Dosage Forms I Final

Front 1

How are tablets dangerous to the lumen of the esophagous?

Back 1

Adhesion leading to irritatiom, inflammation or even ulceration

Front 2

T/F:
The espohagous is coated with muscous with lots of water

Back 2

False, little water

Front 3

Tablets should not be taken by mouth in what positions?

Back 3

On back or stomach

Front 4

Shape, size, surface properties, patient position, volume of water and disease are all factirs predisposing to ?

Back 4

Adhesion

Front 5

How should a tablet be taken to minimize the risk of adhesion?

Back 5

While standing with water at least one hour before bedtime

Front 6

Lozenges, troches, chewable, vaginal inserts, effervescent, fast dissolving, buccal/sublingual are all types of what dosage form?

Back 6

Tablets

Front 7

Are lozenges intended for slow or fast dissolving and for local or systemic effect?

Back 7

Slow
Local

Front 8

Lozenges are formulated like?

Back 8

Candy

Front 9

How are troches made?

Back 9

Compression into a hard disc

Front 10

What is the purpose of mannitol or xylitol in chewable tablets?

Back 10

To give a cooling sensation

Front 11

What is the purpose of effervescent tablets? (2)

Back 11

To mask taste and help break apart tablet

Front 12

How is an effervescent tablet made?

Back 12

By compressing a drug with effervescent salt mixtures (Na bicarb and citric acid)

Front 13

What compound is released from an effervescent tablet?

Back 13

CO2

Front 14

T/F:
Effervescent tablets are generally designed to by dissolved in liquid prior to ingestion.

Back 14

True

Front 15

________ tablets are relatively new and is designed to disintegrate in the mouth before swallowing.

Back 15

Fast- dissolving tablets

Front 16

What are the 2 claims for fast dissolving tablets?

Back 16

Easier to take and swallow (no need for water)
Possible faster onset on action (due to faster disintegration/ dissolution)

Front 17

When would fast- dissolving tablets not have a faster onset of action?

Back 17

When the drug particles are coated, in this case the dissolution is rate limiting

Front 18

What are 3 ways to make a fast- dissolving tablet?

Back 18

Lyophilization (freeze- drying)
Direct compression with disintergrates
Molding

Front 19

What is the problem with using effervescent excipients in direct compression to formulate fast- dissolving tablets?

Back 19

Very hydroscopic (larger SA) so must be well protected

Front 20

Why are lyophilization made fast dissolving tablets often handled and packaged with care?

Back 20

Very sponge- like so brittle

Front 21

Sublingual and buccal drug delivery is also know as?

Back 21

Transmucousal drug delivery

Front 22

What is the name of the area lining the cheek between the cheek and gum?

Back 22

Buccal

Front 23

What is the ventral surface of tongue and floor of mouth?

Back 23

Sublingual area

Front 24

What are the 2 general purposes for administering drugs to the oral cavity?

Back 24

To achieve systemic effect
To achieve local effect

Front 25

Structures and properties of the oral mucosae are ____________ between the intestinal mucosa and epidermis.

Back 25

Intermediate

Front 26

The epithelium of the oral mucosae has what types of cells?

Back 26

Squamous

Front 27

What is the 2 characteristics of the oral mucosae epithelium?

Back 27

Principle barrier for drug absorption
Highly vascularized (good for systemic delivery)

Front 28

What is the purpose of keratinization in the oral mucosae?

Back 28

To form tough barriers (palate)

Front 29

T/F:
Buccal and sublingual membranes are keratinized.

Back 29

False, they are NOT keratinized

Front 30

Which membrane is thicker, the buccal or the sublingual?

Back 30

Buccal

Front 31

Which is more permeable, the buccal or sublingual membrane?

Back 31

Sublingual

Front 32

What is the pH of saliva?

Back 32

7

Front 33

What variation in the oral mucosae is critical for drug delivery?

Back 33

Saliva, but can also wash it away

Front 34

What are the advantages of sublingual/ buccal delivery? (3)

Back 34

1. Avoidance of GI acid degradation, GI enzymtic degradation, and hepatic first pass effect
2. Can achieve rapid onset of action and high blood levels
3. Can also be used for prolonged action

Front 35

By avoiding the passage of GI degradation, where does the drug drain into when taken sublingual or buccal?

Back 35

Jugular vein

Front 36

What drug is an example of the advantages to rapid onset and high blood levels in buccal/sublingual delivery?

