively separate the drugs from its degradation products, it can be employed as stability-indicating method for the determination of instability of these drugs in bulk and pharmaceutical dosage form.

  6. A review on bilayer tablets of multi drug combination of anti-retro viral drugsDownload Article

    Patil Sagar N, Dr. Shailesh Sharma
    • Article Type: Research Article
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    • Pages (093-100)
    • No of Download = 381

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    Multilayer tablets are novel drug delivery systems where combination of two or more drugs in a single unit having different release profiles which improves patient compliance, prolongs the drug(s) action. Bilayer tablets are prepared with one layer of drug for immediate release while second layer designed to release drug, later, either as second dose or in an extended release manner. Trilayer tablets are prepared with one layer of drug for immediate release while second and third layers designed to release drug, later, either as second dose or in an extended release manner. These Multilayer tablets are suitable for sequential release of two or more drugs in combination, separate incompatible substances, and also for sustained release tablet in which one layer is immediate release as initial dose and second layer is maintenance dose. Acquired immune deficiency syndrome epidemic is one of the greatest challenging facing the medical community today. Combination of three drugs commonly used in the management of the Human Immunodeficiency Virus (HIV) infection. Zidovudine (AZT), the first anti‐HIV compound approved for the clinical use is widely used for treatment of AIDS either alone or in combination with other antiviral agents and Zidovudine is water soluble and soluble at all pH ranges and absorbs throughout the gastrointestinal tract and so sustained release tablet is better approach than the conventional dosage form. Lamivudine is a potent antiviral agent used in the treatment of AIDS. Lamivudine is a potent nucleoside analog reverse transcriptase inhibitor. Lamivudine is rapidly absorbed with a bioavailability of over 80% following oral ingestion. Lamivudine are administered multiple times a day because of its moderate half-life of 5 to 7 hours. Tenofovir disoproxil is an antiretroviral medication used to prevent and treat HIV/AIDS and to treat chronic hepatitis B. The active substance is tenofovir, while tenofovir disoproxil is a prodrug that is used because of its better absorption in the gut.

  7. RP-HPLC method development and validation of levamisole in pure and pharmaceutical formulationDownload Article

    B.Thangabalan, Anusha.G, S.Manohar Babu, B. Ram Sarath Kumar
    • Article Type: Research Article
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    • Pages (101-107)
    • No of Download = 609

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    A simple, fast, precise, selective and accurate RP-HPLC method was developed and validated for the determination of levamisole from pharmaceutical formulation. Chromatographic separation was achieved on a YMC C18 column (250 x 4.6mm, 5 µ particle size) using a mobile phase acetonitrile and water in the ratio of 80:20%V/V. The flow rate was 0.7ml / min and effluent was detected at 217nm. The retention time of levamisole was found to be 6.2min. Linearity was observed in the concentration range of 10 -50µg / ml .The method was validated according to ICH guidelines with respect to specificity, linearity, accuracy, precision and robustness. The method developed can be used for the routine analysis of levamisole.

  8. Design & in vitro evaluation of floating microspheres using misoprostolDownload Article

    K. Ranjith Kumar, D.V. R. N. Bhikshapathi, B.Haarika
    • Article Type: Research Article
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    • Pages (108-117)
    • No of Download = 333

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    The present research was aimed to prepare Misoprostol floating microspheres for sustained release using polymers such as sodium alginate and Hydroxy propyl methyl cellulose (HPMC K4M) by ionotropic gelation method. Drug and excipient compatibility studies were carried out by FT-IR and no interaction was observed. The prepared microspheres were evaluated for the Percent drug content, entrapment efficiency and In-vitro dissolution studies. Different formulations were prepared with different concentrations of polymers, among all the formulations F12 was selected as optimized formulation based on the micromeretic and physico chemical parameters including drug release studies. In vitro release study of formulation F12 showed 99.11% drug release after 12 h in a controlled manner, which is desired for disease like peptic ulcer. In vitro release profiles from optimized formulation F12 were applied on various kinetic models. The best fit with the highest correlation coefficient was observed in zero order and Higuchi model, indicating diffusion controlled principle. The marketed product IR tablet shows the drug release of 95.23% within 1 h. The results obtained from evaluation and performance study of different types of Misoprostol microspheres that system may be useful to achieve a controlled drug release profile may help to reduce the dose of drug, dosing frequency and improve patient compliance when compared with marketed product.

