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Drugs (1) (Oral Delivery Mode (Oral (Survive Digestive GI tract, pH 1-3),…
Drugs (1)
Oral Delivery Mode
Oral
Survive Digestive GI tract
pH 1-3
Intravenous
Subcutaneous
Intramuscular
Lotions
Eyedrops
Small Molecule Drugs
Diazepam (Fig 7)
Ibuprofen (Fig 8)
Prozac (Fig 9)
Omeprazol (Fig 10)
Atorvastatin (Fig 11)
Lipinski Rule of 5
Orally Active Drug
No more than 1 violation
Criteria
<= 5 H Bond Donors
<= 10 H Bond Acceptors
MW < 500 D
log P < 5
Function
Bind to proteins/enzymes
Modify Activity
Dissolved before absorption into blood
Examples
Antibiotics
Inhibit bacteria & viral proteins
Antivirals
Inhibit bacteria & viral proteins
Abused Drugs
Morphine (Fig 12)
Heroine (Fig 13)
Diacetylated Morphine
More Hydrophobic
Higher Uptake
Selectivity
3D Target Protein Structure
Bioavailability
How much administered drug is available?
IV Injection
100%
Oral Ingestion
5-10%
Loss in gut & liver
Nasal Delivery
~80%
Concentration of Drug in Blood (Fig 1)
Adverse Side Effects (Fig 2)
Administration Route Selection
Factors
Drug Stability
Target Organ Location
Drug Action Onset
Drug Release Rate
Drug Conc
Injection Vol
Drug Irritability
