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What is the primary function of a plasticizer in a polymer coating?

  • To enhance the color consistency of the coating
  • To improve flexibility and adhesion properties of the film (correct)
  • To increase the polymer's molecular rigidity
  • To reduce manufacturing costs of the polymers
  • Which of the following is NOT a recommended component of aqueous coating?

  • Glycerin
  • Tweens
  • Low molecular weight polyethylene glycol
  • Castor oil (correct)
  • What concentration range of plasticizers is commonly recommended for film formers?

  • 10-70% w/w
  • 0-5% w/w
  • 15-40% w/w
  • 1-50% w/w (correct)
  • Lakes pigments are preferred colorants for sugar or film coating systems because they:

    <p>Produce more predictable color outcomes (A)</p> Signup and view all the answers

    Opaquants are primarily used in coating solutions to:

    <p>Provide more pastel colors and increase film coverage (C)</p> Signup and view all the answers

    Which plasticizer is primarily water-soluble and commonly used in aqueous coating?

    <p>Low molecular weight polyethylene glycol (D)</p> Signup and view all the answers

    What impact do plasticizers have on the molecular structure of polymers?

    <p>They decrease molecular rigidity and increase flexibility (A)</p> Signup and view all the answers

    Which of the following statements about opaquants is true?

    <p>They can mask the color of the tablet core (C)</p> Signup and view all the answers

    Which factor does NOT influence the concentration of plasticizers used?

    <p>Color of the coating (C)</p> Signup and view all the answers

    Which of the following best describes the interaction of plasticizers with polymers?

    <p>They allow polymers to become more flexible (B)</p> Signup and view all the answers

    What is the primary reason for not adding color to tablets until they are quite smooth?

    <p>To avoid a mottled appearance in the final product (D)</p> Signup and view all the answers

    In the context of polishing tablets, which wax is commonly used to achieve luster?

    <p>Carnauba wax (A), Beeswax (C)</p> Signup and view all the answers

    Which of the following is NOT a reason film coating is preferred over sugar coating?

    <p>It provides a sweeter taste (D)</p> Signup and view all the answers

    What is a potential consequence of using a spraying speed that is too high during the pan spray method?

    <p>Uneven drying time resulting in rough tablets (D)</p> Signup and view all the answers

    During the sugar coating process, what is the critical aspect that should be controlled to ensure uniform coating?

    <p>The pan shape, load, and rotational speed (B)</p> Signup and view all the answers

    What is a crucial characteristic of tablets for coating to resist abrasion during the coating process?

    <p>The tablets must possess proper physical strength. (C)</p> Signup and view all the answers

    Which of the following tablet shapes is preferred for coating?

    <p>Consistently intact tablet shapes without defects. (B)</p> Signup and view all the answers

    Which type of coating material is NOT preferred when tablets have surfaces that are affected by coating compositions?

    <p>Film coating materials. (B)</p> Signup and view all the answers

    In the tablet coating process, what happens to tablet surfaces that are brittle?

    <p>They typically become rough in the early phases of coating. (C)</p> Signup and view all the answers

    Which of the following is NOT a primary component in studying tablet coating?

    <p>Tablet size for easy handling. (C)</p> Signup and view all the answers

    What is one of the effects of using coating compositions on tablet surfaces?

    <p>They may cause the surfaces to soften. (A)</p> Signup and view all the answers

    Why must tablets be able to resist chipping during the coating process?

    <p>To withstand mechanical stress from other tablets and equipment. (A)</p> Signup and view all the answers

    What is the ideal shape for tablets during the coating process to prevent agglomeration?

    <p>Sphere (D)</p> Signup and view all the answers

    What happens if a square flat-faced tablet is used during the coating process?

    <p>It forms lumps and glues together (D)</p> Signup and view all the answers

    Which property is NOT essential for coating materials used on tablets?

    <p>Ability to change with aging (C)</p> Signup and view all the answers

    What is the purpose of adding surfactants to the coating solution?

    <p>To ensure proper wetting of the tablet surface (B)</p> Signup and view all the answers

    Which of the following statements about the properties of coating materials is true?

