PharmPK Discussion - Pharmasolve in oral formulations

• On 25 Oct 2010 at 16:39:03, "Shone, Alison" (A.E.Shone.aaa.liverpool.ac.uk) sent the message
  

  
  Hi
   We are looking for a suitable dosing vehicle to try for our insoluble  compounds.  I have been looking to use NMP.  Can anyone tell me what are  the acceptable levels for use in both oral dosing and iv dosing?  From  what I can find out it looks like I can go up to about 25 % in water.   I've no experience with this as a vehicle, any help would be gratefully  received!
   Ally
  
  

  Back to the Top

• On 26 Oct 2010 at 04:54:13, Vaibhav Sihorkar (vaibhav_s.at.aurigene.com) sent the message
  

  
  The following message was posted to: PharmPK
  
  Dear Ally,
  
  I suggest you go to archives of PharmPK of yesteryears and you will find  threads where this has been discussed at length.
  
  I would rather go with a relatively safer approach before using NMP for  either IV or oral use. In brief, preferred is to make use of the  ionization constant of the compound by manipulating the pH with or  without a complexing agent, use of co-solvents and/or surfactant <40%  (make sure that the super-saturation does not lead to massive ppt, and  you do not exceed surfactants>10%), or (if the POC stages of  developments and if oral) micronization/ nanosizing in presence of  stabilizer(s) or an amorphonization of the compound. Generally used  co-solvents/surfactants could be PEG400, PG, Cremophor ELP, Solutol  HS15, Ethanol, or a combination of these. Make sure that your  formulation does not crash out after dilution with relevant bio-media,  and the osmolality is not too high to cause untoward reactions at the  site (if IV). Kindly note that most of these algorithms are not  platforms and are being worked out on a case by case basis.
  
  Still if you want to use NMP, DMA, DMSO or similar, better use it as low  (<5%) as possible and run a vehicle control prior to your main study.
  
  Hope this will help.
  
  regards
  
  Vaibhav Sihorkar, Ph.D.
  [Head, Pharmaceutical Development]
  Aurigene Discovery Technologies Limited
  Hyderabad, INDIA
  
  

  Back to the Top

Copyright 1995-2011 David W. A. Bourne (david@boomer.org)