Within-Day Consistency in Cyclosporine Pharmacokinetics from a Microemulsion Formulation in Renal Transplant Patients

Relative bioavailability of a new oral form of cyclosporin A in patients with rheumatoid arthritis.

“…The results of the present study are in accordance with the results of the single dose study with NEO in healthy volunteers and the steady state study in renal transplant patients by Kovarik et al [8,10].…”

“…A new oral formulation NEO = Sandimmune Neorale) incorporates the drug in a microemulsion preconcentrate containing a surfactant, lipophilic and hydrophilic solvents and ethanol within a hard gelatine capsule [10]. Available doses are 25 mg and 100 mg.…”

“…Furthermore, Muller et al [9] showed in a single dose crossover study in healthy males that the influence of a fat-rich meal on the absorption of CsA from NEO was less pronounced when compared with SGC. Under steady state conditions in renal transplant patients, Kovarik et al [10] showed that CsA was 30% more bioavailable from NEO compared with SGC, independent of food intake.…”

Immunosuppressive Therapy After Cardiac Transplantation

“…After passing the portal blood stream only 30% of the original CsA suspension will be in the systemic blood stream. The first commercially available oral formulation was very variable on absorption and blood concentration and it was tried to overcome this effect [34]. At the beginning of the 1990ies a new Cyclosporine microemulsion (Sandimmun Neoral, Novartis, Basel, Switzerland) was developed, resulting in a higher bioavailability and reducing the individual deviation attributed to ingestion.…”

Optimal Pharmacokinetics of Cyclosporine and Tacrolimus Based Relationship Among AUC, Trough and Peak Concentration

“…In studies monitoring the blood concentration of CYA and TAC for 24 h and comparing the pharmacokinetics of morning and evening, some studies reported that there was no difference in pharmacokinetics between morning and evening 41,42) , whereas several other studies reported that there was a difference [43][44][45] . In the authors' data, the AUC 0-12 , AUC 0-4 , C 2 , and C max following evening administration were significant lower than those following morning administration both in patients treated with CYA and patients treated with TAC 46,47) (Figure 11).…”