additives. The additives are used for stabilizing the formulation or
for therapeutic reasons. The additives are specified according to the
type of proteins (see Note 5).
Table 5
(continued)
Name
Formulation
Protective
efficacy
Experimental conditions
LDH
2 μg/mL LDH, 50 mM sodium
phosphate buffer (pH 7.4) + 400 mM
mannitol + 200 mM sucrose + 10 mg/
mL CHAPS + 10 mg/mL
HP-β-CD + 10 mg/mL sodium
cholate + 10 mg/mL
PEG3000 + 10 mg/mL PEG20000
Activity
retention:
9%
14%
30%
76%
73%
60%
30%
38%
Freeze-drying
PFK
2 mg/mL PFK, 20 mM potassium
phosphate buffer (pH 8.0) + 1%
PEG + 10 mM mannitol + 10 mM
lactose + 10 mM trehalose + 1% PEG
+10 mM mannitol + 1% PEG + 10 mM
lactose + 1% PEG + 10 mM trehalose
Activity
retention:
0%
20%
5%
5%
0%
30%
103%
100%
Freeze-drying
GDH
50 mg/mL GDH, 20 mM potassium
phosphate buffer (pH 7.5) + 500 mM
KCl + 500 mM trehalose + 500 mM
mannosylglycerate
Activity
retention:
65%
32%
86%
95%
Freeze-drying
hGH
Lyophilized formulation 2 mg/mL
hGH + mannitol at 31:1 molar
ratio + trehalose at 31:1 molar
ratio + cellobiose at 31:1 molar ratio
Rate constant:
4.5 per day
0.004 per day
0.002 per day
0.0003 per
day
Storage at temperature of
50
C
Insulin
Lyophilized formulation 1 mg/mL
insulin (pH 4) + 5 mg/mL trehalose
Degradation:
0.04 mg/mL
(18% dimers)
0.02 mg/mL
(1% dimers)
Storage at temperature of
35
C for 7 days
Freeze-Drying of Proteins
691