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PHARM 125 - Pharmaceutics > Excipient list > Flashcards

Excipient list Flashcards

1
Q

What types of bases are used in vaginal dosage forms?

A

Water soluble or water miscible
–> polyethylene glycol or glycerinated gelatin

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2
Q

What are the two types of action that an active ingredient could be used for in a suppository?

A

Local –> anti-fungal, astringent, anti-inflammation, hemorrhoids, anesthetics and antiseptics

Systemic –> antiemetic (N/V) and analgesic

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3
Q

What are the 3 drugs from Top 100 that can be used as an active analgesic ingredient in suppositiories?

A

Acetaminophen, aspirin, and morphine

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4
Q

What is an example of a preservative used in suppositories?

A

Parabens

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5
Q

What is an example of an antioxidant used in suppositories?

A

Butylated hydroxytoluene (BHT)

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6
Q

What are some examples of a plasticizer used in suppositories? (2)

A
  • cetyl alcohol
  • propylene glycol
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7
Q

What is the purpose of a plasticizer in suppositories?

A

reduces brittleness and increases flexibility

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8
Q

What are absorption enhancers used for in suppository formulation?

A

Surfactants to increase wetting and spreading, may increase permeability of the rectal membrane

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9
Q

What is an example of a viscosity enhancer used in suppositories?

A

Also called suspending agents; Silicon dioxide

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10
Q

What are some properties of an ideal suppository base?

A
  • melt at body temperature or dissolve and disperse in the rectal fluids
  • release drug readily/compatible with drugs
  • stable on storage and when heated above its melting point
  • non-absorbable
  • non-toxic and non-irritant to rectal mucosa
  • keeps shape when handled
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11
Q

What are the two classifications of suppository bases? Give two examples of each.

A
  1. Fatty/pleaginous/hydrophobic bases:
    - cocoa butter
    - synthetic/semi-synthetic
  2. Hydrophilic/water soluble/water miscible bases:
    - glycerinated gelatin
    - polyethylene glycols (PEG)
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12
Q

What are some of the physical characteristics of Cocoa butter or Theobroma oil?

A
  • yellowish-white solid with chocolate like odour
  • mixture of triglyceryl esters of palmitic, stearic, oleic and other fatty acids (mostly unsaturated)
  • softens at 30o and melts at 34-35o (B-form)
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13
Q

What are some of the advantages of cocoa butter/theobroma oil as a suppository base?

A
  • melts readily on warming
  • compatible with many ingredients
  • non-irritating
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14
Q

What are some of the disadvantages of cocoa butter as a suppository base?

A
  • polymorphism when heated above melting point
  • adherence to mold
  • should be refrigerated
  • slow deterioration during storage
  • poor water absorbing capacity
  • leakage from body
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15
Q

How are semi-synthetic fatty bases (or hydrogenated vegetable oil bases) made?

A

hydrolyzing vegtable oil and re-esterfying the acids with glycerol

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16
Q

What is Fattibase a mixture of?

A

Palm, palm kernel, coconut oil, self-emulsifying glyceryl monostearate and polyoxyl sterate

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17
Q

What is the melting point range of Fattibase?

A

35.5-37o

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18
Q

What is Witepsol a mixture of?

A

triglycerides of saturated fatty acids (C12-C18) range

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19
Q

What is the melting point range of Witepsol?

A

33-350

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20
Q

What category of suppository bases do Fattibase and Witepsol fall into?

A

Semi-synthetic fatty bases

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21
Q

What are some advantages of semi-synthetic fatty bases?

A
  • no polymorphism
  • tolerance to oxidation
  • rapid solidification
  • better contraction
  • improved drug release and bioavailability with presence of surfactants
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22
Q

What are some of the disadvantages of semi-sythetic fatty bases?

A
  • some bases need to be stored in the fridge
  • become brittle if cooled quickly (Witepsol)
  • may have dehydrating effect because of the surfactants
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23
Q

What is the composition of glycerinated gelatin bases?

A

10% water

70% glycerin

20% gelatin

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24
Q

What are glycerinated gelatin bases frequently used for and why?

A

Vaginal suppositories → they have a laxative effect which is not compatible with rectal dosage forms

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25
Q

What are some of the advantages of glycerinated gelatin bases?

A
  • slowly dissolves in mucous lining (makes it better for antiseptics than fatty bases because of slow dissolving ~30-40 minutes)
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26
Q

What are some of the disadvantages of glycerinated bases?

