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CH344 > AP - Drug Product Design Considerations > Flashcards

AP - Drug Product Design Considerations Flashcards

1
Q

What is a drug substance?

A

The API e.g. aspirin

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2
Q

What is a drug product?

A

The final formulation that is being administered to the patient. It is the most suitable dosage form for delivering the drug.

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3
Q

Name one formulation characterisation test.

A
  • Hardness
  • Disintegration profile
  • Dissolution
  • Friability
  • Wettability
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4
Q

Name one drug substance characterisation test.

A
  • pKa
  • Solubility
  • Stability
  • Log P
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5
Q

What is the most common dosage form for transdermal drug delivery?

A

Patches

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6
Q

Define transdermal drug delivery.

A

Transdermal drug delivery systems facilitate the passage of therapeutic quantities of the drug substances through the skin and into the general circulation to elicit their systemic effect.

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7
Q

In order for transdermal drug delivery to be effective, what is necessary?

A

Need to have enough concentration to go into the body and through the circulatory system in order to give a therapeutic effect e.g. HRT, contraception

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8
Q

Define topic drug delivery

A

Topical drug delivery systems are designed to deliver the drug INTO the skin for treating dermal disorders, with the skin as the target organ.

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9
Q

What is the difference between transdermal and topical drug delivery?

A

Transdermal goes into systemic circulation. Topical does not go into systemic circulation at all; it only has a local effect.

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10
Q

Average area of skin?

A

1.6 to 1.8m^2

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11
Q

How many layers are there in the skin?

A

Three.

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12
Q

What is the outermost layer and what is it’s function?

A

Epidermis.
First barrier - will prevent anything to go into systemic circulation.
Impermeable.
Protective.
Main barrier that decided if the drug even gets in.

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13
Q

What is the layer beneath the epidermis?

A

Dermis.

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14
Q

What is the layer beneath the dermis?

A

Adipose tissue (fat layer)

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15
Q

Why do you need to focus on cosmetic appeal?

A

It is visible, therefore not affect compliance in any way.

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16
Q

Advantages of formulation characteristics?

A
  • Ease of manufacture
  • Ease of use by patient
  • Cosmetically elegant and appealing products
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17
Q

Disadvantages of formulation characteristics?

A
  • Dosage control can be difficult (how much is ‘finger size’) –> this is not enough to cause really bad adverse side effects though
  • Not all drugs can be delivered by this route (because absorption is very limited
  • Amount of drug available for systemic action is limited due to physicochemical parameters of the drug e.g. Log P (lipophilocity) , pKa (ionisability), solubility
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18
Q

What are some pre formulation information you require?

A
  • Identification and chemical info (NMR, mass spec)
  • Validated analytical method (HPLC, GLC, UPLC) - to quantify how much of the drug is present in the sample
  • Solubility:
    a) aqueous - water/ ethanol etc
    b) non aqueous - fats/ oils/ liquid paraffin/ waxes
  • Stability - is it stable? as a powder? accelerated stability testing. Is it stable in: oxygen, light, heat
  • Toxicity
  • Physicochemical parameters
    a) Melting point (change in chemical structure will show)
    b) pKa
    c) Log P
    d) partical size
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19
Q

Name a few topical and transdermal formulations

A 
Ointments
Creams
Pastes
Gels
Lotions
Solutions
Aerosols
Patches
Oils
Lacquers
Powders
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20
Q

What excipients are commonly used in a solvent?

A 
Water
Ethanol
Propylene glycol
IPP
IPM
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21
Q

What excipients are commonly used in a formulation base (usually gel or matrix)

A

WSP
Hard paraffin
Carbomer
Cellulose (gel mix)

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22
Q

What excipients are commonly used in an antioxidant? (if the drug is susceptible to oxidation in light, oxygen etc)

A

Vitamin E
Ascorbic acid
Propyl gallate

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23
Q

What excipients are commonly used in a metal chelator?

