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Pharm 125 > Rectal and Vaginal DF > Flashcards

Rectal and Vaginal DF Flashcards

1
Q

What are suppositories?

A
  • used inside rectum
  • melt, soften, or dissolve at body temperature
  • semi solid or solid dosage forms intended to be inserted into body orifices

Vaginal - inserts or pessaries
Urethra - inserts or bougies

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2
Q

What are the advantages?

A
  • People who cannot swallow
  • Treats lower parts of GI tract diseases
  • GI tract irritant drugs
  • Once daily use
  • Local and systemic effect
  • Avoids first pass metabolism if administered correctly
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3
Q

What are the disadvantages?

A
  • Poor compliance
  • Variation of absorption
  • Discomfort and leakage
  • Irritation of mucous membranes
  • Upward movement of suppository from local site can increase first pass metabolism
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4
Q

What is the shape of rectal suppositories? Weight? Local action? Systemic action? How much does the drug content vary?

A
  • Bullet and Torpedo shape
  • 1 g (child), 2g (adult), 4-5 g (rectal rocket)
  • Local action: Hemorrhoids, Infection, Itching
  • Systemic action: Antinauseants, analgesics, hormones
  • Content varies from 0.1 to 30-40%
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5
Q

Shape of vaginal inserts? Weight? Bases? Uses?

A
  • Globular, oval or cone shaped
  • 3 to 5 g
  • Bases are water soluble or water miscible (polyethylene glycol or glycerinated gelatin)

Uses:
Contraceptives (Nonoxynol-9, spermacide)
Vaginal hygiene (antiseptics)
Gyno ailments (vaginal infections, hormone deficiency)

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6
Q

Shape of urethral inserts? Size? Weight? Uses?

A
  • Cylindrical
  • 3-6 mm in diameter, 50 mm in length for females, 125 mm for males
  • 2 g (females), 4 g (males)

Uses:

  • Erectile dysfunction
  • Local anesthetic for urethral examination
  • Antibacterial
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7
Q

What are the active ingredient examples?

A

Local action

Antifungal: Clotrimazole
Astringent: Bismuth Subgallate
Anti-inflammation: Hydrocortisone
Hemorrhoids: Zinc sulfate
Anesthetics and antiseptics

Systemic action

Antiemetic: Prochlorperazine, Dimenhydrinate
Analgesic: Diclofenac, Acetaminophen, Aspirin, Morphine

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8
Q

What are the additives?

A 
Preservatives: Parabens
Antioxidants: Butylated Hydroxytoluene 
Plasticizers: Propylene glycol, Cetyl alcohol
Solubilizing agents: Surfactants
Absorption enhancers: Surfactants 
Viscosity enhancers: Silicon dioxide
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9
Q

What should ideal suppository bases look like?

A
  • Melt at body temp or dissolve in rectal fluids
  • Stable if heated above mp
  • Non toxic or non irritant to membrane
  • Release drug easily
  • Stable on storage
  • Non-absorbable
  • Be compatible with drugs
  • Keep its shape when handled
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10
Q

What are the fatty/oleaginous/hydrophobic bases?

A
  1. Cocoa butter

2. Synthetic/semi synthetic fatty bases (Witepsol, Fattibase)

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11
Q

What are the hydrophilic/water soluble/ water miscible bases?

A
  1. Glycerinated gelatin

2. Polyethylene glycols (PEG)

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12
Q

What is cocoa butter?

A
  • Yellowish white solid with a chocolate like odour
  • Mixture of triglyceryl esters of palmitic, oleic, stearic and other fatty acids
  • Softens at 30 and melts at 34-35 (B form)
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13
Q

What are the advantages of cocoa butter?

A
  • Melts readily on warming, sets rapidly on cooling
  • Compatible with many ingredients
  • Non irritating
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14
Q

What are the disadvantages of cocoa butter?

A
  • Polymorphism when heated above its MP
  • Adherance to mold
  • Should be refrigerated
  • Slow deterioration during storage
  • Poor water absorbing capacity
  • Leakage from body
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15
Q

What are semi synthetic fatty bases?

A

hydrolyzing vegetable oil + hydrogenation + re-esterifying the acids with glycerol

Fattibase:

  • mixture of palm, palm kernel and coconut oil, self emulsifying glyceryl monostearate, polyoxyl stearate
  • mp: 35.5 to 37 degrees

Witepsol:

  • Triglycerides : Saturated fatty acids (C12 and C18 range)
  • Mp range of 33-35 degrees
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16
Q

What are the advantages and disadvantages?

