Pharmaceutical cyclosporin formulation with improved biopharmaceutical properties, improved physical quality and greater stability, and method for producing said formulation

US6551619B1 · kind B1 · utility

Assignee

• Pharmatec International S.R.L. · IT

Inventors

• Lawrence John Penkler · Gqeberha, ZA
• Rainer Muller · Penzberg, DE
• Stephan Anton Runge · Eckernförde, DE
• Vittorino Ravelli · Milano, IT

Key dates

• Filing date: Jan 22, 2001
• Grant date: Apr 22, 2003
• Expiry date: Jan 22, 2021

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y10S977/906
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to solid, particulate lipid-based excipients which are loaded with cyclosporine. Said excipients have improved biopharmaceutical properties for cyclosporines in vivo, are of a better quality (in terms of fineness, homogeneity of the particles, inclusion of the medicament) and are more physically stable in the particulate formulation (no aggregation or gel formation). The invention also relates to a therapeutic treatment with cyclosporine formulations which produce an average blood level concentration in the steady state range of 300 ng/ml to over 1000 ng/ml, preferably over 800 ng/ml, especially up to 900 ng/ml, preferably 400 ng/ml to 800 ng/ml in the absence of high initial blood level concentrations essentially over 1500 ng/ml, especially over 1200 ng/ml. This blood level concentration is preferably maintained for an extended period of at least 5 hours, preferably at least 7 hours.