    <p>They must aesthetically enhance the product (B)</p> Signup and view all the answers

    What characterizes the non-enteric materials used for tablet coating?

    <p>They tend to solubilize in the GI tract (C)</p> Signup and view all the answers

    What property should coating materials have regarding their interaction with common additives?

    <p>They should exhibit full compatibility (C)</p> Signup and view all the answers

    Which of the following coating characteristics is most critical for ensuring the coating adheres properly?

    <p>Surface hydrophobicity/hydrophilicity matching (D)</p> Signup and view all the answers

    Why is it important to ensure that coating materials do not bridge or fill the debossed tablet surfaces?

    <p>It prevents drug release interference (C)</p> Signup and view all the answers

    What is the main advantage of using Hydroxypropyl Methylcellulose (HPMC) in tablet coating?

    <p>It can incorporate color and other additives without difficulty. (B)</p> Signup and view all the answers

    Which statement best describes the non-ideal property of Hydroxypropyl Methylcellulose (HPMC)?

    <p>It can cause bridging and filling of debossed tablet surfaces. (D)</p> Signup and view all the answers

    Why is Ethyl Cellulose (EC) not suitable for use alone in tablet coating?

    <p>It is soluble in organic solvents but not in water. (C)</p> Signup and view all the answers

    Which of the following characteristics is NOT true for Ethyl Cellulose (EC)?

    <p>It has good solubility in water. (A)</p> Signup and view all the answers

    What is the primary reason for applying enteric coating to tablets?

    <p>To protect the drug from stomach enzymes. (D)</p> Signup and view all the answers

    Which of the following is NOT a benefit of using Hydroxypropyl Methylcellulose (HPMC) in film coating?

    <p>Bridging of tablet surfaces. (A)</p> Signup and view all the answers

    What problem is typically encountered when using Hydroxypropyl Methylcellulose (HPMC) alone as a coating agent?

    <p>It can fill debossed surfaces on tablets. (B)</p> Signup and view all the answers

    Which enteric material is known to solubilize based on pH changes in the gastrointestinal tract?

    <p>Cellulose Acetate Phthalate. (B)</p> Signup and view all the answers

    Among the following, which property of HPMC contributes to its effectiveness as a coating agent?

    <p>Ability to incorporate additives seamlessly. (C)</p> Signup and view all the answers

    Flashcards

    Tablet Coating Process

    A process involving three main parts: tablet properties, coating compositions, and coating processes, to coat tablets.

    Ideal Tablet Shape for Coating

    Tablet shape crucial for withstanding coating process stresses and maintaining integrity during coating.

    Tablet Physical Properties

    Factors like strength, stability, and resistance to mechanical stress that affect the tablet's ability to withstand the coating process.

    Tablet Shape for Coating

    Tablets must have an intact shape and no imperfections to maintain integrity during coating.

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    Coating Compositions

    Substances used in coating tablets, including solvents, plasticizers, colorants, and opaquants, which affect coating and protection.

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    Preferred Tablet Properties

    Important and desirable characteristics for tablets to endure the coating process, including strength and shape integrity

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    Brittle Tablet Surfaces

    Tablets that become rough in the coating process due to sensitivity to heat and coating materials, and thus are unacceptable for film coating.

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    Tablet Coating

    The process of applying a thin, protective layer to tablets, usually for taste masking, controlled release, or improved appearance.

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    Why are square tablets bad for coating?

    Square tablets tend to stick together during coating because coating materials collect between the flat surfaces.

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    Tablet Surface Compatibility

    The tablet's surface must be compatible with the coating material to ensure proper adhesion and wetting.

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    What are surfactants used for in coating?

    Surfactants are added to coating solutions to improve the wetting of the tablet surface by the coating material.

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    What are film-forming materials?

    Polymers that are used to create the protective film coating around the tablet.

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    Non-enteric Coating Materials

    These materials dissolve in the GI tract, releasing the drug quickly.

