Pre-Midterm Flashcards

1
Q

8 advantages of Solid Dosage Forms

A

Unit dose
Cost of shipping
No breakage or leakage
Masking taste less difficult
More portable
Require less space per dose
Good physical and chemical stability
Elegant distinctive appearance which has a high patient acceptability

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2
Q

Disadvantages of a solid dosage form

A

Potential bioavailability problems
Potential irritant effect on GI mucosa
Occasional difficulty in formulation
Manufacturing can be more technical or
specialized

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3
Q

What are the Physical Properties of Solids

A

a) Particle size
b) Mixing powders

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4
Q

What are the Types of compounded powders

A

Bulk powders for internal use
Other bulk powders

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5
Q

Dissolution rate:

A

the rate at which the particle dissolves.
By increasing the surface area, one may increase the bioavailability for some poorly soluble drugs, because there is often a direct relationship between dissolution rate and bioavailability and drug absorption.

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6
Q

Suspendability

A

the ability of particle to remain undissolved but uniformly dispersed in a liquid vehicle.

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7
Q

Accuracy of dosage form

A

there must be uniform distribution of drug substance in a powder mixture or dosage form, and to ensure batch-to-batch uniformity.

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8
Q

Penetrability

A

the ability of particle to reach their intended location, e.g. to be inhaled deep into the respiratory tract particles should be 1-5 μm.

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9
Q

Non-grittiness

A

do not want solid particle in dermal products to feel “gritty”. Finer particles allow for a smoother texture and better appearance and flow. This is also important for oral products such as chewable tablets.

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10
Q

Chemical stability

A

refers to degradation reactions (e.g. oxidation and hydrolysis). Smaller particles have an increased surface area, leaving them more exposed and vulnerable to reactions with oxygen, water and light.

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11
Q

Flowability

A

effect on flow properties of powders and mixing of powders and granules. This is important in the manufacturing of tablets and capsules.

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12
Q

Compressibility

A

effect on adhesion and “sticking” together when compressing granules into tablets. This is important in the manufacturing of tablets and capsules.

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13
Q

the larger the mesh#

A

the smaller the particles

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14
Q

Monodisperse powders

A

powders containing particles of uniform size, RARE

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15
Q

Polydisperse

A

particle size varies a great deal

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16
Q

Comminution

A

Comminution is the mechanical process of reducing particle size of a solid substance to a finer state of subdivision.

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17
Q

Small-scale comminution

A

Most commonly involves the use of a mortar and pestle and is done by
the pharmacist or technician.

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18
Q

trituration

A

the process of grinding a drug in a mortar to reduce its particle size

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19
Q

levigation

A

the process of mixing a powder with a liquid or semi-solid vehicle (the levigating agent), in which the powder is insoluble, to form a smooth paste

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20
Q

pulverization by intervention

A

particle size reduction with the aid of an additional material, which can be later, removed

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21
Q

lSpatulation

A

blending powders with a spatula on a tile or paper

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22
Q

Advantages (of powders as a dosage form)

A

Flexibility in compounding.

Suitable for infants and young children who cannot swallow tablets or capsules.

Rapid onset of drug action because disintegration is not required.

Can be applied to many body cavities such as ears, nose, tooth socket, and throat.

Relatively good chemical stability.

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23
Q

Disadvantages of powders

A

Potential for misunderstanding of the correct method of
use that can lead to inaccurate dosing.

