Notes in Modified Release Products

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Published	11/09/2023	Reasons for Creating Modified-Release ProductsDeliver right {{c1::amount}} of therapeutic agent at {{c1::right time and to right place}}Patience {{c1:…
Published	11/09/2023	Evolution of Modified-Release Drug Delivery System (3)50-60s  {{c1::Delayed}} release, {{c1::sustained}} release70s  {{c1::Control}} of rele…
Published	11/09/2023	Classification Based on Mechanisms of Drug Release (Product Design) (4){{c1::Dissolution}} controlled - coating and matrix systems{{c1::Diffusion}} co…
Published	11/09/2023	Prodrugs (5){{c1::Active}} structure or parent drug is in its {{c1::latent}} form.Undergoes {{c1::biotransformation in vivo}} to be con…
Published	11/09/2023	Prodrugs Rationale: Improved Performance (6)Physical{{c1::Chemical Stability}}, {{c1::Solubility}}, {{c1::Taste/Odor}}Biopharmaceutical{{c1::Absorptio…
Published	11/09/2023	Examples of Prodrugs (7){{c1::Pivampicillin}} --> {{c1::Ampicillin}}{{c2::Prodrug is better absorbed.}}{{c1::L-Dopa}} --> &n…
Published	11/15/2023	Slide 9
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Published	11/09/2023	Factors to be Considered in Design of Modified Release Products (13){{c1::Half-life}}: 2-8 hours{{c1::Size of Dose}}: 0.5 – 1 G{{c1::Ionization, pKa}}…
Published	11/09/2023	Rate Controlling Mechanism (14)governed by the {{c1::slowest rate}}e.g. release rate, permeation ratemore than one mechanism may be utilized
Published	11/09/2023	Dissolution-Controlled Systems{{c1::Dissolution}} of the drug in the medium controls the {{c1::rate}} of drug release.Drugs with a {{c1::slow dissolut…
Published	11/15/2023	Noyes - Whitney Equation Slide 16
Published	11/15/2023	Design of Dissolution-controlled Delivery Systems IMPORTANTDrugs have multiple layersOutermost layer is the dissolving coat, which can vary in {{c1::t…
Published	11/15/2023	2 examples of Dissolution controlled products Slide 19{{c1::spansules capsules}}{{c1::injection dosage form}}
Published	11/15/2023	Spansules{{c1::beads with different coating thickness surrounding the API}}e.g.{{c1::benzedrine}}{{c2::amphetamine sulfate}}{{c1::ornade}}{{c2::phenyl…
Published	11/15/2023	Dissolution Controlled Products{{c1::Contac Capsules®Phenylpropanolamine HCl, Chlorpheniramine Maleate, Atropine Sulfate, Scopolamine HBr, Hyoscyamine…
Published	11/15/2023	Polymer Dissolution/Erosiondrug is {{c1::coated or entrapped}} in polymer which is {{c1::initially insoluble but becomes soluble over time due to hydr…
Published	11/15/2023	Enteric Coatings1884 –{{c1::Dr. Paul Unna introduced keratin-coated pills}}Late 1880’s to 1930’s – {{c1::Numerous substances and their combination wer…
Published	11/15/2023	Diffusion Controlled SystemsFick's First LawJ = - D (dC/dX){{c1::flux = - diffusion coefficient of drug x (change in conc. of drug/change in thickness…
Published	11/15/2023	Reservoir System{{c1::A core of drug (reservoir) surrounded by an inert polymeric membrane. }}{{c1::Polymers used for coating include ethyl cel…
Published	11/15/2023	Reservoir System:MOA: Rate of drug release is controlled by {{c1::the rate of diffusion across the polymer coating.}}
Published	11/15/2023	Reservoir System MechanismdMt/dt=ADK/h×ΔCdMt =  {{c1::Mass of drug released after time, t}}dMt/ dt =  {{c1::steady-state release r…
Published	11/15/2023	Reservoir System: Zero Order Releasesame equationDesign a system with {{c1::constant A, D, K, h and DC}} dC may be constant if drug in reservoir …
Published	11/15/2023	Reservoir System DisadvantagesIf the system is {{c1::implanted}}, it must be {{c1::removed}} after depletion of the system or failure.If the syst…
Published	11/15/2023	Matrix SystemsThe drug may be {{c1::suspended and/ or dissolved}} in the polymer matrix which {{c1::swells and facilitates release}}.Dr…
Published	11/15/2023	Matrix SystemDrug is dispersed in a {{c1::solid dispersion medium}} which is insoluble ({{c1::non-erodible}}) or less soluble ({{c1::erodible}}) …
Published	11/15/2023	Non-erodible mediums {{c1::increase}} membrane thickness over time
