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PH107:Pharmaceutical Dosage Form, Drug Delivery System & Medical Devices > DOSAGE FORM DESIGN CONSIDERATIONS > Flashcards

DOSAGE FORM DESIGN CONSIDERATIONS Flashcards

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USMLE® Step 1 flashcards
1
Q

study on the: formulation, manufacture, stability, and
effectiveness of pharmaceutical dosage forms

A

Pharmaceutics

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2
Q

-Selective use of these non-medicinal agents

A
  • Pharmaceutical ingredients or excipients
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3
Q

Uses of Pharmaceutical ingredients or excipients

A

Solubilize
Thicken
Stabilize
Flavor
Suspend
Dilute
Preserve
Efficacious
Emulsify
Color
Appealing closure forms

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4
Q

Requirements of a proper design & formulation
of dosage form

A

a. Consideration of drug substances: Physical, chemical and biological
characteristics
b. Compatible with one another - stable, efficacious, attractive, easy to
administer, and safe
c. Manufactured under appropriate measures of quality control and packaged in
containers to make the product stable
d. Labeled to promote the correct use and stored under conditions to maximize
shell life

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5
Q

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

A

Coated tablets

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6
Q

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

A

Enteric-coated

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7
Q

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

A

Capsules,
Flavored syrups

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8
Q

To provide liquid preparations of substances
that are either insoluble or unstable in the
desired vehicle.

A

(Suspension)

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9
Q

To provide clear liquid dosage forms of
substances.

A

Syrups, Solutions

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10
Q

To provide rate-controlled drug action.

A

Controlled-release tablets

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11
Q

To provide optimal drug action from topical
administration sites.

A

Ointments, Creams,
Transdermal patches

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12
Q

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

A

Suppositories

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13
Q

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

A

Injections

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14
Q

To provide for optimal drug action through
inhalation therapy

A

Inhalants, Inhalation
aerosols

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15
Q

the framework for product
development.

A

Determine desired product type

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16
Q

Develop and examine initial formulations of the product:

A

a. desired features: drug release profile bioavailability

clinical effectiveness

b. pilot plant studies and production scale-up.

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17
Q

a formulation that best meets the goals of the product

A

Master Formula

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18
Q

Factors to consider before formulation of a medicinal agent in
one or more dosage forms:

A

a. Therapeutic matters (nature of the illness)
b. manner it is treated (locally or through systemic action)
c. age and anticipated condition of the patient.

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19
Q

Before the formulation of a drug substance into a dosage form, it is
essential that:

A
  • It is chemically and physically characterized
  • It defines the nature of the drug substance

This information provides the framework for the drug’s combination
with pharmaceutical ingredients in the preparation of the dosage
form

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20
Q

Considerations for physical characteristics:

A
  • Particle size
  • Crystalline structure
  • Melting point solubility.
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21
Q

Determination of chemical properties

A

-Structure form
- Reactivity

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22
Q

Evaluation of the purity of the chemical substance for:

A
  • Identification and for evaluation of its chemical, physical, and biological properties
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23
Q

Three ways liquid drugs be given in solid form

A
  • Sealed in soft gelatin capsule
  • Developed into a solid ester or salt form suitable for tablets or drug
    capsules
  • Mixed with a solid or melted semisolid material
  • melted mixture is poured into hard gelatin capsules to harden &
    capsules sealed
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24
Q

It gives an indication of particle size and size range of the raw material
along with the crystal structure.
Provide information in formulation processing attributable to
changes in particle or crystal characteristics of the drug.
* Example: spherical and oval powders flow more easily than needle-shaped
powders and make processing easier

A

MICROSCOPIC EXAMINATION

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25
Q

Determines the: purity of the substance
compatibility of various substances before inclusion in the
dosage form

A

MELTING POINT DEPRESSION

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25
Q

depressed melting point

A

Impure substance

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26
Q

sharp melting point

A

Pure substance:

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27
Q

*Phase diagrams constructed determine:

A
  • existence and extent of the
    presence of solid and liquid phases in
    binary, ternary and other mixtures
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28
Q

substances can exist in more than one crystalline form

A

POLYMORPHISM

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29
Q

usually exhibit different physicochemical properties
(including melting pt and solubility)

A

Polymorphic forms

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30
Q
  • Evaluation of: a. Crystal structure (Techniques: microscopy, IR spectroscopy,

thermal analysis, x-ray diffraction)

b. Polymorphism
c. Solvate form

  • Changes in crystal characteristics can influence bioavailability and chemical and physical stability
    can cause implications in dosage forms process functions
A

Polymorphic forms
POLYMORPHISM

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31
Q

is defined as the maximum concentration of a substance
that can be completely dissolved in a given solvent at a certain
temperature and pressure level

A

Drug solubility

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32
Q

Determined by equilibrium solubility method

A
  • excess amount of drug + solvent = shaken at constant temp. over a
    prolonged period of time until equilibrium is obtained
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33
Q

for therapeutic efficacy.

