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What is a drug product?
- A finished dosage form
- Formulated to present as a dosage form
What is a drug product a mixture of?
- Acitve drug
What are some example of drug products?
- ORal: Syrups Elixirs Soltions Tablets Capsules
- External: Ointments Pastes Creams
- Parentals: IV, IM, IT, ID, SC, infusions,
T/F The design and formulation of drug products require a thorough understanding of the biopharmaceutic principles of drug delivery
What are the biopharmaceutic properties of the drug molecules that allow for the design and development of drug properties?
- The physiochemical properties of the drug
- the Route of administration, including the anatomic and physiologic nature of the application
- EX: Oral, topical, injectable, implant, transdermal patch
- The desired pharmacodynamic effect
- EX: rapid/immediate prolonged sustained extended activity
- The toxicologic properties
- The nature and safety of the excipients
- The expected role/effect of excipients and dosage form on drug delivery
How does the drug product design modulate the bioavailability of the active drug substance?
- Rapid and complete absorption
- Slow sustained rate of absorption
- Virtually no absorption
What does the drug product design depend on?
What are important in determining the distribution, onset, intensitty and duration of drug action?
The rate of drug release from the product and extent of drug absorption
Ka the absorption constant is rate limited by what?
Ka is dissolution rate limited
What are the pharmaceutical factors affecting drug bioavailability?
- The type of drug product
- The nature of excipients in the drug product
- The physiochemical properties of the drug molecule
- The route drug administration
- For a drug release from the solid dosage formulation the drug product must disintegrate into smaller particles
- A pharmaceutical factor affecting drug bioavailability
defined as the rate or time that a drug takes to dissolve in the fluids at the site of absorption
What is the rate limiting step in absorption?
WHat is the role of excipients?
Added to the formulation to provide certain functional properties to the drug and dosage form
Do excipient affect the the kinetic of the drug?
Yes it can alter medium
What should an ideal excipient be?
Should be phyacodynamically inert
What can the excipient of magnesium sterate do?
It can repeal water and reduce dissolution rate
What adverse effect of shellac happens when it ages?
It can crosslink upon aging and decrease the dissolution rate
What happens to the percent dissolve drug when the percent of magnesium stearate is increased?
The percent dissolved will decrease
What happens to the plasma drug level with an increased level of magnesium stearate?
The drug plasma levels will decrease
What is the correlation between in vivo and in vitro that should be considered?
Want to predict the in vivo performance from it in vitro characterisics
What does in vitro testing provide?
It provides the ability to evaluate the drug product and the ability to redesign it
T/F A pharmaceutical equivalent product may not be bioequivalent
When absorption increases in vivo, what happens to dissolution in vitro?
Absorption in vivo increases so does dissolution in vitro
What happens when solubility in vitro increases what happens to Cmax in vivo?
Solubility increases in vitro = Cmax in vivo increases
What affect the Cmax vs solubility correlation?
- Proper/Poor formulation
- Perfusion/Diffusion limited
What is the correlation between In vitro solubility and in vivo plasma concentration?
When in vitro solubiltiy increases, in vivo plasma concentration increases
What factors affect the correlation between in vitro solubility and in vivo plasma concentration?
- Dissolution rate
- Formulation drug product design
What are pharmacodynamic consideration?
- Desired therapeutic response
- Toxic and adverse effects
- Acute illness need rapid delivery
- Chronic ilness - sustained / extended delivery
What are the drug product considerations from his slides?
- Pharmacokinetic of the drug
- Bioavailability of the drug
- Dose and potency considerations
- Frequency of administration / application
What are some pharmacodynamic factors with consideration to the patient
- Side effects
- Allergic reaction
When selecting dosage for design, what should you considered?
- Route of administration
- Size of the dosage
- The anatomic and physiologic characterisics of the administration site such as membrane permeability and blood flow
- The physiochemical properties like pH osmotic pressure and presence of physiologic fluids
- the site of administration
What is the order of the saftest dosage forms?
Oral liquids >Suspension > Emulsion > Powders > Capsules > Tablets
What affects pH of the compartment (stomach/digestion?
- GI motility
- Presence of food
- Gastro-intestinal emptying time
- Hepatic first past effect
What type of dosage form diffuses and pentrates mucosal membranes?
Where does buccal dosage form get absorbed?
Why would buccal dosage form be well absorbed?
Buccal pouch offers a large surface area for absorption and is well perfused
T/F buccal dosage form can offer rapid deliery or delay release
What dosage form circumvents hepatic first pass effect?
What is an advantage of nasal dosage form?
The nsaal mucosa is highly perfused and is ready accessible
What dosage form administerated into the respiratory system?
Inhalation dosage form
What are the advantages of drugs given by inhalation dosage form?
- Rapid absorption and rapid onset of activity
- Avoidance of first pass effects or metabolism prior to systemic absorption
- Localized drug action at the lungs and minimize systemic toxicity
What dosage form is 100% bioavailable?
What dosage form offers sustained drug delivery?
What time of soluble drug can be readily absorbed in the colon?
What are the physiochemical properties?
- pH profile
- partition coefficient
- excipient interaction