A
  • osmotic laxative effect
  • more difficult to prepare and handle
  • dissolution time depends on the age of the base, content and quality of the gelatin
  • hygroscopic → leads to irritation and dehydration of mucosa
  • incompatible with protein precipitants like acids
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27
Q

Why were two forms of gelatin developed and what is the difference between types A and B?

A

Developed to use with either cationic or anionic antiseptics

→ type A = cationic

→ type B - anionic

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28
Q

How can you adjust the physical properties of PEG bases?

A

Varying the mixture of high and low molecular weight polymers

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29
Q

What is Polybase a mixture of?

A

PEGs and polysorbate 80 (surfactant)

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30
Q

What are some of the advantages of PEG bases?

A
  • easier to prepare
  • contracts significantly and does not stick to mold → makes it easier to remove
  • no cool storage required
  • does not leak from the body
  • absorbs water well
  • good solvent properties
  • reliable, slow release of drug (30-50 minutes to dissolve)
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31
Q

What are some of the disadvantages of the PEG base?

A
  • hygroscopic → should be moistened with water before insertion
  • contract significantly on cooling → may form pits/holes
  • incompatible with phenolic substances
    • tannic acid
    • aspirin
    • benzocaine
    • salicylic acid
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32
Q

What is the difference between group 1 and 2 excipients for tablets?

A

Group 1 → processing and compression characteristics of the tablet (diluents, binders, glidants and lubricants)

Group 2 → gives physical characteristics to the finished tablet (disintegrants, surfactants, colours, flavours, sweetening agents, polymers)

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33
Q

What is the purpose of diluents in tablet formulation?

A

Added to increase the bulk to make the tablet a practical size for compression

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34
Q

What role does lactose play in the formulation of a tablet? Are there different types for direct compression and wet granulation?

A

Lactose = diluent

For direct compression use anhydrous and spray dried lactose

For wet granulation use monohydrate grades

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35
Q

What role does microcrystalline cellulose play in tablet formulation?

A

Microcrystalline cellulose = diluent OR binder

Used in direct compression; 100 um

Used in granulations; 50 um

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36
Q

What does dicalcium phosphate dihydrate do in tablet formulation?

A

Dicalcium phosphate dihydrate = diluent

→ excellent flow properties and brittle

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37
Q

What role does calcium carbonate/sodium carbonate play in tablet formulation?

A

Diluent

→ brittle material

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38
Q

What role does starch play in the formulation of a tablet?

A

Starch = Diluent OR disintegrant OR binder

39
Q

What role does dextrose, sucrose, mannitol or sorbitol play in the formulation of tablets?

A

Diluents OR filler and sweetener in effervescent or chewable tablets

40
Q

What does a binder do in the formulation of tablets?

A

Imparts cohesive qualities to powdered material and to the tablet formulation

Ensures tablet remains intact after compression

41
Q

What happens when you have too little or too much/too strong of the binder in tablet formulation?

A

Too much = inhibits disintegration

Too little = tablet falls apart

42
Q

What are the two types of binders?

A

Solution binder → added as the granulation fluid (more effective and most common)

Dry binder → added before wet granulation or mixed with other ingredients before compaction

43
Q

What are some examples of solution binders?

A
  • starch mucilage (most common - 10-20% in aqueous solution)
  • sucrose solution
  • polyvinylpyrrolidone
  • gelatin
  • cellulose derivatives
44
Q

What are some examples of dry binders?

A
  • microcrystalline cellulose
  • polyvinylpyrrolidone
  • pre-gelatinized starch (easier to prepare than starch mucilage)
45
Q

What does a lubricant do in tablet formulation?

A

Prevents adhesion of the tablet material to the surface of the dies and punches

Facilitates ejection of the tablets from the die cavity

46
Q

What are some examples of insoluble lubricants used in tablet formulation?

A
  • magnesium stearate (most common)
  • calcium stearate
  • stearic acid
  • light mineral oil
47
Q

What are some examples of soluble lubricants in tablet formulation?

A
  • sodium benzoate
  • PEG 4000 and 6000
  • sodium lauryl sulfate (also used as a surfactant to help dissolution rate)
48
Q

What are the most effective lubricants?

A

Hydrophobic lubricants

49
Q

At what point in the formulation would you add in a lubricant?

A

LAST → after all of the other components have been thoroughly mixed

50
Q

What does ‘bolting’ the lubricant mean?

