PSC 4215 - Exam 1 - Combined - Semisolid dosage forms, Suppositories, Drug discovery

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180 Terms

1

3 Semisolid dosage forms

Creams, Ointments, Gels

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2

Ointments

Semi solid preparation used on the skin and mucous membranes

(body opening with moist lining such as the eye)

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3

2 Main effects of oinments

Local and Systemic

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4

Why must systemic effects of ointments be considered in pregnant or nursing patients?

Harmful drugs can enter fetal circulation and breast milk

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5

What risk does overuse of topical drugs on large areas pose?

Increased absorption → Systemic effect → Overdose

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6

Why is retinol (a Vitamin A derivative) dangerous in pregnancy?

It is teratogenic, which means it causes fetal defects, even in small amounts

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7

How do absorbed topical drugs reach systemic circulation? (2)

Blood and Lymphatic system

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8

Why do weak basic drugs accumulate in breast milk?

Breast milk is acidic, so it traps weak bases such as morphine and acetaminophen

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9

What is the purpose of topical dermatological products?

Deliver drugs into the skin to treat dermal disorders

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10

What is the target organ of topical dermatological products?

Skin

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11

How do transdermal products differ from topical dermatological products?

Delivers drugs thru the skin to reach system circulation

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12

What is the target organ of transdermal products?

Systemic circulation

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13

Why are transdermal products used instead of oral medications?

Special populations that require systemic circulation

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14

Medicated vs Unmedicated dermatological products

  • Medicated products contain active drugs

  • Unmedicated products do not contain active drugs

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15

What are 2 functions of non-medicated dermatological products?

  • Emollients → Softeners

  • Anti-dehydrates → Retains moisture

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16

What is the role of the base and vehicle in topical preparations?

  • Base → Provides structure and consistency

  • Vehicle → Acts as a carrier for active ingredients

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17

What are 2 non medicated ointments that are hydrophobic? What is it used for?

  • Vaseline and Aquaphor

  • Physical effects

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18

What is the function of hydrophobic ointments like Vaseline or Aquaphor?

It forms a protective barrier to enhance wound healing

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19

What are the two types of wound healing in which hydrophobic ointments like Vaseline or Aquaphor are commonly used?

  • Primary wound healing → Closed wounds such as stitches

  • Secondary wound healing → Open wounds (to recover from bottom up)

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20

What are the two main types of ointment bases?

Hydrophobic and Hydrophilic

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21

Define the following:

Hydrophilic

Hydrophobic

Lipophilic

Lipophobic

  • Hydrophilic → Attracts water

  • Hydrophobic → Repels water

  • Lipophilic → Attracts fat

  • Lipophobic → Repels fat

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22

4 Major types of semisolid bases

  1. Oleaginous bases

  2. Absorption bases

  3. Water removable bases

  4. Water soluble bases

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23

T/F: Oleaginous bases are greasy and hydrophobic hydrocarbons

T

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24

3 Reasons to use oleaginous (hydrocarbon) bases

  • Emollient effect (Softener)

  • Anti-dehydrate protection (Retains moisture)

  • Occlusive dressing (Barrier, does not allow anything to pass thru)

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25

Why do oleaginous bases remain on the skin for long periods?

It is immiscible with water (does not mix, forms distinct layers)

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26

What prevents bacteria from growing in oleaginous bases?

Lipophilic nature of oleaginous bases

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27

4 Examples of oleaginous bases

  • Petrolatum

  • White petrolatum

  • Mineral oil

  • Yellow ointment

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28

What is Petrolatum (Vaseline), USP? Where is it produced from?

  • It is a purified semi solid hydrocarbon

  • It is a byproduct of petroleum

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T/F: Petroleum was originally discovered thru oil drilling

T

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30

How is white petrolatum produced?

Bleaching petrolatum

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31

2 Components of yellow ointment

Yellow wax and Petrolatum

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32

Mineral oil

Liquid oleaginous base

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33

What is mineral oil used for in ointments?

Levigating agent, it helps mix dry powders into a uniform base, unmedicated

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34

T/F: An oleaginous base helps protect the fluidity of granulation tissue (tissue that forms during the healing of a wound)

T

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35

What are absorption bases useful for?

