Pharmaceutical Drug Delivery Systems

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Questions and Answers

What is the primary mechanism by which drugs can enter the brain through the olfactory system?

  • Paracellular diffusion or axonal transport (correct)
  • Endocytosis through the olfactory bulb
  • Facilitated diffusion via Bowman’s gland
  • Exocytosis from olfactory nerve cells

Why is the olfactory epithelium significant in drug delivery to the central nervous system?

  • It is an area without the blood-brain barrier. (correct)
  • It has a larger surface area than the olfactory bulb.
  • It is the only region where drugs can cross via receptor-mediated endocytosis.
  • It is a major site for metabolic activity.

What is a major challenge when optimizing delivery systems for intranasal drug delivery?

  • Ensuring the drugs are stable at room temperature.
  • Increasing the viscosity of the drug formulation.
  • Decreasing the absorption through the nasal mucosa.
  • Avoiding clearance from the olfactory region. (correct)

Which of the following statements about ocular drug delivery is true?

<p>It is used primarily for treating local ocular conditions. (B)</p> Signup and view all the answers

What disease condition is mentioned as associated with ocular drug delivery?

<p>Blepharitis (B)</p> Signup and view all the answers

What characterizes a generic drug in comparison to its branded counterpart?

<p>It must be identical in safety and efficacy. (D)</p> Signup and view all the answers

Why do generic drug companies often see lower profits compared to branded companies?

<p>They operate in a more competitive market with many alternatives. (A)</p> Signup and view all the answers

What was a significant change in the pharmaceutical landscape during the 90s and 00s?

<p>There was a rise in the acceptance of generic drugs among healthcare professionals. (D)</p> Signup and view all the answers

What role do health ministers typically have in relation to generic drugs?

<p>They support the use of generic drugs to manage health spending. (A)</p> Signup and view all the answers

What is the primary factor that triggers the generic business for a drug?

<p>The expiration of patent protection. (B)</p> Signup and view all the answers

What is an additional benefit of generic drugs for consumers?

<p>They are usually more affordable than brand-name drugs. (A)</p> Signup and view all the answers

What is a hallmark of the lifecycle management strategy utilized by pharmaceutical companies?

<p>To continuously renew patent protection for drugs. (D)</p> Signup and view all the answers

Which type of drug is described as having identical dose and route of administration as the leading brand?

<p>Generic drug (C)</p> Signup and view all the answers

Which term is accurately defined as what the body does to the drug?

<p>Pharmacokinetics (B)</p> Signup and view all the answers

What does bioavailability primarily measure?

<p>Extent and rate of absorption (A)</p> Signup and view all the answers

Which process is considered a major determinant of pharmacokinetics?

<p>Drug liberation (A)</p> Signup and view all the answers

What is the significance of the term 'Tmax' in pharmacokinetics?

<p>It describes the time when the drug reaches its maximum concentration (A)</p> Signup and view all the answers

What does the area under the curve (AUC) represent in pharmacokinetics?

<p>Total drug exposure over time (C)</p> Signup and view all the answers

In the context of intravenous (IV) administration, what aspect of drug absorption is not relevant?

<p>Rate of absorption (D)</p> Signup and view all the answers

What does the term 'duration of action' refer to in pharmacokinetics?

<p>The length of time a drug remains effective in the body (D)</p> Signup and view all the answers

How is the minimum effective concentration (MEC) defined?

<p>The concentration threshold below which the drug is ineffective (B)</p> Signup and view all the answers

What is the primary reason dosage forms are used instead of pure substances?

<p>To ensure accurate dosing and delivery (B)</p> Signup and view all the answers

Which of the following is NOT a requirement of dosage forms?

<p>Placement of drugs directly into blood plasma (B)</p> Signup and view all the answers

What defines an excipient in a pharmaceutical formulation?

<p>All components of a formulation other than the active drug (A)</p> Signup and view all the answers

Which function does NOT pertain to the use of excipients?

<p>Provide the active therapeutic effect (A)</p> Signup and view all the answers

Why is sustained release medication an important feature of dosage forms?

<p>It requires less frequent dosing (B)</p> Signup and view all the answers

What role do excipients play in terms of safety and effectiveness of the drug product?

<p>They enhance stability and bioavailability (B)</p> Signup and view all the answers

Which of these statements about Nurofen's market strategy is accurate?

<p>All Nurofen products contain the same active ingredient and dosage. (C)</p> Signup and view all the answers

What is a potential concern regarding the use of excipients like gelatin?

<p>They may cause allergic reactions (A)</p> Signup and view all the answers

What is a primary reason for film coating ibuprofen tablets?

<p>To avoid gastric mucosal irritation (D)</p> Signup and view all the answers

Which of the following is NOT a requirement for an ideal oral solid dosage form?

