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PHARM 124 > Solutions > Flashcards

Solutions Flashcards

1
Q

Define Solutions

A

A chemically and physically homogenous liquid preparation of two or more substances

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2
Q

List some characteristics of solutions

A

Homogenous one phase system
Uniform distribution of drug throughout the preparation

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3
Q

What is the most common solvent?

A

Water

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4
Q

What is possible other ingredients that may exist within a pharmaceutical solution?

A

Excipients
Colouring
Flavour
Presertevt

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5
Q

What are advantages of solutions?

A

Can be intended for multiple routes of administration
Oral solutions – drug available for absorption
Flexible dosing
No shaking of solutions needed (complete dissolution)

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6
Q

What are some disadvantages of solutions?

A

Drug stability may be compromised
Technical accuracy or delivery devices needed for dose accuracy
Solubility properties of drug must be matched with excipients
Bulky storage and transportation

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7
Q

What dosage forms utilizing solutions?

A

Injectable
Paediatric formulation
Ophthalmic preparation

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8
Q

What are some other solvent vehicles?

A

Alcohol
Isopropyl alcohol
Glycerin
Propylene glycol
PEG

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9
Q

Define Solubility

A

The quality of solute that will dissolve in a specified quantity of solvent to form a saturated solution

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10
Q

Define dissolution

A

The transfer of molecules and ions from a solid phase into a solution

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11
Q

What is the difference betweeen solubility and dissolution?

A

Solubility is a property while dissolution is a phenomenon/process

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12
Q

What are some thing that happen in dissolution?

A

The removal of a molecule of a drug from the solid state
The formation of cavity within the solvent
The accommodation of the drug molecule into the formed
The process involves the breakage of solute-solute and solvent-solvent bonds and the formation of a bond between the solute and solvent

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13
Q

What is the general rule with dissolution?

A

The more soluble the drug
The faster the dissolution into the solvent

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14
Q

List some ways to enhance dissolution

A

Some solids require triturating to reduce the particle size and decrease the solution time
Sometimes heat is required to enhance the dissolution
Some vigorous shaking or stirring is required

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15
Q

Describe dissolution

A

The process by which a drug particle dissolves
A process by which a solid of specific solubility characteristics enter into the solution

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16
Q

The smaller the particles the increase in

A

Dissolution
And
Absorption

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17
Q

List factors that affect solubility

A

Molecular weight
Volume
Presence of functional groups and their position
Acids or bases

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18
Q

What is difference in characteristics between aqueous solution and pure water?

A

Aq has higher boiling point and a lower freezing point

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19
Q

An increase in temp _____ solubility of solids

A

Increases

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20
Q

List the types of solutions

A

Gases in liquids
Liquids in liquids
Solids in liquids

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21
Q

Define miscibility

A

Expresses the mutual solubility of components in a liquid-liquid system

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22
Q

List the Types of liquid pairs

A

Soluble in all proportions
Soluble in definite proportions

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23
Q

List examples of soluble in all proportions (liquid pairs)

A

Alcohol and water
Glycerin and water

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24
Q

List examples of soluble in definite proportions (liquid pairs)

A

Phenol and water (influenced by temp)

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25
Q

What is an example of immiscible?

A

Oil and water

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26
Q

In Gases in liquids how does an increase in pressure affect

A

Increase solubility of gas in liquids

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27
Q

In Gases in liquids how does an increase temperature affect

A

Decrease solubility of gas in liquid

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28
Q

What are the two factors that determine the amount of gas that will dissolve in a liquid?

A

Temperature
Gas

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29
Q

List the factors affecting solubility

A

temperature
pharmaceutical solvents
mixed solvents
complexation

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30
Q

Explain how temperature affects solubility in an exothermic reaction

A

decrease solubility with the increase in temperature

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31
Q

Explain how temperature affects solubility in an endothermic reaction

A

increase solubility with the increase in temperature

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32
Q

Define endothermic

A

positive heat of solution
the solution process requires the input of energy or heat is absorbed when the solute is dissolving

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33
Q

Define exothermic

A

negative heat of solution
in the solution process heat is given off when the solution is dissolving

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34
Q

Define Normothermic

A

heat is neither absorbed nor given off during the solution process

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35
Q

Give an example of exothermic reaction

A

NaOH dissolving in water

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36
Q

Give an example of when endothermic reaction is used

A

creating syrups

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37
Q

Give an example of normothermic

A

KCl

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38
Q

What are the types of pharmaceutical solvents?

