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  • FORMULATION AND EVALUATION OF SUSTAINED RELEASED PELLETS OF TRAMADOL HCl

    ABOUT AUTHORS:
    *S. Patel, M. Patel
    Department of Pharma. Technology,
    L.J.Institute of Pharmacy, Ahmedabad, Gujarat, India
    shivanipatel090390@gmail.com

    ABSTRACT:
    The present research concerns the formulation and evaluation of sustained release pellets filled capsule of opioid analgesic, Tramadol HCl. Developmentof sustained release dosage form is to maintain therapeutic blood levels of the drug for extended period of time. Sustained release formulation provides uniform concentration at absorption site, maintains plasma concentration within a therapeutic range, reduces the dosage frequency and minimizes the side effects (nausea) associated with drug by avoiding dose dumping effect. Oral sustained release pellet formulations of Tramadol HCl were prepared using extrusion-spheronization technique. Pellets provide specific advantages of smoother plasma concentration profile and gradual absorption than tablet. Various polymers like Hydroxy propyl methyl cellulose (HPMC K100M), Carbopol, Xanthan gum, Ethyl cellulose and Eudragit RSPO were used to screen the best polymer combination through preliminary formulations. HPMC K100M and EC were screened and their concentrations were optimized using 32 full factorial design to achieve the aim of sustaining the drug release for 12 hours. Eudragit RSPO was used to coat the pellets. The prepared pellets were studied for different flow properties and drug release studies.

  • 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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