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What is a drug product?
- A finished dosage form
- Formulated to present as a dosage form
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What is a drug product a mixture of?
- Acitve drug
- Excipients
- Organoleptic
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What are some example of drug products?
- ORal: Syrups Elixirs Soltions Tablets Capsules
- External: Ointments Pastes Creams
- Parentals: IV, IM, IT, ID, SC, infusions,
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T/F The design and formulation of drug products require a thorough understanding of the biopharmaceutic principles of drug delivery
T
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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
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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
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What does the drug product design depend on?
Therapeutic objective
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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
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Ka the absorption constant is rate limited by what?
Ka is dissolution rate limited
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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
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Disintegration
- For a drug release from the solid dosage formulation the drug product must disintegrate into smaller particles
- A pharmaceutical factor affecting drug bioavailability
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Dissolution
defined as the rate or time that a drug takes to dissolve in the fluids at the site of absorption
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What is the rate limiting step in absorption?
DISSOLUTION!!!!!!
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WHat is the role of excipients?
Added to the formulation to provide certain functional properties to the drug and dosage form
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Do excipient affect the the kinetic of the drug?
Yes it can alter medium
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What should an ideal excipient be?
Should be phyacodynamically inert
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What can the excipient of magnesium sterate do?
It can repeal water and reduce dissolution rate
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What adverse effect of shellac happens when it ages?
It can crosslink upon aging and decrease the dissolution rate
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What happens to the percent dissolve drug when the percent of magnesium stearate is increased?
The percent dissolved will decrease
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What happens to the plasma drug level with an increased level of magnesium stearate?
The drug plasma levels will decrease
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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
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What does in vitro testing provide?
It provides the ability to evaluate the drug product and the ability to redesign it
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T/F A pharmaceutical equivalent product may not be bioequivalent
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When absorption increases in vivo, what happens to dissolution in vitro?
Absorption in vivo increases so does dissolution in vitro
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What happens when solubility in vitro increases what happens to Cmax in vivo?
Solubility increases in vitro = Cmax in vivo increases
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What affect the Cmax vs solubility correlation?
- Proper/Poor formulation
- Perfusion/Diffusion limited
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What is the correlation between In vitro solubility and in vivo plasma concentration?
When in vitro solubiltiy increases, in vivo plasma concentration increases
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What factors affect the correlation between in vitro solubility and in vivo plasma concentration?
- Dissolution rate
- Formulation drug product design
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What are pharmacodynamic consideration?
- Desired therapeutic response
- Toxic and adverse effects
- Acute illness need rapid delivery
- Chronic ilness - sustained / extended delivery
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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
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What are some pharmacodynamic factors with consideration to the patient
- Side effects
- Allergic reaction
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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
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What is the order of the saftest dosage forms?
Oral liquids >Suspension > Emulsion > Powders > Capsules > Tablets
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What affects pH of the compartment (stomach/digestion?
- GI motility
- Presence of food
- Gastro-intestinal emptying time
- Hepatic first past effect
- Irritation
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What type of dosage form diffuses and pentrates mucosal membranes?
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Where does buccal dosage form get absorbed?
Cheek pouch
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Why would buccal dosage form be well absorbed?
Buccal pouch offers a large surface area for absorption and is well perfused
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T/F buccal dosage form can offer rapid deliery or delay release
T
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What dosage form circumvents hepatic first pass effect?
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What is an advantage of nasal dosage form?
The nsaal mucosa is highly perfused and is ready accessible
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What dosage form administerated into the respiratory system?
Inhalation dosage form
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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
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What dosage form is 100% bioavailable?
INTRAVENOUS
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What dosage form offers sustained drug delivery?
INTRAmuscular
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What time of soluble drug can be readily absorbed in the colon?
Aqueous
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What are the physiochemical properties?
- pka
- pH profile
- POlymorphism
- hydroscopcity
- partition coefficient
- excipient interaction
particle size
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