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UCSD BIMM 118 - Lecture 2

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The Four Cornerstones of PharmacokineticsDrug Administration and AbsorptionOral Drug AdministrationSlide 4Slide 5Slide 6Slide 7Percutaneous Drug AdministrationSlide 9Slide 10Slide 11Other Topical Drug AdministrationSlide 13Parenteral Drug AdministrationSlide 15Drug DistributionSlide 17Slide 18Slide 19Slide 20Slide 21Slide 22Slide 23Slide 24Slide 25Slide 26Slide 27Slide 28Slide 29Therapeutic RangeSlide 31Slide 32Slide 33Drug Metabolism and EliminationBIMM118The Four Cornerstones of Pharmacokinetics•Absorption•Distribution•Metabolism•EliminationAbsorption and distribution are influenced by the formulation:Medicinal Agent --> Formulation --> MedicationGalenic = Science of pharmaceutical formulation(Galenos of Pergamon, 129-199 AD)BIMM118Drug Administration and Absorption•Oral•Topical (Percutaneous)•Rectal or Vaginal•Pulmonal•ParenteralRoutes of Drug Administration:BIMM118Oral Drug Administration•Pills–Antiquated single-dose unit; round, produced by mixing drug powder with syrup and rolling into shape•Tablets–Oblong or disk-like shape, produced through mechanical pressure; filler material provides mass; starch or carbonates facilitate disintegrationQuickTime™ and aTIFF (Uncompressed) decompressorare needed to see this picture.BIMM118Oral Drug Administration•Coated Tablets–Tablet covered by a “shell” (wax, highly specialized polymers = Eudragit®) to facilitate swallowing, cover bad taste or protect active ingredient from stomach acidQuickTime™ and aTIFF (Uncompressed) decompressorare needed to see this picture.BIMM118Oral Drug Administration•Matrix Tablets–Drug is embedded in inert “carrier” meshwork --> extended or targeted (intestinal) release•Capsules–Oblong casing (Gelatin); contains drug in liquid, powder or granulated form•Troches or Lozenges; Sublingual Tablets–Intended to be held in the mouth until dissolvedQuickTime™ and aTIFF (Uncompressed) decompressorare needed to see this picture.QuickTime™ and aTIFF (Uncompressed) decompressorare needed to see this picture.BIMM118Oral Drug AdministrationBIMM118Oral Drug Administration•Aequous Solutions (with Sugar=Syrup)–Mostly for pediatric use–20 drops=1g•Alcoholic Solutions (=Tinctures)–Often plant extracts–40 drops=1g•Suspensions–Insoluble drug particles in aequous or lipophilic mediaQuickTime™ and aTIFF (Uncompressed) decompressorare needed to see this picture.QuickTime™ and aTIFF (Uncompressed) decompressorare needed to see this picture.QuickTime™ and aTIFF (Uncompressed) decompressorare needed to see this picture.BIMM118Percutaneous Drug AdministrationSpecific formulation determined by physician/dermatologist: •based on skin type:–Dry vs. Oily–Young vs. Old–Intact vs. Injured•based on drug properties:–Hydrophilic vs. Lipophilic–Soluble vs. InsolubleBIMM118Percutaneous Drug AdministrationBIMM118Percutaneous Drug Administration•Ointment and Lipophilic Cream–Either pure lipophilic base (lanolin=wool fat; paraffin oil; petrolium jelly) or “water-in-oil” emulsions•Paste–Ointment with >10% pulverized solids (e.g. Zinc- or Titanium-Oxide)•Lotion and Hydrophilic Cream–“oil-in-water” emulsions•Gels–Either alcohol or aequous solution based (Ethanol gels --> Cooling effect)–Increased consistency due to gel-forming agentsQuickTime™ and aTIFF (Uncompressed) decompressorare needed to see this picture.QuickTime™ and aTIFF (Uncompressed) decompressorare needed to see this picture.BIMM118Percutaneous Drug Administration–Single Layer•Inclusion of the drug directly within the skin-contacting adhesive. In this transdermal system design, the adhesive not only serves to affix the system to the skin, but also serves as the formulation foundation–Multi-Layer•Similar to Single-layer, however, the multi-layer encompasses either the addition of a membrane between two distinct drug-in-adhesive layers or the addition of multiple drug-in-adhesive layers under a single backing film–Reservoir•Inclusion of a liquid compartment containing a drug solution or suspension separated from the release liner by a semi-permeable membrane and adhesive.QuickTime™ and aTIFF (Uncompressed) decompressorare needed to see this picture.QuickTime™ and aTIFF (Uncompressed) decompressorare needed to see this picture.QuickTime™ and aTIFF (Uncompressed) decompressorare needed to see this picture.•Transdermal Drug Delivery Systems =“Patches” (Nicotin, Isosorbid-Nitrate)BIMM118Other Topical Drug Administration•Eye Drops•Sterile; Isotonic; pH-neutral•Nose Drops/Nasal Sprays•Viscous Solutions•Pulmonary Formulations•Inhalation anesthetics (Hospital use only)•Nebulizers (mostly propellant operated) •dispense defined amount of Aerosol (= dispersion of liquid or or solid particles in a gas)•Size of aerosol particles determines depth of penetration into the respiratory tract: >100 m: Nasopharynx10-100 m: Trachea, bronchii<10 m: Bronchioli, alveoliQuickTime™ and aTIFF (Uncompressed) decompressorare needed to see this picture.BIMM118Other Topical Drug Administration•Suppositories •Drug incorporated into a fat with a melting point ~35ºC•Rectal: Absorption mostly intended into systemic circulation (e.g. analgesics)•Vaginal: Effects intended to be confined to site of application (e.g. candidiasis)QuickTime™ and aTIFF (Uncompressed) decompressorare needed to see this picture.BIMM118Parenteral Drug AdministrationSterile; iso-osmolar; pyrogen-free; pH=7.4•Ampules–Single use (mostly with fracture ring)•Single and Multi-dose Vials–10-100 ml; contain preservatives•Cartridge ampules•Infusions–Solution administered over an extended period of timeBIMM118Parenteral Drug Administration•Advantages:–100% “Absorption”–Drug enters general circulation without hepatic passage -->No first-pass hepatic elimination–Better bioavailability of hydrophilic drugs•Bioavailability/Speed of Absorption–Intravenous (i.v.): Fastest (infusions; cardio-vascular drugs)–Intramuscular (i.m.): Medium (anti-inflammatory; antibiotics)–Subcutaneous (s.c.): Slowest (vaccines; insulin; depot contraceptives)BIMM118Drug DistributionBIMM118Drug Distribution•To be absorbed and distributed, drugs must cross barriers (membranes) to enter and leave the blood stream. •Body contains two type of barriers which are made up of epithelial or endothelial cells:–External (Absorption Barriers): Keratinized epithelium (skin),


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UCSD BIMM 118 - Lecture 2

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