Table 4. Concentrations of commonly occurring inactive ingredients in biologics.
| Excipient | Number of formulations containing the excipient | Percentage of formulations with listed concentration of the excipient | Number of formulations included in mass analysis | Minimum mass (mg) per 1 ml of volume | Maximum mass (mg) per 1 ml of volume | Average mass (mg) per 1 ml of volume |
|---|---|---|---|---|---|---|
| water | 93 | 0 | 0 | -- | -- | -- |
| sodium chloride | 88 | 52.3% (46) | 45 | 0.01 | 11.69 | 5.73 |
| polysorbate 80 | 66 | 57.6% (38) | 37 | 0.01 | 5.00a | 0.38a |
| sucrose | 56 | 60.7% (34) | 31 | 4.00 | 500.00 | 72.20 |
| mannitol | 48 | 70.8% (34) | 33 | 1.60 | 54.50 | 30.62 |
| sodium phosphate dibasic | 47 | 68.1% (32) | 31 | 0.20 | 13.45 | 2.25 |
| histidine | 40 | 62.5% (25) | 23 | 0.04 | 7.76 | 2.03 |
| sodium hydroxide | 37 | 0 | 0 | -- | -- | -- |
| polysorbate 20 | 36 | 66.7% (24) | 23 | 0.01 | 0.40 | 0.14 |
| sodium phosphate monobasic | 35 | 65.7% (23) | 21 | 0.22 | 12.70 | 2.12 |
| hydrochloric acid | 31 | 3.2% (1) | 0 | -- | -- | -- |
| sodium citrate | 28 | 50.0% (14) | 13 | 0.30 | 12.94 | 4.56 |
| glycine | 27 | 37.0% (10) | 10 | 0.11 | 22.50 | 12.46 |
| albumin (human) | 24 | 50.0% (12) | 12 | 1.00 | 50.00 | 11.61 |
| citric acid | 20 | 60.0% (12) | 11 | 0.06 | 5.25 | 1.13 |
| sodium acetate | 18 | 50.0% (9) | 9 | 0.10 | 6.80 | 1.94 |
| histidine monohydrochloride | 17 | 58.8% (10) | 10 | 0.48 | 4.28 | 1.76 |
| acetic acid | 15 | 40.0% (6) | 6 | 0.41 | 2.25 | 0.96 |
| metacresol | 15 | 93.3% (14) | 14 | 1.50 | 3.15 | 2.32 |
| sorbitol | 12 | 58.3% (7) | 7 | 20.00 | 50.00 | 42.71 |
| arginine hydrochloride | 11 | 54.5% (6) | 6 | 5.37 | 42.10 | 20.82 |
| phenol | 11 | 72.7% (8) | 8 | 0.65 | 5.50 | 2.87 |
| zinc | 11 | 90.9% (10) | 10 | 0.00 | 0.07 | 0.03 |
List of commonly occurring ingredients in biologics, how often the concentration of excipients are reported, and concentration range and average of each ingredient.
aReteplase drug label records the concentration of polysorbate 80 at 5 mg in 1 ml. The second highest concentration drops down to 1.04 mg in 1 ml significantly lowering the average from 0.38 mg/ml to 0.25 mg/ml.