formulation and preformulation Flashcards
the difference between preclinical studies and clinical studies
Objective: Assess safety, efficacy, and potential toxicities.
Participants: Laboratory experiments or animal models; not human subjects.
Setting: Conducted in laboratory settings.
Duration: Precede clinical studies; may take several years.
Regulatory Approval: Data submitted for regulatory approval to initiate clinical trials.
Data Collection: Focus on pharmacokinetics, pharmacodynamics, and toxicity in non-human systems.
Scale: Initial studies often smaller in scale.
Purpose: Provide evidence for potential safety and efficacy before human exposure
while in clinical studies;
Objective: Evaluate safety, efficacy, and tolerability in humans.
Participants: Human subjects categorized into phases (Phase 1 to Phase 4).
Setting: Conducted in clinical settings (hospitals, clinics).
Duration: Can extend over several years; involves different phases.
Regulatory Approval: Required at each phase before progressing; needed for market approval.
Data Collection: Focus on safety, efficacy, dosage, and adverse effects in human populations.
Scale: Involves larger populations, especially in later phases.
Purpose: Determine drug’s safety profile, effectiveness, optimal dosage, and potential side effects in humans.
what do the following abbreviations stand for;
EMA
MAA
IMPD
European Medicines Agency
Marketing Authorisation applications
Investigational Medicinal Product Dossier
the phases of clinical trials, what occurs during these phases, and the approximate number of people involved in them
phase 1: Assess the safety, tolerability, and pharmacokinetics of the drug in a small group of healthy volunteers. 20 to 100
phase 2 : Efficacy and Side Effects. 100 to 500
phase 3 : Confirm the drug’s effectiveness, monitor side effects, and compare it to standard treatments or a placebo in a larger and more diverse population.
several hundreds to thousands
phase 4 : Post-Marketing Surveillance or Pharmacovigilance
drug discovery and design for public use takes approximately how many years and costs approximately how much
15 years
$1 billion dollars
why are new drugs needed
New diseases
Low efficacy of existing drugs
Side effects of existing drugs
Cost of therapy
Sustain industrial activity
why do we need to formulate APIs during drug design
for stability
ease of administration
patient acceptability (taste, colour, elegance)
Formulating a drug and excipients into an appropriate dosage form allows manipulation of dosing frequency
the main steps of formulation science
preformulation studies(Characterisation of API (solubility, melting point, density…).)
formulation development: (Choosing the quantitative formula and its process of manufacture)
scale up and process validation: ( scale up and process validation)
the main objective of preformulation studies
to generate information useful to the formulator scientist in developing the most appropriate, stable and bioavailable dosage form that can be mass-produced
the 4 main areas of focus in preformulation
physiochemical properties
bulk characterisation
stabiloty studies
solubility studies
organoleptic properties
involves the assessment of flavour,odour, appearance and mouthfeel of a food product
what does each of the 4 main areas of preformulation entail
Physicochemical properties: Organoleptic properties Particle size and shape
Purity
Surface area
Bulk characterisation: Crystallinity and polymorphism
Hygroscopicity
Bulk density
Powder flow properties
Solubility studies:
Aqueous solubility/Solubilisation
pH solubility profile /pKa
Log P
Dissolution
Stability studies:
Solid state stability
Solution stability
Bulk stability
Compatibility
hygroscopicity
The tendency of a solid to take up water from the atmosphere, as it is subjected to a controlled RH programme
