1 Flashcards
(52 cards)
Difference between three formulation and formulation
- Formulation is the process of developing a drug candidate into a drug product
- Preformulation is an investigation of physical and chemical properties of a new chemical entity (NCE) alone and when combined with excipients to identify suitability of the NCE to develop an efficacious dosage form.
- Preformulation is a stage that must be undertaken before the formulation can begin
- Starts once NCE shows sufficient pharmacological effect on animal models to forward to evaluation in man
What is the purpose of preformulation studies in drug discovery?
To choose a preferred compound based on formulation and manufacturing needs.
At what stage of drug discovery do preformulation studies begin?
After the hit-to-lead phase, when a compound has shown pharmacological effects.
Why are preformulation studies important for drug development?
They ensure the selected compound has suitable properties for formulation and large-scale production.
What are the key stages in early drug discovery?
→ Target Identification → Target Confirmation → Hit → Hit-to-Lead → Lead Optimization.
What happens at the hit-to-lead stage in drug discovery?
Compounds that show promising activity are further optimized for pharmacological effects.
What is the role of preformulation in pre-clinical studies?
To determine the best formulation for animal studies.
Why are preformulation studies important for volunteer studies?
To optimize the drug formulation for safe and effective human volunteer testing.
At what phase of clinical trials is the final formulation determined?
→ Phase III Clinical Trials, where the formulation is finalized for large-scale manufacture.
What is the last stage of drug development before commercial launch?
Scale-up for launch, ensuring the formulation is viable for mass production.
What is the objective of preformulation studies?
To generate information useful for developing a stable, bioavailable, and mass-producible dosage form.
Why is preformulation important in drug development?
It ensures the drug has suitable physical, chemical, and mechanical properties for formulation.
What are the key properties assessed during preformulation?
Solid-state properties, solubility, partition coefficient, dissolution, stability, rheology.
Why are solid-state properties important in preformulation?
They affect the drug’s crystal form, polymorphism, and stability, influencing its performance.
What are the two main categories of properties in preformulation?
Organoleptic properties and Bulk properties.
What are organoleptic properties, and why are they assessed?
→ Odour, colour, taste, state
- They impact patient acceptability and quality control.
What are bulk properties in preformulation?
Melting point, crystallinity & polymorphism, hygroscopicity, fine powder characterization, powder flow properties
What factors are analyzed in solubility analysis?
pH effects, pKa, solubilization profile, partition coefficient, dissolution.
Why is pKa important in preformulation?
It determines the ionization state of the drug, affecting its solubility and absorption.
What are the key factors in stability analysis?
Solution stability, solid-state stability, stability in toxicology, excipient compatibility.
Why is the melting point measured in solid drugs?
It provides information about purity, thermal properties, and polymorphism.
What technique is used to measure a drug’s crystal structure?
X-ray diffraction.
How does visual inspection help in preformulation?
It assesses the shape and uniformity of the drug’s crystals.
How are solid drugs classified?
Into Crystalline solids and Amorphous solids.