  9. A novel validated quantitative estimation & stability indicating RP-HPLC method for simultaneous estimation of tolperisone HCL and etodolac in bulk and its pharmaceutical dosage formulationsDownload Article

    T. Rama Mohan Reddy & D.V. R. N. Bhikshapathi
    • Article Type: Research Article
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    • Pages (118-126)
    • No of Download = 230

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    A rapid, sensitive and specified RP-HPLC method involving DAD detection was developed and validated for determination and quantification of Tolperisone (TOL) and Etodolac (ETD) in tablet dosage form. Chromatography was carried out on Sunsil, 250 mm x 4.6 mm i.d; 5µ particle size column using filtered and degassed mixture of Acetonitrile and phosphate buffer (pH 2.6) in the ratio of 30:70 v/v as mobile phase at a flow rate of 1 ml/min and effluents were monitored at 267 nm. The pH of the mobile phase was adjusted with the diluent. The method was validated in terms of linearity, precision, accuracy, specificity, Limit of detection, limit of quantification and stability indicating studies. The assay was linear over the concentration range for TOL: 18-42µg/mL and for ETD: 48-112 µg/mL respectively. Accuracy of the method was determined through recovery studies by adding known quantities of standard drugs to the pre analysed test solutions and was found to be between 99.27 – 101.38% within. The % RSD for both TOL & ETD was found to be 0.66 and 0.41 respectively. The stability indicating studies were all in limit and meeting the need of the quantitative analysis. The method does require less than 10 minutes as run time for analysis which enhanced to prove the adoptability of the method for routine quality control of the drugs.

  10. Development and validation of RP-HPLC method for the determination of diphenamid in its formulationsDownload Article

    R. Swathi, B. Ramachandra, M. Hanuman Nayak, N.Venkatasubba Naidu
    • Article Type: Research Article
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    • Pages (127-140)
    • No of Download = 392

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    A simple, selective, precise and accurate High Performance Liquid Chromatographic method for the analysis of Diphenamid in its formulations was developed and validated in the present study. The mobile phase consist a mixture of 20mM Ammonium Phosphate (adjusted pH 3.0 with OPA) and Methanol in the proportion 60: 40 (v/v). This was found to give sharp peak of Diphenamid at a run time of 10 min. HPLC analysis of Diphenamid was carried out at a wave length of 250 nm with a flow rate of 1.0mL/ min. The linear regression analysis data for the calibration curve showed a good linear relationship with a regression coefficient 0.999 in the concentration range of 50% to 150%. The linear regression equation was y = 2159.x - 136.1. The developed method was employed with a high degree of precision and accuracy for the analysis of Diphenamid. The method was validated for accuracy, precision, robustness, ruggedness and specificity. The Precision, accuracy, sensitivity, short retention time and composition of the mobile phase indicated that this method is useful for the quantification of Diphenamid.

  11. Optimization of stability indicating RP-HPLC method for the estimation of an anti-cancer drug Sorafenib Tosylate in pure and pharmaceutical dosage formDownload Article

    Ramesh Jayaprakash, Dr. Senthil Kumar Natesan
    • Article Type: Research Article
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    • Pages (141-152)
    • No of Download = 767

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    A simple, specific and precise stability indicating RP- HPLC method has been developed and validated for the estimation of sorafenib tosylate in tablet dosage from using Phenomenex Luna- C18 column (4.5 x 250 mm; 5 µm particle size) as a stationary phase, methanol: acetonitrile: water (65:25: 10 v/v/v) as a mobile phase, flow rate of 1 mL/min and detection was carried out at 248 nm. The retention time of sorafenib was 2.887 minute. RP- HPLC method was developed with linearity range of 20-120 µg/mL of sorafenib tosylate. The correlation coefficient was found to be 0.9997 for sorafenib tosylate. The assay results obtained in good agreement with the corresponding labeled amount by developed method within range of 99.15% - 101.58%. Accuracy, precision, LOD, LOQ, specificity, robustness and ruggedness were met all the acceptance criteria for the validation of analytical method as per ICH Q2 (R1) guideline. This method can be conveniently used to detect the possible degradation product in the dosage form of sorafenib tosylate during stability studies (acidic, alkaline, oxidative, thermal and photolytic). The method proved to be effective on application to a stressed marketed tablet formulation.

  12. A review on comparison of specific serum immunoglobulin g and complement c3 levels in gestational diabetics and normal healthy pregnant women and its complications during pregnancyDownload Article

    Mathew George, Lincy Joseph, Leena P.N, Jeena Varghese
    • Article Type: Review Article
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    • Pages (153-157)
    • No of Download = 306

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    Gestational diabetes mellitus is one of the most common medical complication and a metabolic disorder that occurs during pregnancy. The essential components of humoral immunity are complement and circulating immunoglobulin. Immunoglobulin (Ig),is a large, Y-shaped protein produced mainly by plasma cells that is used by the immune system to identify and neutralize pathogens such as bacteria and viruses. The complement system, a complex protein network initially identified as part of the innate immune system, is as an essential regulator of cell and tissue homeostasis.. Maternal antibodies Ig G are transported across the placenta which protects the newborn. As there are only few studies in Indian literature regarding the comparison of specific serum immunoglobulin g and complement c3 levels in gestational diabetics and normal healthy pregnant women .This review is design to compare the levels of serum immunoglobulin G and complement C3 in Gestational diabetics and normal healthy pregnant woman and its complications during pregnancy.

