[pharma] absorption (2)
TRANSCRIPT
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AbsorptionAbsorptionOf Of
DrugsDrugs
Dr. Naveed Iqbal AnsariDr. Naveed Iqbal Ansari
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DefinitionDefinition
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Cell membraneCell membrane
StructureStructure
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Schematic diagram of an absorption membraneSchematic diagram of an absorption membrane
Lattice ofprotein
Lattice ofprotein
Inner lipoidalmatrix
Aqueous pores
Hydrophilic tail
Hydrophobic head
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The Process
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Simple TransportSimple diffusionFiltration
Facilitated TransportActive transportFacilitated diffusionPinocytosis
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Facilitated Diffusion
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Active Transport
Active Transport
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Endocytosis
Endocytosis
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Factors Affecting absorptionFactors Affecting absorption
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PharmacologyPharmacology
DrugsDrugs Tissue Tissue
1. Physico-chemical 1. Physico-chemical Routes of Routes of
PropertiesProperties Administration Administration
2. Quantity2. Quantity
(dose)(dose)
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Factors related to the drugFactors related to the drug
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Physico-Chemical PropertiesPhysico-Chemical Properties
1.1. Molecular weight/sizeMolecular weight/size
2.2. NatureNature
3.3. ValencyValency
4.4. Lipid/Water partition co-efficientLipid/Water partition co-efficient
5.5. IonizationIonization
PkaPka
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SolubilitySolubility
Lipid SolubilityLipid SolubilityPresence of benzene ringPresence of benzene ringHydrocarbon chainHydrocarbon chainHalogen (Bromine, Chlorine)Halogen (Bromine, Chlorine)
Water solubilityWater solubilityPresence of alcohol (-OH)Presence of alcohol (-OH)Amide (-CO.NHAmide (-CO.NH22))Carboxylic (-COOH)Carboxylic (-COOH)Formation of Glucuronide & Sulfate Formation of Glucuronide & Sulfate
conjugatesconjugates
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QuantityQuantity
DoseDose
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Factors related to the bodyFactors related to the bodyRoutes of administrationRoutes of administration
a.a. For local effectsFor local effectsa.a. SkinSkinb.b. GITGITc.c. Respiratory tractRespiratory tract
b.b. For systemic effectsFor systemic effectsa.a. SkinSkinb.b. GITGITc.c. Respiratory TractRespiratory Tractd.d. Par-enteralPar-enteral
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Routes of Drug DeliveryRoutes of Drug Delivery
Parenteral(IV)
Inhaled
Oral
Transdermal
Rectal
Topical
Parenteral(SC, IM)
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Absorption from the SkinAbsorption from the Skin
Must cross several cell layers Must cross several cell layers (stratum corneum, epidermis, (stratum corneum, epidermis, dermis) to reach blood vessels.dermis) to reach blood vessels.
Factors important here are:Factors important here are:
lipid solubilitylipid solubility
hydration of skinhydration of skin
site (e.g. sole of feet vs. site (e.g. sole of feet vs. scrotum)scrotum)
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Factors Affecting Absorption Factors Affecting Absorption from the GI Tractfrom the GI Tract
FORMULATIONFORMULATION Disintegration of dosage form and Disintegration of dosage form and
dissolution of particlesdissolution of particles Chemical stability of chemical in gastric Chemical stability of chemical in gastric
and intestinal juices and enzymesand intestinal juices and enzymes Motility and mixing in GI tractMotility and mixing in GI tract Presence and type of foodPresence and type of food Rate of gastric emptying Rate of gastric emptying Blood flow to GI tractBlood flow to GI tract Passage across GI tract wallPassage across GI tract wall
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Absorption from the LungsAbsorption from the Lungs
For gases, vapors and volatile liquids, For gases, vapors and volatile liquids, aerosols and particlesaerosols and particles
In general: large surface area, thin In general: large surface area, thin barrier, high blood flow rapid barrier, high blood flow rapid absorptionabsorption
Blood:air partition coefficient – Blood:air partition coefficient – influence of respiratory rate and influence of respiratory rate and blood flow blood flow
Blood:tissue partition coefficientBlood:tissue partition coefficient
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Par-enteral routePar-enteral route
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Bioavailability
for i.v.: 100%for i.v.: 100% for non i.v.: for non i.v.:
ranges from 0 to 100%ranges from 0 to 100%
lidocaine bioavailability 35% lidocaine bioavailability 35% due to destruction in gastric due to destruction in gastric acid and liver metabolismacid and liver metabolism
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Sustained release Sustained release preparationspreparations
depot injections depot injections (oily, viscous, particle size) (oily, viscous, particle size)
multilayer tablets multilayer tablets (enteric coated)(enteric coated)
sustained release capsules sustained release capsules (resins)(resins)
infusorsinfusors (with or without sensors)(with or without sensors)
skin patches skin patches (nicotine, GTN)(nicotine, GTN)
pro-drugspro-drugs liposomesliposomes
Targeted drugs , antibody-directedTargeted drugs , antibody-directed