pharmacology药理学浙江大学教学信息化平台.pptxVIP

会计学;;2. Transport of Drug in the Body;2.1 Transmembrane Transport of Drugs (1) Non-carrier Transport Simple diffusion（简单扩散/单纯扩散） Filtration（滤过）;;;Another classification Passive transport Simple diffusion（简单扩散/单纯扩散） Filtration（滤过） Facilitated diffusion（易化扩散） Active transport Active transport (主动转运) Pinocytosis/exocytosis（入胞/出胞）;A. Simple diffusion;Determinants of simple diffusion For most drugs of small molecules (usually are weak acids or weak bases): Lipid-soluble or un-ionized forms pKa of the drug and pH of the body fluid The pKa is the pH at which the concentrations of the ionized and un-ionized forms are equal.;Henderson-Hasselbalch equation Weak acid drugs: pH - pKa = log ( [A-] / [HA] ) pKa - pH = log ( [HA] / [A-] ) Weak base drugs: pKa - pH = log ( [BH+] / [B] ) pH - pKa = log ( [B] / [BH+] );;Three types of functional membrane proteins. ;Models of transmembrane transport across the lipid bilayer;2.2 Free and Bound Forms Plasma protein binding Tissue / organ affinity;3. Fate of the drug in the body Absorption Distribution Metabolism (Biotransformation) Excretion － ADME;3.1 Absorption Absorption is the transfer of a drug from its site of administration to the blood stream. Gastrointestinal tract Parenteral injection - i.m., s.c. Inhalation Transdermal ;(1) Gastrointestinal tract Route: Oral Sublingual Rectal Absorption sites: Oral Gastric Intestinal Rectal;Factors influencing absorption: blood flow to the absorption site total surface area available for absorption contact time at the absorption surface physic-chemical properties of the drug first-pass elimination;(2) Parenteral injection intramuscular injection ( i.m. ) subcutaneous injection ( s.c. ) Determinants Local blood flow; Solubility of the drug (3) Others Inhalation; Intranasal; Transdermal