A

EDTA

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24
Q

What excipients are commonly used in preservatives?

A

Methyl and propyl paraben

benzalkonium chloride

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25
Q

What excipients are commonly used for skin penetration enhancers?

A 
Ethanol
Propylene glycol
Glycofurol
Miglyol
IPP
IPM
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26
Q

What is the excipient EDTA used for?

A

Metal chelator

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27
Q

What are the excipients water, ethanol, propylene glycol, IPP, IPM used for?

A

Solvent

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28
Q

What is the excipient propyl gallate used for?

A

Antioxidant

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29
Q

What is the excipient carbomer used for?

A

Formulation base

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30
Q

What are the excipients methyl paraben, propyl paraben and benzalkonium chloride used for?

A

Preservatives

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31
Q

What base does an ointment have?

A

Hydrophobic/ oleaginous base.

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32
Q

What application is ointment for?

A

External application to the skin or mucous membrane.

33
Q

How is the drug in an ointment dissolved?

A

It is dissolved into the base or in an appropriate solvent and incorporated into the molten base.

34
Q

What does an ointment form on the skin?

A

It forms a greasy film on the skin.

35
Q

What does the greasy film that is formed by using an ointment do? (3 things)

A
  • Prevents loss of moisture
  • Increases skin hydration
  • It’s occlusive nature allows drug permeation through the skin
36
Q

What conditions are ointments suitable for?

A

Inflammatory skin conditions such as:

  • Psoriasis
  • Eczema
  • Dermatitis
37
Q

What are the drawback of ointments?

A

It is very oily and can stick to clothes therefore patient compliance may be affected.

38
Q

What are the excipients used in ointments and what property must they have?

A

ASHCAWES - need to be non aqueous

Antioxidant
Solvent base
Hydrocarbon base
Chelating agent
Absorption base
Water soluble base
Emulsifying base
Silicone
39
Q

EDTA is an example of?

A

A chelating agent.

40
Q

Polyethylene glycol (PEG) is an example of?

A

A water soluble base.

41
Q

Lanolin and Wool alcohol are examples of?

A

Absorption bases.

42
Q

Isostearyl isostearate and cetomacrogol are examples of?

A

Emulsifying agents.

43
Q

Propylene glycol, IPP and IPM are examples of?

A

Solvents.

44
Q

Dimethicone and Cyclomethicone are examples of?

A

Silicones - for cosmetic use.

45
Q

Give examples of hydrocarbon bases/ fats.

A 
WSP
Hard paraffin
Peanut oil
Coconut oil (Miglyol)
Liquid parrafin
Sesame oil
46
Q

What is the method of preparation for an ointment formulation?

A

Drug dissolved in solvent.
Heat Liquid paraffin + WSP + Dimethicone.
Add drug solution to molten base and allow to cool with stirring.

47
Q

Define cream.

A

Semi solid preparations for external application.

48
Q

Advantages of cream over ointment?

A

Better patient compliance. Very easy to apply. Not as viscous and sticky. Cosmetically appealing.

49
Q

Disadvantages of cream over ointment?

A

Have to make sure drug stays in solution and does not precipitate out.
Not all drugs are suitable to be delivered as creams.

50
Q

What kind of excipient is propyl gallate?

A

Anti oxidant.

51
Q

Name two penetration enhancers.

A

Ethanol and propylene glycol.

52
Q

What is the most important excipient in a cream?

A

Surfactant. To ensure the formulation remains stable.

53
Q

What is the second most important excipient in a cream (if water based)?

A

Preservative. Presence of water exposes risk to microbial contamination therefore need methyl or propyl paraben to prevent this from occuring.

54
Q

What are the excipients used in a cream?

