Vaginal Route Flashcards

1
Q

Are vaginal routes less common than rectal routes?

A

YES

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2
Q

What effect can they have?

A

Local BUT systemic is possible

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3
Q

Are formulation designs similar to rectal?

A

YES

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4
Q

What is the drug absorption for systemic?

A

Passive diffusion into bloodstream

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5
Q

What physiological factors influence absorption?

A
Vol
Viscosity
pH
Stage of menstrual cycle
Age 
Sexual activity
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6
Q

What drug related factors influence absorption?

A
Drug solubility
Ionisation behaviour
Molecular weight
Release characteristics 
Dosage form
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7
Q

What are the advantages?

A
Smaller doses
Systemic possible
Suitable when oral restricted
Avoids GI tract + 1st-pass metabolism 
Self administration + removal 
Overcomes inconvenience + pain caused by parenterals route
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8
Q

Why can smaller doses be used?

A

Local action

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9
Q

Why is systemic absorption possible?

A

Large SA + highly vascularised

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10
Q

What are disadvantages?

A

Gender specific
Systemic treatment not popular
Menstruation cycle + hormones affect systemic
Vaginal fluid vol variations affect local
Acidic pH of vagina affect degradation of drug
Require use of special applicator

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11
Q

Describe ideal vaginal dosage forms

A
Long-acting
Easy to apply
No local irritation
Colourless, odourless + don't leak 
Not affect sexual activity 
Don't stain pants
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12
Q

What are the semi-solid formulations?

A

Creams, ointments + gels

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13
Q

Why is pH of semi-solid formulations modified?

A

To match vaginal pH

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14
Q

What do semi-solid formulations require?

A

Collapsible tubes, with suitable applicator

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15
Q

What is an issue with semi-solid formulations?

A

Delivery of accurate dose is hard

Applicators cost to produce

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16
Q

What is the size of semi-solid formulations?

A

Single dose containers in 3-5ml dose per application

17
Q

Describe vaginal tablets

A

Solid, single dose preparations similar to oral tablets

18
Q

What is the shape of vaginal tablets?

A

Ovoid

19
Q

What are advantages of vaginal tablets?

A

Ease of storage + use
Low cost
Well-controlled large-scale production
Rapidly disintegrate in small vol of vaginal fluid

20
Q

What may be added to vaginal tablets?

A

Disintegrants

Lactose as filler

21
Q

Why is lactose as a filler added to vaginal tablets?

A

Natural substrate for vaginal microflora that converts lactose to lactic acid

22
Q

Describe vaginal suppositories

A

Similar to rectal
Solid, single dose
API dissolved/dispersed in base
1g

23
Q

What base is used for vaginal suppositories?

A

Glycerol-gelatin base

24
Q

What must glycerol-gelatin base be dispersed in for vaginal suppositories?

A

H2O

25
Q

What do vaginal suppositories require?

A

Applicator + suitable training for insertion

26
Q

Describe vaginal rings

A

Solid formulation that provide controlled release of drug over time
Flexible, circular system containing drug in polymer network

27
Q

What is an example of a vaginal ring?

A

NuvaRing

28
Q

What is a vaginal ring used for?

A

Contraception

29
Q

Describe process of a vaginal ring

A

Insert
Leave in for 3 weeks
Replace after 7 day break

30
Q

What are the drug-release mechanisms?

A

Melting

Disintegration

31
Q

Describe what happens in melting

A

Melt at body temp

= release drug + molten mass disperses into available space

32
Q

Describe what happens in disintegration

SOLID dosage form

A

Release drugs by dissolution or disintegration, followed by dispersion contents in vaginal fluid

33
Q

Describe what happens in disintegration

SEMI-SOLID dosage form

A

Release drugs by diffusion + dispersion of contents from formulation to vaginal fluids

34
Q

How are vaginal + rectal suppositories manufactured?

A
Use moulding method
Base heated to above melting temp
Drug dispersed in heated liquid
Molten product poured into mould
Cooled
OR directly injected into final packaging (mould strips)