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PharmSci Exam 1 > Lecture 3: Pharmaceutical Formulations And Delivery Systems > Flashcards

Lecture 3: Pharmaceutical Formulations And Delivery Systems Flashcards

1
Q

Pharmaceutics

A

Area of study concerned with the formulation, manufacture, stability and effectiveness of dosage forms

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2
Q

Biopharmaceutics

A
  • study of the relationship between the physical, chemical and biological properties of a drug substance, dosage form and drug action
  • study of physiochemical factors of drug dosage forms that influence the rate and extent of systemic drug absorption
  • aim of biopharmaceutics is to adjust the delivery of the drug substance to the site of action to provide optimal therapeutic activity
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3
Q

Importance of drug delivery

A
  • a drug is not effective unless it is present at its site of action for an adequate period of time
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4
Q

What percentage of drugs that are developed fail because they cannot be adequately delivered to the desired target?

A

50%

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5
Q

What are two approaches to achieve efficient drug delivery?

A
  • suitable drug delivery system/dosage form

- drug modification

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6
Q

What is a drug substance?

A

Active pharmaceutical ingredient (API)

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7
Q

What are pharmaceutical ingredients?

A

AKA excipients or non-medicinal agents

Components other than the active drug included in the final dosage form

Generally viewed as being inert

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8
Q

What makes up the drug product?

A

Drug substance + excipients (pharmaceutical ingredients)

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9
Q

Why creat dosage forms?

A
  • consistent accurate dosage administration
  • convenient administration
  • palatable form of administration
  • controlled-release of drug upon administration
  • protect drug substance from environmentally-induced degradation
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10
Q

Types of dosage forms

A
  • liquid
  • solid
  • semi-solid
  • pharmaceutical inserts
  • parenterals
  • novel drug delivery systems
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11
Q

What are these examples of:

Powders, granules, tablets, aerosols, creams…

A

Dosage forms

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12
Q

What are these examples of?

Binders, flavors, sweeteners, film coatings, disintegrants…

A

Pharmaceutic ingredients

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13
Q

What is the purpose of pharmaceutic ingredients?

A
  • improve patient acceptability
  • improve product stability
  • optimize production processes
  • enable product identification
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14
Q

What are some preformulation considerations?

A
  • physiochemical characteristics of the drug
  • target site for the drug
  • intended therapeutic use
  • age of target population
  • compatibility
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15
Q

Preformulation studies of drug substance

A
  • solubility
  • dissolution rate
  • particle size and distribution
  • membrane permeability
  • polmorphism
  • pKa/dissociation constants
  • stability
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16
Q

Dissolution

A

Process by which a solid of only fair solubility enters solution

Time for drug substance to dissolve in fluids at absorption site

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17
Q

Dissolution rate

A

A solid particle with surface area S [cm2] dispersed in a solvent of volume V is surrounded by a stagnant layer of thickness h [cm]

Diffusion coefficient D [cm2/sec]

M is the mass of solute dissolved in time t

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18
Q

Noyes-whitney equation for dissolution rate

A

DM/dt = DS/h(Cs - C)

dC/dt = dS/vh (Cs-C)

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19
Q

Modified release

A

Dosage forms with drug release features based on time, course, or location that are designed to accomplish therapeutic or convenience objectives not achieved with immediate-release forms

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20
Q

Modified released products examples

A

Orally administered tablets and capsules
Transdermal patches
Ocular, parenteral, subdermal, vaginal forms

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21
Q

USP differentiates modified release as

A

Extended release

Delayed release

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22
Q

Delayed release dosage forms

A

Release drug at a time other than immediately after administration

Enteric-coated tablets

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23
Q

Extended release dosage forms

A

Sustained

Those that allow a reduction in dosing frequency compared with a conventional (immediate release) dosage form

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24
Q

Controlled release systems include what?

A

A component that can be engineered to regulate essential characteristic (rate or duration of release) and have a duration of action longer than a day

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25
Q

Rationale for extended release

A
  • many drugs are inherently short-lasting and require multiple daily dosing
  • multiple daily dosing is inconvenient for the patient
  • conventional immediate release forms cause sequential therapeutic blood level peaks and valleys
26
Q

Advantages for extended-release dosage forms

A
  1. Less fluctuation in drug blood levels
  2. Frequency reduction in dosing
  3. Enhanced convenience and compliance
  4. Reduction in adverse side effects
  5. Reduction in overall health care costs
27
Q

What makes drugs suitable for extended release?

A
  1. Neither very slow nor very fast rates o absorption and excretion
  2. Uniformly absorbed from the gastrointestinal tract
  3. Administered in small doses
  4. Good margin of safety
  5. Treatment of chronic rather than acute conditions
28
Q

What are some advantages for the patient for using tablets and capsules?

