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Intestinal Permeability
Determination and Absorption of
soluble drugs
Lecture 5
Intestinal Permeability
• Human Jejunum (In Vivo)
– Most Reliable
• Rat In Situ
– Next Most Reliable
• Tissue Culture
– Mo...
Tissue Culture
Gastrointestinal Transit
• Fasted vs. Fed States
• Gastrointestinal Transit Times
– Rule of ‘3’
• Controlled Release Dosag...
Transit Rule of ‘3’
Examples
• Propranolol
– Peff(Human) = 2.91 x 10-4
cm/sec
– Fabs = 99%
– Bioavailability ~20%.
• Atenolol
– Peff(Human) = ...
Water Insoluble Drugs
• Metamorphic
limestone
• CaCO3
• Ksp= 9x10-9
= [Ca++
]
[CO3] = x2
• x = solubility = 9.4 x
10 -5
M
...
Predicting Absorption
• Solubility/Dissolution
• Permeability
• Dose
• Transit
Intestinal Permeability Determination and Absorption of Soluble Drugs, as Presented by Dr. Gordon Amidon
Intestinal Permeability Determination and Absorption of Soluble Drugs, as Presented by Dr. Gordon Amidon
Intestinal Permeability Determination and Absorption of Soluble Drugs, as Presented by Dr. Gordon Amidon
Intestinal Permeability Determination and Absorption of Soluble Drugs, as Presented by Dr. Gordon Amidon
Intestinal Permeability Determination and Absorption of Soluble Drugs, as Presented by Dr. Gordon Amidon
Intestinal Permeability Determination and Absorption of Soluble Drugs, as Presented by Dr. Gordon Amidon
Intestinal Permeability Determination and Absorption of Soluble Drugs, as Presented by Dr. Gordon Amidon
Intestinal Permeability Determination and Absorption of Soluble Drugs, as Presented by Dr. Gordon Amidon
Intestinal Permeability Determination and Absorption of Soluble Drugs, as Presented by Dr. Gordon Amidon
Intestinal Permeability Determination and Absorption of Soluble Drugs, as Presented by Dr. Gordon Amidon
Intestinal Permeability Determination and Absorption of Soluble Drugs, as Presented by Dr. Gordon Amidon
Intestinal Permeability Determination and Absorption of Soluble Drugs, as Presented by Dr. Gordon Amidon
Intestinal Permeability Determination and Absorption of Soluble Drugs, as Presented by Dr. Gordon Amidon
Intestinal Permeability Determination and Absorption of Soluble Drugs, as Presented by Dr. Gordon Amidon
Intestinal Permeability Determination and Absorption of Soluble Drugs, as Presented by Dr. Gordon Amidon
Intestinal Permeability Determination and Absorption of Soluble Drugs, as Presented by Dr. Gordon Amidon
Intestinal Permeability Determination and Absorption of Soluble Drugs, as Presented by Dr. Gordon Amidon
Intestinal Permeability Determination and Absorption of Soluble Drugs, as Presented by Dr. Gordon Amidon
Intestinal Permeability Determination and Absorption of Soluble Drugs, as Presented by Dr. Gordon Amidon
Intestinal Permeability Determination and Absorption of Soluble Drugs, as Presented by Dr. Gordon Amidon
Intestinal Permeability Determination and Absorption of Soluble Drugs, as Presented by Dr. Gordon Amidon
Intestinal Permeability Determination and Absorption of Soluble Drugs, as Presented by Dr. Gordon Amidon
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Intestinal Permeability Determination and Absorption of Soluble Drugs, as Presented by Dr. Gordon Amidon

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Lecture #5 from the Drug Delivery Foundation's 2009 Oral Drug Delivery Conference: http://www.ddfint.org/previous-events/2017/5/22/odd2009-strategies-for-oral-drug-delivery

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Intestinal Permeability Determination and Absorption of Soluble Drugs, as Presented by Dr. Gordon Amidon

  1. 1. Intestinal Permeability Determination and Absorption of soluble drugs Lecture 5
  2. 2. Intestinal Permeability • Human Jejunum (In Vivo) – Most Reliable • Rat In Situ – Next Most Reliable • Tissue Culture – Most Common • Caco2, MDCK (Epithelial) Cell Lines
  3. 3. Tissue Culture
  4. 4. Gastrointestinal Transit • Fasted vs. Fed States • Gastrointestinal Transit Times – Rule of ‘3’ • Controlled Release Dosage Forms
  5. 5. Transit Rule of ‘3’
  6. 6. Examples • Propranolol – Peff(Human) = 2.91 x 10-4 cm/sec – Fabs = 99% – Bioavailability ~20%. • Atenolol – Peff(Human) = 0.3 x 10-4 cm/sec – Fabs = 42% – Bioavailability = ~50 % • Cephalexin – Peff (Human)= 1.56 x 10-4 cm/sec – Fabs = 94% – Bioavailability = ~40%
  7. 7. Water Insoluble Drugs • Metamorphic limestone • CaCO3 • Ksp= 9x10-9 = [Ca++ ] [CO3] = x2 • x = solubility = 9.4 x 10 -5 M • x = 10 µg/ml
  8. 8. Predicting Absorption • Solubility/Dissolution • Permeability • Dose • Transit

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