KinetiSol Enhanced Amorphous Compositions of Ritonavir

Summary
  • KinetiSol enables enhanced RTV amorphous compositions
    • Higher drug loading
    • Improved performance by enabling use of more efficient stabilizers
  • Equivalence to Norvir established at double the drug loading
  • KinetiSol RTV-AI more suitable for combination products
  • Enablement of alternative polymers potentially provides an IP/FTO advantage

ritonavir

Norvir®: Ritonavir Loading Limitation
  • Norvir amorphous intermediate (AI) composition tablet:
  • 15% Ritonavir
  • 74% Copovidone
  • 10% Span 20
  • 1% Fumed silica

ritonavir1

  • Low drug loading in Norvir AI
  • Large tablet size
  • Limited applicability for fixed-dose combination products

ritonavir2

ritonavir4

ritonavir5

KinetiSol Enhanced Ritonavir
ComponentPercent (w/w)
Ritonavir25 – 30
Hypromellose acetate succinate65 – 73
Surfactant2 – 5
  • Substantial increase in drug loading vs. Norvir
  • Acidic polymer carrier – more efficient RTV stabilizer/concentration enhancer
  • Uniquely enabled by KinetiSol
    • RTV is unstable to heat + acid
    • Could not be processed by melt-extrusion without extensive degradation
In-Vitro Performance, Non-sink

ritonavir6

  • KinetiSol RTV-AI targets drug supersaturation to the proximal intestine
  • Similar RTV concentration to Norvir in intestinal medium at double the drug loading
    • Enabled by the more efficient acidic polymeric carrier

CASE STUDIES

Read about exciting new breakthroughs

KinetiSol® has been the subject of numerous research articles published in top peer-reviewed journals in recent years. These papers demonstrate unique capabilities of the KinetiSol®process and its benefits for amorphous solid dispersion processing. Key advantages of the KinetiSol® process are illustrated in these case studies.

 

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