<p>Drug must have a bitter taste (B)</p> Signup and view all the answers

Which of the following dosage forms allows for rapid absorption through the mucous membranes of the mouth?

<p>Sublingual tablets (A)</p> Signup and view all the answers

What challenge is faced in the formulation of drugs with poor flow properties?

<p>Inability to produce tablets (A)</p> Signup and view all the answers

What is the primary purpose of disintegrants in tablet formulation?

<p>To ensure the tablet breaks up in the GI tract (C)</p> Signup and view all the answers

Why is it challenging to formulate high-dose, low-potency drugs?

<p>They may have poor flow and compressability (D)</p> Signup and view all the answers

What type of ingredient is used to provide bulk and compressibility in tablet formulation?

<p>Diluents (B)</p> Signup and view all the answers

Which medication has a significantly lower dosage compared to typical drugs, requiring careful measurement?

<p>Ethinyl estradiol - 0.01 mg (B)</p> Signup and view all the answers

What is the significance of the pH level ranging from 4.0 to 5.5 in relation to skin permeability?

<p>It is the optimal range for skin barrier function and drug stability. (A)</p> Signup and view all the answers

Which population group is likely to have reduced skin permeability due to age-related factors?

<p>Premature babies and the elderly due to thinner skin layers. (A)</p> Signup and view all the answers

What mechanism is primarily used by microneedles to enhance drug delivery through the skin?

<p>Temporary increase in skin permeability. (B)</p> Signup and view all the answers

How does transdermal delivery facilitate systemic effects for potent drugs?

<p>It ensures sustained drug concentrations over extended periods. (C)</p> Signup and view all the answers

What is a potential outcome when using drug delivery patches?

<p>Control over the timing of drug delivery can be adjusted. (B)</p> Signup and view all the answers

Which pathway is described as a 'cutaneous first-pass' mechanism?

<p>Chemical modifications of drugs in skin tissues. (D)</p> Signup and view all the answers

What is a primary feature of the LidoSiteâ„¢ delivery system?

<p>Uses iontophoresis to enhance drug delivery. (D)</p> Signup and view all the answers

What aspect of skin physiology significantly impacts drug absorption?

<p>Local physiological conditions affecting epithelial barrier. (B)</p> Signup and view all the answers

Flashcards

Pharmacokinetics (PK)

The study of how the body affects a drug, including absorption, distribution, metabolism, and excretion.

Pharmacodynamics (PD)

The study of how a drug affects the body, including its mechanism of action and therapeutic effects.

Liberation

The process of drug release from its dosage form, like a tablet or capsule.

Absorption

The movement of a drug from its administration site into the bloodstream.

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Distribution

The distribution of a drug throughout the body, reaching different tissues and organs.

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Metabolism

The process by which the body breaks down a drug into metabolites.

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Excretion

The elimination of a drug and its metabolites from the body, primarily through urine and feces.

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Plasma Concentration vs Time

A graphical representation showing the concentration of a drug in the plasma over time.

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What is a dosage form?

The way a drug is delivered to its target site within the body.

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What is an excipient?

Components of a formulation that are not the active drug. They are usually non-medicinal and help with things like stability, taste, and processing.

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Why is dose control important?

Ensuring the correct amount of drug is delivered to the patient. This is important for safety and effectiveness.

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How do dosage forms protect drugs?

Dosage forms help protect drugs from degradation, like being broken down by stomach acids or other factors. This ensures the medicine remains effective.

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How do dosage forms affect drug absorption?

Dosage forms can change the rate at which a drug is absorbed into the body. This allows for controlled release or sustained release of medicine.

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Why are there different dosage forms?

Different dosage forms are needed because they offer various benefits. This can include better patient compliance, drug stability, and more effective delivery.

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How do dosage forms address taste and odor issues?

Dosage forms mask unpleasant tastes and odors, making it easier for patients to take medication.

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How do dosage forms achieve controlled or sustained release?

Dosage forms can be designed to release the drug over a specific time period, ensuring a sustained or controlled release of the active ingredient.

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What is a Generic Drug?

A drug that is chemically identical to an original brand-name drug, but sold under a different name. Generics are often cheaper because they do not require the same level of research and development as the original brand.

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What is the 'Generic Business'?

The period when a drug's patent protection expires, allowing other companies to manufacture and sell generic versions of the drug.

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What is 'Lifecycle Management'?

A drug company's strategies to extend the market life of their brand-name drugs, often by developing new formulations, uses or indications for the drug, potentially delaying generic entry.

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What does it mean for a generic drug to be 'bioequivalent'?

A drug that is considered to be the same in quality and effectiveness as the original brand-name drug.

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What was the '90's - 00's: The Era of Generics'?

The era when generic drug companies gained significant ground in the pharmaceutical market due to several key factors, including increasing aging populations, growing middle class, and government policies favouring generic drugs.

