Munson Lectures Flashcards

1
Q

Routes of Administration

A

Ophthalmic
Otic
Nasal
Oral
Sublingual
IM
SubQ
IV
Topical
Rectal
Urethral
Vaginal

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2
Q

Percentages of Routes of Administration

A

Oral - 47%
Parenteral - 18%
Pulmonary - 16%
Transdermal - 11%

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3
Q

Tablets/Capsules

A
  • stable
  • accurate dose
  • easy to use
  • lower cost
  • taste mask and controlled release

Disadvantage:
- not suitable for infants
- not suitable for non-oral medications

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4
Q

IV

A
  • fast drug action
  • suitable for drugs who can’t tolerate GI movement
  • suitable for patients unable to swallow

Disadvantage:
- expensive
- not convenient
- painful at times

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5
Q

Transdermal

A

local treatment

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6
Q

Intranasal Spray

A
  • local treatment
  • systemic drug delivery
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7
Q

How to Choose?

A

dictated by disease state, convenience, and marketing

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8
Q

Types of Solid Dosage Forms

A
  • tablets
  • gelcaps
  • loose powders
  • lyophilized powder
  • controlled release
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9
Q

Types of Tablets

A
  • Compressed (uncoated or sugar coated)
  • film coated
  • enteric coated
  • layered
  • chewable
  • tablet for solution
  • effervescent
  • dispensing
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10
Q

Advantages of Tablet to Manufacturer

A
  • simplicity and economic for preparation
  • stability
  • convenience for packaging
  • shipping/ dispensing was easy
  • accuracy of dosing
  • compactness
  • portability
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11
Q

Advantages of Tablets for Patient

A
  • accuracy of dosing
  • compactness
  • portability
  • blandness of taste
  • easy administration
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12
Q

Sugar-Coated Tablets

A
  • formed by compression
  • used for taste masking or identification
  • enhance stability
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13
Q

Process of Sugar Coated Tablet

A
  • sealing coat
  • subcoat to interface between sealing and main coat
  • apply multicoat of starch, calcium carbonate, etc
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14
Q

Film-Coated Tablets

A
  • avoid use of moisture and water
  • place markings on tablets
  • polymeric
  • add colorant
  • unique properties pertaining to release
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15
Q

Multiple Compression Tablet

A
  • inner core and a coating
  • inner core was a sugar tablet
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16
Q

Multiple Layer Tablet

A
  • lightly compress one layer
  • then add another layer
  • used for different types of release
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17
Q

Enteric-Coated Tablet

A
  • resist dissolving in stomach pH but dissolved in higher pH
  • used in drugs than can irritate stomach
  • CANNOT BE CRUSHED OR CHEWED
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18
Q

Chewable Tablets

A
  • help solubility
  • avoid swallowing problems
  • no disintegrant
  • mannitol filler is common
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19
Q

Effervescent Tablet

A
  • dissolve in glass of water prior to administration
  • release carbon dioxide
  • facilitates fast action
  • must be avoided from moisture so placed in blister packs
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20
Q

Hard Gelatin Capsule

A
  • used in most capsules
  • made from collagen

Manufacturing
- snap together or heat sealed

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21
Q

Soft Gelatin Capsule

A
  • added softening agent
  • used for liquids, suspensions, pastes
  • made from collagen

Manufacturing
- used two ribbons

22
Q

Difference between Solid vs Solution

A

Solid
- slow acting
- more stable
- more convenient
- common for oral

Solution
- faster acting
- less stable
- for injections commonly

23
Q

Preformulation of Dosage Form

A

determining the physiochemical properties necessary to formulate compound

24
Q

Formulation of Dosage Form

A

determining the route and composition of final dosage form

25
Q

Manufacturing of Dosage Form

A

what unit operations are necessary

26
Q

Solubility

A

maximum amount of solute that can be dissolved in a given amount of solvent

mostly a low solubility

27
Q

3 States

A

Completely Soluble
Supersaturated
Very supersaturated

high levels of supersaturation will cause crystallization

28
Q

Physical Stability

A
  • transformation to different crystal forms

crystalline to amorphous, hydrates, solvates, etc

29
Q

Chemical Stability

A
  • chemical reaction involved
  • results in degradation product that must be characterized
30
Q

Types of Chemical Reactions

A

Hydrolysis
Oxidation
Photolysis
Dehydration

31
Q

Why can’t we administer drug substance?

A
  • unstable
  • taste masking needed
  • hard to administer
32
Q

How to make a stable dosage form that is easy to administer?

A

Add other ingredients that help stabilize the dosage form —> excipients

33
Q

Types of Excipients

A
  • Diluent
  • Disintegrant
  • Binder
  • Lubricant
  • Glidant
  • Controlled Release
34
Q

Diluent

A
  • referred to ask bulking agent
  • needed to make the practical weight for tablet
  • helps in the composition
  • enhances powder flow in manufacturing
35
Q

Examples of Diluents

A

Microcrystalline cellulose

Lactose

Calcium Phosphate

Starch

36
Q

Disintegrant

A
  • breaks up the solid dosage form enhancing dissolution
  • performed by water uptake or swelling
37
Q

Examples of Disintegrants

A

Sodium Starch Glycolate

Croscarmellose

Crospovidone

Starch

38
Q

Binders

A
  • gives tablet the mechanical strength
  • performed by water uptake or swelling
39
Q

Example of Binders

A

Polyvinyloyrrolidone

Starch

Microcrystalline cellulose

Polymer

40
Q

Lubricant

A
  • prevents adherence of tablet to the die
  • levels of 0.5-2%
  • overlubrication is bad
41
Q

Example of Lubricant

A

Magnesium Stearate

Stearin Acid

Lubritab

Talc

42
Q

Glidant

A
  • improves powder flow
  • stops friction
  • very fluffy
43
Q

Example of Glidant

A

Silica

Talc

44
Q

Controlled Release

A
  • used to extend the release of the drug from matrix
  • can be used to coat a tablet for specific release in body
45
Q

Example of Controlled Release

A

Hydroxypropylmethylcellulose

Xanthan gum

Eudragits

46
Q

Coloring Agent

A
  • improve esthetics
  • identification technique
  • control product

MUST BE APPROVED BY FDA

47
Q

What is needed to be known about the drug?

A

Physiochemical properties

Mechanical properties

Bio pharmaceutical properties

48
Q

Physical and Chemical Properties

A

Aqueous Solubility
- concentration at which the solution is in equilibrium with solid phase
- depends on temperature and pressure
- key to bioavailability

Dissolution Rate
- determines how quickly drug goes into solution
- can be enhanced by fast moving agents
- important for in vivo

Ionization Constant
- protonated or unprotonated?

Polymorphism
- ability for molecule to adopt two or more conformations of molecules in crystal
- can effect bioavailability
- can have multiple crystalline forms

Amorphous
- unstable and wants to crystallize
- enhanced bioavailability
- enhanced solubility

Hydroscopicity
- amount of water taken up by solid
- can effect stability and manufacturing

49
Q

Mechanical Properties

A

Compression and Compaction
- Elastic: reversible and deforms
- Plastic: irreversible and deforms
- Fracture: material breaks

50
Q

Manufacturing Unit Operations

A

Weighing
Blending
Milling
Granulation
Drying
Compaction
Coating
Packaging