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Biopharmaceutics > Rectal and Vaginal Drug Delivery > Flashcards

Rectal and Vaginal Drug Delivery Flashcards

1
Q

When a child is having a seizure, then giving medication via _____ would be beneficial

A

a suppository

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2
Q

Suppositories are the most beneficial for which populations?

A

children and the geriatric populations (population that cannot swallow)

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3
Q

Dosage forms that quickly melt under ______

A

body temperature

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4
Q

What are the main characteristics of suppository formulations?

A
  • appropriate for circumstances were GI admin or absorption is problematic
  • suitable for drug candidates that are susceptible under GI conditions
  • beneficial for drug application in children, the elderly and special populations
  • tradition limited the use of these supps
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5
Q

What are the local effects that suppositories can have?

A
  • pain control
  • infection
  • inflammation
  • constipation
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6
Q

What are the systemic effects that suppositories can have?

A
  • asthma
  • fever control
  • rheumatic arthritis
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7
Q

What are the drug factors that influence the absorption of suppositories?

A
  • solubility
  • pKa
  • partition coefficient (need a good partition coefficient rather than a high one- need to have a good balance)
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8
Q

What is the proper placement of a suppository in the rectum? What happens when it is pushed too high up?

A
  • need to give drug absorption in the lower to middle veins in the rectum - this will give the best absorption
  • if you push the suppository up- then the veins will take the drug to the liver first and then will decrease the bioavailability of the drug
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9
Q

Does rectal drug absorption give 100% bioavailability?

A

no

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10
Q

What is the effect of the pH of the rectum?

A
  • pH is 7.5 - has little buffer capacity
  • there is a weak acid/base with non-ionized molecules have higher absorption
  • drug solution decides the final pH
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11
Q

What is the effect of the 3 mL of solution in the rectum?

A
  • drug dissolution is important to the absorption rate and extent
  • passive diffusion is the main absorption mechanism
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12
Q

What are the main parameters that much be met to ensure absorption tom a suppository?

A
  1. Partition coefficient: rate limiting form vehicle to the body
    - dependant on both drug and vehicle fluid
  2. pKa- rate limiting from body fluid into the blood- lipid soluble is more preferable
  3. Particle size - dictate solubility (increase SA)
    - 50-100 micrometer particles are preferable
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13
Q

What is the role of surfactants in a suppository?

A
  • promote wetting, partition and permeation
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14
Q

What is the ideal suppository base?

A
  • nontoxic/non-irritating, nonsensitizing tissues
  • compatibility with a wide variety of drugs
  • no metastable forms
  • wetting and emulsifying properties
  • high water number (another word for partition coefficient)
  • stability over storage
  • easy manufacturing process
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15
Q

What is the main advantage of using cocoa butter as a base?

A
  • non reactive, non toxic, versatile
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16
Q

What are the disadvantages of using cocoa butter?

A
  • polymorphism/softening point/cost
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17
Q

What are the principle vehicles for suppository preps?

A
  • semisynthetic fatty triglycerides
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18
Q

What are the main hydrophilic vehicles that can be used in suppositories?

A
  • glycerin/sodium stearate water
  • gelatin/glycerin/water
  • PEG 1000
  • higher melting point
  • slower drug dissolution
  • hygroscopic
  • drug instability
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19
Q

What kind of vehicles are generally used for vaginal suppositories?

A
  • hydrophilic vehicles
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20
Q

Do hydrophilic or hydrophobic vehicles have the shower onset of action?

A
  • hydrophilic vehicles are- it requires water to come into the vehicle first to dissolve the medication
  • these are all hygroscopic- this is because the drug has to pull water from the environment
21
Q

What are the 4 ways of moulds for preparing suppositories?

A
  • hand moulding
  • compression moulding
  • pour moulding
  • automatic moulding
22
Q

What properties need to go under quality control in testing the suppositories?

A
  • appearance
  • weight
  • disintegration
  • melting behaviour
  • softening time
  • mechanical strength
  • drug content
  • drug release
23
Q

Use of ____ as a solvent is generally avoided in rectal suppositories

A

water

24
Q

Why is water generally avoided in rectal supps?

