Apidra (insulin glulisine) - Sanofi Canada

Table 7. Pharmacokinetic and Pharmacodynamic Results for s.c Apidra ® and Huminsulin ®
Normal 100
APIDRA
(N=18) 2
Huminsulin Normal 100 1
(N=24) 3
Dose 0.3 U/kg
Pharmacokinetic Parameters
0.3 IU/kg
AUC0-end
(µU.min.mL-1)
25076 ± 3209 17417 ± 2348
Cmax
(µU.mL-1)
142 ± 25 56 ± 16
MRT (min) 136 ± 28 229 ± 41
Tmax
72
120
Min (*)
50 – 112
60 - 240
T10%- AUC
39
58
Min (*)
28 – 64
45 - 81
T90%- AUC
242
448
Min (*)
169 – 345
321-590
T 1/2 (min) 56 ± 17 64 ± 28 4
Volume of Distribution
(mL/kg)
930 ± 216 2375 ± 963
Glucose Infusion Rate – Pharmacodynamic Parameter
GIR-AUC (0-end)
(mg/kg)
1476 ± 300 3032 ± 743
Values represent mean and standard deviation, unless denoted with (*) to indicate the
median, minimum & maximum range.
1
Historical data and different radioimmunoassay from Apidra study
2
Type 1 Diabetes patients
3
Healthy adult subjects.
4 N=23
Absorption and bioavailibility: Pharmacokinetic profiles in healthy volunteers and diabetes
patients (Type 1 or 2) demonstrated that absorption of insulin glulisine was up to twice as fast
with a peak concentration approximately up to twice as high compared to regular human insulin.
In a study in patients with type 1 diabetes (n=20) after subcutaneous administration of 0.15 U/kg,
the median time to maximum concentration (Tmax) was 55 minutes (range 34 to 91 minutes) and
the peak concentration (Cmax) was 82 µU/mL (range 42 to 134 µU/mL) for insulin glulisine
compared to a median Tmax of 82 minutes (range 52 to 308 minutes) and a Cmax of 46 µIU/mL
(range 32 to 70µIU/mL) for regular human insulin. The mean residence time of insulin glulisine
was shorter (median: 98 minutes, range 55 to 149 minutes) than for regular human insulin
(median: 161 minutes, range 133 to 193 minutes) (see Figure 2).
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