Back 36

SL NTG 1-3 minutes

Front 37

T/F:
The buccal delivery can be used for prolonged action and can last up to several hours.

Back 37

True

Front 38

What are the 3 disadvantages of sublingual/ bucaal drug delivery?

Back 38

1.Relatively low permeability for most dugs
2. The drug can be washed away
3. Sometimes unpredictable bioavailablity

Front 39

What was the 1st patch drug?

Back 39

NTG

Front 40

What type of drugs are best absorbed in sublingual/ buccal drug delivery?

Back 40

Small, lipophillic drugs

Front 41

Why does sublingual/buccal drug delivery have relatively low permeability as a disadvantage?

Back 41

Because of their skin- like barrier properties

Front 42

How can a drug be washed away in sublingual/buccal delivery? (3)

Back 42

Saliva, eating, and drinking

Front 43

What product is designed for rapid release over a short period of time?

Back 43

Sublingual products

Front 44

What product is generally designed for slower drug release over a sustained period of time?

Back 44

Buccal products

Front 45

Why are buccal products usually better for slower drug release over a sustained period of time?

Back 45

They have a lower permeability
They are easier to keep in place

Front 46

What will happen to a sublingual delivered drug if it wasnt rapidly released over a short period of time?

Back 46

It would be washed away before being absorbed

Front 47

T/F:
All buccal delivered products are intended for slower drug release.

Back 47

False, some give fast relief
eg. fentanyl

Front 48

Why should drugs and excipients be bland and non irritating?

Back 48

To avoid stimulating saliva flow

Front 49

What are the 2 examples mentioned in the notes of sublingual dosage forms?

Back 49

Compressed and molded tablets

Front 50

Sublingual tablets are designed to?

Back 50

Dissolve rapidly and leave little residue

Front 51

Why are compressed sublingual tablets lightly compressed?

Back 51

To facilitate disintegration

Front 52

What is the purposes of lactose in SL NTG tablets?

Back 52

To reduce volatility and explosive risks by absorbing NTG

Front 53

What are two examples of SL compressed tablets?

Back 53

Isosorbide dinitrate and nitroglycerin

Front 54

What type of SL dosage form is prepared by forcing a moistened blend of drug and excipients into a mold, followed by forcing the wet mass out of the mold and allowing to dry?

Back 54

Molded tablets

Front 55

T/F:
Molded tablets tend to be harder then compressed tablets

Back 55

False, softer

Front 56

What are the excipients found in NTG tablets that where mention in the table?

Back 56

Lactose and polyethylene glycol

Front 57

What is the purpose of Polyethylene glycol in NTG tablets?

Back 57

Lower vapor pressure

Front 58

Tablets are usually dried under _________ conditions to limit NTG evaporation.

Back 58

Ambient

Front 59

What kind of container must NTG tablets be dispensed in?

Back 59

Glass, NTG interacts with plastic and will pass through it

Front 60

NTG should be discarded ____ months after opening because NTG slowly evaporates.

Back 60

6

Front 61

T/F:
Nitroglycerin- Nitrolingual spray has a short shelf life.

Back 61

False, long

Front 62

Chewing gum, lozenges, lollipops, mucoadhesive tablets, and orally disintegrating tablets are all what types of dosage forms?

Back 62

Buccal

Front 63

Nicorette has a _______ hepatic 1st pass and ______ buccal absorption.

Back 63

Nicorette has a _high_ hepatic 1st pass and _good_ bucall absorption

Front 64

In nicorette, nicotine is bound to a _______ exchange resin that requires _______ in order to be effective.

Back 64

In nicorette, nicrotine is bound to a _cation_ exchange resin that requires _chewing_ in order to be effective

Front 65

Why is nicorette formulated with a buffer?

Back 65

To raise the pH to 8.5 to increase the nonionized form to increase absorption.

Front 66

The systemic bioavailablity of nicorette depends on the _____ saliva is held in the mouth.

Back 66

Time

Front 67

What happens when nicotine is swallowed?

Back 67

Hepatically metabolized

Front 68

What dosage form is Commit, nicotine polacrilex, that is similiar to nicorette in function?

Back 68

Lozenges

Front 69

T/F:
Lollipops are essentially lozenges on a stick.

Back 69

True

Front 70

Fentanyl citrate lollipops, Actiq, have what two characteristics of lollipops?