A

non-polar and polar

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39
Q

Define polarity

A

a separation of electric charge leading to a molecule or its chemical groups having an electric dipole moment, with a negatively charged end and a positively charged end

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40
Q

List the small or no dipolar characteristics

A

fixed oils - non volatile
hydrocarbons

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41
Q

List the uses of non polar solvents

A

vehicle for injections
external preparations

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42
Q

Explain of polar solvent

A

potable water

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43
Q

What is the natural salts in potable water?

A

Ca, Mg, Fe, K & Na
organic matter
atmospheric gases
suspended materials

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44
Q

Rendering water potable requires?

A

removal of insoluble matter by settling and filtration
destruction of pathogenic organisms by chlorination

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45
Q

List primarily semi polar solvents

A

alcohol
isopropyl alcohol
glycerin
propylene glycol
polyethylene glycol 400

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46
Q

What is the most common solvent?

A

alcohol

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47
Q

explain why alcohol is used

A

by mixing with water it creates a hydro alcoholic solution both alcohol and water soluble compounds

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48
Q

Advantages of Semi Polar solvents

A

better solubility for many compounds
can be used as co solvent
better stability

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49
Q

How can semi polar solvents have better drug stability

A

decreases hydrolysis
bacterial growth

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50
Q

Limits for Alcohol in OTC products

A

Children < 6 = < 0.5%
Children 6-12 = <5%
Adults = <10%

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51
Q

List miscible with a wide range of solvents

A

caster oil
water
alcohol

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52
Q

List the types of alcohols

A

denatured alcohol
absolute alcohol
diluted alcohol NF
rubbing alcohol

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53
Q

Define denatured alcohol

A

has additives to render it more poisonous and unfit for internal uses

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54
Q

Define absolute alcohol (100%)

A

dehydrated alcohol UPS
water free ethanol

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55
Q

Define diluted alcohol NF

A

prepared by diluting Alcohol USP with an equal volume of purified water
useful as hydro alcoholic solvent in pharm preps

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56
Q

Define rubbing alcohol

A

around 70% by volume
effective antiseptic -disinfectant
for external use only

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57
Q

Define Miscible solvents

A

a solute may be more soluble in a mixture of solvents than in one solvents

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58
Q

Explain the cosolvent effect

A

the solubility is improved if some alcohol is added to an aqueous formulation

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59
Q

Explain mixed solvents

A

if there are two or more solvents and two or more solutes in formation
each soluble should be dissolved in the solvent in which it is most soluble before mixing with other liquids

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60
Q

Explain Complex formulation

A

complexes are loose molecular association that can either increase or decrease solubility

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61
Q

What points should be shared in counseling when using a complex formulation?

A

tell pt to avoid taking milk or dairy products containing calcium within 2 hours of taking tetracycline

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62
Q

What should you avoid with calcium and iron?

A

certain antibiotics
certain medications used to treat osteoporosis
thyroid medication

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63
Q

when preparing a solution, solubility is improved by

A

stirring
elevated temp
reduction of particle size
salt form rather than base form
sometimes: mixed solvent system

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64
Q

List ways that drug concentrations of a drug can be expressed

A

mol/L
mol/kg
g/l
w/v, w/w, v/v
ppm

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65
Q

Why are additives added to oral adminstration?

A

storage stability, enhance solubility, taste

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66
Q

Requirements in the preparation of oral solutions

A

physical stability
chemical stability
microbiological stability

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67
Q

Describe Physical stability and list examples

A

stability that can be seen or felt

no discoloration/cloudness
no precipitation
no loss of elegance
no loss of taste

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68
Q

Define chemical stability

A

there must not be changes to the molecular structure of the drug

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69
Q

What are some factors of chemical stability?

A

pH
hydrolysis and oxidation

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70
Q

How can you reduce these chemical instabilities?