A

Aqueous phase:
Oil Phase: WSP, liquid paraffin, miglyol, vegetable oils

SPACSGP

  • Surfactant: Cetomacrogol 1000 (oil soluble), Sorbitan monooleate, Polysorbate 80, Tween 80 (water soluble surfactant)
  • Preservative: Methyl paraben, propyl paraben
  • Antioxidant: Vit E, BHT, BHA, Propyl gallate
  • Chelating agent: EDTA
  • Silicone: Dimethicone
  • Gelling agent: Carbomer, HEC, HMPC
  • Penetration enhancer: Ethanol, Propylene glycol
55
Q

Define gel.

A

A semi solid system formed by aggregation of colloidal particles interpenetrated by a liquid.

56
Q

What are the two types of gel?

A

Aqueous

Non aqueous

57
Q

Example of an aqueous gel?

A

Cellulose, xanthan gum

58
Q

Example of non aqueous gel?

A

Silicone gels

59
Q

Advantages of gels?

A

Patient compliance. Very easy and cosmetically appealing.

60
Q

Disadvantages of gels?

A

Drug must have sufficient solubility. If not, then use a co solvent system OR use complexing agents.

61
Q

Excipients for gels?

A

APPSGP

(Aqueous gel)

    • Antioxidant: Propyl gallate, Ascorbic acid
  • pH regulation: buffer system
  • Penetration enhancer: Ethanol, Propylene glycol
  • Silicone: Dimethicone, Cyclomethicone, Elastomer
  • Gelling agent: carbomer, HEC, HPMC, Xanthan gum, cellulose
  • Preservatives: methyl/ propyl paraben, phenoxy ethanol/ benzoic acid
62
Q

Define paste

A

A semisolid dosage form that is intended for topical application. It generally contains a high concentration of dispersed solids and has a stiff consistency.

63
Q

Creams, pastes and lotions have similar excipients. What is the one excipient that pastes and lotions have that creams do not?

A

Dispersing agent - Hydrated silica

64
Q

Define lotion

A

Lotions are aqueous solutions or suspensions from which water evaporates to leave a thin uniform coating go powder on the skin.

65
Q

Main advantage of lotion is that it provides?

A

soothing effect to skin.

66
Q

Define solution

A

A liquid preparation with one or more components in a single or multiple miscible solvents for drug delivery.

67
Q

Advantages of solution

A
  • Ease of preparation
  • Ease of application
  • Aqueous and non-aqueous
  • Single or multiple controlled applications
68
Q

Excipients in solution.

A

CAPP

  • Chelating agent: EDTA
  • Antioxidant: BHT, BHA, Vit E, Propyl gallate
  • Preservative: Methyl and propyl paraben
  • Penetration enhancer: Ethanol, Propylene glycol
69
Q

Define aerosol

A

Pharmaceutical aerosols are pressurised dosage forms that upon actuation emit a fine dispersion of liquid and/or solid materials containing one or more active ingredients in a gaseous medium.

70
Q

Advantages of aerosol

A
  • ease of administration
  • quick acting
  • covers large surface area
71
Q

There are two types of container and valve assembly. They are:

A

continuous valve

metered dose valve

72
Q

What are the two types of patches?

A

Transdermal matrix patch and Transdermal membrane patch

73
Q

Define lacquer

A

A type of nail varnish. Usually for nail drug delivery.

74
Q

Solvents in lacquer are highly…

A

volatile.

75
Q

Excipients in lacquer.

A 
SARS
Solvents: Ethanol, Butyl/ Ethyl acetate
Antioxidant: BHT, BHA, Propyl gallate, Vit E
Resins: Eudragit, Gantrez
Surfactants: Glycerol triacetate
76
Q

Typically these are used as a bulking base for powders:

A

Talc or starch

77
Q

Particle size for powder should be..

A

Less than 150 um to avoid irritation.

78
Q

Tests performed on topical formulations:

A
  • Rheology
  • Homogeneity of drug dispersion in the formulation
  • Stability of drug in formulation
  • Microscopy and macroscopy to determine any particulates
  • pH
  • Preservative efficacy testing
  • Microbial content
  • Particle size
  • Drug absorption/ permeation across inert/ skin membranes

CH344 (13 decks)

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