Advanced Oral Dosage Formulation Approaches
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Questions and Answers

What is a major advantage of extended-release formulations compared to immediate-release formulations?

  • They offer more convenience and consistency in drug delivery. (correct)
  • They provide inconsistent plasma concentrations.
  • They lead to increased adverse reactions.
  • They require more frequent dosing.

    • What factor significantly influences the rate of diffusion in diffusion-controlled release systems?

  • The color of the polymeric membrane.
  • The viscosity of the dissolution medium. (correct)
  • The shape of the drug molecules.
  • The temperature of the drug reservoir.

    • In reservoir systems of diffusion-controlled release, what role does the polymeric membrane play?

  • It prevents any contact with the drug reservoir.
  • It controls the rate at which drugs diffuse out. (correct)
  • It dissolves the drug molecules.
  • It increases the molecular size of the drug.

    • Which of the following most accurately describes the release of drugs in non-porous diffusion systems?

    <p>Release follows Fick’s Law of diffusion.</p> Signup and view all the answers

    What aspect of porous diffusion systems influences drug release the most?

    <p>The size and dimensions of the pores in the membrane.</p> Signup and view all the answers

    What is the primary characteristic of delayed release medication?

    <p>Drug is released at a time later than administration</p> Signup and view all the answers

    What factor most commonly triggers the disintegration of delayed release drugs?

    <p>pH level</p> Signup and view all the answers

    Which patient condition may lead to an early release of enteric coated drugs?

    <p>Higher than normal stomach pH</p> Signup and view all the answers

    What purpose do enteric coatings serve for certain medications?

    <p>To protect sensitive drugs from the stomach environment</p> Signup and view all the answers

    Why is a delayed release formulation preferred for aspirin?

    <p>It avoids gastrointestinal mucosa damage</p> Signup and view all the answers

    What is a potential issue with the gastrointestinal pH affecting delayed release formulations?

    <p>It can vary, making outcomes unpredictable</p> Signup and view all the answers

    What type of polymers are most commonly used in enteric coatings and delayed release formulations?

    <p>Polymethacrylates</p> Signup and view all the answers

    Which advice should be given to a patient taking enteric coated tablets?

    <p>Swallow the tablet whole without crushing</p> Signup and view all the answers

    What is the primary objective of modified release drug delivery systems?

    <p>To modulate the rate of drug input in the intestinal tract</p> Signup and view all the answers

    Which of the following is NOT an advantage of modified release dosage forms?

    <p>Immediate relief of symptoms</p> Signup and view all the answers

    Which drug property is critical for formulating modified release dosage forms?

    <p>High lipophilicity (logP 1-5)</p> Signup and view all the answers

    Which type of modified release design allows for a drug to be released at a specific time in the gastrointestinal tract?

    <p>Programmed release</p> Signup and view all the answers

    What is the potential benefit of absorbing drugs from the colon in modified release formulations?

    <p>Improved bioavailability due to lesser drug degradation</p> Signup and view all the answers

    How does solubility influence modified release dosage forms?

    <p>Good solubility provides multiple formulation options</p> Signup and view all the answers

    Why is it important for the daily dose of a drug in a modified release formulation not to exceed 1g?

    <p>To keep the dosage form within a manageable size for swallowing</p> Signup and view all the answers

    What happens if a drug is inactivated by enzymes faster than it is released?

    <p>Higher presystemic drug loss</p> Signup and view all the answers

    What mechanism primarily controls drug release in hydrophobic matrix systems?

    <p>Diffusion and erosion of the polymer</p> Signup and view all the answers

    Which of the following polymers is NOT commonly used in hydrophobic matrix systems?

    <p>HPMC</p> Signup and view all the answers

    What effect do larger pore sizes in a hydrophobic matrix have on drug release?

    <p>Enable faster release of the drug</p> Signup and view all the answers

    What is a common result of drug depletion closest to the surface of a hydrophobic matrix?

