Pharmacology Parenteral Preparations Quiz
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Questions and Answers

Some drugs leach the plasticizer DEHP from ______ containers.

PVC

Type II glass cannot be reused due to the removal of its ______ layer.

internal

One of the advantages of glass bottles is that they are ______ and chemically inert.

transparent

Water for injection (WFI) is completely free of ______ and of high chemical purity.

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

Flexible containers made of ______ do not require an air tube due to their ability to drain solutions by gravity.

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

Sterile preparations include parenteral preparations, ophthalmic preparations, and ______ solutions.

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

Parenteral preparations bypass the ______ canal.

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

IV injection involves administration of Small Volume Parentals (SVP) directly into the ______.

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

IV infusions can provide parenteral nutrition (PN) and total parenteral ______.

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

A general advantage of parenteral preparations includes rapid correction of fluid and electrolyte ______.

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

One limitation of parenteral preparations is that they can be ______ and painful.

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

Mistakes in parenteral preparations, like toxic dose or presence of contaminants, are difficult to be treated and can lead to major ______.

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

Solutions are often composed of ______ as a primary solvent.

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

Suspensions are typically used for drugs that are ______ in water.

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

The common particle size range for suspensions is ______ µm.

<p>5-10</p> Signup and view all the answers

O/W emulsions are commonly used for ______ injections.

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

One major drawback of suspensions is ______.

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

Dry powder formulations are often used for ______ drugs.

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

Reconstituted powders may become a solution or ______ upon mixing.

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

IV emulsions are considered ______ in their application.

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

The pharmacist must be aware of the final reconstitution ______.

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

Solutions are made isotonic with isotonic ______ solution (0.9 % NaCl).

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

The amount of solute required for tonicity adjustment can be calculated using the freezing point ______ method.

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

Packaging materials can include rubber, glass, and ______.

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

Vials are glass bottles with rubber caps that are sealed with an aluminum seal covered with ______ cover.

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

Ampoules are single-dose glass containers for ______ solutions.

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

Pre-filled syringes have the advantage of overcoming problems of particle release and air ______.

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

Parenterals with a volume of 100-1000 ml are classified as ______.

<p>large volume parenterals (LVP)</p> Signup and view all the answers

One of the limitations of vials is the potential for ______ contamination.

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

Parenterals with a volume of less than 100 ml are classified as ______.

<p>small volume parenterals (SVP)</p> Signup and view all the answers

The components of parenteral products include container, active ______, solvent, and additives.

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

Small volume parenterals may include solutions, emulsions, or ______.

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

Multi-dose vials can have limitations such as incomplete sealing and the release of ______ particles.

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

To achieve controlled drug delivery, one method is to increase ______ size.

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

The use of buffers in solutions is important for maintaining ______ balance.

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

Crystalline forms of insulin, such as ______, are preferred over amorphous forms.

<p>insulin lente</p> Signup and view all the answers

Sterile preparations must be completely free from ______.

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

Presence of ______ in parenteral preparations can be fatal during intravenous administration.

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

Preservatives, such as antimicrobial agents, are used to maintain product ______.

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

Specifications of parenteral preparations include sterility, clarity, absence of pyrogens, tonicity, and ______.

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

Long acting injections can be classified under ______ forms of parenteral products.

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

Study Notes

Sterile Pharmaceutical Preparations

  • Sterile pharmaceutical preparations include parenteral preparations, ophthalmic preparations, dialysis solutions (and irrigation solutions), radiopharmaceuticals, and plasma expanders.

Parenteral Preparations

  • Definition: Parenteral preparations are sterile dosage forms delivered to the patient by a way outside the alimentary canal (bypassing it).
  • "Parenteral preparations are sterile preparations intended for administration by injection, infusion, or implantation into human or animal bodies."
  • Parenteral preparations include:
    • Introduction and definitions
    • Advantages and limitations
    • Types of injections (IM, IV, SC, ID, Intraspinal, Intraperitoneal)
    • Classification of injections (small volume parentrals (SVP), large volume parentrals (LVP))
    • Specifications and requirements
    • Components of parenteral products
    • Production process
    • Compendial quality control testing

Differences between IV Injection and IV Infusion

  • IV injection: administration of small volume parentrals (SVP) medications by syringe into a vein, directly into the bloodstream.
  • IV infusion: administration of large volume parentrals (LVP) via a catheter into a vein, directly into the bloodstream.

