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Dosage (Lec) > M1 LESSON 2: DOSAGE FORM DESIGN > Flashcards

M1 LESSON 2: DOSAGE FORM DESIGN Flashcards

1
Q

THE GENERAL AREA OF STUDY CONCERNED WITH THE FOLLOWING AREAS OF PHARMACEUTICAL DOSAGE FORM DESIGN

A

PHARMACEUTICS

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2
Q

PHARMACEUTICS FORM DESIGN

A

⦿Formulation
⦿Manufacture
⦿Stability
⦿Effectiveness

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3
Q

THE NEED FOR DOSAGE FORM
PRIMARY REASON

A

FOR THE SAFE AND CONVENIENT DELIVERY OF ACCURATE DOSAGE

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3
Q

To provide liquid preparation of substances that are either insoluble or unstable in the desired vehicle _________ or clear preparation ____________

A

Suspension and Solution

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3
Q

Why is there a need for dosage forms?

A

To protect drug substances from the destructive influences of atmospheric oxygen or humidity

  • Coated Tablets
  • Sealed Ampules
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3
Q

To protect drug substances from the destructive influence of gastric acid after oral administration

A

Enteric Coated Tablets

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4
Q

The formulation that best meets the goal of the product is the

A

“MASTER FORMULA”

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4
Q

to provide for insertion of drug into one of the body’s orifices

A

Rectal
Vaginal Suppositories

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4
Q

To provide placement of drug directly in the bloodstream or body tissues

A

Injection

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4
Q

To conceal bitter, offensive or salty taste or odor of a drug substance

A

Capsule, Coated Tablets, Syrups

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5
Q

To provide rate - controlled drug action

A

Controlled Release Tablet, Capsule, Suspension

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5
Q

PRE-FORMULATION CONSIDERATIONS

A
  1. Physical Description
  2. Microscopic examination
  3. Heat vaporization
  4. Melting point depression
  5. Phase rule
  6. Particle size
  7. Polymorphism
  8. Solubility
  9. Dissolution
  10. Membrane permeability
  11. Partition Coefficient
  12. Dissociation Constant
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6
Q

to provide optimal drug action from topical administration sites

A

Ointment
Creams
Transdermal Patch
Opthalmic Preparation
Ear Preparation
Nasal Preparation

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6
Q

(patched and its contents go through the layers of the skin)

A

Transdermal Patch

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6
Q

ability to get to a site of action and elicit response

A

◼biological property

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7
Q

Through Inhalation therapy

A

Inhalants, Inhalation Aerosols

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7
Q

THERAPEUTIC CONSIDERATIONS

A
  1. The nature of the illness
  2. The manner in which it is treated
  3. The age and the anticipated condition of the
    patient
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7
Q

GENERAL CONSIDERATIONS In
DOSAGE FORM DESIGNS

A
  1. PHYSICAL AND CHEMICAL
    PROPERTIES OF THE DRUG SUBSTANCE
  2. THERAPEUTIC CONSIDERATIONS
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7
Q

physical description, particle size, crystalline structure, melting point and solubility

A

◼physical property

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7
Q

● The amount of heat absorbed when 1 g of liquid vaporizes

● Operation of implantable pumps delivering medicine

● Aerosol dosage forms

● Nasal inhalants for treating nasal decongestion

● Particle size affects vapor pressure; the smaller the particle size the greater the vapor pressure

A

HEAT VAPORIZATION

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7
Q

( structure, form, and reactivity

A

◼chemical property

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7
Q

◼the purity of the chemical substance is essential for its identification and for evaluation of its chemical, physical, and biological properties

A

PHYSICAL DESCRIPTION

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7
Q

HYDRATES AND SOLVATES

A
  1. Hygroscopic powder
  2. Deliquescent powder
  3. Efflorescent powder
  4. Organic Salt Consideration
  5. Organic Ester Consideration
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7
Q

Kinds of Solubility

A

Very Soluble
Freely Soluble
Soluble
Sparingly Soluble
Slightly Soluble
Very Slight Soluble

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7
Q

the smaller the particle size the greater the?

