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Drug Dosage Forms > Dosage Form Design: Pharmaceutical And Formulation Considerations > Flashcards

Dosage Form Design: Pharmaceutical And Formulation Considerations Flashcards

1
Q

Study on formation, 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

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3
Q

Uses of pharmaceutical ingredients

A

solubilize
thicken
stabilize
flavor
suspend
dilute
preserve
efficacious
suspend
emulsify
color
appealing
closure forms.

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4
Q

THE NEED FOR DOSAGE FORM DESIGN

A
  • To protect the drug substance from the destructive influences of atmospheric oxygen or humidity. (Coated tablets)
  • To protect the drug substance from the destructive influence of gastric acid after oral administration. (Enteric-coated)
  • To conceal the bitter, salty or offensive taste or odor of a drug substance. (Capsules, Flavored syrups)
  • To provide liquid preparations of substances that are either insoluble or unstable in the desired vehicle. (Suspension
  • To provide clear liquid dosage forms of substances. (Syrups, Solutions)
  • To provide rate-controlled drug action.
    (Controlled-release tablets)
  • To provide optimal drug action from topical administration sites. (Ointments,Creams, Transdermal patches)
  • To provide for insertion of a drug into one of the body’s orifices (Suppositories)
  • To provide placement of drugs directly in the bloodstream or body tissues (Injections)
  • To provide for optimal drug action through inhalation therapy (Inhalants, Inhalation aerosols)
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5
Q

GENERAL CONSIDERATIONS IN
DOSAGE FORM DESIGN

A

Determine desired product type
Develop and examine initial formulations master formula

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6
Q

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

A
  • Therapeutic matters
  • manner it is treated
  • age and anticipated condition of the patient.
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7
Q

PREFORMULATION STUDIES

A
  1. PHYSICAL DESCRIPTION
  2. MICROSCOPIC EXAMINATION
  3. MELTING POINT DEPRESSION
  4. PHASE RULE
  5. PARTICLE SIZE DISTRIBUTION
  6. EVALUATION OF POLYMORPHISM
  7. SOLUBILITY
  8. DISSOLUTION RATE
  9. MEMBRANE PERMEABILITY
  10. BASIS OF PH-PARTITION COEFFICIENT
  11. PKA / DISSOCIATION CONSTANTS
  12. STABILITY
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8
Q

Three properties of Physical Description

A
  • Physical Property
  • Chemical Property
  • Biologic Property
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9
Q

What are under the Physical Properties?

A
  • Crystalline structure
  • particle size
  • melting point solubility
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10
Q

What are under the Chemical Properties?

A
  • Structure
  • Form
  • Reactivity
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11
Q

Its ability to get to site of action and elicit a biologic response

A

Biologic Property

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12
Q

What is under the Microscopic Examination?

A

particle size
size range
crystal structure

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13
Q

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

A

MELTING POINT DEPRESSION

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14
Q

Two Types of Substances

A

Pure subs: sharp melting point

Impure subs: depressed melting point

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15
Q

Phase diagrams constructed determines:

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

PHASE RULE

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16
Q
  1. PARTICLE SIZE DISTRIBUTION
A

affects : physical–chemical properties of drug sub’s:

  • dissolution rate
  • bioavailability
  • content uniformity
  • stability taste
  • texture
  • flow properties
  • absorption
  • sedimentation rate
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17
Q

substances can exist in more than one crystalline form

A
  1. EVALUATION OF POLYMORPHISM
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18
Q

Different physical-chemical properties (incl. melting pt. & solubility)

A

Polymorphic forms

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19
Q
  • Determined by equlibrium solubility method

Drug possess aqueous solubility - for therapeutic efficacy.

  • Insoluble compounds: incomplete/erratic absorption
  • Solubility & particle size
  • Solubility & pH
A

SOLUBILITY

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20
Q

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

A

DISSOLUTION RATE

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21
Q

increased by decreasing the particle size

A

Dissolution rate of drugs

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22
Q

use a highly water soluble salt of the parent Substance.

