Pharmaceutics 1 Exam 1 study guide

Dissolution

Liquid (solution)

lower

higher

condensation

freezing

melting

amorphous

Because of it's bioavailability and solubility

Classifies drugs by water solubility and permeability

Class II

C

POOR (less than 10mg/ml is considered poor)

API and nonvolatile molecule

Better bioavailability

More stable

They prescribe schedule of dosing

A dose given at the beginning of treatment to start getting the effect of a drug

A larger than usual, initial dose

The minimum serum concentration of the drug that is able to produce the desired therapeutic effect

This is the lowest concentration of an antimicrobial drug that prevents physical growth of a microorganism after incubation with media

This is the best level of blood serum concentration that produces does related toxic effects

It is the amount that produces the desired intensity of the effect in 50% of the individuals

It is the amount that produces toxic affects and 50% of individuals

It is the ratio between a drugs, median, toxic dose and its median effective dose (TD 50/ED 50)

Any product approved for use in the diagnosis, cure, treatment or prevention of disease and that is intended to affect structure or any function of the body

It is a physical form of a pharmaceutical formulation. It is also a vehicle for the convenient and safe delivery of the accurate and precise dose of an active pharmaceutical ingredient combined with inactive ingredients.

Tablets, capsules, suppositories, solutions, suspensions, ointments, creams, gels, aerosol

Size, shape, texture, taste/odor, appearance

Specialize dosage forms with a specific drug release rate and or a preprogrammed drug release site

Ensuring Bioavailability - the rate and extent to which an API is absorbed and becomes available at the site of action

Protection drug substances

Ensuring unit dose precision

Therapeutic considerations of the disease state and patients

Physical and chemical properties of the drug substance

Biopharmaceutical considerations

Enteral - oral, rectal, sublingual

Parenteral - IV, IM, subcutaneous, pulmonary, transdermal, nasal, otic, ocular

Systemic

Systemic

Mainly local pulmonary

Local

Typically systemic

Solutions, suspensions, capsules, uncoated tablets, coated tablets

Absorption, distribution, Metabolism, Excretion

Circulatory system

Tissues

GI tract

IV, IM, subcutaneous, sublingual, buccal, and transdermal

Any drug that is not recognized as being safe and effective in the conditions recommended for its use, and the labeling among qualified experts. A new chemical entity, a new formulation or method of manufacture a new combination of two or more old drugs a new use a route of administration or dosage form for an established drug.

The first food and drug law established in 1906

Plants

Minerals and animals

Micro organisms

Organic synthesis (artificial)

High purity, less expensive and large scale production with a short time

Recombinant DNA or monoclonal antibodies

To find active ingredients, or modify the chemical structures of existing active ingredients of drugs to form the basis of a new agent. Ideally, this process should result in a goal drug.

A goal drug can produce a desired effect, can be administered by the most desirable route ,can be administered at a minimal dosage and frequency, shows optimal onset and duration of activity has no side effects, and after exerting unnecessary affect, it should be eliminated from the body effectively and without residual effects.

A lead compound is a prototype, having desired activity, the also undesirable characteristics. I.e. poor ADME profile

Drug activity is the particular biological affect

Drug potency is the strength of the biological affect

A compound worthy of extensive biological pharmacological and animal testing

Pro drug is a compound that requires metabolic biotransformation after administration to produce the desired pharmacologically active compound

Drug metabolism studies

Clinical observations

Rational design

High throughput screening

One in every 10,000 compounds

Pre-clinical testing is an activity to assess the potential of Lead compounds as safe and effective therapeutic agents.

the key components of pre-clinical testing are toxicology studies, thermal, kinetic studies and material properties studies

It deals with the adverse or undesired effects of drugs

The therapeutic index equals the safe drug concentration/effective drug concentration

Preformulation studies are performed to understand the physical and chemical properties of Lead compounds to enable the optimal formulation design.

The properties of interest are solubility, partition coefficient, dissolution rate, solid state form, particle size and morphology, and stability

IND application is an investigational new drug application, and it is the first step of application for FDA approval.

Phase 1 is known as the human safety phase. It usually contains 20 to 80 participants and is several months long.

Phase 2 is known as the effectiveness phase it contains 100 to 300 participants and can last up to two years

Phase 3 is known as safety, effectiveness and dosage phase it usually contains 1000 to 3000 participants and it can last anywhere from 1 to 4 years.

A NDA application can be filed for if the three phases of clinical investigation show sufficient drug safety and therapeutic effects, this is to gain marketing permission for the new drug product in the US.

Phase 4 is known as the post marketing surveillance phase. It is continue data collection for drugs after they are marketed.

it looks at long-term effectiveness and any serious or unexpected, adverse side effects or drug interactions.

ANDA applications grant a marketing approval of a generic duplicate drug product which is comparable to an innovative drug product in dosage form strength route of administration, quality, performance characteristics, and intended use.

Generally includes no pre-clinical, or clinical data to establish safety and effectiveness.

A BLA application, or Biologics license application, requests for the manufacture and marketing of Biologics.

These products include blood products, vaccines, toxins, cellular and genetic therapies.

Orphan drug development is for the more than 5000 known rare diseases.

Orphan drug development requires two clinical trials, except for seizures conditions where there are no other therapies available.

A dry substance composed of finely divided particles

The science of small particles,

Particle size and size distribution

Shape

Angle

True density

Bulk density

Porosity

Voids

True volume

Bulk volume

Bulkiness

Equivalent sphere diameter used to describe size, r

May be measured by volume, surface area, mass, or linear dimension

Affects mixing and blending, dose uniformity, powder flow, aerosolization, dissolution, suspendability of suspensions

#60 sieve = 250um

The size of a sphere can be described by a single number, r

True density = density of the particles

P=m/v

Bulk density = density of powder

Pa= m/Vbulk

True volume = V

Space occupied by the powder, microscopic

V = mass/ density

Bulk volume = Vbulk

Volume occupied by the selected weight of a powder, macroscopic

True volume + porosity

Void as a percent instead of decimal ratio

Void x 100

Porosity = (Vbulk - V)/Vbulk x 100

B = 1/Pa

(ML/g)

Reciprocal of bulk (apparent) density

Used to estimate the flow properties of a powder

Measured by allowing a powder to flow through a funnel and fall freely onto a surface

The lower the angle or repose more freely powder flows

Tan q = h/r

The ability of a liquid to spread over a solid surface

The contact angle q = a measure of the wettability

Young’s equation

Young’s question, relates surface free energies to contact angle

Good wetting required for dispersion of powders in liquid media and for the penetration of liquid into tablets.

Wetting problems can often be solved by the inclusion of surfactants into formations

The ratio of the space to volume

Void - Vbulk - V/ Vbulk

Crystalline, amorphous, polymeric

Polymorph 1 and polymorph 2

Made of packed active molecules

Solvate - made of active molecules and solvent molecules

Salt- made of protonated active molecules and deprotonated acid molecules

Co- crystal - active molecule and non-volatile moelcules

Polymorphs, hydrates/ solvates, and salts/ cocystals

Amorphous and amorphous dispersions

Good solubility and poor permeability

Good solubility and good permeability

Poor solubility poor permeability

Molecular structure

Molecular weight

Crystal structure

Stereochemistry

ionization

Temperature

0 degrees

90 degrees or more

Ability to selectively hydrolyze a population of DNA molecules and then join two different DNA molecules

Laboratory produced copies of a specific protein (antibody) produced within cells of higher animals. They can be designed specifically to only target a certain antigen.