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PHRM 828 Exam 2 > Knipp's 1st Set > Flashcards

Knipp's 1st Set Flashcards

1
Q

Excipients

A

Coatings: control diffusion rates and modify release properties

Disintegrants: control regions of release

Lubricants: slow dissolution

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2
Q

Internal Excipient

A
  • swellable matrices
  • non swelling matrices
  • inert plastics
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3
Q

Coating

A
  • applied to outside of solid dosage forms
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4
Q

Goal of Coatings

A
  • protection of agent from air or humidity
  • mask taste
  • special drug release
  • aesthetics to eye
  • prevent inadvertent contact with drug (safety)
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5
Q

Aqueous Film Coatings

A
  • film forming polymer
  • plasticizer for flexibility and elasticity
  • colorant
  • vehicle
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6
Q

Enteric Coatings

A
  • added to dosage forms to prevent early release of API in metabolic regions
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7
Q

Goal of Enteric Coatings

A
  • prevent acid sensitive API from gastric fluid
  • prevent gastric distress from API
  • target API delivery
  • provide delayed/sustained release
  • deliver API to higher local concentration
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8
Q

Sustained Release

A
  • formulated to slow the release of the therapeutic agent so that its appearance in circulation is delayed but sustained in duration
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9
Q

Controlled Release

A
  • reproducibility and predictability in the drug release kinetics

ALLOWS US TO MAINTAIN A NARROW DRUG PLASMA COCENTRATION

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10
Q

Examples of Controlled Release Formations

A
  • Coated beads, granules, or microspheres
  • Multitablet system
  • Micro-encapsulated
  • Drug Embedding in hydrophilic matrix
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11
Q

Steady State

A

rate going into the body must equal the disposition

creates safety window

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12
Q

Characteristics of Drugs Best Suited for Oral Controlled Release

A
  • exhibit neither slow or fast rates of absorption/excretion
  • uniformly absorbed
  • administered in small doses
  • good safety/therapeutic window
  • chronic > acute
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13
Q

Physiological Factors Affecting Absorption

A
  • absorbing surface area
  • residence time
  • pH
  • Permeability
  • dietary effects
  • complexation/protein binding
  • biliary uptake and clearance
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14
Q

Epithelia

A
  • located on the layer of extracellular matrix proteins
  • epithelial cells are polarized
  • endothelial cells line the inside of body cavities, blood vessels, and lymph
  • simple squamous predominantly
  • endothelial cells are actually epithelial cells just in the body
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15
Q

Simple Squamous

A

thin layer of flattened cells that are relatively permeable

lines most blood vessels and placenta

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16
Q

Simple Columnar

A

usually found in GI tract

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17
Q

Translational

A

comprised of several layers with different shapes

stretch

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18
Q

Stratified Squamous

A

multiple layers of squamous cells that cover areas that wear and tear

skin is most important

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19
Q

Composition of Biological Membranes

A
  • all living cells are enclosed by a membrane making it a living unit
  • barrier
  • cell membrane is semi-permeable permitting the rapid passage of some chemicals while rejecting others
  • polarized lipid composition
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20
Q

Does cholesterol only have harmful effects?

A

NO

  • too much or too little is negative
  • provides fluidity at lower levels
21
Q

Intestinal Transport Systems

A

Passive
- non saturable
- paracellular (between cells)
- transcellular (through cells)

Carrier-Mediated
- saturable
- active (energy dependent)
- facilitated diffusion (energy independent)

22
Q

Drug Transporters

A
  • membrane bound proteins found on apical and basolateral surfaces
  • role is to move important molecules across membranes
  • crucial determinant of the distribution of drugs
23
Q

Solute Carrier Transporter

A
  • 43 subfamilies
  • generally influx
  • PepT1, OAT
24
Q

ABC Transporter

A
  • 7 subfamilies
  • generally efflux (multidrug resistance)
  • P glycoprotein
25
Q

Routes of Permeability

A
  • influx transporter
  • passive transcellular
  • passive transcellular and efflux
  • passive paracellular
  • metabolism
  • efflux
26
Q

Absorptive Transporter

A

transfer substrates into systemic blood circulation

27
Q

Secretory Transporter

A

transfer their substrates from blood circulation into bile, urine, lumen

28
Q

GI Tract Epithelia

A

Buccal: stratified squamous
Sublingual: simple squamous
Esophagus: stratified squamous
Trachea: psuedostratified squamous
Stomach: columnar
Small/Large Intestine: columnar
Upper Rectum: simple columnar
Lower Rectum: stratified squamous

29
Q

Role of Stomach

A
  • digest food and control the flow of contents into intestine

acts as food reservoir
processes food into chyme
regulates food delivery
pH protects from bacteria

30
Q

Role of Stomach Cont.

A

Fasted pH = < 3
Fed pH = 5-7

Emptying halftime = 30 min

31
Q

Organization of Stomach

A

Fundus: contains gas and produces contractions to move contents

Body: reservoir for ingested food

Antrum: contains pyloric region and controls flow into small intestine

32
Q

Intestine Facts

A

Mouth to Anus Time = 24-32 hours

Small Intestinal Time = 3 hours

MOST ABSORPTION OCCURS IN SMALL INTESTINE

pH = 5-6.5

33
Q

Why Intestine?

A

LOTS MORE SURFACE AREA TO GET ABSORBED

increases in surface area in SI due to folding such as (folds of kerckring, villi, microvilli)

34
Q

Characteristics of Colon

A
  • 125 cm log from caecum to anus
  • transport much slower than intestine
  • varies in thickness
  • illeocaecal valve limits food flow from ileum to caecum
  • responsible for water and electrolyte absorption
35
Q

Colon Structure

A

Serosa: squamous epithelium covered with adipose tissue

Muscularis Externa: inner circular muscle layer

Submucosa and muscosa

36
Q

3 Layers of Colon

A

Muscularis mucosae

Lamina Propria

Epitheliium

37
Q

Rectum

A
  • highly folded
  • stratified squamous of lower rectum allows for high drug absorption
  • low residence time
38
Q

Factors influencing Drug Solubility

A
  • buffer capacity
  • bile salts
  • regional fluids
  • other drugs
  • potential issues from endogenous substrates
39
Q

Challenges for Assumptions of GI Tract Physiology

A
  • transporters and enzymes vary
  • diet and chemical expose varies
  • GI fluid composition varies
  • pharmacogenetics and genomics are issues
  • drug nutrient and drug drug interactions

ONE SIZE FORMULATIONS DO NOT FIT ALL

40
Q

Disposition

A

comprised of distribution and elimination

41
Q

Elimination

A

comprised of metabolism and excretion

42
Q

ADMET

A

Absorption
Distribution
Metabolism
Excretion
Toxicity

43
Q

Nature of Pharmokinetic Processes

A
  • described by concentration time profiles
  • compartments represent similar spaces
  • reversible or irreversible
  • linear or nonlinear
  • fast and slow tend to disappear
44
Q

Bioavailability

A

rate and extent of drug absorption

45
Q

Absolute Bioavailability

A

AUC of a given dosage form compared with AUC of same dose injected intravenously

46
Q

Relative Bioavailability

A

AUC of a given dosage form compare to an arbitrary reference standard

47
Q

Bioequivalent

A

DOES NOT mean therapeutic effect of two dosage forms are equivalent

48
Q

Dose

A
  • amount of chemical in which whole organism is treated
  • local concentration of chemical at response site

PHRM 828 Exam 2 (3 decks)

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