A

Hydrolysis can be controlled by using non-aqueous solvents e.g. alcohol
Oxidation can be controlled by adding antioxidants e.g. ascorbic acid, sodium bisulfate

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71
Q

Explain microbiological stability

A

Enhanced by the use of solvents with “preservative” action e.g. >20% glycerin, alcohol

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72
Q

Explain why it need to be palatability

A

The product must taste good
Sweeteners e.g. sucrose, sorbitol, etc.
Flavours

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73
Q

Explain the need for a pleasing appearance

A

The product must look good “pharmaceutical elegance”.
in order to be used and sold

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74
Q

How could we have pleasing appearance?

A

often add colors or viscosity inducing agents to solutions

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75
Q

List characteristics of the Ideal additive

A
  1. pharmacologically inactive and non-toxic
  2. potent, therefore can be used in low concentrations
  3. no unpleasant odour or flavour
  4. compatible with drug and other excipients
  5. stable to changes in pH or exposure to light and heat etc.
  6. soluble in the vehicle/solvent
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76
Q

What are the types of flavors?

A

salty
bitter
sour
sweet

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77
Q

What is the mechanism of taste?

A

*A substance dissolves in the water layer on the tongue
*The solution is in contact with the taste cells and initiates a nerve impulse
*The impulse is transmitted via the cranial nerve to the brain; the perception of taste results

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78
Q

What must happen for the substance to be tasted?

A

they must be dissolved

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79
Q

Explain sweet

A

low molecular weight poly-hydroxyl compounds (e.g. sucrose, sorbitol, mannitol)
(number of OH groups ∝ sweetness)

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80
Q

Explain Sour

A

a result of H+ ions, therefore proportional to [H+]/acidity

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81
Q

Explain bitter

A

high molecular weight salts, free
bases and nitrogen containing compounds like amides (e.g. caffeine, codeine)

82
Q

Which flavour is the most objectionable and most common?

A

Bitter

83
Q

Explain Salty

A

low molecular weight salts and ionic compounds (anion + cation)
(e.g. NaCl, ammonium chloride, Na salicylate)

84
Q

What is one major thing to keep in account when selecting flavoring agents?

A

look at str of empds in your formula and can estimate what it’ll taste like

85
Q

List flavoring techniques

A
  1. Physiological
  2. Physical
  3. Masking or overshadowing 4. Blending
  4. Chemical
86
Q

Explain how physiological flavoring techniques work

A

anaesthetizethetastebuds/receptors

87
Q

How does physical work for flavoring

A

prevent dissolution of drug

88
Q

Examples of physiological flavoring techniques

A

carbonated beverages
stores produce in fridge
apply ice cubes on tongue before taking the medication

89
Q

Examples of physical flavoring techniques

A

use of a viscous fluids
formulate an emulsion instead of a solution
coating tablet

90
Q

Explain how overshadowing flavoring techniques work

A

Addition of a flavour whose intensity is longer and stronger than the taste of the drug

91
Q

Explain how blending flavoring techniques work

A

add flavours which compliment the taste and modify the flavour perception

92
Q

List examples of blending flavoring technique

A

sour taste - blended with fruit flavours
bitter taste - adding salty, sweet and sour flavour

93
Q

Explain how chemical flavoring tech works

A

drug can be complexed or a prodrug can be made
used in drug product manufacturing
Should not affect the overall therapeutic profile of the drug Microencapsulation or nanoencapsulation also done

94
Q

Give an example of chemical flavoring technique

A

tetracycline dispensed as HCl salt

95
Q

What are 2 categories of sweeteners?

A

natural sweeteners
artificial sweeteners

96
Q

List of desired properties of sweeteners

A

Colourless
Odourless
Solubility in water at the concentration needed for sweetening
Pleasant tasting
No aftertaste
Stable over a wide pH range

97
Q

Examples of Sweeteners - Sugars

A

Sucrose
Lactose
Dextrose

98
Q

Define Sucrose

A

disaccharide (glucose,fructose)
standard for sweetness

99
Q

What are some possible concerns with sucrose?