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What is 'Patent Extension'?

The practice of a company extending the patent protection for its brand-name drug by developing minor variations or new applications for the drug, often criticized for potentially delaying access to cheaper alternatives.

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How did the acceptance of generics play a role in their rise?

The acceptance of generic drugs by doctors, pharmacists, and patients, contributing to the success of the generic market.

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How did government policy support the growth of generic drugs?

The use of generic drugs by governments to reduce healthcare costs, leading to a major shift in the pharmaceutical industry.

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Low Dose Formulation Challenges

Difficulty in manufacturing tablets due to the drug's small dosage, making it challenging to ensure a consistent and uniform blend.

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High Dose Formulation Challenges

High dose drugs can be difficult to formulate into tablets because they have poor flow and compression properties, making it hard to produce compact and stable tablets.

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Why are ibuprofen tablets film-coated?

Film coating tablets helps to protect the stomach lining from irritation caused by the active drug, reducing the risk of ulcers and digestive problems.

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What are tablets?

A solid, compressed medication typically in round, oval or square shapes.

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Tablet Excipients

Excipients are inactive ingredients used in tablet formulation to help with various aspects of the manufacturing process and the tablet performance.

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Dissolution of Tablets

Dissolution is essential for oral solid dosage forms to release the drug and make it available for absorption. This process depends on disintegrants, which break down the tablet into smaller particles.

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Buccal and Sublingual Tablets

Sublingual and buccal tablets are placed under the tongue or between the cheek and gum, respectively. They dissolve rapidly and are absorbed directly into the bloodstream, bypassing the stomach and liver.

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Ideal Oral Solid Dosage Form

Oral solid dosage forms are popular because they are convenient and often the most cost-effective way to deliver medication. They must be stable, bioavailable, with consistent drug content, and easy to produce.

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Olfactory epithelium

A specialized area in the nasal cavity where the blood-brain barrier is weak, allowing direct drug entry into the brain.

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Nose-to-Brain Drug Delivery

A drug delivery route utilizing the nose to directly deliver drugs to the brain, bypassing the blood-brain barrier.

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Axonal transport

The process by which a drug moves from the administration site to reach the brain through the olfactory nerve cells.

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Blood-Brain Barrier

A barrier that protects the brain from harmful substances in the blood.

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Ocular Drug Delivery

Drugs administered directly to the eye for local treatment, not suitable for delivering drugs throughout the body.

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What factors influence skin permeability?

Skin permeability can be influenced by various factors such as patches, pH levels, age, injuries or diseases, and location on the body.

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What is cutaneous first-pass metabolism?

A process where the skin metabolizes drugs, breaking them down into simpler components that can be eliminated from the body.

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What is Iontophoresis?

A method that applies electrical current to the skin to enhance drug delivery by opening up the pores and allowing for deeper penetration into the skin.

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How do microneedles increase skin permeability?

Microneedles are tiny needles that can temporarily increase skin permeability without causing pain, allowing for efficient delivery of drugs, biologics, and vaccines.

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What is pharmacokinetics?

The study of how the body affects a drug, covering aspects like absorption, distribution, metabolism, and excretion.

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What is pharmacodynamics?

The study of how a drug affects the body, including its mechanism of action and therapeutic effects.

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How does transdermal drug delivery benefit from bypassing first-pass metabolism?

Transdermal drug delivery offers a way to bypass the first-pass metabolism in the liver.

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What is the advantage of sustained drug concentrations with transdermal delivery?

Transdermal drug delivery offers sustained drug levels in the body, helping maintain therapeutic efficacy.

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Study Notes

Fundamentals of Pharmacy/Pharmacology: The Science of Medicines

  •  This unit covers the fundamentals of pharmacy and pharmacology, focusing on the science of medicines.
  •  Lecture 1 introduces the unit's topics.
  •   An outline is provided detailing topics like the reasoning behind the study of the science of medicine, pharmaceutics, the medicine approval process, the journey of a medicine, teaching and learning methods, assessment procedures, support and help resources.
  •  Year One units are broken down in Pharmacy and Pharmacology, detailing specific subjects with credit values.
  •  Why study the science of medicines? This is a core topic exploring the chemistry of drugs, drug discovery and the connection to health and disease
  • The science of medicines: This encompasses topics such as drug discovery and the chemistry of drugs associated with health and disease in the context of delivery to the patient.
  • "From bench to bedside" illustrates the journey a new treatment takes to become an NHS prescription, taking 10+ years from drug discovery to getting the drug available for patients. This process involves stages like lab testing, clinical trials, marketing authorisation, initial price setting, and appraisal by NICE and then to funding decision and availability.
  • Pharmaceutics: Key study point involving drug formulation, drug delivery systems and biopharmaceutics.

