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  • SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME NOVEL HETEROCYCLES DERIVED FROM 2-ARYLIDENE-1-TETRALONES

    About Authors:
    Roshni Patel*, Prof. Arun Parikh, Prof. Vijayalakshmi  Gudaparthi
    Department of Pharmaceutical Chemistry, L.J.Institute of Pharmacy,
    S.G.Highway, Ahmedabad-382210
    *roshanimpharm@gmail.com

    ABSTRACT
    Medicinal chemistry involves chemical aspects of identification, and then systematic, thorough synthetic alteration of new chemical entities to make them suitable for therapeutic use. Indazoles have an important role in medicinal chemistry. Indazole  nucleus is an important class of nitrogen containing heterocyclic widely used as key building block for the synthesis of various pharmaceutically important agents. Indazole possess wide range of biological activities such as bactericidal, fungicidal, analgesic, antihypertensive, anti-inflammatory and antitumor. In the present study we have synthesized some novel 3,3a,4,5-tetrahydro-2-(substituted benzenesulphonyl)-3-(substituted phenyl)-2H-benzo[g]indazoles, by condensation of  1-tetralone with different substituted aromatic aldehydes and the resulted 2-(substituted benzylidene)-3,4,-dihydronaphtalen-1-ones on reaction with hydrazine hydrate in methanol followed by treatment with different substituted sulfonyl chlorides in pyridine gave the titled compounds.The synthesized compounds were characterized by IR, NMR and Mass spectral analysis. All newly synthesized derivatives were evaluated for antibacterial activity against  gram + ve and gram-ve bacteria B.cereus, S.aureus and E.coli respectivelyand antifungal activity againstC.albicans and all the synthesized compounds showed significant antibacterial and antifungal activity.

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  • RISK OF HYPERTENSION IN DIABETES PATIENT AS COMPARED TO NON DIABETIC

    About Authors:
    Gupta S*, Singal A
    Apex Institute Of Pharmaceutical Sciences,
    Jaipur, Raj., India
    *somesh.gupta88@gmail.com

    Abstract
    The aim of the present study was to correlate the occurrence of hypertension in the diabetics’ patient by the survey report on hypertension associated with diabetics’ patient. The effect of this study is symbolize that 70% patient have diabetes with hypertension and 30% patient with hypertension only so we can say that in this survey as the BGL increased leads to increased in B.P. And it was also found to be that aged patients have more risk of diabetes. Over 60- 70 year age group patient have 40% risk to get diabetes.

  • FORMULATION AND EVALUATION OF TASTE MASKED ORODISPERSIBLE TABLETS BY ION – EXCHANGE RESINS

    About author:
    Ashish Vishwakarma
    Department of Pharmaceutics,
    Chandigarh College of Pharmacy,
    Mohali-140307
    ashish1931@gmail.com

    ABSTRACT-
    Acceptability of any drug dosage form mainly depends upon its taste i.e. mouth feel. In the formulation of   oro-dispersible tablet of bitter drug, the main challenge is to mask the bitter taste of drug, because the drug is dispersed and released in mouth. This is more essential in the formulation for pediatric and geriatric, bed ribbon and non-cooperative patients. There are many methods of taste masking but the main objective of this article is to explore method, technology and evaluation to mask taste of bitter drug by ion-exchange resins. Here we will study the formulation and evaluation of various oro-dispersible tablets of bitter drug. This is more economical, easiest and efficient method for taste masking.

  • Polyanhydride Microspheres for Controlled drug delivery to the Lung

    About Authors:
    Abdulrhman A. Akasha
    Department of Pharmaceutics, Faculty of Pharmacy,
    Tripoli University, Libya-13645
    akashaabdu@yahoo.co.uk

    Abstract
    Bioerodible microspheres may provide a vehicle for achieving good aerosolisation characteristics, whilst offering a slow release depot from the pulmonary deposited fraction.  Polysebasic anhydride (PSA) was synthesised by a melt-polycondensation process using nitrogen gas under high vacuum. The products were characterised by 1H-NMR (2 & 20 KDa) and DSC (melting point: 68 & 83 °C), and with a yield (81 & 89 %) of prepolymer and polymer respectively. The polyanhydride was converted into microspheres using an oil in oil emulsification procedure.  The polymer was dissolved in dichloromethane and using 1 to 5% Span 85 or oleic acid as stabilizer, dispersed into silicone oil. The dichloromethane was removed by evaporation, the microspheres recovered and washed with petroleum ether. Laser diffraction analysis of the microspheres indicated a mean microspheres size <5 mm.  The presence of rough non-porous spheres was demonstrated by SEM.  Initial in vitro experiments were undertaken to examine the degradation rate in 0.1 M phosphate buffer at 37 °C, pH 7.4.  The process was followed for 24 hr, by which time 73% of the microsphere mass had eroded. However release of salbutamol base occurred more rapidly with 95% lost within 6-10 hr. The fact that 74% was released in the first 10 min suggest a high fraction of surface adsorbed drug. Microcarrier systems for slow release may provide a vehicle for achieving good aerosolisation characteristics, whilst offering a slow release depot from the pulmonary deposited fraction. The produced rough and non-porous microspheres containing salbutamol base were subjected for Deposition process using Andersen Mark II Cascade Impactor. The Deposition was assessed from both a Spinhaler and Rotahaler after 5s activation at a flow rate of 28.3L/min.  This resulted in an average of 33.5% (Rotahaler and 17.5% (Spinhaler) of the dose found between stages 2 and the filter corresponding to microspheres in the size range 4.7 to 0.4 mm.

