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

BMC Research Notes

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

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
t_max-burst, hours, median	2	1.0	0.5	0.02
C_max-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*
t_max-erosion, days, median	20	14 and 34	20.0	12
C_max-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
AUC_0-last, d·ng/mL (± SD)*	179 ± 62.0	163 ± 33.7	86.1 ± 73.2	247 ± 33.4
AUC_0-2d, 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

*The AUC_0-last was measured over 52 days (AUC_0-52d) for Sandostatin LAR, over 62 days (AUC_0-62d) for formulations A and B, and over 82 days (AUC_0-82d) for formulation C.
^†C_max-burst of formulation A is significantly different to that of Sandostatin LAR.
AUC, area under the plasma concentration-time curve; C_max, maximum plasma concentration; SD, standard deviation; t_max, time to C_max.

ISSN: 1756-0500