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Absorption of Drugs
Absorption of Drugs
2.
3.
CELL MEMBRANE
70-100 angstrom units
Trans-cellular absorption Para-cellular absorption
Passive diffusion Convective transport (Pore transport) Facilitated diffusion Active transport Ionic diffusion Ion-pair transport Endocytosis Phagocytosis Pinocytosis
Shabaz & Prasanna; Manipal university, Manipal
PASSIVE DIFFUSION
1. Passive diffusion
It is called as non-ionic diffusion. Membrane transport of drug and other chemicals directly through the lipid or aqueous channel is called passive diffusion. The rate of drug transfer is directly proportional to the concentration or electro chemical gradient. Greater the area and lesser the thickness of the membrane, faster the diffusion; thus more rapid is the rate of drug absorption from intestine than from stomach. It follows FICKS FIRST LAW of diffusion.
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1. Passive diffusion
FICKS FIRST LAW of diffusion states drug molecule diffuses from a region of higher conc. to the lower conc. until equilibrium is attained.
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dQ/dt: rate of drug diffusion (amt/time) D: diffusion coeff. Of drug through membrane A: surface area of membrane Km/w: partition coeff. of drug bet. lip. Membrane & aq. GI fluid CGIT-C : conc. Diff. in drug in GI fluid and plasma h: thickness of the membrane
Hmmmm..
equation Cefazolin
FACILITATED DIFFUSION
Carrier mediated transport system operates down the conc. gradient
E.g.- Vit. B12 & IF
ABC proteins
ATP-Binding Cassette Transporters (ABC)
P-glycoprotein (P-gp or MDR1) Multidrug Resistance Associated Proteins
ACTIVE TRANSPORT
Low to high conc.
Energy required E.g Enalapril small peptide carrier system
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INTESTINE TRANSPORTERS
AA transporter Oligopeptide transporter Phosphate tranporter MCA transporter Gabapentin Captopril Foscarnet Pravastatin
IONIC DIFFUSION
Rate of permeation is Unionized mole.> anions > cations
Endocytosis
Cellular uptake of macromolecular nutrients like Fats, starch, oil soluble vitamins like A, D, E & K and drugs like insulin. It includes two processes: a. Phagocytosis (Cellular uptake of solid particles) b. Pinocytosis (Uptake of fluid solute)
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Summary of Mechanisms
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Solubility
Lipid soluble drugs drugs
that can be dissolved in lipids fatty substances that make up cell membranes including the blood-brain barrier
that can dissolve in water they will not passively move through a cell membrane so they require active transport
Bioavailability
Bioavailability indicates a measurement of the rate and extent (amount) of therapeutically active drug which reaches the general circulation. Absolute bioavailability is the absolute fraction of dose which is available from a drug formulation in general circulation. It is measured by comparing AUC after i.v. and extravascular administration. Relative bioavailability is a relative amount and relative rate of availability if two formulations (other than i.v.) are compared.
1. PHARMACEUTICAL FACTORS II. Dosage form Related Factors a. Disintegration time b. Dissolution time c. Manufacturing variables d. Excipients e. Nature & type of dosage form f. Product age & storage condition
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ii Compression Force
d. Excipients
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CAPSULES
ABSORPTION POWDERS SUSPENSIONS EMULSIONS SOLUTIONS
GRANULES
Deaggregation
fastest
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