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Advantages and disadvantages of each drug delivery route: Oral
- Advantages
- Most common. The simplest, easiest, most economical method of administration.
- High patient accaptance and adherence to a regimin.
- Disadvantages
- First pass effect
- Not suitable for the drugs poorly absorbed or significantly destroyed in GI tract.
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Advantages and disadvantages of each drug delivery route: Parenteral
- Advantages
- Reliability, precision of dosage, timed control of onset of action
- Disadvantages
- Disconfort, possibility of infection, tissue damage, need trained personnel
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Advantages and disadvantages of each drug delivery route: Mucosal
- Advantages
- Avoid the first pass effect, relative ease and convenience
- Disadvantages
- Small area of absorption (nasal, oral), taste (oral)
- Delivery limited by molecular weight of a drug
- Local tissue irritation, sensitivity to pathologic conditions
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Advantages and disadvantages of each drug delivery route: Transdermal
- Advantages
- Easy to apply and remove
- Avoid the first pass metabolism
- Disadvantages
- Lag time to reach steady state (2-6 hrs)
- Limited by polarity, size of the drug
- My need permeation enhancement via chemical and/or physical means
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Advantages and disadvantages of each drug delivery route: Targeted
- Advantages
- Reduce sede effects of drugs on heathy tissues and enhance drug uptake by targeted cells
- Disadvantages
- ?
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Advantages and disadvantages of each drug delivery route: Local
- Advantages
- Reduced systemic side effects
- Reduced dose requirement
- Disadvantages
- Need to know the locations to be treated
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Medical motivations of drug delivery systems
- Increase efficacy, enable activities
- Decrease toxicity
- Increase patient compliance, convenience
- Enabling tools
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Economic motivations of drug delivery systems
- Increase patent life, market share with unique drug delivery systems
- Increase patient and physician acceptance
- Avoid costs of developing a new chemical entity
- List three areas where tablets transport.
- Stomach
- SI
- Colon
- List pH of main parts of GI Tract
- Stomach: 1-3
- SI: 5-8
- Colon: 5-8
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List GI transit times for tablets
- Cumulative (hrs)
- Stomach: 0.5
- Jejenum: 1.75
- Ileum: 3.25
- ICJ 4.5
- Colon: 24.5
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List surface area of GI tract (m^2)
- Duodenum: 2 (where most abs happens)
- Jejnum: 180
- Ileum: 280
- Colon: 1.5
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Define enteric coating
A coating around a tablet that will keep it from dissolving until it reaches SI (ph ~7)
- Summarize the five factors that affect absorption of drugs from tablets
- Permeability-how easy drug goes through membrane
- Dissolution-dissolving
- Efflux-along with metabolism, destroys drug
- Metabolism
- Formulation-how smart tablets are made (this controls dissolution)
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Know that solid form affects dissolution
Formulation
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Know that drugs can exist in polymorphs, solvates, and amorphous solid forms
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Know that amorphous forms give higher bioavailability than crystalline forms
Know the steps in development of the optimum solid form
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Know the parameters of the unit cell (a, b, c….)
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Know the estimated cost of the ritonavir problem
$900,000,000
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Know steps in controlling the solid form
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Know that an X-ray diffraction pattern is a fingerprint that can be used to identify a solid form
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Know the four aspects of formulation
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Know the factors used to select the best salt of Ketoprofen
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Know why the solubility of a carboxylic acid increases at high pH
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In the case study know why we want amorphous drug
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Know at least 3 types of tablets
- Simple Uncoated Tablets
- No coating
- Aspirin
- Effervescent Tablets
- Alka-seltzer
- Sugar Coated Tablets
- Prefilm coating
- Advil
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Know that granulation enlarges the particles and improves flow
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Know that the more binder the larger the particles
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Know that in a noninteracting formulation the drug particles are not altered or changed
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Know that content uniformity means that each tablet/capsule contains between 85-115%
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Know that the KV problem involved oversize tablets
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Know that capsules are classified as either hard or soft
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Know two advantages and two disadvantages of capsules
- Advantages:
- Hard shell capsules allow for a degree of flexibility of formulation not obtainable with tabs
- Bioequivalence studies of tablet formulations may be conveniently blinded by inserting tablets into capsules
- Disadvantages:
- More costly
- More likely to become lodged in esophagus
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Know best ways to prevent esophageal adhesion
- Take medication with water
- Continuous flow of saliva
- Remain standing for 90 secs
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Know the largest and smallest capsule sizes
- Largest: 000 (1.096 g/cm^3)
- Smallest: 5 (0.104 g/cm^3)
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Know steps in capsule filling
- Step 1 Rectification: The empty capsules are oriented so that all point the same direction
- Step 2 Separation of caps from bodies
- Step 3. Dosing of fill material.
- Step.4. Replacement of caps and ejection of
- filled cap‐sules:
- Step 5. Ejection of the Capsules
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Know formulation design for first in human testing
- First in human studies are done during drug
- Development
- The dose is based on the No Observed Adverse Event Level seen in Animals
- If possible the drug is placed in a capsule without other ingredients
- This means the drug must be in its most soluble form that is stable and handleable
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Know specifications for capsules for first in human testing
Specifications: moisture, assay, impurities, dissolution
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Know advantages & disadvantages of soft gelatin capsules
Look up
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Know that soft gelatin capsules can contain a suspension or a liquid
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