PHBP | Part I Flashcards
Science that examines the inter-relationship of the physicochemical properties of the drug, the dosage form, and route of administration on the rate and extent of systemic drug absorption.
BIOPHARMACUETICS
The study of the time course of drug movement in the body during absorption, distribution, and elimination.
PHARMACOKINETICS
The study of the relation of drug concentration or amount at the site of action and its pharmacologic response.
PHARMACODYNAMICS
Metabolism + Excretion
Elimination
Distribution + Elimination
Disposition
rate at which the solid drug enters into solution
DRUG DISSOLUTION
rate limiting step in bioavailability
DRUG DISSOLUTION
Equation involved in Drug Dissolution
Noyes-Whitney Equation
PS and SA Relationship
↓ particle size = ↑ surface area = ↑ absorption
Ratio solubility of the drug at equilibrium in a non-aqueous solvent water phase compared with oil phase (octanol)
PARTITION COEFFECIENT
Drugs that have relative relationship with octanol possess ____
positive integers
Drugs that have relative relationship with water possess ____
negative integers
Drugs that are weak electrolytes (acids or bases) exist in both an ionized form and a nonionized form in solution.
Extent of Ionization
The choice of salt form for a drug depends on the desired physical, chemical, or pharmacologic properties.
Salt Formation
ability of a drug to exist in more than one crystalline form
Polymorphism
ability of a drug to exist as optically active stereoisomers or enantiomers
Chirality
Enantiomer of Ibuprofen that is pharmacologically active
S-enantiomers
Drugs may exist in hydrated, or solvated form or as an anhydrous molecule
Hydrates
species formed by the reversible or irreversible association of two or more interacting molecules or ions
Complex
complexes that typically involve a ring-like structure formed by the interaction between a partial ring of atoms and a metal
Chelates
Metal in hemoglobin
IRON
Metal in insulin
Zinc
Metal in cyanocobalamin
Cobalt
Delivery of active ingredient from a dosage form into solution
Liberation
The process with the slowest rate constant in a system of simultaneous kinetic processes
Rate Limiting Step
Serves as the rate limiting step in Liberation
Dissolution
The process of uptake of the compound from the site of administration into the systemic circulation.
ABSOPRTION
Bound to surface of skin or mucosa
Adsorption
Drug reaches the deepest layer of the skin, yet does not reach the blood capillaries
Penetration
Penetration and permeation
Sorption
Other name of Cell Membrane
Plasma membrane
Outermost layer of cell
Semipermeable structure composed primarily of lipids and protein
Cell Membrane
Transport food and other molecules into the cell and transport wastes out of the cell
Channel proteins
Gather info about the cell’s surroundings
Receptor Proteins
Identify the type of cell, important for cell recognition
Cell Surface Markers
Theory:
Composed of two layers of phospholipids between two surface layers of proteins
Lipid bilayer or Unit Membrane Theory
Theory:
Consists of globular protein embedded in a dynamic fluid, lipid bilayer matrix proteins embedded in a phospholipid bilayer.
Fluid Mosaic Model
Moving material in and out of the cell
Transport Mechanisms
The difference in the amount of a substance inside and outside of the cell
Concentration Gradient
Major physiologic processes that occur in the gastrointestinal systems (3)
-Secretion
-Digestion
-Absorption
Total Transit Time
0.4 to 5 days
Components of Total Transit Time (3)
Gastric Emptying
Small Intestinal Transit
Colonic Transit
Small Intestinal Transit (time)
3-4 hours; 7 hours
Fasting state
4-8 Hours
Fed State
8-12 hours
Oral Cavity secretion level
pH 7 (6.2 to 7.6)
Salivary amylase which digests starches
Ptyalin
Lubricant in Oral Cavity
Mucin
Connects pharynx and the cardiac orifice of the stomach
Esophagus
pH Level of esophagus
pH 5-6
Prevents acid reflux from the stomach
Esophageal sphincter
Stomach
Fasting State
Fed State
Fasting State - pH 2-6
Fed State - pH 1.5 to 2
Stomach acid secretion is stimulated by _____ and ____
Gastrin
Histamine
Empty stomach:
____mL of gastric fluid
100mL
Maximum capacity of stomach
1.1 to 1.2L
3 Types of Glands (Stomach)
-Mucous glands
-Chief (Zymogenic cells)
-Parietal Cells
Small intestine duodenum pH level
pH 6 to 6.5
____ prodrugs are hydrolyzed in SI duodenum
Ester
____ enzymes are present in SI duodenum
Proteolytic
SI Duodenum Bile Secretion
600mL/day; 750mL/day
400-800mL
SI Duodenum pancreatic juice
300-500 mL/day
____ glands and ____ patches are absent in SI Jejunum
Brunner’s glands
Peyer’s Patches
Intestinal fluid in SI Jejunum
3000mL/day
Terminal and longest part of the small intestine
Ileum
Ileum is rich in immune tissue called ______
Lymphoid follicles
Colon pH
pH 55 to 7
Drugs that are absorbed well in colon are good candidates for _________ dosage form
Oral Sustained-Release
Length of rectum
15cm
Has the greatest capacity for the absorption of drugs from the GI tract
Duodenum
The ______ circulation receives about 28% of the cardiac output and is increased after meals.
Splanchnic circulation
In Lymphatic circulation, drugs are absorbed through _____ or _____ vessels under the microvilli
lacteal or lymphatic
refers to the transfer of the drug from the blood to extravascular fluids and tissues
DISTRIBUTION
carries blood to the tissue
Arteries
carries blood to the heart
Veins
_____ drugs generally diffuse across cell membranes more easily than highly polar or water-soluble drugs.
Lipid Soluble Drugs
An important factor in determining the initial distribution of drugs
Blood Flow
Drug diffuse rapidly across the membrane.
Perfusion or Flow Limited
Drug distribution is limited by slow diffusion of drugs cross the membrane
Diffusion or Permeability Limited
The ______ of liver are very permeable and allow the passage of large-molecular-weight molecules.
Sinusoidal capillaries
Layer of glial cells which have tight junctions, surrounds the capillary endothelial of the brain and spinal cord
Blood Brain Barrier
Alter the permeability of skin and allow drugs and larger molecules to permeate inward or outward.
Burns
Estimate the extent of drug distribution in the body
Volume of distribution (VD)
most abundant protein in human blood plasma
Albumin
Low plasma conc binds primarily basic cationic drugs
a-acid glycoprotein
Macromolecular complexes lipids and protein
Lipoprotein
45% of total volume
May bind both endogenous and exogenous compounds
Erythrocytes
Transport certain endogenous subs (corticosteroid)
Globulins