  13. Design and evaluation of microspheres loaded with nizatidineDownload Article

    A.Shylaja Rani, D.V. R. N. Bhikshapathi
    • Article Type: Research Article
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    • Pages (158-168)
    • No of Download = 243

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    A novel ionotropic gelation technique was employed to design and develop sustained release Nizatidine microspheres for oral administration. Calcium chloride was selected as cross linking agent and sodium alginate as polymer to control the release profile of the Nizatidine from microspheres. The S1 to S14 formulations were subjected to micromeritic properties, swelling index, % yield, encapsulation efficiency and in vitro drug release. Fourier transform infrared spectroscopy (FTIR) and scanning electron microscope (SEM) were characterized for the prepared microspheres. The optimal formulation used for fabrication of microspheres was dispersion with 2% (w/v) sodium alginate, 10% (w/v) calcium chloride, and the drug Nizatidine content was 450mg based on solid weight in the dispersion. It was indicated that Nizatidine had no interactions with excipient by the FTIR and DSC. The optimized formulation (S6) showed the particle size, bulk density, tapped density, angle of repose, Carr’s index and swelling index of 82.45±0.09 µm, 0.52g/ml, 0.59g/ml, 20˚.54, 7.95%, 97%, respectively. The % yield, %EE and Cumulative % drug release of S6 was found to be 98.3%, 96.3% and 98.54%, respectively. The in vitro drug release was showed the 98.07±0.46% within 12h. The optimized formulation followed the Zero order and Higuchi kinetics indicated the diffusion controlled release mechanism. SEM studies showed the optimized formulation had particles of spherical in shape. The optimized formulation S6 was found to stable. All the results proved that the ionotropic gelation is a novel and promising technique for preparing sustained-release microspheres, and suitable for industrial production due to its successive and controllable step in preparation.

  14. Method development and validation of simultaneous estimation of metformin and glibenclamide in combined tablet dosage form by RP-HPLC methodDownload Article

    Dr.A.Yasodha, B.Kavitha, G.Venkataih, A.Sivakumar
    • Article Type: Research Article
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    • Pages (169-189)
    • No of Download = 358

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    A new simple, accurate, rapid and precise isocratic high performance liquid chromatographic (HPLC) method was developed and validated for the determination of Metformin and Glibenclamide in tablet formulation. The proposed HPLC method utilizes Develosil ODS HG-5 RP C18, 250 mm x 4.6 mm I.D; 5 μm with a flow rate of 1.0 mL/min, mobile phase consisting of Methanol : Acetate buffer (pH=3.0) = 75:25 (v/v) at a detection wavelength 256 nm. The method was validated in terms of accuracy, precision, linearity, limits of detection, limits of quantitation, and robustness. This optimized method has been successively applied to pharmaceutical formulation and no interference from the tablet excipients was found. Retention times of Metformin and Glibenclamide were found to be 2.24 min, and 3.28 min with a tailing factor 1.30, 1.29and 2603, 3534 as theoretical plates respectively which are within the limits. All the parameters were validated according to the ICH guidelines and found to be within limits. Limit of detection (LOD) and Limit of quantification (LOQ) were estimated from the signal-to-noise ratio. The LOD values of Metformin and Glibenclamide were found to be 0.062 and 0.018 µg/mL respectively. Metformin and Glibenclamide LOQ’s were found to be 0.19, and 0.056µg/mL respectively. Linearity ranges for Metformin and Glibenclamide were 2-10 µg/mL, and 3-15 µg/mL respectively. Percent recovery study values of Metformin and Glibenclamide were found to be within 98-100 %. This new method was successfully developed and validated as per ICH guidelines, can be utilized for the quantitative estimation of Metformin and Glibenclamide in pharmaceutical dosage forms.

  15. Comparative pharmacokinetics of PLGA & PCL based long acting injectable (LAI) risperidone microsphere formulationsDownload Article

    Harish Kaushik Kotakonda, Nagulu Malothu, Yellu Narsimha Reddy
    • Article Type: Research Article
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    • Pages (190-200)
    • No of Download = 525

