IAM.PC.DD2
Predicting Drug Membrane Permeability
The IAM.PC.DD2 is used to predict drug membrane permeability. The ester bonding of the DD2 packing offers more hydrophobicity than the DD phase. This material is a diacylated or double chain ester PC ligand denoted as EsterIAM.PC.DD2, and is endcapped with C10/C3 alkyl chains, as illustrated in Figure 1.
Column Advantages
The IAM.PC.DD2 packing offers the following advantages:
- More Hydrophobic
The IAM.PC.DD2 offers more hydrophobicity, thus giving longer retentions to compounds not well retained on the IAM.PC.DD packing. Retentions are typically double on the IAM.PC.DD2 column than on the DD column and exhibit excellent correlation for groups of compounds. - Greater Stability
Another distinct advantage of the IAM.PC.DD2 packing is its ability to tolerate mobile phases between pH's 7.0 and 7.5, thus resulting in longer column life under these conditions. - Excellent Correlation to Traditional Methods
Intestinal Tissue Correlation
Table 1 shows that drug permeability predicted by inverted rat intestines correlates well to drug retention factors, k'IAM, measured on both the DD and DD2 columns.
Table 1. Correlating Drug Partitioning into IAM With Rat
Intestinal Drug Absorption |
| Sample | % Absorption of
Inverted Rat
Intestine | (k')
IAM.PC.DD | (k')
IAM.PC.DD2 |
| m-nitroaniline | 77 | 3.875 | 10.838 |
| p-nitroaniline | 68 | 8.576 | 16.086 |
| salicylic acid | 60 | 1.936 | 6.963 |
| p-toluidine | 59 | 1.554 | 4.546 |
| aniline | 54 | 0.811 | 2.069 |
| m-nitrobenzoic acid | 53 | 1.213 | 4.403 |
| phenol | 51 | 2.965 | 6.544 |
| benzoic acid | 51 | 0.531 | 2.088 |
| acetanilide | 42 | 1.797 | 5.096 |
| antipyrine | 32 | 0.685 | 3.350 |
| theophylline | 29 | 0.583 | 1.478 |
| acetylsalicylic acid | 20 | 0.197 | 0.931 |
| r (correlation factor) | | 0.8088 | 0.8025 |
r is calculated by plotting log k' vs. log % Absorption of Inverted Rat Intestine.
Note that both correlation factors, r, are virtually the same for the DD and DD2 columns.
Chromatographic Conditions
Column: IAM.PC.DD2, 10 cm x 4.6 mm i.d.
Mobile Phase: 0.01 M DPBS Buffer, pH 5.4
Flow Rate: 1.0 mL/min
Load: 10 µL
Detection: UV 220 nm
Drugs Studied
1. m-Nitroaniline, 2. p-Nitroaniline, 3. Salicylic Acid, 4. p-Toluidine, 5. Aniline, 6. m-Nitrobenzoic acid, 7. Phenol, and 8. Benzoic Acid, 9. Acetanilide, 10. Antipyrine, 11. Theophylline, 12. Acetylsalicylic acid.
Figure 2. Drug absorption in this intestinal tissue model correlates well with k'IAM measured on the IAM.PC.DD2 columns.
| Product | Particle Size | Column Dimensions | Regis
Product # | U.S. Price |
|
| IAM.PC.DD2 | 10 µm, 300Å | 10 cm x 4.6 mm i.d. | 774011 | $1,186.88 |  |
| IAM.PC.DD2 | 10 µm, 300Å | 15 cm x 4.6 mm i.d. | 774014 | $1,635.25 | |
| IAM.PC.DD2 | 10 µm, 300Å | 3 cm x 4.6 mm i.d. | 774010 | $669.93 | |
| IAM.PC.DD2 Guard Cartridges** | 10 µm, 300Å | 1 cm x 3.0 mm i.d. | 774013 | $337.60 | |
| IAM.PC.DD2 Guard Kit* | 10 µm, 300Å | 1 cm x 3.0 mm i.d. | 774012 | $400.90 | |