PHBP | Part I Flashcards by Xei Lee

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

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The study of the time course of drug movement in the body during absorption, distribution, and elimination.

PHARMACOKINETICS

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The study of the relation of drug concentration or amount at the site of action and its pharmacologic response.

PHARMACODYNAMICS

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Metabolism + Excretion

Elimination

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Distribution + Elimination

Disposition

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rate at which the solid drug enters into solution

DRUG DISSOLUTION

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rate limiting step in bioavailability

DRUG DISSOLUTION

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Equation involved in Drug Dissolution

Noyes-Whitney Equation

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PS and SA Relationship

↓ particle size = ↑ surface area = ↑ absorption

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Ratio solubility of the drug at equilibrium in a non-aqueous solvent water phase compared with oil phase (octanol)

PARTITION COEFFECIENT

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Drugs that have relative relationship with octanol possess ____

positive integers

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Drugs that have relative relationship with water possess ____

negative integers

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Drugs that are weak electrolytes (acids or bases) exist in both an ionized form and a nonionized form in solution.

Extent of Ionization

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The choice of salt form for a drug depends on the desired physical, chemical, or pharmacologic properties.

Salt Formation

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ability of a drug to exist in more than one crystalline form

Polymorphism

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ability of a drug to exist as optically active stereoisomers or enantiomers

Chirality

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Enantiomer of Ibuprofen that is pharmacologically active

S-enantiomers

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Drugs may exist in hydrated, or solvated form or as an anhydrous molecule

Hydrates

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species formed by the reversible or irreversible association of two or more interacting molecules or ions

Complex

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complexes that typically involve a ring-like structure formed by the interaction between a partial ring of atoms and a metal

Chelates

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Metal in hemoglobin

IRON

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Metal in insulin

Zinc

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Metal in cyanocobalamin

Cobalt

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Delivery of active ingredient from a dosage form into solution

Liberation

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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