A
  • accuracy of dosage
  • ease of administration
  • compactness
  • portability
  • readily identified
  • blandness of taste
29
Q

What are some advantages for the manufacturer using tablets and capsules?

A
  • simplicity of preparation

- stability

30
Q

Capsules

A
  • Enclosed in hard or soft shell
  • Primary composition of shell is gelatin
  • Commonly used in clinical drug trials
  • flexibility of being filled extremporaneously or in large quantities commercially
31
Q

Capsule size ranges

A 
Largest = 000 (~600mg)
Smallest = size 5 (~5mg)
32
Q

What are the goals of capsule formulation?

A
  • provide accurate dosage
  • insure good bioavailability
  • ease of production
  • good stability
  • attractive appearance
33
Q

What is gelatin NF made up of?

A

Partially hydrolyzed collagen of animal skin, CT and bones

34
Q

What is gelatin type A?

A

Acid processing of pork skins

35
Q

What is the pI of type A gelatin?

A

7.0 - 9.0

36
Q

What is type B gelatin made out of?

A

Alkali processing of bones and animal skins

37
Q

What is the pI of type B gelatin?

A

4.8 - 5.0

38
Q

Bone and pork skin gelatin contributions

A
  • bone gelatin contributes firmness

- pork skin gelatin contributes plasticity and clarity

39
Q

What are the two main physiochemical properties of gelatin?

A
  • bloom strength

- viscosity

40
Q

What is bloom strength?

A

Empirical measure of gel strength

Measured in bloom gelometer

41
Q

Properties of gelatin

A
  • insoluble in cold water
  • soluble in hot water
  • soluble in warm gastric fluid
  • tasteless
  • biodegradable
  • stable in dry form
  • susceptible to microbial decomposition
42
Q

Why is gelatin ideal material?

A
  • swells, but is insoluble in cold water and readily soluble in water
  • ability to form thermally reversible gel
  • excellent film forming properties
  • freely soluble in stomach secretions
  • as a protein, gelatin is digested to AAs that can be absorbed
43
Q

Soft gelatin capsules

A
  • Gelatin + glycerin or sorbital + preservative
  • Preservative need because of higher % water in final capsule
  • may be single or two tone in color
  • filled and formed simultaneously
44
Q

Two general classes of tablets

A

Compressed (large scale production)

Molded (small scale operations)

45
Q

Types of compressed tablets

A
  • sugar coated
  • film coated
  • enteric coated (delayed release)
  • controlled reelase
46
Q

Qualities of a good tablet

A
  • accurate and uniform weight
  • homogeneity
  • absence of incompatibilities
  • stability and hardness
  • ease of disintegration
  • reasonable size and shape
  • pleasing appearance
  • ease of manufacturing
  • economy of production
47
Q

Enteric-coated tablets

A
  • form of delayed-release
  • designed to pass unchanged through stomach
  • tablet disintegration in intestine allowing drug dissolutioin and absorption
48
Q

What type of drugs are enteric coatings used for?

A
  • shown to have substantially higher absorption in intestine when stomach is by-passed
  • unstable at gastric pH
  • irritating to gastric mucosa
49
Q

Diluents (fillers bulking agents)

A
  • increase bulk for ease of compression and adjust to desired size and shape

EX: dicalcium phosphate, lactose, kaolin, mannitol, sodium cholride

50
Q

Binders or adhesives

A
  • promote particle adhesion

- impart cohesiveness to formulation for tablet integrity

51
Q

What is the optimum binder amount and type are used to ensure?

A
  • sufficient tablet harness

- timely disintegration and dissolution

52
Q

Common binders or adhesives

A 
Starch paste
Gelatin
Sugars
Waxes
Poly (PVP)
Gums
Polyethylene glycol
Cellulose derivatives
53
Q

Lubricants and antiadherents

A
  • prevent adhesion of material to machine components
  • facilitate ejection of tablets from the die by reducing adherence to die walls
  • ## minimize wear of the punches and dies
54
Q

Common compounds with lubricants and antiadherents

A
  • talc
  • magnesium stearate
  • calcium stearate
  • polyethylene glycol
55
Q

Disintegrants

A
  • promote the breakup of the tablet (after administration) into smaller particles
  • pre-requisite to drug absorption
  • draw water into the tablet by capillary effect. Causes tablet to swell and burst apart
56
Q

Commonly used disintegrants

A

Starches

Modified starches

57
Q

Colorants

A
  • enhance aesthetic appearance
  • aid product identification
  • lack of international agreement on approved list of pharmaceutical colors limits globally acceptable choices
58
Q

Flavoring agents and sweeteners

A
  • routinely used for chewable tablets

- flavors are available as oils or spray dried beadlets

59
Q

Commonly used sweeteners

A

Mannitol
Xylitol
Lactose
Dextrose

60
Q

Wetting agents

A
  • used along with poorly soluble drug

- enhance dissolution rate

PharmSci Exam 1 (4 decks)

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