MIDTERM 01 - Dosage Form Design Considerations Flashcards by Juan Carlos Cornelio

Study on the formulation, manufacturing, stability, and effectiveness of pharmaceutical dosage forms

Pharmaceutics

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Other term for pharmaceutical ingredients

Excipients

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Used to protect the drug substance from the destructive influences of atmospheric oxygen or humidity

Coated tablets

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Used to protect the drug substance from the destructive influence of gastric acid after oral administration

Enteric-coated

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Used to conceal the bitter, salty, or offensive taste or odor of a drug substance

Capsules, Flavored syrups

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Used to provide liquid preparations of substances that are either insoluble or unstable in the desired vehicle

Suspension

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Used to provide clear liquid dosage forms of substances (SS)

Syrups, Solutions

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Used to provide rate-controlled drug action

Controlled-release tablets

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Used to provide optimal drug action from topical administration sites (OCT)

Ointment, Creams, Transdermal patches

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Used to provide for insertion of a drug into one of the body’s orfices

Suppositories

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Used to provide placement of drugs directly in the bloodstream or body tissues

Injections

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Used to provide for optimal drug action through inhalation therapy

Inhalants, Inhalation aerosols

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Formulation that best meets the goals of the product

Master formula

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Defines the nature of the drug substance

Preformulation studies

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Includes physical description, chemical properties, and purity of the chemical substance

Physical description

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Done for the indication of particle size and size range of the raw material along with the crystal structure

Microscopic examination

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Determines the purity of the substance

Melting point depression

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Rule that determines existence and extent of the presence of solid and liquid phases in binary, ternary, and other mixtures

Phase rule

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Affects physical-chemical properties of drug susbtances

Particle size

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Where substances can exist in more than one crystalline form

Polymorphism

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Forms that usually exhibit different physicochemical properties

Polymorphic forms

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Is defined as the maximum concentration of a substance that can be completely dissolved in a given solvent at a certain temperature and pressure level

Drug solubility

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Time it takes for the drug to dissolve in the fluids at the absorption site

Dissolution rate

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2 methods in determining dissolution rates of chemical compounds (CP)

Constant surface method, Particulate dissolution

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Method that involves the characteristic of compound and solvent under fixed experimental conditions (Methods in determining dissolution rates)

Constant surface method

The value of the constant surface method is expressed as __________

mg dissolved/min/cm2

Used to study the influence of particle size, surface area, and excipients upon the active agent (Methods in determining dissolution rates)

Particulate dissolution

Law that describes the relationship of diffusion and dissolution of the active drug in the dosage form and when administered in the body

Fick's law (Law of diffusion)

Law that relates to a steady-state flow (Fick's law)

Fick's 1st law

Law that relates to a change in concentration of drug with time, at any distance, or a non-steady state of flow (Fick's law)

Fick's 2nd law

Determines degree and rate of passage of drug through the membrane sac

Membrane permeability

Is a measure of a molecule's lipophilic character; that is the preference for the hydrophilic or lipophilic phase

Partition coefficient

Extent of ionization of drug (strong effect on formulation and pharmacokinetic parameters of the drug); is determined by potentiometric titration

pKa/Dissociation constants

Extent that a product retains within specified limits and through its period of storage and use

Stability

Drug molecules interact with water molecule to yield breakdown product (Types of destructive process)

Hydrolysis/Solvolysis

Involves the loss of electrons from an atom or molecule (Types of destructive process)

Oxidation

Are molecules or atoms containing one or more unpaired electrons

Free radicals

The active ingredient retains chemical integrity and labeled potency within the specified limits (Types of stability)

Chemical stability

The original physical properties, appearance, palatability, uniformity, dissolution, and suspendability are retained (Types of stability)

Physical stability

Involves the sterility/resistance to microbial growth (Types of stability)

Microbiologic stability

The therapeutic effect remains unchanged (Types of stability)

Therapeutic stability

No significant increase in toxicity occurs (Types of stability)

Toxicologic stability

Description of the drug concentration with respect to time

Rate reactions

Estimate the shelf life of a product that has been stored or to be stored under a different set of conditions

Q10 method

Is a major determinant in stability

Optimum pH range for stability

pH 5 & 6

Are agents used to increase stability

Buffering agents

Are drugs prepared in dry state; they are packaged in sealed containers with air replaced by inert gas

Oxygen sensitive drugs

Catalyst to oxidation reactions

Light

Reaction between two or more identical molecules with resultant formation of new and generally larger molecules

