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Pharmaceutics 2 Winter Final > 6 - Vaginal > Flashcards

6 - Vaginal Flashcards

1
Q

What are advantages to the vagina as a dosage route?

A
  • Large surface area
  • Dense vascularization
  • Avoids first-pass metabolism
  • Relatively high permeability to many drugs
  • Opportunity for delivery systems that can continuously release drug for prolonged time periods
  • Self-administration
  • Systemic exposure reduced and potential systemic SE avoided
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2
Q

Is the vagina used more often for local or systemic products?

A

Local

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3
Q

What is the shape, length, and width of the vagina?

A
  • S-shaped
  • 2 cm wide
  • 6-10 cm long
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4
Q

What is the mucosa of the vagina similar to?

A

Buccal mucosa

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5
Q

Is there fluid in the vagina?

A

Yes, a thin film of vaginal fluid

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6
Q

What is the pH of the vagina? How is this maintained?

A
  • For women of reproductive age, pH = 3.5-4.5
  • Maintained by lactobacilli producing lactic acid
  • For women younger or older than reproductive age, pH is neutral to slightly basic
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7
Q

What can affect the pH of the vagina?

A

Infection

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8
Q

What is the surface area of the vagina?

A

50-60 cm^2

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9
Q

Vagina allows easy and rapid absorption of ______ drugs

A

Lipophilic

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10
Q

What determines absorption in the vagina? How can this be improved?

A
  • Contact time w/ vagina

- Improved by adding bioadhesives gel or device like a vaginal ring

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11
Q

How do different types of drug get absorbed by the vagina?

A
  • Lipophilic drugs cross by passive diffusion

- Hydrophilic and ionized substances of low MW are absorbed by paracellular route

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12
Q

What is the volume of fluid in the vagina? What does this mean for systemic absorption?

A
  • 2-3 mL

- Dissolution may be a rate-limiting step for systemic absorption for drugs w/ poor water solubility

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13
Q

What can help if a drug has a poor dissolution rate in the vagina?

A

Formulate as a solution or gel instead of a suppository or tablet

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14
Q

Where do blood vessels of vagina drain? What does this mean for first-pass metabolism?

A
  • Drain into inferior vena cava

- First-pass metabolism is avoided

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15
Q

Does vaginal fluid contain enzymes? What effect does this have?

A
  • Yes

- Can deactivate some drugs before absorption can occur

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16
Q

What are some disadvantages to the vagina as a dosage route?

A
  • pH of vaginal fluid and thickness of epithelium vary w/ a px age, menstruation and presence of infection –> may affect drug permeability and result in variable drug absorption; products for local use may be absorbed & cause systemic SE
  • Some formulations may leak or slip out
  • Irritation from drug or delivery system can occur
  • Some px reluctance
17
Q

What is the most common dose form for the vagina?

A

Suppository or tablet

18
Q

What drugs are used in intra-vaginal rings?

A
  • Contraceptives
  • Hormones
  • Anti-HIV medications
19
Q

What is another name for a vaginal suppository?

A

Pessary

20
Q

What is the purpose of a base for a vaginal suppository? What are the common bases used?

A
  • Dissolve in vaginal fluid and release drug

- Polyethylene glycol or glycero-gelatin

21
Q

What is the typical weight of a vaginal suppository?

A

3-5 g

22
Q

What do vaginal tablets often contain?

A

Bioadhesive polymers which help tablet adhere to vaginal mucosa

23
Q

What is the purpose of a polymeric matrix in a vaginal tablet?

A

Absorbs water from vaginal fluid and swells to release drug

24
Q

What are the common drugs found in vaginal gels/ointments/creams?

A
  • Spermicides
  • Antimicrobials
  • Hormones
25
Q

What are disadvantages to vaginal gels/ointments/cream?

A
  • Tendency to leak out of vagina

- Repeated application often required b/c product washed away by vaginal fluids

26
Q

What are vaginal rings composed of?

A

Ethylene vinyl acetate copolymers or polymers of silicone

27
Q

How are vaginal rings often formulated? How is release rate controlled?

A
  • As a reservoir type, where drug is in center lumen of ring and released through polymer membrane by passive diffusion
  • Release rate controlled by changing thickness of polymeric membrane

Pharmaceutics 2 Winter Final (9 decks)

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