Table 1.
Select lipoic acid (LA) studies in healthy volunteers.
| Reference | LA dose administered to human subjects | AUC of LA in plasma …† | Cmax of LA in plasma … | Subjects |
|---|---|---|---|---|
| Teichert et al. [17] | a) 200 mg racemic LA, oral tablet b) 600 mg racemic LA, oral tablets c) 200 mg racemic LA, intravenous |
a) 46.82 ±21.46 μg*min/ml b) 157.83 ±35.82 μg*min/ml c) 157.97 ±35.05 μg*min/ml |
a) 0.66 ±0.33 μg/ml b) 2.85 ±1.49 μg/ml c) 8.32 ±2.35 μg/ml |
12 (crossover) |
| Carlson et al. [18] | 600 mg Na-R-LA, oral solution | 441.6 ±160.2 μg*min/ml | 16.0 ±6.32 μg/ml | 12 |
| Breithaupt-Grogler et al. [19] |
600 mg racemic LA, oral tablet | R-LA: 2348.04 h*ng/ml S-LA: 1243.24 h*ng/ml |
R-LA: 1812.32 ng/ml S-LA: 978.20 ng/ml |
15 |
| Mignini et al. [20] | a) 600 mg Thioctacid, oral tablet b) 600 mg Tioctil N, oral tablet |
a) 3510.9 ±1088.6 ng*h/ml b) 3563.5 ±1374.1 ng*h/ml |
a) 1338.6 ±751.8 ng/ml b) 1215.8 ±560.5 ng/ml |
16 (crossover) |
| Bernkop-Schnurch et al. [21] |
766.8 mg LA bound to chitosan, once by oral sustained release tablets |
0-12h: 183.8 ±101.4 μg*min/ml 0-6h: 108.1 ±61.5 μg*min/ml 6-12h: 75.7 ±94.8 μg*min/ml |
0-12h: n/a 0-6h: 1354.5 ±807.1 ng/ml 6-12h: 497.5 ±1074 ng/ml |
8 |
| Amenta et al. [22] | a) 600 mg Thioctacid, oral tablet b) 600 mg Tiocronal, oral tablet c) 600 mg Biodynoral, oral tablet d) 600 mg Tiobec retard, oral tablet |
a) 3270.9 ±372.8 ng*h/g b) 2925.2 ±448.4 ng*h/g c) 3142.3 ±331.5 ng*h/g d) 3187.4 ±152.8 ng*h/g |
a) 1266.2 ±237.7 ng/g b) 2290.5 ±286.6 ng/g c) 2262.8 ±392.8 ng/g d) 1397.7 ±070.4 ng/g |
8 (crossover) |
| ‡ Teichert et al. [23] | 600 mg racemic LA, oral dose, q.d. for 4 days | Day 1: 891.0 nmol*min/ml Day 4: 995.5 nmol*min/ml |
Day 1: 19.8 nmol/ml Day 4: 21.1 nmol/ml |
8 |
| Teichert et al. [24] | 600 mg racemic LA, oral dose, q.d. for 4 days | Day 1: 923.5 ±216.91 nmol*min/ml Day 4: 998.91 ±145.8 nmol*min/ml |
Day 1: 36.19 ±10.35 nmol/ml Day 4: 31.45 ±8.2 nmol/ml |
9 |
…
Values are reported in the original units.
†
Areas under the curve (AUCs) are from last time measured, except the study [21] using sustained release LA tablets.
‡
This study also included patients with kidney disease, not reported here.