Polymerization

2 processes where one or more active chemical groups are removed (CD)

Chemical decarboxylation, Deamination

Process that involves the decomposition of carboxylic acid and release of carbon dioxide

Decarboxylation

Process that involves the removal of nitrogen containing group from organic amine

Deamination

Use of exaggerated conditions of temperature, humidity, light, and others

Accelerated stability testing

Studies that determine the most stable of the proposed formulations for a drug product

Short term accelerated studies

Testing where temperature elevations in 10° increments higher than used in accelerated studies

Stress testing

The product is subjected to different climatic zones nationally and internationally

Long term stability studies

Holds the article and is or may be in direct contact with the article

Container

It is in direct contact with the article at all times

Immediate container

Part of the container

Closure

It is cleaned and dried prior to it being filled with the drug

Closure and container

May be combinations of paper, foil, plastics, or cellophane

Packaging materials

May be single-unit dispensed in paper, plastic, and foil cups

Oral liquids

Required by many pharmaceutical products to protect them from photochemical deterioration

Light resistant containers

May be added to plastic to decrease the transmission of short UV rays

UV absorbers

Light resistant containers must meet the USP standards which define the acceptable limits of light transmission at any wavelength of light between __________ and __________ nm

290-450 nm

Container that is significantly difficult for children under 5 years of age to open

Child-resistant container

Includes initial regulations called for its use for aspirin products and certain household chemical products

Child-proof closures

Highly resistant, borosilicate glass

Type I glass

Treated soda-lime glass

Type II glass

Soda-lime glass

Type III glass

General purpose soda-lime glass

Type NP glass

Should make up only at most a 14 days supply and must be stored in a refrigerator

Pharmacist

Used to dissolve the drug substance (Types of pharmaceutical ingredients and excipients)

Solvents

Used to make the product more palatable (Types of pharmaceutical ingredients and excipients)

Flavors and sweeteners

Used to enhance the appeal (Types of pharmaceutical ingredients and excipients)

Colorants

Used to prevent microbial growth (Types of pharmaceutical ingredients and excipients)

Preservatives

Used to prevent decomposition (Types of pharmaceutical ingredients and excipients)

Stabilizers

Used to increase bulk of the formulation (Types of pharmaceutical ingredients and excipients)

Diluents/Fillers

Used to cause adhesion of the powdered drug (Types of pharmaceutical ingredients and excipients)

Binders

Used to promote tablet breakup after administration (Types of pharmaceutical ingredients and excipients)

Antiadherents/Lubricants

Used to promote tablet breakup after administration and coatings (Types of pharmaceutical ingredients and excipients)

Disintegrating agents

Can mask unwanted taste (Types of pharmaceutical ingredients and excipients)

Sweetening pharmaceuticals

Most commonly used sweetening pharmaceutical

Sucrose

Clause that states that no new food additives may be used if animal studies/appropriate tests showed that it caused cancer

Delaney clause

2 sweetening pharmaceutical used in foods; "generally recognized as safe" (SC)

Saccharin, Cyclamate

Sweetening pharmaceutical that is banned due to possible carcinogenicity, genetic damage, and testicular atrophy

Cyclamates

First artificial sweetener with requirement for pre-marketing proof of safety

Aspartame

Sweetening pharmaceutical that is structurally similar to saccharin; 130 times as sweet as sucrose and is excreted unchanged in the urine

Acesulfame potassium (nonnutritive sweetener)

New sweetening agent; is natural, nontoxic, safe, and is 30x sweeter than cane sugar/sucrose

Stevia (Stevia rebaudiana Bertoni)

Used in pharmaceutical preparations for aesthetics (Types of pharmaceutical ingredients and excipients)

Coloring pharmaceuticals

Thich black viscid liquid that is a byproduct of destructive distillation of coal

Coal tar (pix carbonis)

Added to pharmaceutical preparation in the form of diluted solutions (Coloring pharmaceuticals)

Dyes

Commonly used in the form of fine dispersions or suspensions (Coloring pharmaceuticals)

Lakes

90% of the dyes used in products are synthesized from the derivative of __________

Benzene (Aniline)

Regulates the use of color additives in foods, drugs, and cosmetics

FDA

Additives which are added in foods, drugs, and cosmetics

FD&C color additives

Additives which are added in drugs, some in cosmetics and medical devices

D&C color additives

Additives which are restricted to external parts of the body

External D&C color additives

Are suitable substances added to enhance a drug's permanency or usefulness

Preservatives