colonic drug delivery Flashcards

1
Q

what are the routes of administration for the medicines in the lower GIT?

A
  • intestinal drug delivery
  • parenteral
  • rectal
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2
Q

what separates SI and the colon?

A

ileocaecal junction

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3
Q

how can the dosage form stay in the ileocaecal junction?

A

it dependeds on the dosage form

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4
Q

what is the role of the colon?

A

Remove liquid from incoming material & kneads colonic contents firmly → peristaltic waves covering only short distances

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5
Q

what affects the GI tract delivery?

A

if empty stomach/ light brekfast/ heavy brekfast/ empty stomach

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6
Q

why would you need drug delivery to the colon?

A
  • A form of targeted drug delivery
  • Local diseases, IBD such as Crohn’sdisease & ulcerative colitis •Systemic absorption of drug poorly absorbed or unstable in upper GIT, e.g. peptide and protein •Modified release dosage form, as chronotherapy to manage asthma, arthritis and hypertension
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7
Q

what are some of the different approaches to delivery in the colon?

A
  • Utilising of presence of special bacterial flora of colon
  • Utilising of pH variations along GIT & pH of an inflamed colon
  • A time controlled drug release assuming that gastrointestinal transit follows a defined time pattern
  • Combined approaches
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8
Q

how could you utilise colonic bacteria flora in drug delivery?

A

•Digested by enzymes of the colonic bacteria
–Polymer cross-linked with azoaromatic groups
–Pectin and pectin/chitosan mixtures

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9
Q

why would you speilise glassy a amylose?

A

–Chains of glassy a amylose entangles in fixed position by H bonds reduces flexibility of aamylose molecules –Not digested by pancreatic amylases
–Hydrolysed by bacterial aamylases

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10
Q

what is glassy a amylose?

A
  • High amylose starches from genetic modified maize
  • Contain amylose and amylopectin
  • Use of butanol/water mixture
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11
Q

what is the mixed film produced by glassy a amylose?

A

water insoluble film forming polymers (e.g. ethyl cellulose)
•Affect film forming capability and film strength, degree of film swelling
•Drug release via diffusion

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12
Q

what happens when there is an aqueous disperson of an amylose-butanol complex.

A

when it is heated it loses butanol to give you an amylose solution

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13
Q

what happens to an amylose solution when colled or otherwise?

A

when cooled- precipitatated

retrogradation= phase separation and loss of water to give a gel

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14
Q

what happens to amylose gel when it cools fast/slowly?

A

slow- solid crystals

fast- further water loss and glassy amylose film

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15
Q

how do you test the efficiency of amylose coating films?

A
  • Standard dissolution tests using–Simulated gastric fluid (pepsin)–Simulated intestinal fluid (pancreatinand taurocholicacid)
  • Dissolution tests with solutions containing bacterial a-amylase (source: Bacillus licheniformis)
  • Fermentation tests in faecal slurry
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16
Q

what do the properties of the a- amylose=ethyl cellulose films depend on?

A

–Ratio of a-amylose to ethyl cellulose

–Coating thickness

17
Q

how would the bacteria change in the jejuenum and illeum in IBD?

A

INC e/coli

dec clostridiales

18
Q

how would the large intestine microbiota change in IBD?

A

INC IN: bacterioidetes and peptostrepotococcus

decrease in bifidobacteria, eubacteria and e.coli

19
Q

how do we utilise ph changes for drug delivery?

A

pH sensitive coating materials, e.g. Eudragit®, phthalates
•System consists of two layers of coating polymers separated by a protective layer
•Outer coating dissolves at ~ pH 6 (enteric coat) •Inner coat (closest to core) to dissolve a pH < 4 –5•Inflammation of colon is linked to decrease in pH•inner coat dissolves or swells and releases drug at target site

20
Q

what problems is there is using ph changes for colon drlivery?

A

blems: Treatment will result in change of pH towards normal (i.e. >pH 6)•Device might fail at later stages of treatment
•Other factors that could alter the pH towards normal during treatment: •Change diet, presence of fatty acids, development of gas (CO2)