A

for higher dissolution rate

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23
Q

2 methods in determining dissolution rates of chemical compounds

A

1.Constant surface method
2.Particulate dissolution

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24
Q
  • intrinsic dissolution rate of the agent
  • Characteristic of compound & solvent under fixed experimental conditions mg dissolved/min/cm square
A

Constant surface method

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25
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

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26
Q
  • describes the: relationship of diffusion & dissolution of the active drug in the dosage form & when administered in the body
A

FICK’S LAW (LAW OF DIFFUSION)

27
Q

relates to a steady state flow

A

1st Law of Fick’s

28
Q

relates to a change in conc. of drug with time, at any distance, or a nonsteady state of flow

A

2nd Law of Fick’s

29
Q

Everted intestinal sac

A
  • 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
30
Q

To produce a biologic response______

A

drug molecule must first cross a biologic membrane

31
Q

measured by the oil-water coefficient

A

Molecules’ lipophilic character

32
Q

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

  • Dissociation constant
  • lipid solubility
  • pH
A

BASIS OF PH-PARTITION COEFFICIENT

33
Q

Indication of absorption expectations:

A

Data from basic physicochemical studies: pKa, solubility & dissolution rate

34
Q

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

A
  • Dissociation constant
  • lipid solubility
  • pH
35
Q

strong effect on formulation & pharmacokinetic parameters of the drug

A

extent of ionization of drug

36
Q
  • for the pharmacist important:
    *predicting precipitation in admixtures
    *calculating solubility of drugs at certain pH values
A

determined by potentiometric titration

37
Q

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

A

STABILITY

38
Q

Stability studies conducted in the
preformulation phase:

A
  • Solid-state of the drug alone
  • Solution phase with the expected excipients
39
Q

Evaluation of physical and chemical stability of pure drug substances - important for preformulation.

A

DRUG AND DRUG PRODUCT STABILITY

40
Q

Chemically drug substances with different susceptibilities toward chemical instability:

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

A

Drug Stability : Mechanisms of Degradation

41
Q

MOST FREQUENTLY ENCOUNTERED DESTRUCTIVE PROCESS:

A

-Hydrolysis (solvolysis process)
-Oxidation

42
Q
  • (drug) molecules interact with water molecule to yield breakdown product.
  • susceptible to the hydrolytic process: esters, substituted amides, lactones, and lactams
A

Hydrolysis (solvolysis process)

43
Q

Oxidation

A

-loss of electrons from an atom or molecule;

-involves free radicals (free radicals (molecules or atoms containing one or more unpaired electrons).

-destructive to: aldehydes, alcohols, phenols, sugars, alkaloids & unsaturated fats & oils

44
Q

OTHER DESTRUCTIVE PROCESS IN PHARMACEUTICAL PREPARATIONS

A

Polymerization

45
Q

reaction between two or more identical molecules with resultant formation of new & generally larger molecule

A

Polymerization

46
Q

Process where one or more active chemical groups is removed:

A
  • Chemical decarboxylation
  • Deamination
47
Q

Decarboxylation decomposition of RCOOH & release of CO2

A

Chemical decarboxylation

48
Q

Removal of nitrogen containing group from organic amine (ex. Insulin)

A

Deamination

49
Q

DRUG AND DRUG PRODUCT STABILITY:

A
  • KINETICS AND SHELF LIFE
  • RATE REACTIONS
  • Q10 METHOD
50
Q

A. KINETICS AND SHELF LIFE
(FIVE TYPES OF STABILITY)

A

CHEMICAL AI
PHYSICAL
MICROBIOLOGIC
THERAPEUTIC
TOXICOLOGIC

51
Q

retains chemical integrity and labelled potency w/in the specified limits

A

CHEMICAL AI

52
Q

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

A

PHYSICAL

53
Q

sterility/resistance to microbial growth

A

MICROBIOLOGIC

54
Q

therapeutic effect remains unchanged

A

THERAPEUTIC

55
Q

no significant increase in toxicity occurs.

A

TOXICOLOGIC

56
Q

description of the drug concentration with respect to time.

A

RATE REACTIONS

57
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

58
Q

IMPORTANCE OF DRUG STABILITY

A

in preclinical testing and in clinical (human) trials
- for a true and accurate assessment of the drug/drug prod evaluated

marketed drug product
- for the safety and effectiveness when distributed and during the entire course of its shelf-life and use

59
Q

water reduced or eliminated from the system

A

ENHANCING STABILITY (DRUGS SUBJECTED TO HYDROLYSIS)

60
Q

waterproof protective coating applied in the tablet.

A

water-liable drugs

61
Q

major determinant in stability

A

pH

62
Q

optimum stability

A

pH 5 & 6

63
Q

increases stability

A

buffering agents

64
Q
  • catalyst to oxidation reactions
  • preparations packaged in light resistant or opaque containers
A

LIGHT

Drug Dosage Forms (8 decks)

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