A

high water solubility but may reduce the water solubility of other solutes/drug
may pose a problem for diabetic pt
has a tendency to crystallize on the threads of bottle caps
inversion & caramelization

100
Q

Define Lactose

A

milk sugar
disaccharide –> galactose-glucose
less sweet than sucrose

101
Q

Define dextrose

A

glucose, corn sugar
monosaccharide
less sweet than sucrose
generally not used in oral products but sometimes as IV solutions

102
Q

List types of sweeteners - artificial polyols

A

glycerine
propylene glycol

103
Q

List types of sweeteners - natural polyols

A

sorbitol
mannitol
xylitol
sucralose
stevia

104
Q

Define Sorbitol

A

approximately 2.6 cal/g (4 for sucrose), more slowly absorbed
less sweet than sucrose (0.6 x sucrose)
Can cause gas/flatulence

105
Q

Define Mannitol

A

approx, half the caloric value of sucrose
less sweet than sucrose
high intake has laxative effects

106
Q

Define Xylitol

A

approx. equal sweetness to sucrose but absorbed more slowly, negligible affect on blood sugar metabolized irrespective of insulin
more expensive than sucrose

107
Q

Define Saccharin

A

tends to have a bitter metallic after taste

108
Q

define cyclamate

A

approx. 30 times sweeter than sucrose

109
Q

define aspartame

A

non-carb nutritive sweetener
ADR - seizures, headache

110
Q

Problems with Aspartame

A

intolerance in pt with PKU
- this is a deficiency in the enzyme phenylalanine hydroxylase

111
Q

Define Sucralose

A

600 x sweeter than sucrose
not metabolized (non-caloric)
not bitter after taste

112
Q

Define Stevia

A

200 x sweeter than sucrose –> some after taste

113
Q

Why is flavoring needed?

A

most flavors are bitter and require sweetening to make them more pleasant to taste

114
Q

Why use colors?

A

to enhance the esthetic quality of the preparation
to act as a sensory adjunct to flavor

115
Q

Why do pt usually reject dark colors?

A

because they are often associated with poisons

116
Q

Two possible instances this speculation will not work?

A

Not practical for a child because they have not yet developed color/aroma/taste correlation.

It is deterrent if the patient must take multiple doses, so it is best to avoid this method when possible

117
Q

As a compounding pharmacist do you think it is safe to use liquid stock colorants available in grocery store as they are also FD&C approved?

A

No
need material safety data sheet
- impurities
- stability
-interaction

118
Q

Types of Natural Coloring Agents

A

mineral pigments
plant pigments
animal pigments

119
Q

Define mineral pigments

A

primarily used for lotions, cosmetics and other external preparation

120
Q

define pigments

A

insoluble materials that give colors when dispersed in some liquid

121
Q

List some examples of mineral pigments

A

yellow ferric oxide
white titanium dioxide
red (red ferric oxide and carbon black)

122
Q

List some examples of plant pigments

A

green chlorophyll
orange B carotene
yellow saffron

123
Q

List synthetic color certifications

A

FD&C
D&C
external D&C

124
Q

Explain what FD&C

A

food, drug and cosmetic

125
Q

Explain what D&C

A

drug and cosmetic

126
Q

Explain D&C

A

not allowed in products for lips

127
Q

Problems with Synthetic Color Agents

A

carcinogenicity probability
hypersensitivity
hyperactivity

128
Q

When are preservatives CI?

A

neonates
ophthalics
parenteral greater than 30 ml

129
Q

Alternative strategies when preservatives are needed but contraindicated:

A

Prepare single doses
Prepare a limited quantity that will be used within a short time period
store under refrigeration and label with a short beyond use date

130
Q

Requirements for preservations

A

activity needs to be broad spectrum
must reduce a microbial population significantly and prevent subsequent re-growth
synergistic combinations like benzalkonium pathogens like P aeruginosa

131
Q

Define Antioxidants

A

divert the oxidative process

132
Q

How do antioxidants work?

A

by reacting with one or more compound in the formulation to prevent free radical medicated chain reaction

133
Q

Antioxidants for aqueous systems

A

for ascorbic acid
Na sulfite
bisulfite

134
Q

Antioxidants for oil systems

A

BHA
alpha-tocopherol

135
Q

Define buffers

A

control the ph of solution and therefore the staiblity of the product
buffer solution contains a weak acid and its conjugate base so that the pH of the solution changes little when acid is added

136
Q

What are viscosity Inducing agents?