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    Ideal Properties of Coating Materials

    Coating materials should be soluble, aesthetically pleasing, stable, tasteless, and non-toxic.

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    Resistance to Cracking

    Coating materials should be strong enough to prevent cracking or chipping to ensure prolonged effectiveness.

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    HPMC Coating

    Hydroxypropyl methylcellulose (HPMC) is a versatile coating material used for air suspension and pan-spray coating. It offers good solubility in organic and aqueous solvents, doesn't interfere with drug release, and is flexible, tasteless, and odorless.

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    HPMC Non-Ideal Trait

    HPMC, when used alone, can bridge and fill in the grooves of tablets. This can lead to uneven coatings and challenges.

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    Ethyl Cellulose (EC) Coating

    Ethyl Cellulose (EC) is a coating material completely insoluble in water and stomach fluids. It's often mixed with water-soluble polymers like HPMC to control water solubility.

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    Enteric Coating Purpose

    Enteric coatings are designed to protect the drug from the stomach's acidic environment or to protect the stomach from the drug itself.

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    Enteric Coating Materials

    Enteric materials, like HPMCP, Cellulose Acetate Phthalate, and Acrylate Polymers, dissolve at different pH levels within the gastrointestinal tract.

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    HPMC Advantages

    HPMC excels as a tablet coating due to its solubility in organic and water-based solvents, non interference with drug release, flexibility, lack of taste and odor, and stability in different conditions.

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    EC Advantages

    Ethyl Cellulose (EC) is non-toxic, colorless, odorless, and tasteless, and is stable in most environments.

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    EC Limitation

    Ethyl Cellulose (EC) can be brittle without plasticizers.

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    Enteric Coating Benefits

    Enteric coating can protect the drug from stomach enzymes, protect the stomach from harsh drugs, or allow for controlled drug release in the gut.

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    HPMCP

    Hydroxypropyl Methyl Cellulose Phthalate (HPMCP) is an enteric coating material that is soluble in the higher pH environment of the intestines, but not in the acidic stomach.

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    Plasticizer's Role

    A substance added to coating solutions to make the film flexible and improve its adhesion to the tablet.

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    Plasticizer Function

    Plasticizers decrease the rigidity of the polymer, allowing the coating film to bend and conform to the tablet surface.

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    Why Use Plasticizers?

    Without a plasticizer, the coating film would be too brittle and might crack or peel off the tablet.

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    Common Plasticizers for Aqueous Coatings

    Examples include polyethylene glycol (PEG), Tweens, and Spans, these help to make the coating flexible and allow it to adhere well to the tablet.

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    Plasticizers for Organic Coatings

    Examples include castor oil and Spans, these are used when the solvent used is not water.

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    Lakes Pigments

    These are colored pigments used in tablet coatings.

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    Opaquant Function

    Opaquants are fine powders that help to create a more pastel color and improve the coverage of the coating.

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    Opaquant Advantage

    Opaquants are cheaper than colorants and can be used to reduce the amount of colorant needed in the coating solution.

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    Titanium Dioxide

    This is the most common opaquant used in tablet coatings.

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    What makes lakes pigments ideal for coatings?

    Lakes pigments are preferred because they provide consistent, evenly distributed color, ensuring a more reproducible coating for each tablet.

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    Grossing Syrups

    The first syrup coats applied in tablet coating, often containing suspended powders.

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    Why is color added later in sugar coating?

    Premature color addition to rough tablets can create a mottled, uneven appearance in the final tablet.

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    Finishing step in sugar coating

    Applying a few clear syrup coats to provide a smooth, even surface.

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    Polishing in sugar coating

    Achieving the desired shine (luster) by using waxes like beeswax or carnauba wax.

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    Film coating advantage

    It's faster, more economical, and offers flexibility with film-forming polymers.

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    Study Notes

    Tablet Coating

    • Tablet coating is adapted from food preservation processes.
    • The first air suspension coater was created by Dr. Dale Wurster in 1950.
    • Wurster introduced airflow and perforated coating pans into the tablet coating machine.
    • His work led to the first reproducible and uniform tablet coating.

