PharmPK Discussion - Lipid based formulation: Discriminating Dissolution Media

• On 11 Dec 2012 at 09:59:10, Bhupesh Pratap (bpratap.at.astron-research.com) sent the message
  

  
  Dear All
  
  We are in process of developing a lipid based formulation using
  phospholipon 90G (Drug characteristic: pH dependent solubility almost
  insoluble in highly acidic and highly basic pH, Bioavailability 20%) and
  we need to test the same in a bioequivalence study against reference
  product which does not contain any lipid in the formulation.
  
  We are able to discriminate our formulation using lipolysis media but
  comparison can not be done with reference as it does not contain lipid.
  Does anyone come across any dissolution method (reflecting Fasting and
  Fed condition)  where a lipid formulation can be compared with one which
  does not contain lipid?
  
  Thanks in advance
  
  Regards
  Bhupesh
  
  

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• On 12 Dec 2012 at 05:24:39, Vaibhav Sihorkar (vaibhav_s.at.aurigene.com) sent the message
  

  
  The following message was posted to: PharmPK
  
  Dear Bhupesh,
  
  The lipid-based formulations primarily (except if it is class III, i.e.,
  surfactant >70-80%) digest (lipid digestion pathway) before getting
  absorbed, whereas non-lipid formulations do not undergo the same path.
  Of course, the active might undergo the same, but the lipid milieu might
  influence this. In wake of this, its' really difficult to generate a
  discriminating media towards in vitro dissolution to discriminate both,
  the reference non-lipid-based and your lipid-based formulation. This
  needs to be done on a case by case basis, by understanding the active,
  the intended objective and the end purpose.
  
  Even if you discriminate using any bio-relevant media like, FaSSIF or
  FeSSIF, it could be of documentary significance only as the processes
  might be different to the disposition of a lipid versus non-lipid based
  formulations in git.
  
  Hope this helps.
  
  Vaibhav Sihorkar
  Head, Pharmaceutical Development
  Aurigene Discovery Technologies Ltd.,
  Bollaram Road, Miyapur,
  Hyderabad - 500049. A.P., India
  
  

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• On 13 Dec 2012 at 09:11:01, Ashok kumar Meena (ashok_meena.-a-.jubilantbiosys.com) sent the message
  

  
  The following message was posted to: PharmPK
  
  Hello Vaibhavand & Bhupesh,
  Nice clarification just I would like to add in continuation lipid base
  formulation pathway towards in into GIT, start emulsification itself in
  to stomach due to presence of high concentration of surfactant in SMEDDS
  type of formulations in case of non surfactant based formulation the
  emulsification start with bile salts in small intestine. The emulsion
  globules size may be in nano or micron size range. Fine emulsion
  globules moved to small intestine part and get started to lipids
  digestions with lipase enzyme at the same time the absorption of drug in
  form of micelle of lipids and surfactant start absorption by GALT(gut
  associated lymphoid tissues) . The drug directly reaches into lymphatic
  system than it reaches to systemic circulation. This will help to avoid
  the first pass metabolism of into liver and will get high plasma
  concentration and AUC.
  
  Regards
  Ashok Meena
  --
  Ashok Kumar Meena
  Pharmaceutical Development, Jubilant Biosys Limited, #96, Industrial
  Suburb, 2nd Stage, Yeshwanthpur
  Bangalore-560022
  
  

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