A

used to change the consistency of a preparation to render it more resistant to flow
makes the product easier to pour for the pt
may improve appearance and palatability

137
Q

For topical solutions, viscosity is essential:

A

for achieving desired smoothness and consistency
ease in applying
will remain in contact with affected area like in ophthalmic formulations to increase residence time

138
Q

List some examples of viscosity inducing agents

A

methylcellulose
carboxymethylcellulose
hydroxypropyl methylcellulose
acacia
tragacanth
bentonite

139
Q

What is the challenge with viscosity?

A

creates difficulty when trying to dissolve drugs in the vehicle

140
Q

What is the solution to viscosity affecting dissolution?

A

do not try dissolving drug in a viscous medium
add viscosity inducer after dissolving the drug

141
Q

Explain surface active agents

A

chemicals that contain both hydrophilic & hydrophobic regions
also called wetting agents
modulate solubility of ingredients to improve stability and sometimes bioavailability

142
Q

Classifications of aqueous solutions

A

syrups
aromatic waters

143
Q

Classifications of non-aqueous solutions

A

elixirs
spirits
tinctures

144
Q

Define aqueous solutions

A

the most prevalent of the oral solution
dissolving a drug in water along with excipients makes an aqueous solution

145
Q

What is always used in preparing compounded aqueous solutions?

A

distilled or purified water

146
Q

why we should know about the compatibilities of medicinal ingredients in solvents used in commercial products?

A

we need to know if something looks wrong so we don’t endanger the pt

147
Q

Define syrups

A

are concentrated, viscous, sweetened, aqueous solutions that may contain less than 10% alcohol

148
Q

List some non medicinal ingredients

A

Citric acid, flavor, glycerin, polyethylene glycol, propylene glycol, sodium benzoate, sodium citrate, sorbitol, sucralose, water and xanthan gum.

149
Q

the most common oral solutions dispensed to patients are ___ and ___?

A

syrup and elixir

150
Q

Compared to syrups, elixirs are generally:
______ sweet

A

less

151
Q

Compared to syrups, elixirs are generally:
______ viscous

A

less

152
Q

Compared to syrups, elixirs are generally:
______ effective in masking bitterness

A

less

153
Q

Compared to syrups, elixirs are generally
Always contain ______ in ranges between _____%

A

alcohol
3-44%

154
Q

Compared to syrups, elixirs are generally:
______ stable physically

A

more

155
Q

Compared to syrups, elixirs are generally:
______ stable chemically

A

more

156
Q

Simple syrup contains ____ w/v or ____ w/w sucrose in water

A

85%
65%

157
Q

Common form of tincture seen in pharmacy is _____ which is used as an _____

A

iodine tincture
antiseptic

158
Q

0.5 grams dissolved in 100 ml of solution –> best way to represent its concentration is ______

A

percentage

159
Q

What level of sugar does the syrup have to be in order to need antimicrobial preservative?

A

<80%

160
Q

Purpose of colorant

A

may be added to a syrup to enhance the appeal of the syrup
mostly it is correlated with the flavor

161
Q

Define cherry syrup

A

a sucrose based syrup containing 47% by volume cherry juice

162
Q

What is the case when the coloring does not match the flavor?

A

raspberry flavor but colorless solution

163
Q

What is cocoa syrup flavored with?

A

vanilla to help with the bitter taste

164
Q

What need to be determined before using a flavoured syrup?

A

if acidic, neutral or slightly basic and whether this will cause a problem with stability of the added medicinal agent

165
Q

Why should we be aware of flavoring agents stability or ph?

A

solubility is dependent on pH
chemical stability of acid or base liable drugs

166
Q

Define Simple Syrup

A

Saturated solution of sucrose in water.

85% w/v or 65% w/w

Sucrose 850g + purified water qs ad 1000ml.

Syrup is fully saturated and self-preservative

If diluted, it will support mold and other microbial growth.

167
Q

What is the compounding methods for a drug within syrup-based formulations?

A

In formulas containing both drug and sucrose, each ingredient is usually dissolved separately and then mixed together in such a way to avoid precipitation

168
Q

Define aromatic waters

A

are clear, saturated aqueous solutions of volatile oils or other aromatic substances
used as flavoring or perfuming solutions

169
Q

What might be used to make aromatic waters?