  • ENHANCEMENT OF DISSOLUTION RATE OF OLANZAPINE USING SURFACE SOLID DISPERSION TECHNIQUE

    About Authors:
    Borse V. G.*, Birajdar A. S., Datal A. A.
    K. T. Patil College of Pharmacy,
    Osmanabad-413501, Maharashtra, India.
    *vishalgborse@gmail.com

    ABSTRACT :
    The objective of this study is to enhance dissolution rate of practically insoluble drug olanzapine, using surface solid dispersion technique. Olanzapine is classified as a thiobenzodiazepine atypical antipsychotic drug used in the treatment of schizophrenia. Surface solid dispersion technique is used to prepare solid dispersion of olanzapine using Crospovidone as carrier. Surface solid dispersion were characterised by saturation solubility studies, drug content and in- vitro dissolution studies. Solubility studies revealed a marked increase in the solubility of olanzapine with an increase in Crospovidone concentration. The best dispersion was selected based on saturation study and release study and evaluated for solid state characterization techniques Differential scanning calorimetry, FT-IR spectroscopy study. The results from DSC and IR indicated that there was no interaction between drug and carriers. Surface solid dispersion of olanzapine shows increase in aqueous solubility 4.42 fold than pure drug. SSD with Crospovidone in 1:9 ratio give highest drug release i.e. 88.87%.Surface solid dispersion is successful technique to improved drug dissolution of olanzapine with the carrier Crospovidone.

  • EVALUATION OF HEPATOPROTECTIVE ACTIVITY OF FICUS RELIGIOSA ON RATS AGAINST CCL4 AND PARACETAMOL INDUCED HEPATOTOXICITY

    About Authors:
    Vivek Chourasia*, Hemant Nagar, H.S. Chandel, Anindya Goswami
    Truba Institute of Pharmacy,
    Karond Gandhinagar Bypass
    Bhopal (M.P.)-India
    *vickyc.chourasia@gmail.com

    ABSTRACT
    Ficus religiosawas investigated for its possible protective effect against paracetamol and CCl4-induced hepatic damage. IV administration of a sub-lethal dose of paracetamol (500 mg/kg) produced liver damage in rats as manifested by the rise in serum level of transaminases (AST and ALT). Ttreatment of rats with Ficus religiosa (200 mg/kg) prevented the paracetamol-induced rise in serum enzymes. The hepatotoxic dose of CCl4 (1.5 ml/kg; orally) also raised the serum AST and ALT levels. The same dose of Ficus religiosa (200 mg/kg) was able to prevent the CCl4-induced rise in serum enzymes. These results indicate that Ficus religiosa possesses hepatoprotective activity.

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  • SIMULTANEOUS ESTIMATION OF FUROSEMIDE AND SPIRONOLACTONE IN COMBINED PHARMACEUTICAL DOSAGE FORM BY RP-HPLC

    About Author:
    Hardik Patel*, Sagar Solanki
    Department of Pharmaceutical Chemistry,
    K.B.Raval College of Pharmacy, Shertha,
    Gandhinagar-382423, Gujarat, India.
    *patel1928@yahoo.in

    ABSTRACT
    A new, simple, rapid, accurate, precise and sensitive method has been developed for the simultaneous estimation of Furosemide and Spironolactone in their combined tablet dosage form. The method was carried out on a Hiber C18 column (250 mm×4.6mm, i.d.5 μm) with a mobile phase consisting of acetonitrile: water at a flow rate of 1 ml/min and the detection was carried out at 237 nm. The retention time of Furosemide and Spironolactone was 3.81 min and 7.28 min. respectively. Linearity for Furosemide and Spironolactone were found in the range of 2-10 μg/ml and 5-25 μg/ml respectively. The developed method was validated in terms of linearity, accuracy, and precision, limit of detection (LOD) and limit of quantification (LOQ). The proposed method can be used for estimation of both drugs in their combined dosage form.

  • DETERMINATION OF SYNTHETIC INTERMEDIATE OF DICLOFENAC SODIUM IN REACTION MIXTURES BY HIGH PERFORMANCE LIQUID CHROMATOGRAPHY

    About Authors:
    1) Mr Jaesh N.Jadhav
    M.Pharm,Sinhagad Institute of pharmacy,Pune.
    2) Mr. J.G. Chandorkar*.
    Head Analytical development laboratory,
    Indofil Industries limited,Thane
    *Jayant.chandorkar@rediffmail.com

    Abstract
    A present work describes a simple & accurate reversed phase HPLC Method for the simultaneous estimation of Ortho Chlorophenol [OCP], 2,6 – Dichlorophenol [DCP], 1-(2,6-Dichlorophenyl) indolin-2-one [VTCL], 1(2,6-Dichlorophenyl) N-Phenyl, N-Chloro Acetyl, 2,6-Dichloro Aniline [VTDL], 1(2,6-Dichlorophenyl) ether [DCPE], 1(2,6-Dichlorophenyl) amine [DCPA] in Diclofenac Sodium bulk manufacturing. This paper describes a new rapid, easy Isocratic reversed phase HPLC method for the separation and estimation of six intermediates and Diclofenac Sodium. The primary purpose of this study is to compile HPLC data on the determination of these seven products, the compilation of such HPLC data being useful as reference guide.