A

A drug must possesses aqueous solubility

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34
Q

incomplete/erratic absorption

A

Insoluble compounds

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35
Q

The smaller the particle size

A

the greater the solubility

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36
Q

If a drug product is formulated into a liquid product:

A

adjustment of pH of solvent to enhance solubility

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37
Q

require extremes in pH outside of accepted physiologic
limits or that may cause stability problems with formulation ingredients.

A

Weak acidic or basic drugs

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38
Q

Adjustment of pH usually has

A

little effect on the solubility of substances other than
electrolytes.

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39
Q

The use of cosolvents or other techniques such as complexation,
micronization, or solid dispersion

A

may improve aqueous solubility

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40
Q

Time it takes for the drug to dissolve in the fluids at the absorption site
(rate-limiting step in absorption).

A

DISSOLUTION RATE

41
Q

Increased Dissolution rate of drugs

A

by decreasing the particle size

42
Q

Dissolution rate of drugs Increased by

A

increasing the solubility of the diffusion layer

43
Q

use a highly water-soluble salt of the parent
substance.

A

For a higher dissolution rate

44
Q

can affect the onset, intensity, and duration of response and control the
overall bioavailability of the drug from the dosage form

A

Dissolution rate

45
Q

2 methods in determining dissolution rates of chemical compounds

A
  1. Constant surface method
  2. Particulate dissolution
46
Q
  • Intrinsic dissolution rate of the agent
  • Characteristic of compound & solvent under fixed experimental conditions
  • Value is expressed as: mg dissolved/min/cm2
A

Constant surface method

47
Q
  • Weighed amount of powdered sample + dissolution medium in constant agitation
    system
  • to study the influence of particle size, surface area, and excipients upon the
    active agent
A

Particulate dissolution

48
Q

Describes the Relationship of diffusion and dissolution of the active drug in the
dosage form and when administered in the body

A

Fick’s law (law of diffusion)

49
Q

Relates to a steady-state flow

A

1st law

50
Q

Relates to a change in conc. of drug with time, at any distance, or a non-
steady state of flow

A

2nd law

51
Q
  • Everted intestinal sac - determines degree & rate of passage of drug through
    the membrane sac by passive & active transport
  • Early assessment of passage of drug molecules across biologic membranes
  • To produce a biologic response - drug molecule must first cross a biologic
    membrane
  • The biologic membrane (lipid barrier) - permits absorption of lipid soluble substance
    by passive diffusion
  • Molecules’ lipophilic character – measured by the oil-water coefficient
A

MEMBRANE PERMEABILITY

52
Q

Interrelationship at the absorption site & absorption characteristics of
various drugs:

A
  • Dissociation constant
  • lipid solubility
  • pH
53
Q

Indication of absorption expectations:

A
  • Data from basic physicochemical studies: pKa, solubility & dissolution rate
54
Q

Selection of appropriate extraction solvents, drug stability, use of salting-out
additives and environmental concerns.

A

PARTITION COEFFICIENT

55
Q

is a measure of a molecule’s lipophilic character;
that is, its preference for the hydrophilic or lipophilic phase. If a solute is added to a
mixture of 2 immiscible liquids, it will distribute between the 2 phases and reach an
equilibrium at a constant temperature.

A

The oil-water partition coefficient

56
Q

strong effect on formulation & pharmacokinetic parameters of
the drug

A

Extent of ionization of drug

57
Q

is determined by potentiometric titration

A

Dissociation constant (pKa)

58
Q

for the pharmacist important:

A

-predicting precipitation in admixtures
-calculating solubility of drugs at certain pH values

59
Q

-Extent a product retains within specified limits and through its
period of storage and use

A

STABILITY

60
Q

Stability studies conducted in the preformulation phase:

A

Stability studies conducted in the preformulation phase:

61
Q

-important for
preformulation.

  • Presence of impurities can lead to erroneous conclusions in some evaluation
    parameters
A

physical and chemical stability of pure drug substances

62
Q

-Chemically, drug substances with different susceptibilities toward chemical
instability:

A

alcohols, phenols, aldehydes, ketones, esters, ethers, acids, salts, alkaloids, glycosides
and others.

63
Q

Most frequently encountered destructive process:

A

-HYDROLYSIS (solvolysis process)
-OXIDATION

64
Q
  • Drug molecules interact with water molecule to yield breakdown product.
    Example: Aspirin or ASA, combines with water molecules and hydrolyzes into a

molecule of salicylic acid and acetic acid

A

Hydrolysis (solvolysis process)

65
Q

Susceptible to the hydrolytic process:

A

esters, substituted amides,
lactones, and lactams

66
Q
  • loss of electrons from an atom or molecule;
  • loss of hydrogen (dehydrogenation) from a molecule
  • involves free radicals (molecules or atoms containing one or more
    unpaired electrons).
  • Destructive to: aldehydes, alcohols, phenols, sugars, alkaloids &
    unsaturated fats & oils
A

OXIDATION

67
Q

Five types of stability

A
  1. CHEMICAL
  2. PHYSICAL
  3. MICROBIOLOGIC
  4. THERAPEUTIC
  5. TOXICOLOGIC
68
Q

–active ingredient retains chemical integrity and labeled
potency within the specified limits.
- important for selecting:
*storage conditions (temperature, light, humidity)
*proper container for dispensing
*anticipating interactions when mixing drugs & dosage forms
- must know reaction order & rate

A

CHEMICAL

69
Q

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

A

PHYSICAL

70
Q

–sterility/resistance to microbial growth

A

MICROBIOLOGIC

71
Q

therapeutic effect remains unchanged

A

THERAPEUTIC

72
Q

no significant increase in toxicity occurs.