Back 70

1. Very lipophillic
2. High hepatic and intestinal 1st pass

Front 71

Lollipop dosage forms should be placed between the _____ and ____ then sucked for ______.

Back 71

Lollipop dosage forms should be placed between the _cheek_ and _gums_ then sucked for _15 minutes_

Front 72

T/F:
Buccal administered lollipops are rapidly absorbed followed by prolonged absorption.

Back 72

True

Front 73

T/F:
Rapid mouth absorption of a lollipop dosage form is about 75% of the drug.

Back 73

False, 25%

Front 74

T/F:
When administered via lollipop, a drug is 75% absorbed in the GI.

Back 74

True

Front 75

Nice features of lollipops include?

Back 75

Its unlikely to be swallowed and can be easily removed (i.e. side effects)

Front 76

Why should lollipop dosage forms must be properly disposed of?

Back 76

To keep away from kids, and Will

Front 77

What is the goal of the buccal dosage form mucoadhesive tablet?

Back 77

To keep in place and slowly disintergrate/dissolve

Front 78

What is the example presented in the lecture of a mucoadhesive excipient?

Back 78

Cellulose derivatives

Front 79

Two examples of mucoadhesive tablets are?

Back 79

Striant (testosterone buccal system) and Nitrogard (NTG)

Front 80

What are 2 charateristics of Striant?

Back 80

1.Releases testosterone, which has a high hepatic 1st pass
2. Stay until removed (~12hrs)

Front 81

T/F:
All orally disintegrating tablets are meant for GI absorption.

Back 81

False, buccal absorption also

Front 82

Zelapar is an example of what buccal administered dosage form?

Back 82

Orally disintergrating tablet

Front 83

Zelapar is for Parkinsons disease. It is prepared via ______ and placed on the tongue where it is rapidly dissolved.

Back 83

Zelapar is for Parkinsons disease. It is prepared via _lyophilization_ and placed on the tongue where it is rapidly dissolved.

Front 84

Absorption of Zelapar is (buccal/ sublingual).

Back 84

Buccal

Front 85

Avoid eating, drinking, chewing, smoking, and talking if practical to avoid distruption are all general guidelines for admistration of what types of tablets? (2)

Back 85

Sublingual and buccal tablets

Front 86

In regards to ophthalamics, benzalkonium chloride is used for what as an excipient?

Back 86

Increasinf penetration thru the epithelium and as a preservative

Front 87

What is the purpose of EDTA in ophthalmics?

Back 87

A chealator and a preservative

Front 88

T/F:
Thimerosal is a preservative.

Back 88

True

Front 89

Acetic acid and sodium acetate act as what in ophthalmics?

Back 89

Buffers

Front 90

Hydroxyethylcellulose and PEG-400 are used for what as excipients?

Back 90

Viscosity

Front 91

Polysorbate is used as a _______ ophthalmics?

Back 91

Surfactant

Front 92

T/F:
Sodium bisulfite is an antioxidant.

Back 92

True

Front 93

Why would an ophthalmic have excipients with a low pH?

Back 93

For solubility

Front 94

Purite is an excipient in refresh tears that acts as? (2)

Back 94

A preservative and an oxidant

Front 95

If an eye drop is a suspension, how long should you shake it?

Back 95

10 seconds

Front 96

What is the purpose of pulling down the eyelid to form a sac?

Back 96

To place a drop in the conjuctival sac

Front 97

How long should you keep your eye closed after placing a drop in your conjuctival sac?

Back 97

At least 30 seconds

Front 98

After applying a drop to the eye and closing it, where should you apply gentle pressure to? What is this preventing?

Back 98

The inner corner for 30 seconds (nasolacrimal occlusion)
This prevents drainage and systemic effect

Front 99

T/F:
You should rinse or wipe off the dropper tip after every use.

Back 99

False, DO NOT rinse, wipe, or touch dropper tip after use

Front 100

T/F:
When applying eyedrops of different medications, it doesnt matter how long you wait in between the 2 drops.

Back 100

False, you should wait at least 5 minutes or else the 2nd drop will wash out the 1st one.

Front 101

Which should you apply 1st? Long acting formulas or short acting formulas?

Back 101

Short acting formulas at least 5 minutes before the long acting formula

Front 102

How long before you apply eye ointment should you apply eye drops?

