Study Set Content:
Rate, primary and secondary sites, and mechanism of the drug’s metabolism in the body
Drug Metabolism
Biochemical transformation into readily-eliminated polar compounds
Drug Metabolism
ADME studies
Drug Metabolism
Adverse or undesired effects of drugs
Toxicology
Toxicity Studies:
Acute or short-term toxicity studies • Subacute or subchronic studies • Carcinogenicity studies • Reproduction studies • Genotoxicity or mutagenicity studie
• Drug solubility
Preformulation Studies
Partition coefficient
Preformulation Studies
Necessary for absorption/transport
Drug Solubility
Dissolution rate
Preformulation Studies
Physical form
Preformulation Studies
Can be increased by modifying the structure, form, complexation, or particle size reduction
Drug Solubility
• Stability
Preformulation Studies
If less than about (blank), may exhibit either incomplete or erratic absorption and produce a minimal response
10 mg/mL
The drug must pass the biological membrane of protein/lipid, which acts as a lipophilic barrier to many drugs.
Partition Coefficient
Speed/rate at which a substance dissolve
Dissolution Rate
• Preference of drug for lipid:water
Partition Coefficient
Indicative of ability to penetrate biologic multiphase systems.
Partition Coefficient
Indicates a drug’s absorption potential
Dissolution Rate
Crystalline versus amorphous
Physical Form
• Both physical and chemical properties
Stability
