Pharmaceutical ciclosporin formulation with improved biopharmaceutical properties, increased physical quality and stability as well as processes for its manufacture

摘要

The invention relates to solid, particulate lipid-based excipients which are loaded with cyclosporin. Said excipients have improved biopharmaceutical properties for cyclosporins in vivo, are of a better quality (in terms of fineness, homogeneity of the particles, inclusion of the medicament) and are more physical stable in the particulate formulation (no aggregation or gel formation). The invention also relates to a therapeutic treatment with cyclosporin 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.