A

vapor pressure

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7
Q

● Gives an indication of particle size and size range of the raw materials along with the crystal structure

● Spherical and oval powders flow more easily than needle shaped powders

A

MICROSCOPIC EXAMINATION

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7
Q

● Used to determine the purity of the substance

● Change in melting point means the product is not pure

A

MELTING POINT DEPRESSION

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7
Q
  • Crystal or amorphous
  • Affects melting point and solubility
A

POLYMORPHISM

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7
Q

To produce biological response, the drug molecules must first cross the biologic membrane (acts as lipid barrier) permits absorption of lipid soluble substance by passive diffusion

A

MEMBRANE PERMEABILITY

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7
Q

is frequently added to increase solubility

A

Salt and ester forms

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7
Q

a useful device for relating the effect of the least number of independent variables (e.g., temperature, pressure, and concentration) upon the various phases (solid, liquid, and gaseous)that can exist in an equilibrium system containing a number of components.

A

PHASE RULE

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7
Q

◼ Should possess aqueous solubility for therapeutic effect

A

SOLUBILITY

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7
Q

Measure of drug’s lipophilic character

A

PARTITION COEFFICIENT

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7
Q

◼ Adjustment in __________ and ________ can increase solubility

A

particle size and pH

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7
Q

Rate-limiting step in the absorption process

A

DISSOLUTION

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7
Q

Certain physical and chemical properties of drug substances, including dissolution rate, bioavailability, content uniformity, taste, texture, color and stability are affected by the particle size distribution

Flow characteristics and sedimentation rates

Particle size influences oral absorption

A

PARTICLE SIZE

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7
Q

Change in melting point means the product is not?

A

pure

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8
Q

 The extent of dissociation and ionization of the drug.

 Extent of ionization has strong effect on drugs absorption, distribution, and elimination

A

pKa / DISSOCIATION CONSTANT

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8
Q

the time it takes for the drug to dissolved in the fluids at the absorption site.

A

Dissolution rate

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9
Q

absorb moisture from air then liquefy

A

Deliquescent powder

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9
Q

tends to absorb moisture from air

A

Hygroscopic powder

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10
Q

give up water of crystallization and may even become damp and pasty

A

Efflorescent powder

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11
Q

drugs are either weak acids or weak bases and have limited water solubility, often used the salts of the product to increase the aqueous solubility

A

ORGANIC SALT CONSIDERATION

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11
Q

Prepared for increase solubility, stability, and resistance to degradation after administration, use of prodrug

A

ORGANIC ESTER CONSIDERATION

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12
Q

PREFORMULATION STABILITY STUDIES

A
  • Solid state stability of the drug alone
  • Solution phase stability
  • Stability in the presence of expected excipients
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13
Q

A solvolysis process in which drug interact with water to yield breakdown products of different chemical constitution

A

HYDROLYSIS

13
Q

Amides, lactones, and lactams are also prone to hydrolytic decomposition

A

HYDROLYSIS

14
Q

Example: Acetylsalicylic acid + water → salicylic
acid + acetic acid

A

HYDROLYSIS

14
Q

Common to aldehydes, alcohols, phenols, sugars, alkaloids, and unsaturated fats and oils

A

OXIDATION

14
Q

prone to hydrolytic decomposition

A

Amides, lactones, and lactams

14
Q

MECHANISMS OF DEGRADATION

A

⦿ HYDROLYSIS
⦿ OXIDATION

15
Q

Involves the loss of electrons from an atom or a molecule

A

OXIDATION

15
Q

The original physical properties, including appearance, palatability, uniformity, dissolution, and suspendability are retained

A

PHYSICAL

16
Q

Each active ingredient retain its chemical integrity and labeled potency, within specified limits.