    <p>Difficulties in achieving zero-order release</p> Signup and view all the answers

    What defines bioerosion in hydrophilic matrix systems?

    <p>Gradual dissolution of the polymer by physiological fluids</p> Signup and view all the answers

    For a slow drug release formulation in hydrophobic systems, which characteristic is preferred?

    <p>High molecular weight polymers with cross-linking</p> Signup and view all the answers

    In a hydrophilic matrix system, what is a primary method of polymer degradation?

    <p>Chemical or enzymatic processes</p> Signup and view all the answers

    Which statement correctly describes the physical state of hydrophobic matrix systems throughout the gastrointestinal tract?

    <p>They remain intact and undigested</p> Signup and view all the answers

    Which type of polymer is primarily associated with enzymatic degradation and potential immunogenic responses?

    <p>Chitosan</p> Signup and view all the answers

    What characteristic of an elementary osmotic pump can cause irritation if the drug becomes stuck in the gastrointestinal tract?

    <p>High osmotic pressure</p> Signup and view all the answers

    Which factor is NOT critical in influencing the release rate of a drug in osmotic controlled release systems?

    <p>pH of the dissolution medium</p> Signup and view all the answers

    What is the primary mechanism by which a push-pull osmotic pump releases drug?

    <p>Osmotically driven pressure from an additional layer</p> Signup and view all the answers

    In an osmotic pump, what is the purpose of the semi-permeable membrane?

    <p>To allow water into the core while preventing drug escape</p> Signup and view all the answers

    Which of the following is NOT a possible strategy for modifying drug release in an osmotic pump system?

    <p>Adding a hydrophobic coating</p> Signup and view all the answers

    What happens when the osmotic pressure is insufficient in drug delivery systems?

    <p>An osmagent may need to be added</p> Signup and view all the answers

    Controlled-porosity osmotic pumps differ from elementary pumps primarily by their?

    <p>Microporous membrane that creates multiple release points</p> Signup and view all the answers

    Which statement about drug solubility in controlled release systems is true?

    <p>Highly soluble drugs are less likely to be good candidates</p> Signup and view all the answers

    What is one key benefit of using synthetic biodegradable polymers over natural ones?

    <p>Greater batch consistency</p> Signup and view all the answers

    What happens if the delivery orifice is too large in a water soluble amino acid device?

    <p>Release becomes diffusion controlled.</p> Signup and view all the answers

    Which of the following is NOT a requirement for drugs intended for sublingual delivery?

    <p>Should be absorbed from the GIT.</p> Signup and view all the answers

    What is a significant disadvantage of sublingual drug delivery compared to buccal drug delivery?

    <p>Constant washing by saliva.</p> Signup and view all the answers

    Which of the following is a major advantage of buccal drug delivery?

    <p>It can provide local and systemic delivery.</p> Signup and view all the answers

    What common polymer is primarily used for the coating membrane in water soluble amino acids delivery systems?

    <p>Cellulose acetate.</p> Signup and view all the answers

    What should patients be warned about when using large dosage forms of water soluble amino acids?

    <p>Excretion of undigested capsule shells may occur.</p> Signup and view all the answers

    Which of the following does NOT belong to the types of dosage forms used in buccal drug delivery?

    <p>Oro-dispersible tablets.</p> Signup and view all the answers

    Which sublingual drug delivery system has a predictable potency and fast absorption?

    <p>Sublingual sprays.</p> Signup and view all the answers

    What is a major drawback of oro-dispersible tablets?

    <p>They can be challenging to retain in the mouth.</p> Signup and view all the answers

    What characteristic contributes to the better retention of buccal dosage forms compared to sublingual forms?

    <p>Less saliva washing.</p> Signup and view all the answers

    Study Notes

    Advanced Oral Dosage Formulation Approaches

    • Solid oral dosage form design aims to deliver the correct drug amount to the site of action at the correct rate, maximizing therapeutic response and minimizing side effects.
    • Modified release design aims to modulate drug input in the intestines to achieve a predefined plasma profile.
    • This includes delayed, sustained, programmed, and site-specific/timed release.