    Tablet Coating Principles

    • Tablet coating increases cost, so decisions are based on multiple factors.
    • Minimizing undesirable taste, odor, or color of the drug.
    • Providing physical and chemical protection for the drug.
    • Controlling the drug's release from the tablet.
    • Protecting the drug from the stomach's acidic environment (enteric coating).
    • Improving the pharmaceutical's appearance through colors and printing.
    • Assisting tablet movement and mobility, particularly for those with dysphagia.

    Tablet Coating Process

    • The process involves the tablet substrate, coating quality, and coating formulation.
    • Each part influences the successful coating of a tablet.

    Tablet Coating: Three Main Parts

    • Tablet Properties: Ideal tablet shape for coating, and tablet physical properties.
    • Coating Compositions: Non-enteric coating materials, enteric coating materials, solvents, plasticizers, colorants, and opaquants.
    • Coating Process: Coating equipment, coating processes (sugar coating, film coating), and evaluation of film and film defects.

    Preferred Tablet Properties for Coating

    • Tablets must withstand intense mechanical stress, and possess an intact shape free of imperfections.
    • Brittle tablet surfaces that soften with heat should not be used for film coating.
    • The ideal tablet shape for coating is a sphere that allows for free rolling in the coating pan, and minimizes tablet-to-table contact.
    • The worst shape is a square flat-faced tablet.
    • Tablet surface hydrophobicity/hydrophilicity should match the coating materials.

    Coating Compositions

    • Coating materials can form a physical deposition on the tablet surface (sugar and wax coatings).
    • Coating materials need to be soluble in the solvent for preparation, produce elegant-looking products, remain stable in the presence of heat, light, moisture, air, and aging.
    • Coating materials should be essentially tasteless, odorless, and colorless.
    • Compatibility with common coating solution additives.
    • Nontoxic and pharmacologically inert.
    • Resistance to cracking.

    Coating Compositions: Film Forming Materials

    • Polymers are used to form the film around tablets.
    • Polymers can be classified as non-enteric and enteric.
    • Non-enteric materials: Tend to solubilize inside the GI tract and release the drug (e.g., Hydroxypropyl methylcellulose (HPMC), Ethyl Cellulose (EC)).
    • Enteric materials: Tend to solubilize depending on the pH of the GI tract (e.g., Hydroxypropyl Methyl Cellulose Phthalate (HPMCP), Cellulose Acetate Phthalate, Acrylate Polymers).

    Non-enteric Materials (Non-Functional FC)

    • Hydroxypropyl methylcellulose (HPMC): Available in different viscosity grades, close to ideal coating polymer for film coating, soluble in organic and aqueous solvents, and flexible and stable. However, when used alone can tend to bridge and fill debossed tablet surfaces.
    • Ethyl Cellulose (EC): Insoluble in water and gastrointestinal fluids, but combined with water-soluble polymers to reduce water solubility, and nontoxic, colorless, odorless, tasteless, quite stable. However, without plasticizers, it can be brittle.

    Enteric Materials

    • The most important reasons for using enteric coating include protecting the drug from the stomach's enzymes, protecting the stomach from the drug, delivering drugs optimally absorbed in the small intestine, and providing a delayed-release component for repeat-action tablets.
    • Ideal enteric coating materials should resist gastric fluids, be permeable to intestinal fluids, and compatible with coating solution components and drug substrates, be stable both alone and in solutions, form a continuous film, be nontoxic, be reasonably priced, and be easy to apply without special equipment.
    • Stomach pH varies from 1-5, enteric materials either resist or are pH sensitive to allow the drug to dissolve and be absorbed in the small intestine.

    Challenges for Enteric Coated Tablets

    • Tablets must pass the USP disintegration test.
    • The pH of the stomach varies from 1 to 5 and varies between individuals.

    Coating Compositions: Specific Materials

    • Cellulose Acetate Phthalate (CAP): Widely used, dissolving above pH 6, but can delay absorption and be hygroscopic.
    • Acrylate polymers (Eudragit): Resistant to gastric fluid, soluble at higher pH levels in the GI tract.
    • Hydroxy Propyl Methyl Cellulose Phthalate (HPMCP): Dissolves at lower pH levels(pH 5-5.5), resulting in higher bioavailability for some drugs.

