Absorption Characteristics of a Microemulsion Formulation of Cyclosporine in De Novo Pediatric Liver Transplant Recipients1,2

Assessment of converting from intravenous to oral administration of cyclosporin A in pediatric allogeneic hematopoietic stem cell transplant recipients

“…In other studies, the mean or median C max have been reported as 1200-1500 ng/ml. 20,37 In our study, the mean peak concentration of CsA (C max ) after oral administration was 1135.37340.6 ng/ml, not excessive C max levels. Therefore, according to this observation, our administration method for the transition period is effective and practical for routine clinical use.…”

“…These observed values were a little higher than those reported for pediatric renal transplant patients, 21.8% 22 and pediatric liver transplant patients, 37.6714.6%. 20 The reason for this difference, between kidney transplants and our study patients, may be due to age and small bowel length. Another study has reported that small bowel length is a significant factor for CsA absorption.…”

“…16,17 Some studies have evaluated the pharmacokinetic properties of CsA in children undergoing organ transplantation. [18][19][20][21][22][23][24][25][26][27] However, few published data are available for the pediatric HSCT population. 12,27 Despite the widespread use of CsA, the administration method, dosage schedule and optimal dose of CsA have not been well established, and a variety of treatment protocols have been accepted at numerous transplantation centers.…”

Improved cyclosporine bioavailability in black pediatric liver transplant recipients after administration of the microemulsion formulation

“…Developed to optimize cyclosporine absorption, NL has been shown to improve the bioavailability of cyclosporine, with a concomitant reduction in intrapatient variability. 16,17 We previously showed such improvements in the bioavailability of cyclosporine after NL administration in both de novo 21 and maintenance pediatric liver transplant recipients. 22 We also showed that the increased cyclosporine bioavailability obtained with NL was caused by increased absorption and not differences in cyclosporine metabolism.…”

“…19,20 In a double-blind, crossover study of de novo pediatric liver transplant recipients, we previously showed that the absolute bioavailability of cyclosporine was significantly greater (P ϭ .01) with the NL formulation than that obtained with the SIM formulation. 21 This is especially relevant from a clinical point of view, because pediatric patients are at an even greater risk for cyclosporine malabsorption in the first few months after transplantation. In addition, we have shown that maintenance pediatric liver transplant recipients who are at least 6 months posttransplantation also experience similar increases in bioavailability (P Ͻ .01) after conversion from the original to the microemulsion formulation of cyclosporine.…”