It helps incorporate aqueous solutions into hydrocarbon bases to create W/O emulsions

(An emulsion is a mixture of two immiscible liquids, where one liquid is dispersed in the other in the form of tiny droplets.)

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36

Are absorption bases easily removable by water washing?

No

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37

Emulsifiable absorption base vs Emulsified absorption base

  • Emulsifiable absorption base → Forms W/O emulsions

  • Emulsified absorption base → Already in W/O emulsion form, but can incorporate more water

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38

4 Examples of absorption bases

  • Lanolin

  • Anhydrous lanolin (anhydrous means without water)

  • Cold creams

  • Hydrophilic petrolatum

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39

What is the dominant base in a “water in oil” emulsion?

What is the dominant base in an “oil in water” emulsion?

  • Oil

  • Water

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40

What are the four components of Hydrophilic Petrolatum, and what are their functions? (CSWW)

  1. Cholesterol → Emulsifying agent → Lipophilic component

  2. Stearyl alcohol → Emulsifier → Hydrophilic component

  3. White wax → Structure

  4. White petrolatum → Base

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41

What is lanolin derived from?

Purified wax like substance from sheep wool

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42

Key function of lanolin

Retains moisture

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43

Water removable base

Oil in water emulsion that resembles creams

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44

T/F: Water removable bases easily wash off with water but require scrubbing

T

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45

Can water removable bases be diluted with water? Why or why not?

Yes bc the external phase is aqueous

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46

What is the main function of water removable bases?

Absorbs serous discharge for fasting healing

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47

In water removable bases, indicate the components that make up the following;

  1. Oil phase (2)

  2. Water phase (2)

  3. Emulsifier (1)

  4. Preservative (2)

  1. Oil phase → White petrolatum, Stearyl alcohol

  2. Water phase → Purified water, Propylene glycol

  3. Emulsifier → Sodium Lauryl Sulfate (SLS)

  4. Preservative → Methylparaben, Propylparaben

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48

Why do water-removable bases need preservatives?

The high water content increases risk of contamination

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49

Do water soluble bases have any oleaginous components?

No

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50

What kind of semi solid base is completely water washable (greaseless), and does not require scrubbing for removal

Water soluble base

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51

What are water soluble bases used for?

Incorporating solids

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52

What type of semi solid base provides the weakest emollient and least protective effects?

Water soluble base

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53

T/F: The higher the water content, the higher the risk of evaporation.

T

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54

2 Examples of water soluble bases

PEG (Polyethylene Glycol Ointment, 3350 and 400) and NF (National Formulary)

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55

Cholesterol

Nonionic, long fatty chain acid

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56

Can cholesterol serve as an emulsifying agent?

Yes, but it must be a mixture of cholesterol and its esters

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57

In cholesterol, what is the result of increasing OH (hydroxyl group)?

It will increase hydrophilicity

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58

What is used to extract cholesterol?

A liquid hydrocarbon such as chloroform (CHCl3)

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59

What semisolid base is best used for thick, dry, calloused skin (e.g., feet, elbows, knees)?

Oleaginous bases

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60

What semi solid base is best used for wound healing, minor burns, or exuding lesions?

Absorption bases

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61
  1. _____ → Greasy, Occlusive, Emollient, Lipophilic

  2. _____ → Greasy, Occlusive, Emollient, Anhydrous, Absorbs water

  1. Oleaginous base (hydrocarbons)

  2. Absorption base

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62
  1. _____ → Not greasy, Not occlusive, Water washable, Can be diluted with water

  2. _____ → Not greasy, Not occlusive, Water washable and soluble, Lipid free

  1. Water removable base

  2. Water soluble base

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63

What are the 5 key factors influencing base selection in topical preparations?

  1. Action Desired (e.g., occlusive, emollient, water-washable)

  2. Physical and Chemical Properties of the Drug

  3. Patient Compliance Factors (e.g., ease of washing, staining potential)

  4. Bioavailability

  5. Stability

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64

What does the "like dissolves like" principle determine in base selection?

Release rate and Duration

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65

What happens if a lipophilic drug is in a lipophilic base? Release & Duration

Slow release → Long duration (Good for chronic conditions)

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66

What happens if a hydrophilic drug is in a hydrophilic base?

