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Journal of Excipients and Food Chemicals
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  This is an Open Access Journal Open Access journal
     ISSN (Print) 21502668
     Published by International Pharmaceutical Excipients Council Homepage  [1 journal]
  • In vitro / in vivo evaluation of procera gum-ethylcellulose microspheres
           for colonic delivery of budesonide

    • Authors: Lalduhsanga Pachuau, Bhaskar Mazumder
      Abstract: The objective of the present research was to develop colonic delivery system for budesonide based on polymer blends of natural polysaccharides from Albizia procera and GI insoluble polymer ethylcellulose. Emulsion solvent evaporation method was followed for preparation of the microspheres. In vitro drug release was studied on a medium simulating gastrointestinal fluid and mechanism of drug release was determined by Korsemeyer-Peppas equation. In vivo performance of the microsphere was evaluated on acetic acid induced colitis in rats. Drug release studies showed microspheres from procera gum-ethylcellulose coating was able to resist premature drug release in the upper GI tract and susceptible to enzyme effects in the colon. Treatment of rats with budesonide test formulation for five days also significantly attenuated the extent and severity of the cell damage and is a promising system for treatment of ulcerative colitis.
      PubDate: 2014-09-18
      Issue No: Vol. 5 (2014)
       
  • Regulation and excipient innovation

    • Authors: Shireesh Apte
      Abstract: None
      PubDate: 2014-09-18
      Issue No: Vol. 5 (2014)
       
  • Interaction and compatibility studies of efavirenz with pharmaceutical
           excipients

    • Authors: Cinira Fandaruff, Andrea Mariela Araya-Sibaja, Rafael Nicolay Pereira, Silvia Lucia Cuffini, Carlos Eduardo Maduro Campos, Cristiane Rodrigues Drago Hoffmeister, Helvécio Vinícius Antunes Rocha, Marco Antônio Segatto Silva
      Abstract: Although excipients have traditionally been thought of as being inert, experience has showed interaction between them and the drugs; therefore, is very useful the knowledge about potential physical and chemical interactions. The compatibility of efavirenz with the excipients: sodium lauryl sulfate, spray dried lactose, hydroxypropylcellulose, magnesium stearate, microcrystalline cellulose and croscarmellose sodium were studied. X-ray powder diffraction (XRPD), Fourier Transform Infrared Spectroscopy (FT-IR), Raman spectroscopy (RS) and Differential scanning calorimetry (DSC) were used as screening techniques. DSC curves of binary mixtures were quite different than efavirenz raw material, suggesting strong interaction and/ or even chemical reactions between efavirenz and excipients with temperature increasing. However, FT-IR, XRPD and RS showed that no interaction and/ or even chemical reaction between efavirenz and excipients occurred at room temperature. Efavirenz is one non-nucleoside reverse transcriptase inhibitor (NNRTI), used in the High Activity Antiretroviral Therapy (HAART) for the treatment of human immunodeficiency virus type 1 infection (HIV-1). This Active Pharmaceutical Ingredient (API) has more than one crystalline form, which may have implications for its behavior during production and also for its in vivo performance. XRPD, DSC, Scanning Electron Microscopy (SEM) and Intrinsic Dissolution Rate (IDR) were used in the solid-state characterization of efavirenz and was determined that the raw material used corresponds with Form I and maintains its crystal structure during the study. IDR indicated that bioavailability problems may arise because of drug-dependent dissolution.
      PubDate: 2014-09-18
      Issue No: Vol. 5 (2014)
       
 
 
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