Click on image to enlarge
- Lead Select Intravenous: Discovery Kit Price: €849
- Availability: In stock.
Do You Want To Know The Absolute Bioavailability Of Your Compound?
Knowledge Is Power
Before rationally selecting your lead, you need to know how your early research compound performs after intravenous administration. This knowledge provides crucial information for determining:
- Absolute bioavailability - how much drug is available to the body after injection of the compound
- Critical pharmacokinetic data - vital to understanding your compound’s behaviour
- Fundamental efficacy data - essential to knowing your compound’s potency
- Relative bioavailability - the amount of an oral dose absorbed compared to an intravenous one
In order to achieve all of this, the dosing of your compound to animals must be fast, reliable and effective. If your lead has low water solubility, testing with the wrong intravenous vehicle can cause problems. It could result in the physical blockage of capillaries (emboli) or a misrepresentation of the pharmacokinetic performance because the compound precipitates in vivo.
The Perils Of Insolubility
Unlike with water soluble compounds, you can’t obtain optimal bioavailability of poorly water soluble compounds by simply applying an ordinary solution or suspension. Ignoring the issue of insolubility can be perilous. If a compound is poorly soluble, finding the right dosing vehicle is not easy. It’s a process complicated by many different factors:
- Limited amounts of the compound
- Multiple leads to evaluate in a short time frame
- Many vehicles cause anaphylaxis and are not suitable for intravenous administration
Ideally, you need a well tolerated vehicle that can dissolve and keep a poorly soluble compound in solution without precipitation after injection. A suitable vehicle should allow the compound to distribute in the body and get a true idea of how the compound is behaving when in solution.
Take Down The Crystal
If you could take insolubility out of the equation by destroying the crystal, you’d be able to:
- Make a back-to-back comparison of the key pharmacokinetic parameters of your lead candidates
- Understand how the compound behaves when administered in a truly dissolved state
- Make more informed decisions about the selection of your lead candidate by understanding its performance without the interference of crystallization
The end result is clear; you’d be empowered to pick the winners from the losers.
How LSIV Can Work For You
The Lead Select Intravenous: Discovery Kit is a standardized dosing vehicle for intravenous use. It’s been developed to give you a first but decisive impression of the bioavailability profile of your compounds in single dosing studies.
It works through simple visual inspection. One quick look will tell you if the dosing vehicle has been successful in dissolving your compound. It is extremely simple to use; each kit comes complete with everything you need to start testing immediately. Your drug-loaded vehicles can be obtained in as little as 30 minutes. The kit is:
- A sterile, visually-clear dosing vehicle
- Designed to solubilize a variety of poorly soluble compounds
- Suitable for use across many different species
Instant Solubilization
The LSIV: Discovery Kit uses the instant solubilization technology developed by the insolubility experts at Phares. The technology uses two vials:
Liquid A: The first vial contains the Transfer Medium (Enhancer in NMP) which is a sterile solvent mixture containing phospholipid. This media breaks up the structure of the compound and dissolves the poorly soluble compound.
Liquid B: The second vial contains the Lipid Dispersion. This sterile dispersion is made up of nano-sized lipid particles that keep poorly soluble drugs in solution. The particles are so small that the dispersion appears clear and transparent when held up to light.
Similar lipids are found naturally in the blood and safely keep poorly soluble compounds dissolved in the body without precipitation.
You Can See Clearly Now
When you’re starting to assess a lead candidate, insolubility can easily cloud your judgment. This kit will give you a clear window into the performance of your compound. For superior intravenous dosing of your compound, get an LSIV: Discovery Kit into your lab today.
To find out how simple it is to use an LSIV: Discovery Kit click here
*LSIV In Larger Volumes*
The LSIV: Discovery Kit is designed for ease of use so the performance of research compounds can be tested in vitro first and then explored rapidly pre-clinically after intravenous administration. To find out more about buying larger volumes of LSIV for Pre-Clinical use click here
Shopping Basket