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Regis Technologies

IAM Drugs Discovery Phase

IAM Fast-Screen Mini Columns

 
Packed with the Ester PC Ligand phase, IAM Fast-Screen Mini columns are a rapid and economically viable screening method for the high throughput estimation of drug permeability. Their benefits include excellent reproducibility, short analysis time and low cost. This can be of great use in characterizing large libraries of compounds.
 
The structure of the ester IAM.PC.C10/C3 packing, selected for the Fast-Screen Mini Column, is shown in Figure 1. This PC analog demonstrates superiority in retention times and stability - essential features for short columns and mass drug screening.
 
The IAM.PC Fast-Screen Mini Column, 1 cm in length by 3.0 mm in internal diameter, was specifically designed by Regis for rapid estimation of drug permeability in high-throughput screening programs. When connected to an HPLC system with an autosampler, a single column can be used in the analysis of hundreds of samples per day with highly reproducible results.
 
The 1 cm Fast-Screen Mini Column is offered not as a separation tool, but rather as a tool for characterizing the chromatographic retention factor (k') of individual analytes. The measured k' of analytes on this column can be used to estimate a value for drug permeability.
 
Column Advantages
Regis Technologies 1 cm Fast-Screen Mini Column for Drug Discovery provides:
  • Excellent correlation to traditional methods
  • Intestinal Tissue Correlation
  • Rapid indication of drug absorption
  • High sample throughput
  • Highly reproducible results
  • Durability
  • Cost effectiveness
  • Ability to establish absorption zones for high throughput screening
  • Products
Excellent Correlation to Traditional Methods
The traditional means of predicting permeability includes use of Caco-2 cell line cultures, intestinal tissue or liposome assays. These are laborious and costly to perform. Data obtained from the IAM Fast-Screen Mini Column correlate well to data obtained from taditional assays. This is summarized in Table 1.
 
Table 1. Comparing k'IAM data with other methods for estimating permeability
Method
Number of Compounds Evaluated
Correlation (r) with IAM Fast-Screen Mini Column
Partitioning into liposomes 23 0.831
Intestinal drug permeability 12 0.839
Caco-2 cell permeability 8 0.909
 
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Intestinal Tissue Correlation
Table 2 shows that drug permeability predicted by inverted Rat Intestines correlates well to drug retention factors, k'IAM measured on the IAM Fast-Screen Mini Columns. Note the short retention times.
 
Table 2. Correlating drug partitioning into IAM with rat intestinal drug absorption
Compound

% absorption of Inverted rat Intestine
IAM Fast-Screen Mini Column Retention Time (sec)
K'(corrected)

m-nitroaniline 77 133.1 15.29
n-nitroaniline 68 177.9 21.84
salicylic acid 60 93.8 9.54
p-toluidine 59 79.7 7.48
aniline 54 52.1 3.45
m-nitrobenzoic acid 53 68.1 5.79
phenol 51 94.6 9.66
benzoic acid 51 43.7 2.22
acetanilide 42 76.2 6.97
antipyrine 32 51.8 3.40
theophylline 29 39.3 1.58
acetylsalicyl acid 20 36.1 1.11
r (correlation factor) = 0.8385
r is calculated by plotting log k' vs. log % absorption of inverted rat intestine

Chromatographic Conditions:
  • Column: IAM Fast-Screen Mini Column 1 cm x 3.0 mm i.d.
  • Mobile Phase: Dulbecco's Phosphate Buffered Saline, pH 5.4
  • Flow Rate: 0.3 mL/min
  • Load: 10 µL
  • Detection: UV 254 nm, 0.1 AUFS
Caco-2 Cell Correlation
 
Chromatographic Conditions
Column: IAM Fast-Screen Mini Column
1 cm x 3.0 mm i.d.
Mobile Phase: 0.01 M DPBS Buffer, pH 5.4
Flow Rate: 0.5 mL/min
Load: 10 µl
Detection: UV 220 nm
Drugs Studied
1. Propranolol
2. Alprenolol
3. Warfarin
4. Metoprolol
5. Hydrocortisone
6. Terbutaline
7. Atenolol
8. (AVP) Arginine-Vasopressin
Figure 1. Drug permeability predicted by Caco-2 cells correlates well to k'IAM measured on the IAM Fast-Screen Mini Columns. 
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Rapid Indication of Drug Absorption
IAM Chromatography is a more rapid alternative to other methods. In a recent study completed by Regis k'IAMs of 12 compounds were compared with absorption data obtained in situ using rat intestines. Retention times for the compounds tested were between 20 and 180 seconds, while retention factors correlated well to the intestinal absorption data.
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High Sample Throughput
IAM Chromatography is of increasing importance in combinatorial chemistry, where it is used to provide an initial estimate of a drug candidates' membrane permeability. Hundreds of samples can be injected into a single Fast-Screen Mini Column using an automated HPLC system. Recently a group of 12 test analytes was evaluated in 10 runs over the course of eight hours. Total run time for the 12 test analytes was only 42 minutes.
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Highly Reproducible Results
The measured values for k'IAM show excellent reproducibility, both from run to run and from day to day (Figure 3).
 

Figure 3. Reproducibility of Results
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Durability
IAM Fast-Screen Mini Columns are extremely durable. Correlation factors, r, for the original k', and k' after 5000 column volumes were identical.
 
Cost Effectiveness
Because the IAM Fast-Screen Mini Column is inexpensive, has a very short analysis time, and provides drug permeability estimates for hundreds of drug candidates in a fraction of the time of conventional methods, the IAM Fast-Screen Mini Column becomes the economical alternative for high throughput screening.
 
Ability to Establish Permeability Zones for High Throughput Screening
Permeability zones can be determined for different analytes when performing large scale drug absorption screening. Thus, rapid IAM analyses can characterize a drug as having low, medium, or high membrane permeability (Figure 4). Regis Technologies manufactures the IAM Fast-Screen Mini Column on-site in its manufacturing facility. This column, as well as all of our other products, must adhere to rigorous manufacturing and quality control specifications before release.
 

Figure 4. Permeability Zone Determination
 
Product
Particle Size Column Dimensions Regis Product #
IAM Fast-Screen Mini Column Kit,2 columns, 1 cartridge holder, Care and use booklet
10 µm, 300Å

1 cm x 3.0 mm i.d

775014

IAM Fast-Screen Mini Columns, Pkg. of 12 columns, Care and use booklet
10 µm, 300Å 1 cm x 3.0 mm i.d 775016
IAM Fast-Screen Mini Columns, Pkg. of 6 columns, Care and use booklet
10 µm, 300Å 1 cm x 3.0 mm i.d 775015
 
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