Intro to Pharaceutics aand Dosage Forms

Pharmaceutics

science of turning a drug substance into a product that patients can safely and effectively use

USP <795>

nonsterile compounding

USP <797>

sterile compounding

USP <800>

hazardous drug handling and compounding

true or false- preparation for compounding can fall under more than one standard

true

parts of drug discovery

two: lead and target

lead in drug discovery

finding a promising compound that may become a drug

methods for lead in drug discovery

natural products

chemical synthesis

combinatorial chemistry

structure-activity relationships

target in drug discovery

finding the biological molecule/pathway that the drug should affect

method for target in drug discovery

genomics

transcriptomics

proteomics

metaabolomics

Drug-development pathway

lead-preclincical testing-IND-clinical trials (phase 1 2 3)- NDA- postmarketing

(refer to flowchart in notes)

phase 1 in pathway

examine safety, tolerability, dose range, side effects, and how the body ADME it

done w small group of volunteers who are healthy

phase 2 pathway

examine whether it works, which dose is best, and side effects; does it acc help?

tested w patients with the condition

phase 3 pathway

tested w much larger patient population to confirm

phase 4 pathway

approved and marketed; look for rare side effects, long term effects, drug interactions, other uses if possible

Drug discovery methods

Bioprospecting, combinatorial chemistry, solid-phase peptide synthesis, recombinant DNA technology

BCSR

Bioprospecting

using biodiversity and natural products to find potential drugs

ex: taxol, cannabinoid products, vinca alkaloids

combinatorial chemistry

rapidly creates a large number of related compounds by combining different chemical building blocks

solid-phase peptide synthesis

peptide is built while attached to solid resin

refer to notes for flowchart

recombinant DNA technology

manipulate and combine DNA from different sources

refer to notes for flowchart

Pharmacogenomics

studies how inherited genetic differences affect a persons response to medication

SNP

“snip”; single nucleotide polymorphism (variation in one DNA nucleotide)

Genetic differences can help predict whether a patient will experience…

a beneficial response

no response

an adverse or toxic response

Dosage Forms

physical product containing active and inactive ingredients that delivers a dose of medication

dosage form characteristics

state of matter

delivery method

release characteristics

route/site

need for dosage forms

protect drugs from oxygen, humidity, stomach acid

accurate dosing

hide taste or odor

more convenient administration

allow insoluble drugs to be given

improve stability and patient acceptability

types of dosage forms

solid

liquid

semisolid

inserts/suppositories

sterile

solid dosage forms

powders, granules, capsules, tablets

ups: accurate doses, better stability, convenient package

downs: difficult to swallow, may disintegrate and dissolve before absorption

liquid dosage forms

solution, syrup, suspension (contains solid particles, needs to be shaken), elixir (hydroalcoholic), tincture (alcoholic), emulsion (immiscible liquid dispersed in another)

semisolid dosage forms

ointments, creams, pastes, gels, foams

local effect

rheology- how a substance flows and deforms, influencing how these spread, release drug, and affect absorption

inserts dosage form

inserted in rectum, vagina, and urethra

melt/soften in body temperature

sterile dosage forms

contains no viable microorganisms

parenteral products (bypass gi tract), ophthalmic products (eye), irrigating solutions (rinsing/washing/flushing)

Immediate release

drug released promptly

delayed release

release begins later

extended release

released over a longer time

controlled release

released at designed, controlled rate

multiple release

separate portions of drug released at different times

delayed vs extended release

delayed: changes when drug release starts

extended: changes how long drug release continues

blood level graphs

MEC: minimum effective concentration

• below? drug may not work

MTC: minimum toxic concentration

• above? toxicity more likely

Excipients

nonmedicinal ingredients combined with the active drug (inactive ingredients)

MUST BE:

• nontoxic

• acceptable to reg agencies

• available

• low cost

• physiologically inert

• physically and chemically stable

• compatible

May be used for:

• dissolving

• thickening

• form an emulsion

• stabilize product

• preserve product

• add color/flavor