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PR3153 > Common Excipients in Formulations > Flashcards

Common Excipients in Formulations Flashcards

Match each excipient to their function

1
Q

Recall Lipinski’s Rule of 5.

A
  • =< 5 H bond DONORS
  • =< 10 H bond ACCEPTORS
  • < 500 Da (< 300Da for hydrophilic, < 1 kDa for lipophilic)
  • Log P < 5
  • Unionised

Use Lipinski’s Rule as a guide rather than a hard and fast rule for drugs/substances. Strategy is to look at the overall molecule based on the Lipinski’s rule, see how many it fulfills and make a decision on whether it passes through BBB.

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2
Q

Acetic and citric acids

A

pH adjustment/ buffer

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3
Q

Sodium hydroxide

A

pH adjustment

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4
Q

Hydrochloric acid

A

pH adjustment

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5
Q

Sodium borate

A

pH adjustment

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6
Q

Boric acid

A

pH adjustment

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7
Q

Sodium acetate, citrate, and phosphates

A

Buffer

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8
Q

Potassium phosphate

A

Buffer

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9
Q

Edetate disodium

A

Metal chelator / Preservative enhancer

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10
Q

Benzalkonium chloride

A

Preservative (known effect on cillia)

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11
Q

Benzethonium chloride

A

Preservative

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12
Q

Benzyl alcohol

A

Preservative

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13
Q

Chlorhexidine (di)gluconate

A

Preservative

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14
Q

Chlorobutanol

A

Preservative (known effect on cillia)

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15
Q

Methylparaben

A

Preservative (known effect on cilia)

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16
Q

Phenylethyl alcohol

A

Preservative

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17
Q

Propylparaben

A

Preservative (known effect on cilia)

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18
Q

Potassium chloride

A

Tonicity adjustment

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19
Q

Sodium chloride

A

Tonicity adjustment

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20
Q

Me-OH-Pr cellulose (Hydroxypropyl Methylcellulose)

A

Viscosity adjustment

21
Q

Celluloses
e.g. Sodium Carboxymethyl Cellulose (Na CMC), Microcrysalline Cellulose, Carboxymethylcellulose (CMC), Hydroxypropyl Methyl Cellulose (HPMC)

A

Viscosity adjustment
Transdermal: viscosity adjustment, matrix polymer

22
Q

Ethanol

A

Solvent
Transdermal: solvent, permeation enhancer

23
Q

Glycerin

A

Solvent/ tonicity adjustment

24
Q

Glycerol

A

Solvent/ tonicity adjustment

25
Q

Glycine

A

Solvent/ tonicity adjustment

26
Q

PEG

27
Q

Polyethene glycol

28
Q

Glyceryl dioleate

A

Solvent/ surfactant

29
Q

Glyceryl monoleate

A

Surfactant
Transdermal: permeation enhancer, bioadhesive, sustained release agent

30
Q

Lecithin

A

Surfactant

31
Q

Polysorbate 20 & 80

A

Surfactant

32
Q

Tyloxapol

A

Surfactant

33
Q

Menthol

A

Flavouring agent

34
Q

Saccharin sodium

A

Flavouring agent (sweetener)

35
Q

Sorbitol

A

Flavouring agent (sweetener)

36
Q

What is Lipinski’s Rule of 5 for CNS Delivery?

A
  • <3 H bond DONORS
  • <7 H bond ACCEPTORS
  • < 450 Da
  • Log P 1-3
  • Unionised

Use Lipinski’s Rule as a guide rather than a hard and fast rule for drugs/substances. Strategy is to look at the overall molecule based on the Lipinski’s rule, see how many it fulfills and make a decision on whether it passes through BBB.

37
Q

Cyclodextrin

A

Transdermal: permeation enhancer

38
Q

What is Lipinski’s Rule of 5 for Transdermal Delivery?

A
  • =< 5 H bond DONORS
  • =< 10 H bond ACCEPTORS
  • < 500 Da
  • Log P 1-3
  • Unionised

Use Lipinski’s Rule as a guide rather than a hard and fast rule for drugs/substances. Strategy is to look at the overall molecule based on the Lipinski’s rule, see how many it fulfills and make a decision on whether it passes through BBB.

39
Q

Propylene glycol

A

Transdermal: solvent, permeation enhancer

40
Q

Hyaluronate sodium

A

Transdermal: viscosity adjustment, humectant, matrix polymer

41
Q

Calcium alginate

A

Transdermal: viscosity adjustment, adhesive, matrix polymer

42
Q

Carbomer

A

Transdermal: viscosity adjustment, adhesive

43
Q

Poly(methyl vinyl ether/ maleic anhydride)

A

Transdermal: viscosity adjustment, adhesive

44
Q

Polyester

A

Transdermal: polymer matrix in backing layer

45
Q

Silicone

A

Transdermal: adhesive

46
Q

Ascorbyl Palmitate

A

Transdermal: permeation enhancer

47
Q

Phenol

A

Preservative

48
Q

Thiomersal

A

Preservative

49
Q

Mannitol

A

Tonicity adjustment / cryoprotectant

Cryoprotectant: for injection solutions that are frozen, to maintain integrity of molecules

PR3153 (10 decks)

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