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Jihong Han's lectures > Suppositories > Flashcards

Suppositories Flashcards

1
Q

What are suppositories?

A

-They are solid dosage froms administered via the body cavities especially rectum and vagina

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2
Q

What are pessaries?

A

-Vaginal supossitories

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3
Q

What other dosage forms are used for rectal and vaginal routes?

A
  • Tablets
  • Capsules
  • Ointments
  • Solutions
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4
Q

Provide some ads for rectal route

A
  • When patients cannot use medicine orally
  • When drugs are not suitable for oral use
  • Can be used for systemic and local delivery
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5
Q

What are some disads for rectal route?

A
  • Poor patient acceptance in some countries
  • Sometimes absorption is slow and erratic
  • Some excipients may be irritant to the rectum
  • Leakage can be a problem
  • Stability can be an issue
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6
Q

What are some advantages for vaginal route?

A
  • Can be used for local and systemic delivery
  • Avoids harsh stomach environment
  • Avoids first pass metabolism of the liver
  • Vaginal wall is good for drug absorption
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7
Q

What are some disads for vaginal route?

A
  • It is gender specific
  • Leakage is unavoidable
  • Patient compliance
  • Menstrual cycle and hormonal variations affect absorption
  • Some excipients can cause irritation
  • Absorption can be affected by pH of the vaginal fluid
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8
Q

The wall of the rectum is smooth and there are no villi. TRUE OR FALSE?

A

TRUE

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9
Q

What is the pH of mucus in the rectum?

A

7.5

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10
Q

The lower and middle veins in the rectum drain directly into the systemic circulation, bypassing the liver portal vein. TRUE OR FALSE?

A

TRUE

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11
Q

The upper veins drains into the liver via the portal vein . TRUE OR FALSE?

A

TRUE

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12
Q

In which part of the GIshould the suppository be inserted?

A

Lower part

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13
Q

What factors affect drug absorption from rectum?

A
  • Area of rectal wall is smaller than small intestine
  • Quantities of fluid available in the rectum is small
  • Properties of the rectal fluid - mostly unknown
  • Pressure from rectal wall - helps in spreading and promotes absorption
  • No esterase or peptidase activity, hence better stability of peptide drugs
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14
Q

Describe the physiology of the vagina

A

-A tubular structure connecting the uterus to the external environment coated with vaginal fluid

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15
Q

What is the pH for vaginal fluid?

A

-Acidic 3.5 - 4.5

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16
Q

The vagina has a rich network of blood vessels leading to inferior vena cava, avoiding the liver portal system. TRUE OR FALSE?

A

TRUE

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17
Q

What factors affect drug absorption from the vagina?

A
  • Passive/transport
  • Age
  • The volume, pH and viscosity of vaginal fluid
  • Stage of menstrual cycle
  • Sexual activity
  • Ionisation of drug molecule
  • size of drug molecules
18
Q

Describe the manufacturing of suppositories?

A
  • Melt the base
  • Ad drug into the base and mix
  • Keep temperature as low as possible
  • Pour drug/base mixture into mould, overfill the mould to allow shrinkage on cooling
  • Cool at controlled rate to let mixture set
  • Scrap of the excess
  • Remove the suppositories
19
Q

How do you maintain quality control?

A
  • Dose uniformity
  • Weight uniformity
  • Mechanical strength
  • Content uniformity
  • Disintergration
  • Drug dissolution/release
20
Q

What are the requirements of the vehicles/bases?

A
  • Must melt after inserted into the body or dissolved in fluid cavity
  • Melting range should be just below 37 degrees
  • Melting range should be small enough for rapid setting when cooled during manufacturing
  • During solidification, the base should have enough volume contraction for ease of removal of the suppositories
  • The molten base shoudl have suitable viscosity
  • Allows satisfactory release
21
Q

What does the hydroxyl number relate to?

A

-The amount of mono and diglycerides in the base

22
Q

What does a high hydroxyl number mean?

A
  • the base is more polar and can absorb more water
  • the base tends to have wider melting range
  • the base may lead to formation of w/o emulsions which may retard drug release
23
Q

What does iodine number mean?

A

-It indicates how unsaturated the base is

24
Q

When the acid content is high, this is not good. TRUE OR FALSE?

A

-TRUE

25
Q

Give a few examples of lipid bases?

A
  • Semi-synthetic lipids

- Cocoa butter (theobroma oil)

26
Q

What is theobroma oil?

A

-A mixture of triglycerides

27
Q

Give examples of water miscible bases?

A
  • Glycerol gelatin base

- Polyethylene glycols of different molecular weights

28
Q

Describe Glycerol gelatin base ?

A
  • Water/glycerol/gelatin
  • Mostly used for vaginal route or for laxative purpose
  • Gelatin content may need to be increased for rectum route
29
Q

Describe Polyethylene glycols of different molecular weights ?

A
  • Melting point is well above body temp, so mixing with body fluid is the main mechanism of drug release
  • Irritant to the rectum due to water attraction from the mucous membrane
30
Q

How can irritation be reduced in the rectum (osmotic pressure) from Polyethylene glycols of different molecular weights?

A
  • By incorporating 20% water

- Moistening the suppository before insertion

31
Q

What are some of the considerations that need to taken during formulation of supoositories?

A
  • Drug stability in the base (determines if the product is of solution or suspension type/ emulsion type)
  • Drug stability and selection of base
  • Surface property (surfactants and wettability)
  • Particle size of drugs (smaller particles settle slower )
32
Q

What emulsion type is not recommended for suppositories?

A

W/O - the relase of drug may be very poor

33
Q

Surfactants help the drug disperse homogenously in the base and help the drug dissolve in the mucous. TRUE OR FALSE?

A

TRUE

34
Q

Smaller particles settle slower, so that in the manufacturing process the suppository does not remain homogenous before the base becomes solid. TRUE OR FALSE?

A

FALSE

35
Q

Small size particle, large SA, improves dissolution and absorption. TRUE OR FALSE?

A

TRUE

36
Q

Mould are made in different sizes, however, these are not the actual weigth of the mould, they refer to the weight of the suppositories produced using theobroma oil. TRUE OR FALSE?

A

TRUE

37
Q

The actual weight of suppositories depends on the the bae used. TRUE OR FALSE?

A

TRUE

38
Q

What is the calibration value?

A

Is the weight of a blank suppository (base only)

39
Q

What is the displacement value of a drug?

A

It is the number of parts by weight of drugs required to displace one part by weight of the base

40
Q

The volume for a given set of moulds is constant. TRUE OR FALSE?

A

TRUE

41
Q

The weight of the suppositories is not affected by the addition of drugs due to density differences. TRUE OR FALSE?

A

FALSE

Jihong Han's lectures (11 decks)

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