Published	11/16/2023	rate of drug releaseDifferent Rate Processes affect the rate of drug release in matrix systemsRate of {{c1::solvent diffusion into polymer matrix}}Rat…
Published	11/15/2023	Examples of Matrix System Products{{c1::Dimetane Extentabs ®}}{{c2::Brompheniramine Maleate from Robins}}{{c1::Roniacol Timespan from Roche}}{{c2::Nic…
Published	11/15/2023	Swelling Controlled Systemdrug {{c1::dissolved in polymer}} initially (t = 0)over time, {{c1::polymer swells from which drug has been released}}conc. …
Published	11/15/2023	Diffusion Controlled Systems Examples{{c1::Transdermal}} {{c1::Ocular }}{{c1::Intrauterine }}{{c1::Implant }}{{c1::Oral }} …
Published	11/15/2023	Ocular SystemTopical delivery in the eyes has a short duration due to {{c1::tears and tear drainage.}}Absorption in the eyes is limited to {{c1::10}}%…
Published	11/15/2023	Examples of Ocular System{{c1::OCUSERT}} by ALZA2 release rates (20 and 40 mcg/hr); controlled by the {{c1::composistion of membranes (EVA)}}di (2-eth…
Published	11/15/2023	Eye Drop vs. Ocusertocusert {{c1::maintains more constant drug release for extended periods of time with one dose}}eye drop requires {{c1::multiple do…
Published	11/15/2023	Intravaginal and Intrauterine SystemsDelivery of {{c1::contraceptive hormones}}The advantages include better {{c2::bioavailability, lower dose, and av…
Published	11/15/2023	ImplantsLong durationAdvances in material sciences make it possible.{{c1::Due to the long term contact with tissue}}, biocompatibility, sterility and …
Published	11/15/2023	Transdermal SystemsAny type of formulation that allows the drug to transit from the {{c1::outside of the skin through various layers of the skin into …
Published	11/15/2023	Advantages of Transdermal SystemsAvoids the vagaries of {{c1::GI}} milieu – unpredictable{{c1::By-pass hepatic clearance}}No {{c1::needles}}…
Published	11/15/2023	Disadvantages of Oral or IV SystemsFairly {{c1::hostile}} environment{{c1::low gastric pHenzymesmucus}}{{c2::Invasive}} (iv){{c2::Multiple d…
Published	11/15/2023	Skin Barrierfour distinct regions: stratum {{c1::corneum, granulosum, spinosum, basale}}stratum {{c1::corneum}} is a stratified squamous epitheliumfun…
Published	11/15/2023	Pathways of Transport Transdermaldrug goes through the {{c1::stratum corneum}}
Published	11/15/2023	Factors affecting Skin PermeabilityHINT: skin has oil{{c1::MW}} - {{c2::large}} {{c1::MW}} = low permeability{{c1::polarity}} - {{c2::lower}} = better…
Published	11/15/2023	Ideal Candidates for Transdermal DeliveryKnown pharmacokinetic and pharmacodynamics informationTotal dose less than {{c1::20}} mg{{c1::Achievable}} ef…
Published	11/15/2023	Types of Transdermal Systems{{c1::semi-solid ointment}}{{c1::cream lotion}}{{c1::viscous dispersions}}({{c2::Nitrobid}}- is an ointment containing 2% …
Published	11/15/2023	Types of Transdermal Systems{{c1::Peripheral Adhesive}}{{c2:: drug-loaded matrix or reservoir, has a RELEASE LINER, controlled by SKIN}}{{c1::Res…
Published	11/16/2023
Published	11/15/2023	Limitations of Transdermal SystemsLong {{c1::lag times – takes way longer than oral}}Low {{c1::permeability coefficient }}Low {{c1::drug solubili…
Published	11/15/2023	Chemical Enhancersincreasing the {{c1::solubility of drug}} in the vehicle increasing {{c1::drug solubility}} in the stratum corneum -partitioning red…
Published	11/15/2023	Enhancement - Iontophoresis{{c1::Anode is positively charged, so place positively charged drug that is pushed away from the anode. Opposite is true fo…
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Published	11/16/2023	Spanules Slide 20beads with different coating thicknesses of the dissolving coating layer that surrounds the drugexamples{{c1::benzedrine}}generic: {{…
Published	11/16/2023	Dissolution-Controlled Products Slide 21{{c1::Contac}} Capsules®{{c2::Phenylpropanolamine HCl, Chlorpheniramine Maleate, Atropine Sulfate, Scopolamine…
Published	11/16/2023	Polymer Dissolution/Erosionpolymer is {{c1::insoluble}} until {{c1::hydrolysis or ionization}} occurs, making it solubleimplies that compounds not sus…
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