Advantages of Parenteral Preparations

  • Delivery of drugs with instability in the GI tract (e.g., insulin, heparin).
  • Administration to patients with poor GI absorption (e.g., streptomycin).
  • Administration to patients with irritating drugs.
  • Administration to patients who are unconscious or uncooperative.
  • Rapid correction of fluid and electrolyte imbalance.
  • Treatment for patients who are nauseated or vomiting.
  • Rapid onset of action—important in emergency situations.
  • Lower drug doses and potential side effects in some cases.
  • Delivery of drugs targeting specific organs.

Disadvantages of Parenteral Preparations

  • Invasive and potentially painful.
  • Risk of trauma from needle or catheter insertion.
  • Potential for mistakes (e.g., toxic dose, incorrect drug, contaminants).
  • Potential complications are challenging to treat.

Types of Injections

  • Intramuscular (IM): Injections made into muscles (5 mL).
  • Intravenous (IV): Direct injection into the vein.
  • Subcutaneous (SC): Injections made under the skin (1.5 mL—e.g., insulin).
  • Intradermal (ID): Injections into the skin dermis (e.g., allergic testing, penicillin).
  • Intraspinal (Intrathecal): Injection through interthecal spaces into the spinal fluid (e.g., spinal anesthesia).
  • Intraperitoneal (IP): Injection into the peritoneal cavity (used in animal studies).

Common Advantages of Intravenous Route

  • Fastest method of systemic administration.
  • Preferred route for emergency situations.
  • IV infusions (LVP) provide large doses of fluids, electrolytes, nutrition, and drugs for hospitalized and unconscious patients.
  • Suitable for patients with serious GI tract problems.

Administration and Precautions for IV Route

  • Risk of introducing pyrogens, toxic agents, or microorganisms into the bloodstream.
  • Solutions must be free of particles or air bubbles (to prevent embolism).
  • Not suitable for suspension-based injections (or oily injections; these are better administered via IM).
  • Does not permit a depot effect.
  • Risk of infiltration.

Infiltration

  • Breakdown or collapse of veins that allows the drug to leak into surrounding tissues.
  • Causes edema (swelling) and tissue damage.
  • Requires trained personnel.

General Limitations

  • Inherent complications from an invasive procedure.
  • Potential trauma from needle or catheter insertion.
  • Potential complications from errors (e.g., improper dose or drug).

2. IM Injections

  • Slower onset of action compared to IV route.
  • Longer duration of action (depot effect).
  • Suspension and oil-based injections dissolve slowly, releasing a drug more gradually in the tissues.
  • More practical for use outside the hospital.
  • Injection volume up to 5 mL.

Classification of Parenterals

  • Two types:
    1. Pharmaceutical classification (solutions, suspensions, emulsions, dry powders)
    2. Volume-based classification (large volume parenterals [LVP], small volume parenterals [SVP]).

1. Pharmaceutical Classification

  • Solutions (aqueous, non-aqueous)
  • Suspensions
  • Emulsions
  • Dry powders

2. Volume Based Classification

  • Large Volume Parenterals (LVP) (100-1000 mL) - generally intravenous.
    • No additives generally.
    • Solutions, emulsions, and suspensions.
  • Small Volume Parenterals (SVP) (< 100 mL)
    • Additives allowed.
    • Solutions, emulsions, or suspensions.

How to Achieve Controlled Drug Delivery for Parenteral Preparations

  • Increasing particle size (e.g., suspensions) and viscosity (e.g., oil solutions and suspensions or viscosity-imparting agents).
  • Using implants (solid sterile dosage forms).
  • Using less soluble salts (e.g., insulin-zinc).
  • Using crystalline forms rather than amorphous forms (e.g., insulin lente).

Insulin Lente

  • Insulin zinc suspension.
  • Intermediate-acting porcine or human insulin with zinc salt added.
  • Suspension contains a 7:3 ratio of crystalline to amorphous insulin.

Assignments

  • Assignment 1: Investigate different insulin formulations on the market, noting variable duration and onset of action.
  • Assignment 2: Collect examples of various parenteral pharmaceutical forms on the market noting the active constituents, doses, labels (excipients used) and reconstitution methods for those forms.

Specifications of Parenteral Preparations

  • Sterility
  • Clarity
  • Absence of pyrogens
  • Tonicity
  • pH

Sterility

  • Sterile preparations must be free of microorganisms and contaminants
  • Presence of pathogens in parenteral preparations is dangerous.
  • Preservatives (antimicrobial agents) are added to maintain sterility.

