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How does Aqueous Solubility affect the bioavailability of drugs
If the drug can be given as a salt the solubility will be increased leading to improved dissolution
How does dissolution rate affect the bioavailability of drugs
Faster dissolution rate = more bioavailable
How does partition coefficient affect the bioavailability of drugs
Drugs with high partition-coefficient value can easily permeate through biological membrane. (hydrophobic)
How does permeability affect the bioavailability of drugs
low permeability means low bioavailability
How does ionization constant affect the bioavailability of drugs
Ionized drugs are not absorbed as efficiently as un-ionized drugs are.
How does polymorphism affect the bioavailability of drugs
Different polymorphs may have different solubilities which affects bioavailability.
Shelf life: more soluble (less stable) forms may transform into the less soluble form
How does crystallinity affect the bioavailability of drugs
crystalline solids usually less soluble, and therefore less bioavailable than their amorphous counterparts.
How does particle size affect the bioavailability of drugs
Smaller particle size means more surface area means more dissolution meaning more bioavailable
How does particle morphology affect the bioavailability of drugs
Irregular particle shapes have more surface area therefore are more bioavailable
How does surface area affect the bioavailability of drugs
Higher surface area means higher dissolution rate meaning more bioavailable
How does hygroscopicity affect the bioavailability of drugs
(the tendency of a solid substance to absorb moisture from the surrounding atmosphere)
The high hygroscopicity causes issues such as alterations to their physicochemical properties, which in turn cause difficulties in subsequent downstream formulation processes, instability during their shelf life, and, eventually, adverse effects on their bioavailability
higher hygroscopicity = less bioavailable
why the oral route is the most popular route for drug administration?
Most convenient
Most cost effective
Great flexibility in dosage regimen
different parts of the GI tract?
Buccal, Esophagus, Stomach, Duodenum, Small Intestine, Large intestine,
barriers to oral drug delivery?
—> Drug needs to remain in solution & not precipitate
—> Resist pH of GI tract
—> Resist enzymatic degradation
—>Diffuse across mucous layer without binding to it
—>Must survive liver enzymes before systemic circulation
the difference between buccal and sublingual drug delivery?
Buccal is cheek, sublingual is under tongue
Buccal tablets are often harder designed to dissolve slowly
Buccal delivery advantages
—> Avoid first pass metabolism and GI elimination
—>Seems to work for patients
—> You can control the permeability
—> Alternative for orally inefficient drugs and noninvasive delivery of protein drugs
Buccal delivery disadvantages
—> Holding dose in mouth is inconvenient
—> if any is swallowed it’ll be treated as an oral dose and subject o first pass metabolism
—> Only accommodates small doses
the advantages and disadvantages of compressed tablets as an oral drug delivery system?
Accuracy in dosing
Blandness of taste
sugar coating
Enteric coating
film coating
Variable release rates
Chewable
Elegant
Efficient-Versatile-Practical
What is the difference between compressed and molded tablets and why are compressed tablets preferred over molded tablets?
What is the purpose of tablet coating?
—> Enhance permeability
—> Mask unpleasant taste
—> Increase stability
—>Increase mechanical integrity
—> Enhance appearance & elegance
—> Protect patient from stains
—>Modify drug release profile
—>Avoid side effects
—>Identity product
—>Avoid incompatibility of active drug substances by physical separation into the core and coat
CT
Compressed tablet
SCT
sugar coated tablet
FCT
film coated tablet
ECT
enteric coated tablet
MCT
multiple compressed tablet
layered
DT
dispensing tablet
(for compounding I think)
What are the two commonest tablet coatings and how are they different? (sugar and film)
What is an enteric tablet coating and why is some tablets coated by enteric coating?
Prevents release during exposure to the stomach to protect the drug or the stomach
Coat with pH sensitive polymers that do not dissolve under acidic conditions
Which properties of drugs can change the passive diffusion of drugs across intestinal membranes?
Size, pka