Science of Medicines = PHARMACEUTICS

  • Drug formulation. This involves accounting for physicochemical drug properties, stability, and delivery routes to produce an appropriate dosage form.
  • Drug delivery systems. This explores the innovative methods of improving drug efficacy, patient compliance and reducing side effects, by targeting drugs to specific cells/tissues.
  • Biopharmaceutics. The study of drug absorption, distribution, metabolism, and excretion (ADME) following administration, to aid the design of dosage forms.
  • Quality control. Ensuring quality, identity, dosage, and safety throughout the manufacturing process of a medicine.
  • Regulatory science. The science of developing new tools, standards, and approaches to assess the safety, efficacy, quality, and performance of medicines.

The journey of a medicine

  •  This unit focuses on turning a drug into a medicine and what happens once it's taken/delivered to the patient.
  • Drug properties, such as molecular weight, lipophilicity, ionization, solubility, dissolution rate, and chemical stability affect the development of the drug delivery system.
  •  The content covers drug properties and how they are used in drug delivery system development, concerning different delivery routes. These include: Lipophilicity, Ionization, Solubility vs pH, Dissolution rate, Chemical stability, and Particle size, crystallinity and hygroscopicity for solid drugs; and Compatibility with excipients and packaging materials.
  • Illustrates the process through the diagram of a drug being transformed into a medicine and how it affects the patient.

Dosage forms

  •  Visual examples of diverse dosage forms
  • Different dosage forms exist depending on the specific drug, desired effects, patient characteristics, and admin route
  •  Illustrates various dosage forms, like tablets and pills, capsules, solutions, creams, ointments, injections, inhalers, etc.,

Effects of drug

  •  (physicochemical properties), dosage form and physiology on release and absorption
  • This section discusses the organs involved in drug's journey into, around, and out of the body, with an overview on ADME and pharmacokinetic components
  •  The detailed analysis of different elements that influence both the release and absorption of a drug in the body. This is connected to the different organ systems of the body and their parts.

Unit overview (MPharm)

  • Provides a detailed breakdown of the unit's syllabus and schedule.
  •  Includes week-by-week lecture schedules, workshops, and tutorials.
  • Includes links and guidance pertaining to assessments for different semesters.

Unit overview (Pharmacology)

  •  A summary of the unit, including weekly schedules, workshops, and assessments; with links to resources.

Semester 1 & 2 topics

  • Key topics for each semester of the unit presented in an organised list format

Learning outcomes

  • Summarizes the key learning outcomes of the unit and the unit's overall objectives.

Teaching on the unit

  • Explains the teaching strategies for the unit.

Teaching on the unit – MPharm only

  • Describes additional teaching approaches specifically for MPharm students.

Problem-based learning (PBL) – MPharm only

  • Presents the approach and detailed tasks for the problem-based learning component of the unit. Explains what to expect in the workshops.

Assessment

  •  A breakdown of assessments for the MPharm and Pharmacology parts of the unit, detailing the components of each examination, and the necessary scores required to pass the unit. 

Moodle

  • Information on access, resources, and communication tools available through the Moodle platform for this course.

Semester 1 topics

  • Detailed outline of topics covered during semester one, in the list format.

Semester 2 topics

  • Detailed outline of topics covered during semester two. Presented in a list format.

What is a medicine?

  • Definition of medicine and its components, along with examples of brands and generics. 

Medicinal product nomenclature

  • Details about the naming convention for medicinal products, differentiating between brand names, chemical names, and trademarks.

Branded Drugs

  • How new medicines are marketed as branded products, the process of obtaining marketing authorization (MA), and the role of patents. 

Patent vs Marketing Life

  • An illustrative graph representing the correlation between patent and marketing lifetimes for drugs.

Pharmaceutical Research & Development (R&D) Industry

  • This section covers the purpose and processes of the pharmaceutical R&D industry.

Pharmaceutical R&D Industry

  •  Focuses on the need for market growth and funding the next generation of compounds, including the need for a pipeline of new chemical entities (NCEs).

Astra Zeneca Pipeline (2014)

  •  Provides a detailed breakdown of Astra Zeneca's drug pipeline, categorizing the compounds by their type and stage.

Pharmaceutical R&D companies have a mixed portfolio of products

  •  Illustrates the portfolio mix of pharmaceutical R&D companies.

Global Distribution of Pharmaceutical Sales

  •  Visually represents the global distribution of pharmaceutical sales, showing percentages allocated to different countries.

Medicines expenditure per person

  •  Provides a table comparison of medicines expenditure per person in different countries, including monetary figures

What $250 of Qvar looks like ...

  •  Visually compares the equivalent price of prescription medications for different purchases.

Blockbuster drug model

  • Overview of the blockbuster drug model in the pharmaceutical industry.

Other sections

  •  More detailed study points from the remaining pages of slides. This covers different aspects of drug delivery, as well as drug testing methodologies

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