A

Lubricant being finely divided by passing it through a 60-100 mesh onto the granulation

51
Q

Are lubricants inert?

A

NO → they effect both dissolution and absorption

smaller concentrations of stearate increase dissolution and absorption

52
Q

What does a glidant do in tablet formulation?

A

Improves flow characteristics of a powder mixture by reducing inter-particle friction

***you do not need a glidant if your powder has good flow

53
Q

At what point in the formulation would you add in a glidant?

A

Always added in the dry state, just prior to compression (during lubrication step)

54
Q

What are some examples of glidants in tablet formulation and what is the most common one?

A
  • colloidal silicon dioxide (most common)
  • talc
  • calcium silicate
  • magnesium carbonate
55
Q

What does a disintegrant do in tablet formulation?

A

Added to a tablet to facilitate it’s breakup or disintegration after administration

56
Q

What are the three major mechanisms of disintegrants in tablet formulation and what are some examples of each?

A
  1. Facilitated water uptake → facilitates transport of liquids into the pores of the tablet (starch, microcrystalline cellulose)
  2. Swelling on contact with water → also called super-disintegrants (sodium starch glycolate, croscarmellose sodium, crospovidone)
  3. Gas production in effervescent tablets → when in contact with water produces CO2 (citric acid, tartaric acid + sodium bicarbonate)
57
Q

What are the most commonly used colouring agents?

A

Iron oxide pigments (red, yellow, black) and indigo carmine (FD&C) Blue 2

58
Q

When should you add colour into the tablet formulation to get a more uniform colour?

A

during the coating step

59
Q

What is the role of wetting and solubilizing agents in tablet formation and what are some examples?

A

Facilitates solubilization or water-insoluble drugs and wetting of hydrophobic tablets

→ SLS, docusate sodium, lecithin, poloaxamer, polysorbate 80

60
Q

What is the purpose of sorbents in tablet formulation and what are some examples?

A

Absorbs oils or oil-drug solutions into a powder mixture during granulation and compaction

→ microcrystalline cellulose, fumed silica, magnesium carbonate, kaolin

61
Q

What are the two types of gelatin used in hard capsule shells?

A

Type A → derived from pork skins by acid processing

Type B → derived from bones and animal skins by alkaline processing (takes longer as you have to decalcify the bones)

62
Q

What are some of the advantages of gelatin hard capsule shells?

A
  • strong flexible film
  • consistent dissolution → soluble in water and GI fluids at body temperature
63
Q

What are some disadvantages of gelatin hard capsule shells?

A
  • cannot be used in vegetarian patients
  • cross linking can happen and greatly slows dissolution
  • mechanical stability is dependant on the water content
64
Q

What ingredients are included in gelatin capsule shells?

A
  • gelatin (20-30%)
  • water
  • colouring agents
  • flavouring agents
  • processing aids (<0.15% of SLS to help gelatin uniformly cover molds)
  • preservatives → parabens
65
Q

What are some advantages of hydroxypropyl methylcellulose (HPMC) hard shell capsules?

A
  • plant-based; good for vegetarian patients
  • immediate and modified release options available
  • low moisture content → great physical stability
  • consistent dissolution → no cross linking
66
Q

What are some disadvantages of HPMC shell types?

A
  • rough capsule surface; not as shiny (could also be considered an advantage because they’re easy to coat)
  • harder to produce uniform colouring
67
Q

What fillings are compatible with hard capsules?

A
  • dry powders
  • pellets
  • granules
  • tablets
  • semi-solids
  • non-aqueous liquids
68
Q

What are soft gelatin capsules?

A

A liquid or semi-solid matrix inside a one-piece plasticized gelatin shell

69
Q

What are the ingredients usually used in soft gel formulation and how much of the weight do they take up?

A
  • gelatin (type B more common) → 40% of gel mass
  • Water (solvent) → 30-40% wet gel mass, 8-16% after drying
  • Plasticizers (glycerin, sorbitol, propylene glycol) → 20-30%
  • preservative (parabens) → 0.1%
  • colour and opacifier (TiO2) → qs
70
Q

What are some alternative polymers that can be used in softgel shell formulation instead of gelatin?

A

Starch and carrageenam

polyvinyl alcohol (PVA)

71
Q

What are the types of fill formulations for soft gel capsules?