A

CHEMICAL

16
Q

Chemical stability is important for;

A
  • Selecting storage condition (temperature,
    light, humidity)
  • Selecting the proper container (glass vs plastic; clear vs amber)
  • Anticipating interactions when mixing drugs
17
Q

FIVE TYPES OF STABILITY

A
  1. CHEMICAL
  2. PHYSICAL
  3. MICROBIOLOGIC
  4. THERAPEUTIC
  5. TOXICOLOGIC
17
Q

Is defined as the extent to which a product retains, within specified limits, and throughout its period of storage and use, the same properties and characteristics that it possessed at the time of its manufacture

A

STABILITY

18
Q

❑ Sterility or resistance to microbial growth is retained

❑ Antimicrobial agents that are present retain effective within specified limits

A

MICROBIOLOGIC

19
Q

The therapeutic effect remain unchanged

A

THERAPEUTIC

20
Q

No significant increase in toxicity occur

A

TOXICOLOGIC

21
Q

Intermediate pH
sodium bi sulfite

A

Aqueous Prep

21
Q

In liquid preparations, water can be frequently replaced or reduced through the use of substitute liquids such as;

A

◼Glycerin, propylene glycol, and alcohol

22
Q

⦿ Use of buffering agents
◼For most hydrolyzable drugs, optimum stability is

A

on the acid side (pH 5 and 6)

23
Q

High pH
sodium sulfite

A

Aqueous Prep

24
Q

Ascorbyl palmitate

A

Oleagenous Prep

24
Q

Low pH
hypophosphorous acid
Ascorbic acid

A

Aqueous Prep

25
Q

Alpha-tocopherol

A

Oleagenous Prep

26
Q

butyl hydroxy anisole

A

Oleagenous Prep

27
Q

Factors that affects oxidation

A
  1. oxygen present as airspace within the container-nitrogen
  2. trace elements in drugs, solvent, container, and stopper- chelating agent eg. EDTA
    (ethylenediaminetetraacetic acid) and calcium
    disodium edetate
  3. light- light resistance or opaque plastic
  4. temperature- cool place
  5. ph of the preparation- maintain solution in pH most favorable to its stability
28
Q

APPEARANCE AND PALATABILITY

A

FLAVOR, FRAGRANCE AND ODOR

29
Q

☺ low MW salts- salty ; high MW salts-bitter
🗉 Increase hydroxyl group, increase sweetness
🗉 Aldehyde is pleasant to taste
🗉 Nitrogen compound- (plant alkaloids)bitter /
(aspartame) sweet

A

FLAVORING

29
Q

Organic esters, alcohols, and aldehydes are

A

pleasant to taste

30
Q

salty

A

low MW salts

31
Q

high MW salts

A

bitter

31
Q

Increase hydroxyl group

A

increase sweetness

32
Q

pleasant to taste

A

Aldehyde

33
Q

plant alkaloids

A

bitter

34
Q

aspartame

A

sweet

34
Q

mask the bitter taste of drugs (Alkaloids,
Epsom salt)

A

Cocoa

35
Q

mask salty taste of drugs (Chlorides of Na, K, and Ammonium)

A

Cinnamon, raspberry and orange flavors

36
Q

combat acid or sour taste of drugs

A

Fruit or citrus flavors

37
Q

prefer sweet, candy-like preparations with fruity flavors

A

Children

37
Q

CONSIDERATIONS IN SELECTING A FLAVORANT

A
  1. TASTE OF THE DRUG SUBSTANCES
  2. AGE OF THE INTENDED PATIENT
38
Q

prefer less sweet with tart rather than a fruit flavor pharmaceutical

A

Adult

39
Q

180 to 200 times sweeter than sucrose;
contraindicated to phenylketonuria

A

ASPARTAME

40
Q

SWEETENING AGENTS

A
  1. Sucrose
  2. Glycerin
  3. Saccharin
  4. Aspartame
  5. Cyclamate
  6. Acesulfame Potassium
  7. Stevia Powder
41
Q

has carcinogenic potential; artificial sweetener

A

CYCLAMATE

41
Q

Commonly used sweetener; from sugar cane/sugar beet

A

SUCROSE

41
Q

less sweet than sucrose

A

GLYCERIN

42
Q

300 times as sweet as sucrose; has a bitter after taste; carcinogenic in animal

A

SACCHARIN

42
Q
A
43
Q

COLORING PHARMACEUTICALS

A

⦿Plant dyes
⦿Minerals
⦿Synthetic

43
Q

Achuete

A

Plant dyes

43
Q

130 times as sweet as sucrose

A

ACESULFAME POTASSIUM

43
Q

natural, non-toxic, safe and about 30 times sweeter than sucrose

A

STEVIA POWDER

44
Q

Ferric Oxide (red); it is mixed in small portion with Zinc oxide imparting a characteristic pink color in Calamine powder

