MIDTERM 01 - Dosage Form Design Considerations Flashcards
Study on the formulation, manufacturing, stability, and effectiveness of pharmaceutical dosage forms
Pharmaceutics
Other term for pharmaceutical ingredients
Excipients
Used to protect the drug substance from the destructive influences of atmospheric oxygen or humidity
Coated tablets
Used to protect the drug substance from the destructive influence of gastric acid after oral administration
Enteric-coated
Used to conceal the bitter, salty, or offensive taste or odor of a drug substance
Capsules, Flavored syrups
Used to provide liquid preparations of substances that are either insoluble or unstable in the desired vehicle
Suspension
Used to provide clear liquid dosage forms of substances (SS)
Syrups, Solutions
Used to provide rate-controlled drug action
Controlled-release tablets
Used to provide optimal drug action from topical administration sites (OCT)
Ointment, Creams, Transdermal patches
Used to provide for insertion of a drug into one of the body’s orfices
Suppositories
Used to provide placement of drugs directly in the bloodstream or body tissues
Injections
Used to provide for optimal drug action through inhalation therapy
Inhalants, Inhalation aerosols
Formulation that best meets the goals of the product
Master formula
Defines the nature of the drug substance
Preformulation studies
Includes physical description, chemical properties, and purity of the chemical substance
Physical description
Done for the indication of particle size and size range of the raw material along with the crystal structure
Microscopic examination
Determines the purity of the substance
Melting point depression
Rule that determines existence and extent of the presence of solid and liquid phases in binary, ternary, and other mixtures
Phase rule
Affects physical-chemical properties of drug susbtances
Particle size
Where substances can exist in more than one crystalline form
Polymorphism
Forms that usually exhibit different physicochemical properties
Polymorphic forms
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
Time it takes for the drug to dissolve in the fluids at the absorption site
Dissolution rate
2 methods in determining dissolution rates of chemical compounds (CP)
Constant surface method, Particulate dissolution
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
pH
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