Back 102

10 minutes at the least

Front 103

T/F:
It is recommended that you do not instill ophthalmic products while wearing contacts unless instructed to by a physician.

Back 103

True

Front 104

What can happen if eye drops are instilled when wearing contacts?

Back 104

BAC can bind to the contact

Front 105

Ophthalmics are suggested to be discarded within 30 days, but can be discarded with no signs of containmination for up to _______.

Back 105

3 months of opening

Front 106

Ointments can cause what kind of vision problem right after application?

Back 106

Blurring

Front 107

How much ointment should be placed via sweeping motion into the conjunctival sac?

Back 107

1/4- 1/2 inch ribbon

Front 108

After applying an ointment to the conjunctival sac, how long should the eye be closed for?

Back 108

1- 2 minutes and the eye should be rolled in all directions

Front 109

When compounding ophthalmics, the same precaution should be taken as with __________, where it should be done in an aseptic environment and technique.

Back 109

Parenterals (injections or infusions)

Front 110

T/F:
When compounding ophthalmics, calculations are involved for figuring out tonicity.

Back 110

True

Front 111

T/F:
Corneocytes form a continuous layer that serves as protection for the skin.

Back 111

False, non- continuous, just overlap

Front 112

What type of cell is a very lipo-like matrix that is opaque in color?

Back 112

Corneocytes

Front 113

T/F:
In the protective layer of the skin, dark groups are nonpolar and can be oxidized.

Back 113

False, polar

Front 114

Lipid material found in the skin is mainly _______ from serine making up ____% while cholesterol makes up __________% and the remainder is ____________.

Back 114

Lipid material found in the skin is mainly _ceremides_ from serine making up _50_% while cholesterol makes up _20-25_% and the remainder is _Fatty acid monoglyceride_.

Front 115

What allows the formation of a covalent bond with ceremide and anchors the lipids to the corneocytes?

Back 115

Long chain FA with hydroxls on the end

Front 116

The narrow-->broad-->narrow bands seen in the skin are due to what?

Back 116

Interdigitalis and Van der Waals interactions that keep the skin together

Front 117

T/F:
Flux is dependent on lipid solubility and water solubility regardless of the vehicle.

Back 117

True... NEED TO KNOW

Front 118

T/F:
A drug must have relatively good solubility in both water and lipids in order to have good flux through the skin.

Back 118

True

Front 119

The closer the solubility values for SAQ and SIPM (or SOCT), the ______ the flux will be.

Back 119

Higher

Front 120

Partition coefficient (K) is (a good/ not a good) predictor of flux.

Back 120

Not a good predictor

Front 121

Why is the partition coefficient a poor predictor of flux?

Back 121

Because the partition coefficient will continually increase as MW of the compound (i.e. drug) increases, without regard to the vehicle being used.

Front 122

Why is the permeability coefficient (P) a VERY BAD predictor of flux?

Back 122

Because it varies (either up or down) as MW of the compound (i.e. drug) increases.

Front 123

If the vehicle the drug is in is water (aqueous vehicle), P ______ with increasing MW

Back 123

Increases

Front 124

If the vehicle the drug is in is lipid, P _________ with increasing MW

Back 124

Decreases

Front 125

T/F:
Partition coefficient is equal to CVEH/CMEM

Back 125

False, should be CMEM/CVEH

Front 126

In the equation for flux (J), J=D/L
What does D stand for and what it states?

Back 126

D is diffusivity coefficient and it states the larger the molecule the slower the process or flux

Front 127

In the equation for flux (J),
J= D/L
What does L state?

Back 127

L states the thicker the membrane the slower the flux

Front 128

The permeability coefficient (P) can be solved by this equation:
P= J/CVEH
What are the units?

Back 128

cm/ hr or any units of distance/ time

Front 129

What are the units for Flux (J)?

Back 129

umole/cm^2hr or any units of #moles/area*time

Front 130

What is known as the “quick” pathway of the drug through structures, such as hair follicles, that have an open pathway through the skin.

Back 130

Initial burst

Front 131

The initial burst is a (low/high)capacity pathway, and so doesn’t really contribute much to flux

Back 131

Low

Front 132

What represents the equilibrium that is achieved while the drug is traveling through the “tortuous” path between corneocytes

Back 132

Steady state

Front 133

T/F:
IPM and long chained alcohols can be used in determining partition coefficients.

Back 133

True