Rapamune®

RapamuneŽ

Case Study 1 – Differentiation through enhanced patient acceptability – Rapamune ® Oral Tablet formulation. Improving Patient Compliance and Convenience with NanoCrystal® Technology


The Challenge
The original form of Wyeth’s novel immunosuppressant, Rapamune® (sirolimus) was: 

  • available as an oral solution
  • had to be stored in a refrigerator
  • had to be reconstituted using a syringe for dose accuracy
  • had to follow a complicated reconstitution procedure where the solution was mixed with water or orange juice prior to administration   




Elan Drug Technologies was approached by Wyeth to overcome the inherent difficulties with Rapamune® Oral Solution.
 
Solution Applied
Elan Drug Technologies’ unique solution was its NanoCrystal® technology.  The technology is a formulation and manufacturing approach for poorly water soluble drugs. Rapamune® is a poorly water soluble compound.
NanoCrystal® technology involves reducing the drug to nanometre-sized particles. By reducing particle size, we increase the drug’s exposed surface area. We then stabilise the particles to maintain the formulation’s particle size.  The result - drug is easier to dissolve and absorb. 
 
Benefit to Patient
By applying our NanoCrystal® solubility enhancing technology, we …..

  • improved dissolution and oral bioavailability
  • enabled preparation of a tablet
  • eliminated complicated reconstitution and storage procedure associated with original form
  • enhanced patient convenience and acceptability
  • provided Patient Choice         

  
“Rapamune® has been available as a once daily liquid but the availability of a tablet formulation has the potential for greater patient convenience” says Professor Peter Friend, Director of the Oxford Transplant Centre.  “Simplifying drug regimens is known to improve compliance”.


Benefit to Wyeth

  • a tablet formulation was available, which has, since launch, dominated product sales (over 96% of product sales)
  • product launch took place in July 2001 and is now launched in US and major markets worldwide          

 

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