Pharmaceutical Dosage Forms Overview
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Pharmaceutical Dosage Forms Overview

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Questions and Answers

What is the primary purpose of buccal tablets?

  • To dissolve completely before swallowing
  • To achieve rapid systemic circulation
  • To provide local effects on mouth ulcers (correct)
  • To replace traditional oral medications

    • Which mechanism allows sublingual tablets to achieve rapid effects?

  • Controlled dissolution rate
  • Extended release formulation
  • First pass metabolism
  • Absorption through the oral mucosa (correct)

    • What is NOT a major limitation of conventional oral formulations?

  • High oral doses required
  • Controlled release delivery (correct)
  • Variation in oral absorption
  • Inconvenience of short plasma half-lives

    • What is an ideal characteristic of a drug for oral controlled release (OCR) formulation?

    <p>High therapeutic index</p> Signup and view all the answers

    Which strategy is NOT commonly used in the formulation of controlled release drugs?

    <p>Increasing the drug's solubility</p> Signup and view all the answers

    What does improving bioavailability in drug formulation aim to achieve?

    <p>Effective concentration at the site of action</p> Signup and view all the answers

    What distinguishes sustained release from delayed release drug formulations?

    <p>Onset of drug absorption</p> Signup and view all the answers

    Which factor is essential for controlling the release rate of a drug?

    <p>pH of the delivery environment</p> Signup and view all the answers

    What is one significant reason for formulating drugs into solid dosage forms?

    <p>To ensure safer and more accurate dosing</p> Signup and view all the answers

    What is a primary advantage of solid dosage forms compared to liquid formulations?

    <p>Solid forms offer more accurate dosing</p> Signup and view all the answers

    Which patient population may have difficulties with solid dosage forms?

    <p>Patients who are unconscious or intubated</p> Signup and view all the answers

    What is the benefit of enteric-coated tablets?

    <p>They prevent drug degradation in gastric acid</p> Signup and view all the answers

    What process is used to create capsules, including hydrogel and softgel capsules?

    <p>Rotary die process</p> Signup and view all the answers

    What is a common limitation of solid dosage forms?

    <p>Slower digestion and absorption rates</p> Signup and view all the answers

    Which formulation type can provide site-specific drug delivery?

    <p>Rectal suppositories</p> Signup and view all the answers

    What characteristic of solid dosage forms contributes to their longer shelf life?

    <p>Stable physical state</p> Signup and view all the answers

    What is the primary advantage of using soft gelatin capsules (SGCs) for drug formulation?

    <p>They are herded-sealed and contain liquid or semi-liquid medication.</p> Signup and view all the answers

    Which component is added to gelatin in SGCs to plasticize the material?

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

    What purpose do the tampered tips and ridges of coni-snap caps serve?

    <p>Prevent premature opening.</p> Signup and view all the answers

    What is the typical residual moisture content in soft gelatin capsules?

    <p>6-10%</p> Signup and view all the answers

    Which of the following is NOT a feature of soft gelatin capsules?

    <p>Self-locking caps</p> Signup and view all the answers

    What is a significant limitation of solid dosage forms?

    <p>Some drugs, particularly biologics, may not be suitable.</p> Signup and view all the answers

    What characteristic of SGCs contributes to their ease of swallowing?

    <p>Smooth and slippery texture</p> Signup and view all the answers

    Which factor is NOT influential in dosage form design?

    <p>Conditions of use</p> Signup and view all the answers

    What distinguishes soft gelatin capsules (SGCs) from hard gelatin capsules (HGCs)?

    <p>SGCs generally contain liquid contents.</p> Signup and view all the answers

    The content uniformity of soft gelatin capsules typically ranges within what percentage?

    <p>± 3%</p> Signup and view all the answers

    Which of the following ingredients is NOT typically found in the formulation of soft gelatin capsules?

    <p>Liquid nitrogen</p> Signup and view all the answers

    What is the range of desirable bloom strengths for gelatins used in capsules?

    <p>150-280 g</p> Signup and view all the answers

    Which property of gelatin is an empirical measure of gel strength?

