Advanced Tablets

zero order

relatively constant release of drug until dose is exhausted

variable

controlled drug delivery that matches a biological rhythm (hypertension; nocturnal asthma)

bioresponsive

controlled drug delivery that is triggered by a biological stimulus (blood glucose)

IV injection

when administered via _______________, 100% of the drug is in the blood right away

infusion

plasma concentration stays consistent when continuously administered; good for long term drug delivery

dissolution

_______________ must occur in order for a drug to diffuse; occur simultaneously for water-soluble drugs

diffusion

movement from an area of high concentration to low concentration resulting from kinetic properties, yields and equal distribution, or spontaneous net movement down their concentration gradient, or a process by which a concentration difference is reduced by a spontaneous flow matter

paracellular diffusion

movement between two cells; dependent on pore size, drug shape, and size

transcellular diffusion

movement across the cell

passive transport

movement of drug across a membrane in a manner driven solely by the concentration gradient

carrier-mediated diffusion

movement across a cell membrane via a specialized transport system embedded in the cell membrane

saturable - can reach a maximum velocity of transport

facilitated diffusion

carrier mediated movement from high to low concentration; no energy input is required

active

carrier mediated movement from low to high concentration; energy input is required

Noyes-Whitney equation

helps to understand the ways to improve the dissolution rate of very poorly soluble compounds to minimize the limitations of oral bioavailability

Noyes-Whitney equation

more

the _______ surface area (S) that exists amongst the particles, the faster the rate of dissolution

lower

the __________ the thickness of the liquid film (h), the faster the rate of dissolution

Fick's Law

law that states that the greater the difference in concentration, the greater the rate of diffusion

sustained release

SR

sustained action

SA

extended release (slow release)

ER, XR, XL

controlled release

CR

modified release

MR

continuous release

CR or contin

delayed release

DR

long acting

LA

coating

______________ requirements:

-core hardness (strength)

-friability

-dimension fluctuation with heat and solvents

-shape

-surface roughness and porosity

-wetting of core by coating droplets (adhesion)

picking and sticking

film coating defect in which the spray rate is too high, there are inadequate drying conditions, the pan speed is too low, there is inadequate atomization, or poor distribution of spray

orange peel

film coating defect due to over drying; caused by excessively dry conditions,excessive spray rate, viscosity of coating liquid too high, or poor atomization

bridging

film coating defect in which there is a loss of coating definition due to poor adhesion to core, non-porous surface, core surface erosion, or spray dried coating

peeling

film coating defect in which there is poor adhesion to the coor and there is low mechanical strength of the coating

cracking

film coating defect in which there is core sensitivity to solvent, core friability, excessive pan speed, and low spray rate

color variation

film coating defect in which there is a low quantity of coating and inadequate tablet mixing, low coating opacity, excessive solids content, or insufficient number of spray guns

effervescent tablets

use if the patient cannot swallow a tablet or if the dose is too large; sensitive to chemical degredation from moisture, light, or oxygen

effervescent tablets (formulation)

organic acid + metal alkali ---> CO2 + H2O + salt

also has colors and sweetener - goal is to be clear when dissolved

acid

component of an effervescent salt that might be citric, malic, tartaric, or adipic

metal alkali

component of an effervescent salt that may be NaHCO3, KHCO3, CaCO3, or K2CO3

sweetener

component in an effervescent that may be acesulfame, potassium, sucralose, or aspartame

10-12

effervescent tablets should be kept at ___________% humidity to prevent autocatalytic reaction

desiccant

a hygroscopic substance used as a drying agent that should be added when packaging effervescent tablets

mouth

site of action for oral disintegrating tablets (ODT)

ODT (oral disintegrating tablet)

solid oral dosage forms that disintegrate rapidly in the oral cavity, with a disintegration time of 30 seconds or less when based on USP

hot melt excursion tablet

powder blend that passes into an extrusion/heating chamber; formulation transforms into viscous fluid as polymers melt; extrusion into tablet mold; rapid cooling to form amorphous carrier in solid phase

bi-layer (or multilayer) tablets

advantages:

-dose convenience for combination therapy and improved theraputic levels

-separation of incompatible components

disadvantages:

-delamination; fixed to one dose concentration

chewable tablet

for children before they can swallow tablets; frequently formulated with mannitol (pleasant, cooling sensitization); antacid tablets are too large for swallowing

molded tablets

extemporaneously compounded; prepare a paste that is hard pressed into the touch; no hand processing

tablet triturate

a small loosely packed tablet to be dissolved in water immediately before injection

generic tablets

method of development in which it is the innovator formulation components from the label information

pill

small, spherical or ovoid mass of a mechanical substance intended to be swallowed whole

lozenge

a small aromatic or medicated candy

dragee

pill that is sugar-coated medicated candy

cachou

a scented lozenge used to sweeten the breath

IR

thrice daily

SR

twice daily

XR

once daily