Preformulations Flashcards
The two major factors considered when selecting our NCE are..
efficacy vs biological target
A situation whereby the NCE with higher efficacy is not used is…
if the other compound has better physicochemical properties meaning it is easier to formulate
Drug development the right therapeutic area can result in…
significant income
Assay development allows us to determine…
molecular
intermolecular properties
The four stages of an assay development are…
identity (UV, IR)
purity (chromatography)
assay (spectroscopy, chromatography)
quality control - should be done throughout
With an assay development, the first formulation is usually an IV injection because…
bioavailability - dose and toxicity predominate in the early stages of preformulation
Assay is unique to…
each drug substance
For the first assay, minimal sample is used in an aqueous solution to..
allow for multiple parameters to be determines - aqueous bc you can determine a wider range of parameters
Solubility is dependent on the..
physical form of the drug
This NCE could be..
polymorph
pseudopolymorph
amorphous
The technique which allows us to determine the solubility of the NCE is..
UV
For this UV, we must have a..
chromophore - functional group with absorption within the UV range
Absorbance of chromophore is affected by…
additional functional groups which has unshared electrons (auxochromes)
UV is used because of its..
cost - cheap
popularity
familiarity
majority of drug entities contain at least one functional group which will absorb in the UV region