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    The objective of the study was to compare and evaluate the pharmacokinetics of biodegradable PLGA & PCL microspheres with Risperidal Consta TM for achieving the sustained delivery of Risperidone in the schizophrenia therapy. Five microsphere formulations of risperidone were prepared by using two PLGA copolymers (50:50 and 75:25) and PCL (PCL 45000 and PCL 80000) polymer. All the five novel microsphere formulations (PLGA1-4 & PCL) and Risperidal ConstaTM was administered to male Sprague Dawley rats through subcutaneous route at different dose. PLGA & PCL formulations achieved higher exposure than Risperidal constaTM ie among PLGA based formulations ranked in the following order (PLGA1(1.6x) > PLGA2 (1.5x) > PLGA3 (1.2x) > PLGA4 (0.9x)) whereas PCL formulation demonstrated 1.3x higher exposure than Risperidal Consta. Simulations of multiple dosing at weekly or 15-day regimen to predict the in vivo profile of risperidone following subcutaneous administration of PLGA1-4 and PCL microspheres formulations and compared with marketed Risperidal ConstaTM revealed pulsatile behavior for all formulations with steady state being achieved by the second dose. Based on simulations it was observed that PLGA & PCL based formulations can be utilised to provide weekly and once in 15 day dosing regimen which could be an effective approach for sustained delivery of this molecule and a possible alternative to the currently available combination therapy. Therefore based on our study we conclude that development of novel microsphere based formulation by combining the PLGA & PCL systems to prepare long acting dosage forms with atypical antipsychotics will ensure patient compliance, reduce side effects, and improve the quality of life for patients who suffer from schizophrenia.

  16. High performance liquid chromatography mass spectrometric (LC-MS/MS) method for the estimation of clopidogrel bisulfate in human plasma by liquid-liquid extraction techniqueDownload Article

    Shaban G. Elosta, Mohamed H. Assaleh
    • Article Type: Research Article
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    • Pages (201-207)
    • No of Download = 443

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    A high performance liquid chromatography mass spectrometric method for the estimation of clopidogrel (CLP), in human plasma in positive ion mode was developed and validated using clopidogrel D3 (CLPD) as internal standard (IS). Sample preparation was accomplished by liquid-liquid extraction technique. The reconstituted samples were chromatographed on Kromasil 100-5C18, 100×4.6 mm, 5µm column using a mobile phase consisting of HPLC grade Acetonitrile: Milli Q/HPLC grade water (90:10, v/v). The method was validated over a concentration range of0.0101 to 5.0315 ng/mL for CLP. This validation report provides the results of selectivity, matrix effect, sensitivity determinations, calibration standards and quality control samples data, precision and accuracy data, the results of recovery, various stabilities, run size evaluation and dilution integrity along with all pertinent supporting documentation.

  17. Estimation of total phenolic and flavonoid content of Hibiscus furcatus Roxb leavesDownload Article

    Najuma Salim, Rahul Pratap, Abdul Vajid Komban, Surya Narayanan, Suma V.K
    • Article Type: Research Article
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    • Pages (208-214)
    • No of Download = 353

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    Hibiscus furcatus Roxb belonging to family, Malvaceae,is a herb ,used in traditional medicine for the treatment of inflammation, hyperdypsia, renal diseases etc. Ethanolic extract of Hibiscus furcatus was fractionated using different solvents of increasing polarity like petroleum ether, chloroform and ethylacetate. The preliminary phytochemical screening showed the presence of carbohydrates, steroids, flavonoids.

  18. Synthesis and evaluation of some novel heterocyclic compounds containing pyrimidine and thiazolidinone rings and their Derivatives as an antimicrobial agentsDownload Article

    Ganesh S Andhale, Sapana M Nagare, SR Pattan, Krishna Kumar K L
    • Article Type: Research Article
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    • Pages (215-221)
    • No of Download = 338

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    A series of (4, 6-disubstituted phenyl) pyrimidine and their derivatives are known for their biological importance. In present research work, we have attempted both Conventional to synthesize 1- (4, 6-disubstituted phenyl) pyrimidin-2yl-2-(4methoxyphenyl) thiazolidine-4-one. A wide spectrum of biological activities like anti-diabetic, anti-bacterial, antifungal, anti-oxidant and anti-inflammatory activities are found to be associated with pyrimidine nucleus. Chalcones were synthesized by claisen-schmidt reaction using aromatic aldehydes and ketones. Then reacting with guanidine hydrochloride the resultant pyrimidine compounds are synthesized. Again its Schiff’s base reaction is carried out and then cycloaddition reaction is done, so (4, 6-disubstituted phenyl) pyrimidin-2 yl-2-(4methoxyphenyl) thiazolidine-4-one derivatives are prepared by using thioglycolic acid. All the synthesized compounds were characterized by IR were recorded for all compounds, 1H-NMR and Elemental Analysis was carried out for prototype of compounds. All the compounds were evaluated for antibacterial (S. aureus and E. coli) activity and antifungal (A. niger and C. albicans) activity at the concentration of 100 µg/mL by using cup-plate agar diffusion method. The activity was measured in terms of zone of inhibition and compared with standard drug Ciprofloxacin for antibacterial activity and Griseofulvin for antifungal activity.

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