Undesirable for bitter or unpleasant tasting drugs

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24
Q

Dentifrices

A

dental cleaning powders, denture powders

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25
What types of substances that do not dissolve gelatin may be encapsulated in capsules.
Dry powders, semi-solids and liquids
26
Water content of HGC shells?
13-16
27
Spot-welded
by means of a heated metal pin pressed against the cap, fusing it to the body.
28
Banded
colored molten gelatin is laid around the joint between the 2 capsule parts in a strip and dried
29
Most common capsule diluents are
Lactose Microcrystalline cellulose Starch
30
Most common capsule disintegrants
Pre-gelatinized starch croscarmellose sodium starch glycolate
31
Disintegrants
Disintegrants serve assist in the break off the powder Mass/granules and help in distributing the drug through-out the stomach.
32
Lubricant and Glidant
Improves fluidity and flow of powders Decreases sticking of powders to metal surfaces
33
Wetting Agents
Surface active agent such as sodium lauryl sulfate are often added to facilitate the wetting of the drug substance by the GI fluids, thus enhancing dissolution.
34
What are the components of a tablet?
Diluent, Binders, Disintegrants, colorants, coatings
35
Examples of diluents for tablets
Lactose Dextrose Starch MCC Mannitol
36
What happens if you have to little binder?
fragile tablets
37
What happens if you have too much binder?
Excessive hardness
38
Example of disintegrants
Corn Starch
39
Potential Problems with Sugar Coating
Many steps of this process involve tumbling – tablets must be hard enough to withstand it Sugar coating pans must mix uniformly or coating goes on unevenly resulting in tablets of different sizes and weights
40
Most common tablet coating
Film Coating
41
What can aqueous tablet coating lead to?
Orange peel effect where the surface due ot failure of spray droplets
42
What is Enteric Coating?
Allows for disintegration in the intestine rather than the stomach.
43
WHat are the physical feautres of a tablet?
Appearance Size Shape Organoleptic Properties
44
Friability test
Ability of tablet to withstand abrasion in packaging, shipping and handling; in other words, its tendency to crumble).
45
What is an acceptable amount of loss during the friability test? %
Usually acceptable value is <1% loss
46
Drug Content Uniformity
Two tests can be used to evaluate whether the amount of drug is uniform from one tablet to another one:
47
Weight Variation
Relies on tablet weight to assess the amount of drug in each unit The greater the amount of drug, the more accurate the method is
48
Content Uniformity
May be applied in all cases (items listed under weight variation) Assesses uniformity of content by assaying each dosage unit.
49
Disintegration
Tablets (or other solid dosage forms) must disintegrate within a specified time period
50
What is the most important test?
Dissolution
51
What is the Dissolution test?
dissolution test measures the amount of time required for a certain % of the drug substance to dissolve under specified conditions (which resemble physiological conditions).
52
What are Molded Tablets?
Prepared by molding rather than by compression
53
What are Molded tablets not appropriate for?
Not appropriate for potent drugs due to difficulties with content uniformity
54
limitations of chewable tablets?
Drug material is bitter and flavouring is important and often5 difficult.
55
What is Mannitol?
Adds sweetness and a cool tase ~50% of formulation in chewable tablets.
56
Effervescent Tablets
Large wafer-like tablets which dissolve rapidly in water Tablet breakup is facilitated by the release of carbon dioxide (CO2) generated from sodium bicarbonate and citric or tartaric acid
57
Where are buccal tablets placed?
Side of cheek
58
What does gelatin do to a tablet?
Makes it soft hence usually a soft chewable
59
What does corn syrup do to a tablet?
Make it hard hence hard lozenge
60
What does polyethylene glycol do?
Make it soft so more likely a soft lozenge
61
Capping
the partial or complete separation of the top or bottom crowns of a tablet from the main body of the tablet.
62
Lamination
the separation of a tablet into 2 or more distinct layers, i.e. transverse cracking and separation of tablet.
63
Causes of Lamination / Capping
Air entrapment in light and fluffy powders Excessive “fines” Too little moisture in granulation Weak granules or too weak a binder Improper adjustment of machinery
64
Picking
the surface material from a tablet that is sticking and being removed from the tablet surface by a punch. Usually associated with letters such as “A”, “B”, “O” and “P”, etc from logos and lettering in the punch surface.
65
Sticking
tablet material adhering to the die wall.
66
Causes of Picking/Sticking
Inadequate lubrication (adhesive components may be present) Insufficiently dried wet granulation Poor finish on punch surfaces
67
What is Whiskering?
fine edge attached but not broken off tablet. End up with high friability values since “whiskers” are removed in friability testing.