Sterilization Methods

  • Moist heat sterilization
  • Dry heat sterilization
  • Ionizing radiation sterilization
  • Gaseous sterilization (e.g., ethylene oxide).
  • Filtration

Preservation

  • Antimicrobial agents are added to multi-dose vials
  • Prevent contamination during production, use, and storage.
  • Preservatives not needed for single-dose containers discarded after opening.
  • Preservative not used if drug has antimicrobial effect.

Ideal Preservative Attributes

  • Active against a wide range of bacteria.
  • Non-toxic at the used concentration.
  • Stable.
  • Compatible with injection components and exhibits no interaction with other ingredients.
  • Preservatives are absorbed preferentially from some closures (natural and neoprene rubber) over others (butyl rubber closures).

Commonly Used Preservatives in Multi-Dose Injections

  • Benzyl alcohol
  • Chlorocresol
  • Cresol
  • Methyl para-hydroxybenzoate (methyl paraben)
  • Propyl para-hydroxybenzoate (propyl paraben)
  • Phenol
  • Thiomersal

Clarity

  • Parenteral solutions must be clear
  • Free from foreign particles (dust, glass, fiber).

Absence of Pyrogens

  • Parenteral solutions must be non-pyrogenic (pyrogen-free).
  • Pyrogens are fever-producing endotoxins found in the outer membrane of Gram-negative bacteria.
  • Pyrogens are often lipopolysaccharides (lipid A linked to a central polysaccharide core).

Sources of Pyrogens

  • Solvents (water).
  • Equipment.
  • Packing materials.
  • Raw materials used in manufacture.

Biological Activity of Pyrogens

  • Injection of pyrogens can cause a toxic effect.
  • Contamination of large-volume parenterals (LVP) can lead to significant problems.
  • Lipid A affects the thermoregulatory center in the brain (leading to fever).
  • High doses can activate the coagulation system causing shock and eventually death.

Pyrogens Characteristics

  • Water-soluble.
  • Non-volatile.
  • Pass through bacterial filters.
  • Heat-stable.

Depyrogenation

  • Depyrogenation is the elimination of pyrogens.
  • Achieved through removal or inactivation of pyrogens from solutions, equipment, and raw materials.

Water Depyrogenation Methods

  • Distillation (BP)
  • Reverse osmosis (USP)
  • Ultrafiltration

Packing Material and Equipment Depyrogenation

  • Remove pyrogens from surfaces—rinse with non-pyrogenic water.
  • Inactivate pyrogens—utilizing dry heat (250°C for 30 minutes for heat-stable materials, not plastic).

pH

  • Ideal pH for parenteral preparations is 7.4.
  • Some injected drugs require different pH values.
  • Some drugs are insoluble at pH 7.4 and others are unstable at this pH, necessitating buffering to achieve stability.

Non-Neutral SVP Solution

  • Formulate at the suitable pH to maintain solubility and stability.
  • Requires a buffer system with low buffering capacity—e.g., acetate (1-2%), phosphate (0.8-2%), and citrate (1-5%) buffers
  • Allows for rapid neutralization of the SVP by the body's natural buffer mechanisms
    • Acceptable pH for tissues (other than IV) is 4-9.
    • Higher or lower pH values can irritate and harm sensitive cells.

Non-Neutral LVP Solution

  • IV infusions should not contain a buffering system.
  • Large volumes necessitate high buffer amounts, leading to toxicity.
  • Full neutralization of a high buffer load in a high volume is difficult, even with a low buffer capacity.
  • IV solutions of non-neutral pH should be infused slowly.
  • Avoid precipitation of the drug during IV infusion by avoiding rapid or large changes in pH.
    • The accepted pH range for non-neutral LVP is 3-10.5.

Tonicity

  • Parenteral preparations should be isotonic to blood plasma.

  • Solutions with osmotic pressure [OP] less than plasma are hypotonic.

  • Solutions with OP greater than plasma are hypertonic.

    • Injection of hypertonic solutions may cause tissue damage.
    • Intrathecal injections must be isotonic to avoid serious changes in the tonicity of cerebrospinal fluid.

  • Injection of hypotonic solutions causes hemolysis.

Tonicity Adjustment Methods

  • Freezing point depression method.
  • Sodium chloride equivalent.
  • Molar concentrations.
  • Serum osmolarity.

Lecture Quiz

  • Compare SVP and LVP solutions based on sterility, clarity, absence of pyrogens, buffer use, and injection of non-neutral, hypotonic, and hypertonic solutions.