    <p>Bloom strength</p> Signup and view all the answers

    What is the primary component commonly used in producing hard gelatin capsules?

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

    Which of the following is NOT an advantage of hard gelatin capsules (HGCs)?

    <p>Difficulties in swallowing</p> Signup and view all the answers

    What characteristic makes gelatin ideal for use in capsules?

    <p>Swells but is insoluble in cold water</p> Signup and view all the answers

    What does diffusion control in drug formulations primarily refer to?

    <p>Mass transfer from high to low concentration</p> Signup and view all the answers

    What is the primary role of the semi-permeable membrane in OROS drug delivery systems?

    <p>To release drug at a controlled rate</p> Signup and view all the answers

    Which factor does NOT affect the diffusional flux according to the content?

    <p>Time taken</p> Signup and view all the answers

    What is meant by matrix disintegration in the context of drug formulations?

    <p>The physical structure breaks down gradually</p> Signup and view all the answers

    In a diffusion-controlled delivery system, the term tortuosity refers to what?

    <p>The complexity of the diffusion pathway</p> Signup and view all the answers

    Which of the following physical strategies is NOT used for solid oral formulations?

    <p>Partition control</p> Signup and view all the answers

    What is the effect of osmotic pressure in drug formulations like OROS?

    <p>It drives water influx leading to drug release</p> Signup and view all the answers

    Study Notes

    Why Pharmaceutical Dosage Forms?

    • Safe and convenient delivery of accurate dosing
    • Project drug substance from atmospheric oxygen or humidity
    • Protect drug substance from gastric acid after oral administration
    • Conceal bitter, salty or offensive taste or odor of a drug substance
    • Provide liquid preparations of an insoluble or unstable drug
    • Provide rate-controlled drug action
    • Provide site-specific drug delivery

     Advantages of Solid Dosage Forms

    • Convenient to carry, readily identified and easily taken
    • Longer shelf life before expiring
    • Efficiently produced
    • Easier to package, distribute, ship, and store
    • The dosing is more accurate, comparing to liquid formulation
    • Possibility of controlled drug delivery

    Disadvantages of Solid Dosage Forms

    • Certain patients population may have difficulty swallowing large tablets or capsules
    • Solid dosage forms are not appropriate for patients who are unconscious or intubated
    • Solid dosage forms take longer to break down, dissolve, absorb, and distribute in the body
    • Therefore, solid dosage form may not fit for emergency intervention
    • Some drugs (esp. biologics) are not suitable in a solid dosage form

    Influential Factors in Dosage Form Design

    • Molecular Size and Volume
    • Drug solubility and pH
    • Partition Coefficient
    • Polymorphisms
    • Stability
    • pKa/Dissociation Constant
    • Particle size and dissolution rate
    • Membrane permeability

    Capsules

    • Solid dosage forms in which the drug is enclosed within either a hard or a soft soluble container or ‘shell’
    • Filled capsules are generally swallowed whole, sometimes caregivers may open the capsule and mix the drug with food/drink

    Hard Gelatin Capsules (HGC)

    • Elegant
    • Easy to use, convenient
    • Smooth, slippery, easily swallowed
    • Tasteless
    • Economical
    • Better bioavailability
    • Diverse formulations i.e., beads, granules, microtablets, semisolids

    Properties of Gelatin

    • Molecular weight ~20-200 kDa
    • Usually mixtures of Type A and B are used
    • Bone gelatin contributes firmness but is hazy
    • Pork skin gelatin contributes plasticity and clarity
    • Two main physicochemical properties:
      • Bloom strength: empirical measure of gel strength, measured in Bloom gelometer, weight in grams required to depress a standard plunger into the surface of 6.67% w/w gel, desirable bloom strengths: 150-280 g
      • Viscosity

    Industrial Manufacture

    • Sealing and banding: prevents separation, tamperproof (not safety proof)
    • Self-locking caps: Snap-Fit, Coni-snap, coni-snap supra (Capsugel), Loxit (Pharmaphil)

    Soft Gelatin Capsules (SGC)

    • A one-piece, hermetically-sealed formulation containing medication in a liquid or semi-liquid state that has been formed, filled, and sealed in one operation.