68
Causes of Whiskering
Especially deep concave punches Punches worn and in poor condition
69
Friability
It refers to the ability of the compressed tablet to withstand abrasion or crumbling in packaging, handling and shipping.
70
Causes of Poor Disintegration
Tablet hardness too high Low amount of disintegrant. May require better disintegrant Too much binder Over lubrication causing “waterproofing”
71
Mottling
an unequal or uneven distribution of colour on or in a tablet.
72
Low Hardness
Low hardness can lead to rapid release of drug from dosage form or tablet will be too fragile for shipping and handling.
73
Dissolution
The transfer of molecules and ions from a solid phase into a solution
74
Factors affecting solubility
Molecular weight, volume. Presence of functional groups and their position. Acids or bases (pH dependent solubility – ionized form more soluble).
75
Increase temperature ___ solubility
decreases
76
Increasing pressure ___ solubility
Increases
77
Miscibility
expresses the mutual solubility of components in a liquid-liquid system (mixes without separating)
78
In an Endothermic solution Solubility ___ with increase temperature
increases increases
79
In an exothermic solution solubility ___ with increased temperature
decrease
80
Primary solvent for many organic compounds
◼ alcohol ◼ isopropyl alcohol ◼ glycerin ◼ propylene glycol ◼ polyethylene glycol 400
81
What is the most common solvent?
Alcohol
82
Advantages of semi-polar solvents?
◼ Better solubility for many compounds ◼ Can be used as co solvent ◼ Better stability for the drug: ◼ Hydrolysis ◼ Bacterial growth ◼ 70% is used as a skin antiseptic or for sterilizing work surfaces (BSC)
83
Limits for Alcohol in OTC products: Children <6 Children 6-12 Adults
0.5 5 10
84
Denatured alcohol
Has additives (ketones or kerosene) to render it more poisonous and unfit for internal use
85
Absolute alcohol (100%)
Essentially water-free ethanol
86
Diluted Alcohol NF
prepared by diluting Alcohol USP with an equal volume of Purified Water USP
87
Rubbing Alcohol:
◼ Around 70% by volume. ◼ Effective antiseptic-disinfectant ◼ For external use only (dye can be added)
88
Miscible Solvents
a solute may be more soluble in a mixture of solvents than in one solvent = co-solvent effect
89
If there are two or more solvents and two or more solutes in a formulation,
each solute should be dissolved in the solvent in which it is most soluble before mixing with other liquids in the preparation.
90
Complexes are
loose molecular associations that can either increase/decrease solubility.
91
Solutions for oral administration often include additives WHY?
Storage stability, enhance solubility, taste etc.
92
What are the 4 primary tastes
Sweet, Sour, Bitter, Salty
93
What is the Flavouring techniques Physiological
anesthetize the taste buds/receptors
94
What is the Flavouring techniques Physical
◼ Prevent dissolution of drug (prevent it from coming in contact with taste buds)
95
What is the Flavouring techniques for Overshadowing
Addition of a flavour whose intensity is longer and stronger than the taste of the drug (e.g. Methyl salicylate)
96
What is the Flavouring techniques for Blending
add flavours which compliment the taste and modify the flavour perception (e.g. Vanillin, benzaldehyde) ◼ sourtaste–blended with fruit flavours ◼ bitter taste – adding salty, sweet and sour flavour
97
Chemical
Drug can be complexed or a prodrug can be made Used in drug product manufacturing
98
Other factors besides taste:
Aroma Texture Viscosity
99
2 categories of sweeteners
Natural sweeteners that include sugars and polyols such as sucrose, Artificial sweeteners
100
What are the sweeteners-Sugars
Sucrose Lactose Dextrose
101
What are the Natural Polyols? (Sugar free)
Sorbitol Mannitol Xylitol
102
Artificial sweeteners
Saccharin Cyclamate Aspartame Sucralose Stevia
103
What is the issue with Aspartame?
Aspartame degrades into diketopiperazine when exposed to high temperatures (180C) Intolerance in patients PKU incidence 1 in 20 000
104
No colour is certified for use in the?
Eye
105
What concentration of dye colour do we usually use?
0.0005-0.001%
106
When should preservatives/antimicrobials not be used?
Formulation used immediately No water is present PH is less than 3 or greater then 9
107
Where are preservatives CI?
Neonates Ophthalmics Volumes greater than 30
108
What are the 2 aqueous solutions?
Syrups and Aromatic waters
109
What are the non-Aqueous Solutions?
Elixirs, Spirits, tinctures
110
What concentration of alcohol is usually in syrups?
up to 10%
111
What are the non medical ingredients in Syrups that we should know? (4)
Glycerin, Propylene glycol, sorbitol, sucralose
112
What % of sucrose should be in syrups before not having to add antimicrobrials
<80%
113
What is simple syrup?
Concentrated with sucrose and has self preservative properties
114
What is the alcohol content of a spirit?
62-85%
115
What is the alcohol concentration oin tinctures?
15-80%
116
What is the concentration of alcohol in elixirs?
3-44%