A

TOXICOLOGIC

73
Q
  • description of the drug concentration with respect to time.
A

RATE REACTIONS

74
Q
  • estimate the shelf life of a product that has been stored or to be
    stored under a different set of conditions.
A

Q10 METHOD

75
Q

*Water reduced or eliminated from the system.
*Water-liable drugs - waterproof protective coating applied in the tablet.
*In liquid formulation - water replaced by substitute liquids.

*Suspending them in nonaqueous vehicle
*For injectable products – anhydrous vegetable oils may be used as solvent

A

Drugs subjected to hydrolysis

76
Q

anhydrous vegetable oils may be used as solvent for

A

injectable products

77
Q

Aqueous preparation is desired
- supplied in dry form for reconstitution before dispensing

A

For unstable antibiotic drugs

78
Q

storage under refrigeration

A

For unstable preparations

79
Q

– major determinant in stability

A

pH

80
Q

optimum stability

A

pH 5 & 6

81
Q

increases stability

A

buffering agents

82
Q
  • prepared in dry state
    *packaged in sealed containers with air replaced by inert gas (Nitrogen,
    carbon dioxide).
A

Oxygen sensitive drugs

83
Q

In Aqueous Preparations:
Ex: Na2SO3, NaHSO3, H3PO3, ascorbic acid

A

add antioxidants (for stability):

84
Q

Inoleaginous/unctous prepns:
Ex: alpha tocopherol, butylhydroxyanisole & ascorbyl parmitate

A
  • add antioxidants (for stability):
85
Q
  • add antioxidants (for stability):
A
  • In Aqueous Preparations: Ex: Na2SO3, NaHSO3, H3PO3, ascorbic acid
  • In oleaginous/unctous prepns:
    Ex: alpha tocopherol, butylhydroxyanisole & ascorbyl parmitate
86
Q

source of difficulty in preparing stable solutions of oxidizable
drugs

A

Trace metals in drug, solvent, container or stopper

87
Q

Trace metals in drug, solvent, container or stopper - Eliminated by:

A

*purification of source of contaminant
*complexing or binding metal by using specialized agents
(chelating agents- Ca disodium edetate & EDTA)

88
Q
  • catalyst to oxidation reactions
  • preparations were packaged in light resistant or opaque containers
A

Light

89
Q

easily oxidizable drugs may be stabilized
in formulation by considering

A
  • selective exclusion from the system of:
    oxygen
    oxidizing agents
    trace metals
    light
    heat
    other chemical
    catalysis
  • add to create and maintain a favorable pH:
    antioxidants
    chelating agents buffering agents
90
Q
  • reaction between two or more identical molecules with resultant
    formation of new & generally larger molecule (Ex: Formaldhyde)
A

Polymerization

91
Q

Process where one or more active chemical groups removed:

A
  • Chemical decarboxylation
  • Deamination
92
Q

Decomposition of Carboxylic acid (RCOOH) & release of CO2

A

Decarboxylation

93
Q
  • Removal of nitrogen containing group from organic amine (Ex. Insulin)
A

Deamination

94
Q

Importance of Drug Stability
* In Pre-clinical testing and in clinical (human) trials

A
  • for a true and accurate assessment of the drug/drug prod evaluated
95
Q

Importance of Drug Stability
* Marketed drug product

A
  • for the safety and effectiveness when distributed and during the entire
    course of its shelf-life and use
96
Q

Product stability assessed before marketing:

  • Formulation
  • Influence of:
A
  • pharmaceutic ingredients present
  • container & closure
97
Q

Product stability assessed before marketing:

A
  • Formulation
  • Influence of:
  • pharmaceutic ingredients present
  • container & closure
  • Manufacturing & processing conditions
  • Packaging components & conditions of warehousing/storage
  • Conditions of shipping, temp., light & humidity
  • Shelf life & patient utilization
98
Q

Stability testing considerations

A
  • Product containers, closures, and other packaging features
  • Parenteral and other sterile prods must meet sterility test standards
  • to ensure protection against microbial contamination
99
Q

Drug instability detected

A
  • Change in:
    a. physical appearance,

b. color,
c. odor,
d. taste, or
e. texture of the formulation

PH107:Pharmaceutical Dosage Form, Drug Delivery System & Medical Devices (13 decks)

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