Micro-Formulation For Intravenous Injection
Source: Cirrus Pharmaceuticals, Inc.
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•Application Note: Micro-Formulation For Intravenous Injection
High-throughput in vitro screening of large numbers of molecules for their agonist or antagonist activity is an important mechanism of drug discovery. However, because receptor binding is only one factor impacting on the overall effectiveness of a drug in the body, early screening in an animal model, usually by IV injection, may be a necessary supplement to the in vitro evaluation. This can become a daunting task if an in vitro screening campaign identifies dozens of strong binders of which only very low milligram quantities are available to formulate for animal testing.
•Application Note: Micro-Formulation For Intravenous Injection
•Application Note: Micro-Formulation For Intravenous Injection
Objectives
- To formulate new chemical entities (NCEs) for IV injection using only 2 to 3 mg of the NCE.
- To develop standardized methods for rapidly carrying out "micro-formulation" of NCEs.
- To test the methods using a series of model compounds.
High-throughput in vitro screening of large numbers of molecules for their agonist or antagonist activity is an important mechanism of drug discovery. However, because receptor binding is only one factor impacting on the overall effectiveness of a drug in the body, early screening in an animal model, usually by IV injection, may be a necessary supplement to the in vitro evaluation. This can become a daunting task if an in vitro screening campaign identifies dozens of strong binders of which only very low milligram quantities are available to formulate for animal testing.
A typical formulation strategy is to first measure the solubility of the drug in various solvents and as a function of pH and then to identify one or more formulation approaches to pursue. The goal is to maximize drug solubility within the constraints of acceptable toxicity, pH, tonicity, and sterility. For drugs with poor water solubility, formulation approaches include high or low pH solutions, micellar dispersions, lipid emulsions, liposomes, and inclusion complexes.
Click Here To Download:•Application Note: Micro-Formulation For Intravenous Injection