PharmPK Discussion - Drugs with poor oral bioavailability due to solubility or poor permeability

• On 26 Jan 2011 at 09:46:26, Mohammad Shadid (shadid78.at.gmail.com) sent the message
  

  
  Hi All,
   I'm searching for some compounds to use for a potential publication  effort and I'm looking to tap into your years of experience.  We need a  set of drugs, almost drugs or failed drugs that had poor oral  bioavailability due to solubility or poor permeability.  We do not want  compounds that had clearance problems, unless if the clearance is due to  carboxylic acid glucuronidation. Moreover, suggestions for drugs that  are difficult to solubilize for IV injections are also welcomed.    Ideally these would be well known (for impact) but they must be charged  with either a single acid or basic group.  You can simply refer me to  names or publications.
    I would greatly appreciate any ideas,
   Thanks,
  Mohammad
  
  

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• On 26 Jan 2011 at 16:59:52, Sanjeev Thohan (sarxconsult.aaa.gmail.com) sent the message
  

  
  How about cyclosporin, omeprazole, hydrochlorothiazide,
  Here is an interesting reference for your perusal: Int J Health Res, June 2009; 2(2): 116
  European Journal of Pharmaceutics and Biopharmaceutics
  Volume 58, Issue 2, September 2004, Pages 265-278
  
   as well as this link
   http://www.2dix.com/pdf-2010/aqueous-solubility-enhancement-of-class-2-dru gs-pdf.php
  
  Top 200 Oral Products in US and GB (newer list than WHO)
  - Just over 50% (110) are oral immediate release products
  Class 1 - ~30%
  Class II - ~30%
  Class III - ~25%
  Class IV - ~7%
  (Unclassified - ~8%)
  
  

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• On 28 Jan 2011 at 15:43:10, "Saghir, Shakil (SA)" (SSaghir.-at-.dow.com) sent the message
  

  
  Dear Mohammad:
  
  I have worked on quite a few poorly absorbed drugs as part of enhanced  drug dissolution project, modifying drug crystals to enhance its  dissolution and oral absorption. I have published several of these work  which I can email to you if you like - two chapters and several posters  that cannot be obtained through references, send me an email.
  
  Naproxen, Nifedipine, Cyclosporine, Ketoconazole, Candesartan cilexetil,  Danazol, and few others.
  
  --
  Shakil A. Saghir, M.S.P.H., Ph.D., DABT
  Senior Toxicology Specialist
  Toxicology & Environmental Research & Consulting
  The Dow Chemical Company
  Midland, Michigan 48674
  
  

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