    Coating Compositions: Solvents

    • Solvents are needed to dissolve or disperse polymers and additives.
    • Ideal solvents should dissolve the polymer system, easily disperse coating components, have low concentrations of polymers without creating excessive viscosity, be colorless, tasteless, odorless, inexpensive, non-toxic, inert, have rapid drying rate, and no environmental impact.
    • Common choices include water, ethanol, chloroform, and acetone but water is preferred due to environmental and economic reasons.

    Coating Compositions: Plasticizers

    • Plasticizers are non-volatile materials that improve flexibility and adhesion properties when incorporated into the film.
    • They can help maintain the flexibility of coated tablets.
    • Common plasticizers include castor oil, glycerin, low-molecular-weight polyethylene glycol (PEG), Tweens, and Spans.

    Coating Compositions: Colorants

    • Colorants can be soluble or insoluble powders.
    • Lakes pigments are a common choice for even color distribution in sugar or film coatings.

    Coating Compositions: Opaquants

    • Fine inorganic powders that increase film coverage and mask the tablet core color.
    • Titanium dioxide is the most commonly used opaquant.

    Coating Process

    • Application of coating materials to moving tablets while simultaneously evaporating the solvent
    • Distribution is done by continuous movement of the tablets through the coating pan.
    • Tablets pass through an application zone where they receive coating materials.
    • Recycled through the application zone until coat is achieved by hot air.

    Coating Equipment: Conventional Pan System

    • A spherical pan mounted angularly and rotate by a motor.
    • Heated air is directed into the tablet bed and exhausted through ducts.

    Coating Equipment: Perforated Pan System

    • A perforated drum that rotates inside a closed chamber.
    • Drying air passes through tablets via the drum's perforations.
    • High coating capacity, and can be automated for sugar and film coating.
    • Coating solution applied through spraying nozzles inside the drum.

    Sugar Coating

    • Frequently used in the past, but a time-consuming process (hours to several days).
    • Excellent appearance.
    • Success strongly relies on the operator's skill, especially with the pan-ladling method.
    • Steps include sealing, subcoating, syruping, finishing, and polishing.
    • Sealing prevents moisture from penetrating the tablet core.

    Film Coating Process

    • Faster and more economic than sugar coating.
    • More versatile film coating polymers that can be used.
    • Slightly increases tablet weight (2-5%).
    • Same equipment as sugar coating can be used.

    Pan Spray Method for Film Coating

    • Introduction of spraying equipment in the film coating process.
    • Automatic control of liquid application.

    Pan Spray Method: Control Variables

    • Variables that depend on the pan shape, load, and speed (e.g., pan variables).
    • Variables concerning speed can result in sticking due to slow speeds or roughness due to high-speed drying issues.
    • The rate of liquid application, degree of atomization, and nozzle-to-bed distance (e.g., spray variables).
    • The Drying Air that needs to be controlled in temperature, volume, and rate.

    Evaluations of Coated Tablets

    • Evaluation of general appearance (color, continuity, size, physical defects).
    • Evaluation of tablet performance (drug release characteristics and stability).
    • Visual inspection is often sufficient for quality assessment.
    • Resistance test is done by rubbing coated tablets on white paper.

    Film Defects

    • Sticking/picking: Overwetting/tackiness causes tablets to stick together or to the pan; poor drying results in stuck films.
    • Roughness: Rough or gritty surfaces from improper spray application; some may dry too rapidly before reaching sufficient mixing.
    • Orange peel effects: Inadequate spreading of the coating solution before drying, appearing bumpy or like an orange peel; too rapid drying and/or excessive viscosity.
    • Bridging/filling: Film may shrink and pull away during the drying stage; due to inadequate plasticizers.
    • Blistering: Rapid solvent evaporation at high temperatures causes inner core issues that are more noticeable during drying in ovens. Milder drying may help.

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