A
  1. Hydrophilic liquids
  2. lipophilic liquid
  3. Self-emulsifying drug delivery systems (SEDDS)
    1. Self-micro emulsifying drug delivery system (SMEDDS)
    2. Self-nano emulsifying drug delivery system (SNEDDS)
72
Q

What are some of the properties of hydrophilic liquid fill formulations in soft gel capsules?

A
  • PEG 400 and 600 are commonly used
    • also propylene glycol and glycerin
  • ethanol and water incorporated below 5-10%
  • problem with drug precipitation when contact with water in the GI tract
73
Q

What are some of the properties of SEDDS/SMEDDS/SNEDDS fill formulations in soft gel capsules?

A
  • oil phase and non-ionic surfactants mixture
  • spontaneous emulsion formation in the GI fluid; stable for a longer time
  • high surface area provided by the surfactant micelles containing solubilized oil and drug
74
Q

What type of base makes up hard lozenges?

A

hard sugar candy base

75
Q

What type of base is used for soft lozenges/pastilles

A

PEG base, sucrose, acacia base

76
Q

What type of base is used in the formulation of chewable lozenges (gummies)?

A

glycerinated gelatin base

77
Q

What was the first type of coating used for tablets and how long does it take?

A

Sugar coating in 1856

→ traditional process = 3-5 days

→ automated process = 1 day or less

78
Q

What was sugar coating largely replaced by and why?

A

Film coating → cheaper, takes less time, gives ability to modify release

79
Q

What does film coating involve?

A

Deposition of a thin, uniform polymer coating onto the surface of the tablets, capsules or multiparticulates/pellets

80
Q

What are some polymers used in immediate-release coating?

A
  • cellulose derivatives → hypromellose or MPMC, hydroxypropyl cellulose (HPC)
  • Vinyl derivatives → polyvinyl alcohol (PVA)
  • acrylic derivatives → methymethacrylate copolymers, methacrylic acid copolymers
81
Q

What are some of the properties of polymers used in film coating?

A
  • good solubility range and pH range
  • good film strength, flexibility and adhesion
  • compatible with film coating excipients
  • stability under storage conditions
  • absence of bad taste
  • non-toxic
82
Q

What are enteric coatings used for?

A

Protect the drug from the stomach acids and deliver it to the intestine

83
Q

What effect does pH have on the polymers used in film coating?

A

Low pH → polymers remain unionized and insoluble

High pH → polymers readily ionize and dissolve (>pH 5)

84
Q

What are some properties of extended-release coatings used in film coating?

A
  • polymers are insoluble in water
  • films are permeable to some extent
85
Q

What are some examples of extended-release polymers for film coating?

A

Ethylcellulose

acrylic resins

polyvinyl acetate (PVA)

86
Q

What are the two types of solvents used in film coating?

A

Organic → alcohols, ketones, chlorinated hydrocarbons, dichloromethane

Aqueous → water is most common

87
Q

What are some of the disadvantages of organic solvents used in film coating?

A
  • expensive; need efficient venting and plant optimization
  • safety issues; flammable, toxic
88
Q

What are some of the disadvantages of aqueous solvents?

A
  • slow evaporation, longer drying time
  • appearance of small amounts (picking) or larger amounts (peeling) of film fragments
  • mottling (colour migration)
89
Q

What is the purpose of a plasticizer in film coating?

A

Improves flexibility of the coatings, reduces risk of film cracking

90
Q

What are some examples of plasticizers used in film coating?

A

Polyols: propylene glycol, glycerin, PEG

Organic esters: diethyl phthalate, dibutyl sebacate, triethyl citrate, tributyl citrate, triacetin

91
Q

What do colourants do in film coating?

A

Improve product appearance and identification, improve coated product stability

92
Q

What type of pigment is preferred for film coating and why?

A

Insoluble is preferred because:

  • reduce permeability of the coating to moisture; improves product stability
  • bulking agent; increases overall solid content in the coating dispersion without increasing viscosity
  • less colour migration
  • opacifying
93
Q

What is the role of the anti-adherent in film coating and what are some examples?

A

Reduces stickiness of the film and prevents substrate agglomeration

→ talc, magnesium stearate, glyceryl monostearate, high MW PEGs

94
Q

What is the role of surfactants in film coating and what are some examples?

A

Emulsifies water-insoluble plasticizers, improves tablet wettability, ensures rapid dissolution of the coating in the stomach

→ polysorbate 80, sorbitan monoleate, sodium dodecyl sulfate

PHARM 125 - Pharmaceutics (5 decks)

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