A

use of talc

170
Q

What are the steps for compounding aromatic water?

A

volatile oil + talc + purified water
thorough agitation for 30 minutes
filtration is performed

171
Q

What is the role of talc?

A

acts as a distribution agent
act as a filter aid

172
Q

Explain how talc acts as a distribution agent

A

increase the surface area of the volatile substance that is exposed to water and to facilitate the saturation of the solution with oil

173
Q

Explain how talc acts as filter aid

A

remove excess volatile substance

174
Q

What are some limiting factors on non aqueous solutions?

A

their irritation or toxicity profiles

175
Q

List some examples of non aqueous solutions for internal use

A

glycerin
alcohol
propylene glycol

176
Q

List some examples of non aqueous solutions for topical solutions

A

aliphatic hydrocarbons
ether
glyceryl esters of aliphatic acids

177
Q

Common non aqueous solutions are

A

elixirs
spiritis
tinctures

178
Q

Define elixirs

A

clear, sweetened hydro alcoholic solution intended for oral use

179
Q

What is the range for elixirs

A

3 to 44%
most 5 to 10 %

180
Q

What level for elixirs does it require antimicrobial preservative?

A

10-12%

181
Q

Compared to syrups, elixirs are
______ able to maintain water and alcohol soluble components in solution

A

more

182
Q

Compared to syrups, elixirs are
______ long term stability

A

more

183
Q

Compared to syrups, elixirs are
______ strict storage conditions due to alcohol

A

more

184
Q

Define compounding elixirs

A

Alcohol soluble constituents are dissolved in the alcohol portion and water-soluble constituents are dissolved in the water portion  simple solution by agitation

185
Q

Why is aqueous solution added to alcohol solution with constant stirring?

A

Order is important to maintain the highest possible alcoholic strength* at all time so that minimal separation of the alcohol soluble components occur

186
Q

What to do if elixir shows precipitation?

A

Glycerin, sorbitol or propylene glycol aids in dissolution
Permit to stand for few hours  provide time to ensure saturation and then remove the insoluble material by filtration.

187
Q

Define spirits

A

alcoholic or hydro alcoholic solutions of volatile substances

188
Q

What alcohol range is need for spirits?

A

62-85%

189
Q

what are most spirits used for

A

flavouring agents in small quantities
stock solution as a convenient means of obtaining a proper amount of flavoring oil

190
Q

Define tinctures

A

Are alcoholic or hydro alcoholic solutions of non-volatile substances prepared from vegetable or chemical substances.

191
Q

What is the alcohol concentration for tinctures?

A

15-80%

192
Q

Why should it be stopped and not exposed to high temperatures?

A

high alcohol content - explosive or evaporation

193
Q

What is tinctures of potent drugs have?

A

10 g of drug per 100 ml

194
Q

What is non potent tinctures?

A

20 g of drug per 100 ml

195
Q

Why do we not use many tinctures?

A

not prescribed anymore usually due to high alcoholic

196
Q

Do tincture need preservatives?

A

no because Alcoholic content of these preparations protects against microbial growth and keeps the alcohol-soluble material in solution

197
Q

What cannot be mixed with tinctures?

A

successfully with liquids too diverse in solvent character without inducing precipitation of the solute.

198
Q

what is one storage requirement for tinctures?

A

Must be stored in light resistant containers and protected from sunlight. Most contents of vegetable oils are light sensitive

199
Q

List some examples of tinctures

A

Oral – may have unpleasant or burning taste due to alcohol content
Oral – example: opium tincture (17-21% ethanol)
Topical – examples: iodine (first aid antiseptic), thimerosol (antiseptic) – these are about 50% ethanol
Flavouring agents – vanilla tincture, sweet orange peel tincture
Glycerin may be included to increase solubility and stability of the active agents in the tincture

200
Q

List some other pharmaceutical liquids

A

Gargles, mouthwashes
Otic solutions
Ophtalmic solutions
Nasal solutions – nasal wash or medicated
Lotions
Liniments
Enemas
Parenteral injectables (SQ, IV, IM)

201
Q

Why are dryg mixtures for reconsitiuted solutions?

A

to extend the shelf life
this drug mixture may then be reconstituted as a solution
have 7 - 14 days

PHARM 124 (14 decks)

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