3.7 Flashcards

1
Q

The rectum is the last ____ cm of the large intestine.

A

15 to 20

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2
Q

The anal canal is the last ____cm of the rectum.

A

4 to 5

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3
Q

The surface area of the rectum has no villi, thus has a relatively (high or low) absorptive surface area.

A

low

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4
Q

The rectal mucosa is the mucous layer of the rectum (rectal fluid) with a volume of ___ ml (100 micrometers thick) and pH of 7.5

A

3

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5
Q

Rectal fluid is about 3 mL which is very little fluid for drug …

A

dissolution

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6
Q

The epithelium of the rectal mucosa is cylindrical single cell layer and goblet cells, but it transitions to a _____ epithelium as it reaches the anus.

A

squamous

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7
Q

______ rectal veins drain to the general circulation (without hepatic first pass metabolism)

A

lower and middle

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8
Q

____ rectal vein drains to the hepatic portal vein which is more GI-like (with hepatic first pass metabolism)

A

superior

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9
Q

Venous Anastomoses is the opening; a natural communication between …

A

two blood vessels

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10
Q

____ can help spread the dosage form and are stimulated by colonic contents– Rectal Motility

A

Rectal contractions

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11
Q

Advantage of Rectal Drug delivery if the oral route is les desirable for the drug…

A

Bypass drug inactivation of upper GIT
(chemical or enzymatic)

Partial avoidance of Hepatic first pass metabolism (only absorbed in the lower rectum to bypass portal drainage)

The rate of absorption is not affected by gastric emptying or GI transit time

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12
Q

Disadvantage of Rectal Drug delivery …

A

Poor, slow, erratic drug bioavailability
- Low surface area

  • Low fluid content
  • complex blood drainage
    (lower suppository placement– avoid portal drainage- which is needed if systemic effect is desirable)
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13
Q

Rectal fluid pH has little buffer capacity meaning the ____ will likely determine the rectal fluid pH

A

dosage form

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14
Q

rectal veins are heavily ____

A

anastomosed

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15
Q

If bioavailability is crucial it is preferred to go to the (oral or rectal route)

A

oral (not rectal since there is poor drug bioavailability)

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16
Q

A problem for high hepatic first-pass drugs, if a systemic effect is desirable but this problem can be offset by a lower suppository placement; however, the dose can spreader higher after …

A

Liquefication

17
Q

Suppositories are produced by hand-rolling, compression, or most commonly …

A

FUSION

18
Q

____ is a way to produce suppositories through melting. It involves gentle heating of suppository base until melted, followed by addition of drug and excipients, then poured into mold, followed by cooling.

A

Fusion

19
Q

______(oil-soluble) bases, upon insertion, these release the drug after melting in the rectum. e.g. cocoa butter

A

Oleaginous

20
Q

Important property of cocoa butter that is an issue for suppository is that it softens and melts to a non-viscous oil meaning…

A

rectal leakage may occur

cocoa butter also undergoes polymorphism

21
Q

If overheating suppositories occurs, it leads to transition to polymorphism which will lead to …

A

premature melting of suppository

melts at room temperature/ before inserting into rectum

22
Q

_______ vegetable oils are cocoa butter substitutes developed to overcome problems with cocoa butter. (Bland/non-irritating, no polymorphism, and emulsifiers used by helping mix the melted base with rectal fluid/faster release)

A

Hydrogenated

23
Q

Water-soluble base: upon insertion, these release the drug after ______ and mixing with rectal fluids.

A

Dissolving (not melting)

24
Q

______ is an example of a water-soluble base use for suppositories.

A

Polyethylene glycol (PEG)

25
Q

PEGs have different melting points, the melting point increases with increasing…

A

MW (molecular weight)

26
Q

PEGs have different aqueous solubilities and have hygroscopicity: both generally decreases with _____ MW

A

increasing

27
Q

A _____ supp can irritate the patient since it can absorb rectal water, leading to a localized epithelium dehydration, and irritation may lead to diarrhea or gas.

A

Hygroscopic

28
Q

____ agents may be necessary for a suspension (not dissolved) that settles during pouring into mold or during cooling.

A

Suspending

29
Q

Settling during (pouring or cooling) would lead to different dose of drug in each suppository.

A

pouring

inaccurate and imprecise drug amounts

30
Q

Settling during pouring and cooling can lead to _______ with zones of high suspensoid (powder) concentration which lead to zones of brittleness and can lead to poor dosage uniformity or two layers of suppositories.

A

Stratification

31
Q

____ may be added to increase the viscosity of the melt to limit stratification. It is a suspending agent to prevent/reduce settling

A

Silica Gel

32
Q

_____ agents help reduce brittleness as a problem with suppository formulations since brittleness may fracture the drug during handling or rapid cooling (lead to weak points in the solid)

A

Toughening (plasicizer)

Avoid freezing and add small amount of this agent

33
Q

Tween 80 is a …

A

Surfactant and toughening agent

34
Q

Tween 80, glycerin, propylene glycol, castor oil, fatty acid monoglycerides are all…

A

toughening agents