Fast release → Short duration (Good for acute conditions)

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67

Used for dry, scaly skin.

Ointments (Oleaginous)

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Applied to weeping or oozing surfaces.

Creams

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69

Applied to intertriginous areas (e.g., skin folds) or where friction occurs.

Lotions

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70

2 Methods for ointment preparation

  • Levigation → Mix components until uniform

  • Fusion → Melt components together, it will cool as you mix, stop when congealed

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71

What is a key limitation of the fusion method?

The active ingredient must be stable at high temperature

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72

Why might preservatives or emulsifiers degrade in the fusion method?

Heat labile (lose stability)

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73

Semi-solid dosage form that contain one or more drugs mixed or dissolved in a base. The base can be water-in-oil (W/O), oil-in-water (O/W), or water-washable (WWB) formulations.

Creams

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74

What are creams used for?

Treat skin disorders such as dermatitis or psoriasis

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75

What application is preferred by patients due to ease of application and removal? (Hint: Less staining than ointments)

Creams

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76

2 Applications for creams

Rectal and Vaginal

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77

Vanishing cream

Oil in water emulsion

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78

Since vanishing creams have a high water content, wha does it form after evaporation?

A thin film

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79

What is added to vanishing creams to retain moisture? (GGS)

Humectants such as glycerin, propylene glycol, sorbitol

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80

_____ Formula:

  • Stearic Acid: 18g

  • Mineral Oil (Light): 2g

  • Lanolin: 0.5g

  • Span 80: 2g

  • Potassium Hydroxide: 0.7g

  • Sorbitol Solution 70%: 3.7g

  • Purified Water: qs ad 100g

Vanishing cream

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81

_____ Formula:

  • Cetyl Esters Wax: 125g

  • White Wax: 120g

  • Mineral Oil: 560g

  • Sodium Borate: 5g

  • Purified Water: 190ml

  • Total: 1000ml

Cream

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82

_____ Formula:

  • Cetyl esters wax

  • White wax 

  • Almond oil 

  • Sodium borate 

  • Stronger rose water 

  • Purified water 

  • Rose oil (enhances patient compliance)

Rose water ointment

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83

List 3 W/O emulsion bases that have aqueous mixtures

Eucerin, Nivea, Polysorb hydrate

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84

Semisolid systems consisting of suspensions of small inorganic particles or large organic molecules interpenetrated by a liquid.

Gels

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85

Single phase gel system vs. Two phase gel system

  • Single phase system → Macromolecules are evenly distributed

  • Two phase system = Magma → Contains floccules of small distinct particles

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86

Example of magma (two phase system gel)

Milk of magnesium, used for heartburn, coats the stomach lining but does not neutralize hydrochloric acid

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87

Thixotropy

Gels thickens when standing, requires shaking before use

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88

9 Examples of penetration enhancers of transdermal preparations

DMSO, EtOH, PG, Glycerin, PEG, Urea, SDS, Poloxamers, Terpenes.

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89

2 Examples of transdermal preparations

Nicotine patches, Hormone patches

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90

Semisolid dosage forms that contain one or more drug substances for topical application.

Paste

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91

What are paste used for? Provide an example

  • Protective barrier

  • Zinc oxide (diaper rash, wounds, eczema)

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92

T/F: Pastes that do not contain active drugs help stabilize medication on the skin.

T

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93

What are the 2 methods to prepare pastes?

Levigation and Fusion

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94

Pastes are used for their stiffness, they remain in place after application and are effectively employed to _____

Absorb serous secretions

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95

Are pastes compatible with hairy parts of the body?

No

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96

Solid/semi-solid adhesive applied to the skin for prolonged contact using backing of paper, fabric, moleskin or plastic

Plasters

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97

What are plasters used for? Provide an example

  • Dead squamous skin (callous)

  • Salicylic acid (for corn removal)

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98

What does it mean if you feel a burning feeling when using a plaster?

It has gone too far into viable skin

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99

What is the surface effect of ointments on the skin?

Forms protective layer

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100

What influence do ointments have on the stratum corneum?

Influences hydration and absorption

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