Manufacturing Pharmacy: Solid DF

diluent/filler/bulking agent

FORMULATION COMPONENTS

• inert substance added to increase the size of the tablet or fill the capsule body

diluent/filler/bulking agent

FORMULATION COMPONENTS

lactose

sucrose

dextrose

starch

sugar alcohols

microcrystalline callulose

calcium salts

kaolin

lactose

FORMULATION COMPONENTS: diluent

• most widely used for tablet formulation

lactose, sucrose, dextrose

FORMULATION COMPONENTS

• diluent incompatible w strong oxidizers, amine drugs and alkali lubricants

lactose monohydrate

anhydrous/spray-dried lactose

FORMULATION COMPONENTS

• lactose is available in 2 forms

wet

FORMULATION COMPONENTS

lactose monohydrate is for ______ granulation

dry

FORMULATION COMPONENTS

anhydrous/spray dried lactose is for ______ granulation

diluent, binder and disintegrant

FORMULATION COMPONENTS

starch acts as (3)

USP grade starch

FORMULATION COMPONENTS

usually possesses poor compression and flowability

modified starch

FORMULATION COMPONENTS

diluents that are freely flowing and directly compressible

modified starches

FORMULATION COMPONENTS

Cellutab, