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Table 1 PK parameters of Sandostatin® LAR®, and formulations A, B and C

From: Pharmacokinetic and technical comparison of Sandostatin® LAR® and other formulations of long-acting octreotide

PK parameters Sandostatin® LAR® Formulation A Formulation B Formulation C
Number of rabbits 7 4 3 3
Actual dose, mg/kg (± SD) 3.34 ± 0.236 3.42 ± 0.410 3.00 ± 1.84 1.27 ± 0.426
Burst phase, days 0-2     
   tmax-burst, hours, median 2 1.0 0.5 0.02
   Cmax-burst, ng/mL, mean (± SD) 3.49 ± 4.21 167 ± 31.1 22.8 ± 18.0 20.5 ± 6.64
Erosion phase, days 2-62*     
   tmax-erosion, days, median 20 14 and 34 20.0 12
   Cmax-erosion, ng/mL, mean (± SD) 9.97 ± 4.21 3.89 ± 1.73, and 2.42 ± 2.11 4.83 ± 3.91 13.3 ± 3.52
AUC0-last, d·ng/mL (± SD)* 179 ± 62.0 163 ± 33.7 86.1 ± 73.2 247 ± 33.4
AUC0-2d, d·ng/mL (± SD) 4.42 ± 5.70 65.3 ± 4.57 2.61 ± 0.680 2.39 ± 0.592
Burst, % (± SD) 2.19 ± 1.97 41.0 ± 6.32 22.2 ± 35.0 1
  1. *The AUC0-last was measured over 52 days (AUC0-52d) for Sandostatin LAR, over 62 days (AUC0-62d) for formulations A and B, and over 82 days (AUC0-82d) for formulation C.
  2. Cmax-burst of formulation A is significantly different to that of Sandostatin LAR.
  3. AUC, area under the plasma concentration-time curve; Cmax, maximum plasma concentration; SD, standard deviation; tmax, time to Cmax.