A

Advantages:

  • Better contraction
  • No polymorphism
  • Rapid solidification
  • Tolerance to oxidation
  • Improved drug release and bioavailability (with surfactants)

Disadvantages

  • Some bases need to be stored in refrigerator
  • Becomes brittle if cooled too quickly (witepsol)
  • May have dehydrating effect
17
Q

What are glycerinated gelatin bases?

A
  • 10% water + 70% glycerin + 20% gelatin
  • Slowly dissolves in the secretions of the mucous lining of the rectum and vagina
  • Used frequently for vaginal suppositories
  • Better for antiseptics than fatty bases - dissolves slowly ~30 to 40 min
  • Used less often than fatty bases because of disadvantages
18
Q

What are the disadvantages of glycerinated gelatin base?

A
  • Have a physiological action (osmotic laxative effect)
  • Hygroscopic
  • Irritation and dehydration in mucosa
  • Difficult to prepare and handle
  • Dissolution depends on age of the base and quality of the gelatin
  • Not compatible with protein precipitants like acids and other agents

Type A gelatin = cationic antiseptic
Type B = anionic antiseptic

19
Q

What are polyethylene glycols or macrogols?

A
  • Mixtures of PEG of various molecular weights
  • Physical properties adjusted by varying weight
  • Gradually dissolve and disperse in fluids
  • Prolonged release of the drug (30 to 50 min to dissolve)
  • Polybase: Mixture of PEGs and polysorbate 80
20
Q

Advantages of PEGs?

A
  • Easier to prepare
  • Do not stick to the mold
  • Contract significantly on cooling
  • No cool storage required
  • Do not leak from the body
  • Absorb water well
  • Have good solvent properties
  • Reliable release of drugs
21
Q

Disadvantages of PEGs?

A
  • Hygroscopic: mucosa irritation
  • Should be moistened with water before insertion
  • Contracts significantly on cooling (forms pits and holes)
  • Incompatible with phenolic substances (tannic acid, aspirin, benzocaine, salicylic acid)
22
Q

What are the rectal cavity physiological factors?

A
  • Small mucus volume (1-3 mL)
  • Low buffer capacity (pH 6.8-7.4)
  • Presence of fecal matter
  • Small SA
23
Q

How is blood supplied to the rectal area?

A
  • Inferior rectal vein carries blood to the inferior venacava and bypasses liver
  • Superior rectal vein carries blood to the superior part of the rectal cavity to the liver
24
Q

What are the formulation and drug properties factors?

A

Melting or dissolution of base

  • Aqueous solubility and dissolution
  • Melting of base

Release and diffusion of drug

  • Solubility of drug in vehicle and rectal fluids
  • Drug particle size
  • Spreading capacity
  • Viscosity of base at rectal temp

Rectal mucosa

  • Pka of drug
  • Buffer capacity
  • Ph induced in rectal fluids
  • Partitition coefficient of drug
25
Q

Drug release from fatty bases?

A

Hydrophilic drugs - good release, good absoprtion

Lipophilic drugs - slow release, remains in base, little absorption (ionized drug or fatty acid base with surfactant)

26
Q

Drug release from hydrophilic bases?

A

lipophilic drugs: good to moderate release, absoption

hydrophilic drugs: moderate release, depends on dissolution of base and diffusion of drug

27
Q

What would you do to if you want to use a lipophilic drug in a lipophilic base?

A
  • Decrease PS
  • Use a surfactant to increase spreading capacity
  • Use a salt form of the drug
28
Q

What are the three methods to prepare suppositories?

A
  • Hand rolling
  • Compression molding
  • Fusion molding
29
Q

What is hand rolling?

A
  • doesn’t require special equipment
  • considerable skill
  • use cocoa butter for better manipulation
30
Q

What is compression molding? Advantages and disadvantages?

A
  • base and ingredients are combined by mixing into a paste like consistency
  • mixed mass is forced into molds

Advantages:

  • good for heat labile substances
  • good for drugs that are insoluble in base

Disadvantages:

  • requires special suppository machine
  • limited shapes
31
Q

How are the quality control tests done?

A
  • Visual examination (appearance, texture, colour)
  • Melting behaviour
  • Disintegration test
  • Release of drug
  • Weight uniformity
  • Uniformity of active ingredients
  • Mechanical strength

Pharm 125 (4 decks)

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