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 was approached by Wyeth to overcome the inherent difficulties with Rapamune® Oral Solution.

Solution Applied
Elan’s 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 nanometer-sized particles. By reducing particle size, we increase the drug’s exposed surface area. We then stabilize 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            

Sales in $Millions

Rapamune® Sales Worldwide      

  Rapamune® is a registered trademark owned by Wyeth Pharmaceuticals