A
  • acceleration of vehicle oxidation
  • precipitation of dissolved substances
  • instability in the presence of water
  • potential growth of bacteria and fungus
  • little impact on drug absorption
25
Q

What are the properties of enemas?

A
  • easy drug absorption

- application inconvenience

26
Q

What are the properties of soft capsules that are liquid filled?

A
  • satisfactory drug absorption

- limited use

27
Q

What are the properties of effervescent tablets? How do they work?

A
  • large amount of liquid required
  • limited use
  • can release gas and CO2
  • this stimulates peristalsis and helps with constipation
28
Q

What is the use of a repHresh vaginal gel?

A
  • used as a lubricant

glycerin can be used as a base

29
Q

What is the purpose of EDTA?

A
  • it is a metal chelating agent- stops the oxidation of the drug in the product
30
Q

What is sorbitol used as?

A
  • used as a humectant and promotes water absorption
31
Q

What are the 4 layers of the vagina?

A
  1. epithelium
  2. lamina propria
  3. blood vessels
  4. muscularis

– the drug has to get through all 4 layers of the body

32
Q

What is the cervicovaginal fluid?

A
  • transudate from vaginal and cervical cells, cervical mucous, endometrial and oviductal fluid
33
Q

What are the changes that happen to the epithelial layer of the vagina?

A
  • there are changes of 200 to 300 micrometers during the menstrual cycle
34
Q

What is the job of the rugae?

A
  • distensibility, support, increased SA
35
Q

What is the purpose of the vaginal fluid? The volume?

A
  • provides enzymes, proteins, carbs, amino acids, alcohols, ketones
  • 0.5-10 mL/day
  • allows the pH to stay around 3.5-4.9
36
Q

What is the function of the cervical mucous?

A
  • can function as a barrier

- 90% water, electrolytes, glucose, amino acids, proteins, trace elements, glycerol

37
Q

What is the HIV viral vaginal entry mechanism?

A
  • the immune cells that are protecting the vaginal area can be attacked by the HIV viruses, grow within the immune cells, burst the cell and then cause the travelling of the virons throughout the body
38
Q

A high fluid production in the vagina can do what do a drug?

A
  • can wash out the drug from the environment
39
Q

What are the different factors that are affecting the siRNA delivery?

A
  • pH (3.8-4.5) - hydrolysis, increase during menstruation and presence of semen
  • vaginal fluid volume (1-11 mL/day)
  • nucleases (RNase)
  • entrapment in the mucosal layer
  • infections/microflora (bacterial vaginitis, decrease microflora during menstruation)
  • epithelium thickness (changes of 200 - 30 um during menstruation)
40
Q

What are the advantages of vaginal gels?

A
  • does not require a healthcare practitioner
  • portable
  • discreet
41
Q

What are the disadvantages of using vaginal gels?

A
  • messy
  • require to apply prior to sexual intercourse
  • require time to disperse
  • dose may not be accurate
  • short acting (depending on formulation)
42
Q

What are the advantages of vaginal films?

A
  • does not require a healthcare practitioner
  • not messy
  • discrete, portable
43
Q

What are the disadvantages of vaginal films?

A
  • require time to melt/disperse
  • require to apply prior to sexual intercourse
  • short acting (depending on formulation)
  • possibly limited use in high temperature climates
44
Q

What are the advantages of vaginal tablets?

A
  • do not require healthcare practitioners
  • not messy
  • portable
  • fairly discreet
45
Q

What are the disadvantages of vaginal tablets?

A
  • require time to melt/disperse
  • require to apply prior to sexual intercourse
  • short acting (depending on formulation)
  • possibly limited use in high temperature climates
46
Q

What is the main disadvantage of using an intravaginal ring?

A
  • sRNA cannot withstand extrusion temperatures
47
Q

What is the main advantage of using a vaginal foams

A
  • does not require a healthcare practitioner

- considered not messy when compared to gels

48
Q

What is the main disadvantage of using foams?

A
  • requires time to disperse
  • require to apply prior to sexual intercourse
  • short acting (depending on formulation)
49
Q

What is the ideal vaginal delivery system?

A
  • safe
  • non irritating
  • resist degradation by nucleases
  • resist inactivation due to low pH
  • resist entrapment in the mucosal layer
  • access appropriate cells targeted by virus
  • effective

Biopharmaceutics (6 decks)

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