Excipients Flashcards

1
Q

What is an excipient?

A

An additive that has no therapeutic effect

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2
Q

What are the purposes of an excipient?

A
Enhancement of:
Delivery
Acceptability
Stability
Handling
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3
Q

What are the ideal properties of an excipient?

A

Inert
Safe- Non-toxic
Quality-assured-: Appropriate purity or grade, compliance to BP standards
Economical

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4
Q

Excipients for powder mixtures

A

Dilutent- increases bulk of tablet
Binder- helps particles to stick
Disintegrant- breaks up tablet into granules (H20)
Glidant- enhances powder flow
Anti-adherent- Prevent powders sticking to surfaces
Lubricant- Reduces friction

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5
Q

What are the 6 excipients?

A
Lactose
Starch
Cellulose
Talc
Colloidal silicon dioxide
Magnesium Stearate
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6
Q

What are the subtypes of excipients?

A
Monohydrate
 anhydrous
spray-dried
 Natural
pre-gelatinised powder
crystalliine
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7
Q

What is lactose?

Is it water-soluble?

A

Glucose and galactose
Water-soluble
GRAS-listed (regarded as safe)
Maillard reaction: instability with amine containing drugs

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8
Q

What are the different forms of lactose?

A

Lactose monohydrate
Anhydrous lactose
Spray dried lactose

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9
Q

What are the difference in the sub types?

A

The preparation of the excipients

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10
Q

What is lactose monohydrate?

A

Crystallised from superunsaturated lactose solutions

Odourless, white

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11
Q

What is lactose monohydrateprimarily used as?

A

Dilutent for tablets and capsules

Binder for wet granualtion in tabletting

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12
Q

How do you prepare anhydrous lactose?

A

Dry the lactose solution, then reduce the powder and crush it

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13
Q

What is anhydrous lactose primarily used as?

A

Dilutent and binder for hard-shell capsules

Direct compression tablets

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14
Q

What does granualtion mean?

A

Aggregate the powders to form larger clumps

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15
Q

How is spray-dried lactose prepared?

A

By spray-drying lactose solution

Start as liquid droplets, then solidify into spherical particles (high compactibility)

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16
Q

What is spray-dried lactose used as?

A

Dilutent
Binder
Direct-compression tableting

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17
Q

What is starch?

A

Made up of amylose and amylopectin

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18
Q

What are the two types of starch?

A

Natural

Pregelatinised

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19
Q

What protein does starch contain?

A

Wheat protein

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20
Q

What does starch naturally exist as?

A

Starch granules

1) Corn starch
2) Pea starch

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21
Q

What are the properties of Natural starch?

A

Odourless
Tasteless
White
Fine powder

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22
Q

What is natural starch primarily used as?

A
Binder
Dilutent
Disintegrant
Anti-adherent
Lubricant
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23
Q

What are the properties of pregelatinised starch?

A

Odourless
Slight characterstic taste
White
Fine powder

24
Q

What is pregelatinised starch primarily used as?

A

Binder- better binder properties due to fluffiness (cohesion with partciles)
Dilutent
Disintegrant

25
Q

What types of granualtion is pregelatinised starch used in?

A

Wet granualtion
Dry granulation
Direct-compression

26
Q

What are the two types of cellulose?

A

Powdered cellulose and Microcrystalline cellulose

27
Q

What type of glycosidic bond does cellulose have?

A

B-1,4 glycosidic bond

28
Q

How is cellulose obtained?

A

From the pulp of a fibrous plant

29
Q

Which agent is cellulose incompatible with?

A

Strong oxidising agent

30
Q

What groups are good binders and good dilutents?

A

Polysaccharides/saccharides

31
Q

What is powdered cellulose primarily used as?

A

Dilutent - hard-shell capsules
Binder
Disintegrant
Glidant

32
Q

What is the E number of cellulose?

A

E460

33
Q

What is microcrystalline cellulose?

A

Modified form of natural cellulose

34
Q

What are the properties of microcrystalline cellulose?

A
Porous
Hygroscopic
Crsytalline
White
Odourless
Tasteless
35
Q

How is microcrystalline cellulose prepared?

A

Partially depolymerised cellulose obtained through controlled acid hydrolysis then spray-dried

36
Q

What is a good substitue for lactose for a filler?

A

Microcrystalline cellulose

37
Q

What makes a good disintegrant?

A

Things that swell in water

38
Q

What is talcum powder alrgely used as?

A

Used as a lubricant largely

39
Q

What is talcum powder

A

A hydrous magnesium silicate

40
Q

How is Talc prepared?

A

Mineral–mined, pulverised and purified

41
Q

Why do we need to purify substances?

A

It may contain asbestos which is carciogenic

42
Q

What are the primary traits of lubricants and glidants?

A

High specific surface area

43
Q

What is Talc primarily used as?

A

Glidant
Anti-adherent
Lubricant
Dissolution retardant

44
Q

Is Talc water-soluble?

A

No, it would prevent lactose from dissolving in water if it was water soluble.

45
Q

What are the properties of Talc?

A

Odourless
White
Crystalline powder

46
Q

What does Talc do to larger particles?

A

Coats them to reduce cohesion, adhesion and friction

47
Q

What is Colloidal silicon dioxide?

A

Major component in glass

48
Q

What are the properties of Colloidal SO2?

A

Odourless
Tasteless
White/bluish powder

49
Q

What makes it particlulary effective?

A

Has a very high specific surface area and is insoluble in water

50
Q

How is Colloidal SO2 prepared?

A

By flame pyrolysis of chlorosilanes (forms agglomerates throughout process), in hydrogen-oxygen flame

51
Q

What is Colloidal SO2 primarily used as?

A

Glidant
Disintegrant
Adsorbent

52
Q

What is Magnesium stearate?

A

Fatty acid with a VV high specific surface area?

53
Q

What is Magnesium stearate primarily used as?

A

Lubricant (to reduce friction)

54
Q

What are the physical properties of Magnesium stearate?

A

Greasy to the touch
Faint odour
Taste of stearic acid

55
Q

What is the solubility of Magnesium stearate?

A

Insoluble in water, ehtanol and ether (due to fatty acid group)

56
Q

Which agents is Magnesium stearate incompatible with?

A

Strong oxidising agents, including strong acids and alkalis, iron salt

57
Q

How does it accelerate aspirin degradation?

A

Increasing solubility and hydrolysis by elevating pH.