  • MOLECULAR CHARACTERIZATION OF A BEGOMOVIRUS ASSOCIATED WITH CLERODENDRON INERME

    About Authors:
    Sanjay Kumar Yadav*1, Anjana Yadav1, Shahana Majumder2
    *1Dept of Pharmaceutical Chemistry, B.B.S. Institute of Pharmaceutical & Allied Sciences, Greater Noida, (U.P.), India
    1Dept of Biotechnology, Chhatrapati Sahu Ji Maharaj University, Kanpur, (U.P.), India
    2Dept of Biotechnology, Sharda University, School of Engineering and Technology,
    Greater Noida, (U.P.), India
    *sanjay_yadav3333@yahoo.co.in

    ABSTRACT
    Viruses are pathogens with an extremely narrow host range. Their phylogenetic origin is vague, tough it has always been considered that viruses are genes that became vagrant after having excluded themselves of the host’s or a related species’ genome (Anderson et.al., 2004). Viruses are usually units consisting of nucleic acids and coat proteins called capsids. Viroids consist only of RNA, i.e. they contain no protein at all. Except for a few cases, Viruses have no energy metabolism of their own. Consequently, they cannot perform syntheses and are thus unable to replicate themselves. Depending on their host species, it is distinguished between plant viruses multiplying almost exclusively within plant cells, bacterial viruses (bacteriophages) that depend on living bacteria, and animal viruses. The genetic information of viruses is either encoded by single-stranded RNA (Most plant viruses), double-stranded RNA (Wound tumor viruses), single-stranded DNA (Gemini viruses) or double stranded DNA (Cauliflower mosaic virus). Based on the shape of the viruses particle, it is distinguished between rod shaped and icosahedral viruses with a capsid that seem almost spherical. Viruses’ cause many disease in humans of international importance for example  smallpox polio, hepatitis etc. viruses cause also many important plant disease and are responsible for huge loss in crop production and quality in all part of the world. Around 25 years ago, when genomic properties of geminiviruses were studied, many scientists regarded them as ‘friends of humans’, because of their  potential as gene transfer vectors in plant genetic engineering and non-harmful effects on host plants. But far from being friends, these viruses have now emerged as foes and are a serious threat to world agriculture now. Increase in international commodity trade, intercontinental transportation networks and a changing global climate have contribute to the spread of this virus and its whitefly vector (Moffat et.al.,1999).

  • FORMULATION AND EVALUATION OF GASTRORETENTIVE FLOATING DRUG DELIVERY SYSTEM OF PIOGLITAZONE HYDROCHLORIDE

    About Authors:
    *Thoriya J. G, Patel S. D, Tank H. M
    Matushree V. B. Manvar College of Pharmacy- Dumiyani,
    Rajkot
    *thoriya.jignesh@gmail.com

    ABSTRACT
    Pioglitazone HCl is used for the management of type-2 diabetes. It is an absorption window limited drug, whose solubility decreases with increase in the pH and has a short half life of 3-7 h. Here an attempt is made to developed the floating matrix tablets, which design in way that after oral administration the GI resistant time is  prolonged and thus to give sustained action with increase in the bioavailability of the drug. Pioglitazone HCl showed maximum absorption at wavelength 269 nm in 0.1N HCl. various formulations were developed by using release rate controlling and gel forming polymers like HPMC, and Carbopol-934 in single and combinations by direct compression method with the incorporation of sodium bicarbonate as gas generating agent. The prepared tablets were characteristics by drug content, floating property, swelling and in vitro dissolution test using USP dissolution test apparatus Type – II (paddle method) in dissolution medium of 0.1 N HCl. The in vitro dissolution results of all tablets were computed by using dissolution software. The prepared tablets were found to be good hardness, diameter, weight variation, thickness, friability drug content, floating property and in vitro drug release. Drug-polymer compatibility studies by FTIR gave conformation about drug purity and showed no interaction between drug and selected polymers. All the formulations had floating lag time below 3 minutes and constantly floated on dissolution medium for more than 12 h. Swelling studies indicated significant water uptake and contributed in drug release. From among all the developed formulations, as F7 prolonged the drug release (95.45 %) for longer period of time (12 hrs.); they were selected as best formulations. The best formulations were found to be stable during stability studies for two months. Thus, selected formulations satisfied floating time, swelling index and in vitro drug release profile requirements for a floating drug delivery system.Tablets of Pioglitazone HCl prepared with HPMC K4M, HPMC K100M and Carbopol 934P were found to be acceptable floating property, water uptake and in vitro drug release.

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