Components of Parenteral Preparations

  • Container (packaging)
  • Active constituent
  • Solvent (Water for Injection [WFI], other solvents)
  • Additives

Packaging Containers

  • Glass ampoules, rubber-stoppered vials or glass/plastic bottles or syringes.

Packing Materials

  • Glass, rubber, and plastic materials frequently used.

Ampoules

  • Single-dose glass containers.
    • Glass neck should be scratched (or self-breaking).
    • May release small glass particles into the solution.

Vials

  • Multi-dose or single-dose containers (1-100 mL).
  • Glass bottle with rubber or synthetic cap and sealed with aluminum seal.
  • Rubber material can be natural or synthetic.
  • Limitations: incomplete sealing, air contamination, release of rubber particles, or adsorption of components (e.g., preservatives).

Pre-filled Syringes

  • Overcomes particle release and air contamination risks.
  • Limitations: expense and need for specialized machinery.

Plastic Containers

  • LVP single-dose IV infusion bottles (100-1000 mL).
  • Different polymers (polyethylene, polypropylene, or PVC).
    • Additives: plasticizers, opacifiers included.
  • Advantages: handling and transportation.
  • Disadvantages: leaching and adsorption of drugs.

Flexible (PVC) Containers

  • Adsorb some drugs (nitroglycerin).
  • No air-tube needed for drainage.

Semi-Rigid (PE) Containers

  • More compatible with many drugs/solutions.
  • Need for aeration (for drainage)

Glass Bottles

  • Advantages: transparent, chemically inert.
  • Used for incompatible drugs and plastics.
    • Disadvantages: breakage during transport.
    • Need for aeration (for drainage)
  • Composition:
    • Soda-lime glass commonly used (releases alkalinity).
    • Sulphated glass has a treated internal surface.
    • Type I glass made of silica dioxide + boron oxide, does not release alkalinity.

Solvents for Injection

  • Aqueous (e.g., water, co-solvents).
  • Non-aqueous (e.g., oils, oily materials).

Grades of Water

  • Water for Injection (WFI): Potting water may have contamination (organisms, particles, dissolved gases, or minerals). This is purified.
  • Sterile Water for Injection (SWFI) is packed in sealed containers for single-dose use. Sterilization of whole container occurs after filling.
  • Bacteriostatic Water for Injection (SWFI) contains a bacteriostatic agent; suitable for multi-dose use.

Co-solvents

  • Water-miscible solvents mixed with water in some parenteral preparations .Enhance solubility of some drugs; act as stabilizers.
    • Glycerin, ethyl alcohol, and propylene glycol are examples.
  • Higher concentrations can be toxic or irritating.

Non-aqueous Solvents

  • Used to dissolve drugs that are not water-soluble.
  • Stabilize drugs that are susceptible to hydrolysis (e.g., barbiturates).
  • Provide a sustained effect for certain drugs (e.g., steroids, digoxin).

Additives

  • Antimicrobial agents, buffers, tonicity-adjusting agents, antioxidants, and surfactants.
    • Provide an effective, safe, and elegant preparation.

Antioxidants

  • Added to stabilize products against degradation caused by oxidation—this avoids losses of drug activity over the shelf-life.
    • Ascorbic acid, cysteine, sodium metabisulfite, and tocopherol are examples.

Surfactants

  • Used to improve wetting, prevent crystal growth, and improve syringeability of suspensions and emulsions.
    • Sorbitan monooleate and polyoxyethylene sorbitan monooleate are examples.

Production of Parenteral Solutions

  • Produced in a high-standard clean room environment.
  • Contamination leads to particulate matter or microorganism or pyrogens problems.
    • Raw materials, personnel, and production area must be carefully selected and considered.
    • Personnel must be trained, observe rigorous hygiene, and wear special protective clothes.
    • Clean rooms are fitted with laminar flow hoods and HEPA filters.
    • Maintain sterility and pyrogen-free conditions.
    • IV admixtures can be produced.
    • Admixtures should be handled under aseptic conditions.

Quality Control Testing and Evaluation (BP)

  • Testing for containers (glass, plastic, rubber closures).
  • Whole batch testing (e.g., leaker, clarity tests).
  • Sample testing for various properties (e.g., sterility, endotoxin levels, clarity).
    • Includes compendial methodology considerations.

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Sterile Pharmaceutical Preparations PDF

Description

Test your knowledge on parenteral preparations, including their advantages, limitations, and specific characteristics regarding containers, solutions, and administration routes. This quiz will challenge your understanding of key concepts in pharmacology relevant to intravenous and sterile solutions.

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