    Advantages of SGCs

    • Elegant
    • Easy to use, portable, convenient
    • Smooth, slippery, easily swallowed
    • Taste masking
    • Requires the drug to be liquid, or at least dissolved, solubilized, or suspended in a liquid vehicle (e.g., clofibrate®, reduces serum triglycerides; is ethyl ester prodrug of clofibric acid, replaced by fenofibrate) or drugs in a liquid vehicle (e.g., digoxin, Lanoxicaps®).
    • Metered liquid fill very accurate
    • Homogeneous – content uniformity of ± 3% reported
    • Local effect: mesalamine

    Buccal & Sublingual Tablets

    • Bypass the first pass metabolism

    Buccal Tablets

    • Intended to dissolve in buccal cavity (or gums)
    • Usually designed to dissolve slowly
    • Prolonged effects – contains bioadhesive to adhere to inside of mouth
    • Duration of effect: 15-45 mins to 6-8 hours
    • Fentanyl citrate (Actiq) intrabuccal/transmucosal lozenge
    • Ideal for drugs that can be destroyed or poorly absorbed in GI
    • Local effects – mouth ulcers (directly on affected area)
    • Lozenges (troches)

    Sublingual Tablets

    • Placed under the tongue
    • Allow to dissolved
    • Rapid effect
    • Avoids first pass effect
    • Examples: glyceryl trinitrate (rapid effect), testosterone (poor GI availability – no longer in US)

     Controlled Release Dosages

    • Control rate of drug delivery (release)
    • Control onset, duration, and intensity of effect
    • Control site of absorption
    • Reduce total dose required
    • Improve bioavailability
    • Improve safety (particularly of drugs with low TI)
    • Improve efficacy of drugs with short plasma half-lives
    • Improve compliance

    Terminology

    • Controlled delivery
    • Sustained delivery
    • Prolonged delivery
    • Delayed delivery
    • Pulsed delivery, repeat action
    • Localized delivery
    • Site-specific delivery, targeted delivery

    IDEAL DRUG FOR OCR FORMULATION

    • A low molecular weight, freely water-soluble drug that is well and/or predictably absorbed and metabolized after oral administration, with a low plasma half-life (< 8 h) and high therapeutic index (> 10).

    Formulation Strategies for CR formulations

    • PHYSICAL (most common). Controlled dissolution, diffusion, disintegration (erosion), pH effects, osmosis, density.
    • CHEMICAL - prodrugs.
    • BIOLOGICAL e.g., antibodies
    • MECHANICAL e.g., pumps
    • PHARMACOLOGICAL.e.g.Probenecid-penicillin

    PHYSICAL STRATEGIES

    • Diffusion control
    • Dissolution control
    • Erosion (disintegration)
    • Osmotic control
    • pH dependent
    • Ion-exchange
    • Density control (low and high)
    • Partition control (NOT for solid oral formulations)

    Diffusion-based formulation

    • Diffusion through semi-permeable membrane (film coating). Reservoir system
    • Diffusion through nondisintegrating matrix (tablet but also semi-solid ointment or viscous liquid)

    Diffusion Controlled Delivery

    • Diffusion is the mass transfer of drug molecules by random motion from a region of high concentration to lower concentration. 𝑀
    • The diffusional flux is proportional to the concentration gradient, dC/dx. 𝑑𝐶

    Diffusion Controlled Delivery

    • Diffusion through insoluble, non-disintegrating matrix
    • If matrix disintegrates, drug release rate depends on rate of disintegration, dissolution, or both.
    • Matrix

    OROS

    • Drug reservoir- conventional tablet
    • coating - semipermeable
    • Principle of operation: water flows into tablet due to osmotic pressure, at a rate controlled by permeability of membrane. Water dissolves drug, increases hydrostatic pressure inside tablet. Drug in solution forced to leave via orifice.

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    Description

    Explore the importance, advantages, and disadvantages of pharmaceutical dosage forms. This quiz will cover the various aspects of solid dosage forms, including their benefits and limitations in medical applications. Test your understanding of drug delivery systems.

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