    Modified Release Drug Delivery

    • Aims to manipulate drug release from dosage forms to deliver API at desired rates and predefined time points or specific sites in the gastrointestinal tract (GIT).
    • Advantages include controlled release rate and site, improved efficacy, optimized performance, and reduced side effects.
    • Enables local GIT treatment.
    • Drug properties such as solubility and permeability influence modified release dosage forms.

    Solubility

    • Good solubility allows for more formulation options.
    • Very low solubility drugs are intrinsically sustained-released due to slow dissolution.

    Permeability

    • Drugs must be sufficiently permeable (lipophilic, logP 1-5) to provide faster absorption than release from the dosage form.

    Transport mechanism

    • Oral drug absorption varies based on specific transport mechanisms in different parts of the gut. Drugs with limited absorption windows may require different administration times for optimal absorption.
    • Daily dose should not exceed 500 mg-1g to manage swallowing.

    Enzymatic Inactivation

    • Drugs inactivated by enzymes faster than released will have higher presystemic drug loss.
    • Absorption from the colon may increase bioavailability as some enzymes (CYP3A4) are absent there, preventing drug degradation.

    Types of Modified Release

    • Delayed Release: Drug is released after administration with a lag time before being detectable in the blood. Dosage forms disintegrate after the stomach.
    • Extended Release: Formulated for extended drug availability, leading to reduced dosage frequency. Allows for more consistent plasma concentrations and fewer adverse effects.

    Diffusion Controlled Release

    • Reservoir Systems: Drug molecules are contained in a reservoir surrounded by a polymer membrane.
    • Diffusion though the membrane controls drug release rate. The dissolved drug then diffuses out the dosage form.
    • Porous systems: the size and dimension of the pores are related to the pore-forming agent. Drug release occurs through the porous pathways.
    • Matrix systems: drug substance is homogeneously dispersed with rate-controlling material. Drug release through erosion of the polymer or diffusion.

    Osmosis Controlled Release

    • Osmosis occurs when water moves through a semipermeable membrane from high concentration to low.
    • Release rate is independent of pH.
    • Osmotic pumps use a semi-permeable membrane to maintain a constant osmotic pressure. Fluid volume in the gut controls drug release.

    Sublingual Drug Delivery

    • Drugs placed under the tongue are absorbed into the bloodstream, avoiding first-pass metabolism.
    • Advantages include fast absorption, predictable potency, and convenience.
    • Disadvantages include incompatibility with food, issues with controlled release, and difficulty maintaining positioning.

    Buccal Drug Delivery

    • Drug delivery through the buccal mucosa.
    • Advantages include patient compliance, rapid onset, high accessibility, and reduced toxicity compared to other routes.
    • Advantages could also include ease of administration in pediatric or geriatric patients.
    • Disadvantages include a lower absorption rate than sublingual.

    Coronary Stents, Devices, and Thrombolytic Drugs

    • Percutaneous coronary intervention combines coronary angioplasty with stenting.
    • Bare metal stents are simple scaffolds without coatings; drug-eluting stents release bioactive agents to reduce restenosis.
    • Drug-eluting stents use polymer coatings which carry anti-proliferative drugs to prevent restenosis.
    • Bioresorbable stents dissolve gradually, reducing long-term impacts.

    Pharmaco-mechanical Thrombectomy Systems

    • Combines mechanical clot removal with thrombolytic drug infusion via catheter.
    • Advantages include reduced duration and dose of medication, minimizing the impacts of systemic medication.
    • Disadvantages are the same as with mechanical thrombectomy alone.

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    Advanced Oral Dosage Formulation Approaches PDF

    Description

    This quiz focuses on advanced principles of oral dosage form design, emphasizing modified release strategies for optimal drug delivery. It covers aspects such as the manipulation of drug release rates, the benefits of solubility, and the importance of targeting specific sites within the gastrointestinal tract. Test your knowledge on these critical concepts in pharmaceutical formulation.

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