A

Minerals

45
Q

natural, non-toxic, safe and about 30 times sweeter than sucrose

A

ACESULFAME POTASSIUM

46
Q

can cause allergic reactions to patient who has sensitivity reaction to aspirin;

FDA requires the listing of this dye on the labels of food and ingested drugs containing the substance

A

FD & C Yellow No. 5 (tartrazine)

46
Q

used in food, drugs, and cosmetics

A

FD & C

46
Q

Coal tar dyes, anthracene dyes, aniline dyes

A

Synthetic

47
Q

approved for use in drugs, some in cosmetics, and some in medical devices

A

D & C

48
Q

changes of colorant according to toxicological findings

A

a) withdrawal of certification
b) the transfer of colorant from one certification category to another
c) the addition of new color to the list

48
Q

the use of which is restricted to external parts of the body, not including the lips or any body surface covered by mucous membrane

A

External D & C

49
Q

DRUG PRODUCTS REQUIRING COLORANTS

A

⦿ Capsules
⦿ Compressed tablets
⦿ Sugar-coated tablets
⦿ Suspension

50
Q

DRUG PRODUCTS THAT DO NOT CONTAIN COLOR ADDITIVES

A

● Ophthalmic products
● Parenteral products
● Ointments
● Suppositories

51
Q

Products requiring preservatives

A
  1. Syrups
  2. Emulsions
  3. Semisolid preparations
  4. Ophthalmic products
  5. Parenterals (multiple-dose package)

⦿ Chlorobutanol, benzalkonium chloride and phenyl
mercuric nitrate are the frequently used
preservatives in ophthalmic preparations because of
their low degree of irritant qualities
PRESERVATIVES
⦿ Acidic preservatives are more effective in acid media, while
alkaline preservatives are less effective in acid or neutral media
but more effective in alkaline media
⦿ Examples:
1. Benzoic acid and sodium benzoate
2. Alcohol
3. Cresol and Phenol
4. Chlorobutanol, Benzalkonium chloride and phenyl mercuric
acetate
5. Paraben

52
Q

Products NOT requiring preservatives

A
  1. Alcoholic and hydroalcoholic solutions
    ● 15-20% alcohol in solution will prevent microbial contamination
    ● Elixirs, tinctures, and spirits are self-preserving
  2. Large Volume Parenterals
53
Q

the amount added to liquid preparations ranges from 0.0005 to 0.001% depending upon the colorant and the depth of color desired.

A

LIQUID DYES

54
Q

FD and C lake is a pigment consisting of a substratum of alumina hydrate on which the dye is adsorbed or precipitated.

Suitable for coloring products in which the moisture levels are low.

A

LAKE PIGMENTS

55
Q

Parenterals and Ophthalmic preparations are
sterilized by

, however may still require additional preservatives

A

AUTOCLAVING, BACTERIAL FILTRATION
and DRY HEAT

56
Q

are the frequently used preservatives in ophthalmic preparations because of their low degree of irritant qualities

A

Chlorobutanol
Benzalkonium chloride
Phenyl mercuric nitrate

57
Q

are less effective in acid or neutral media but more effective in alkaline media

A

alkaline preservatives

57
Q

are more effective in acid media

A

Acidic preservatives

58
Q
  1. Benzoic acid and sodium benzoate
  2. Alcohol
  3. Cresol and Phenol
  4. Chlorobutanol, Benzalkonium chloride and phenyl mercuric acetate
  5. Parabens (Methyl- and propylparaben) - antifungal
A

PRESERVATIVES

Dosage (Lec) (2 decks)

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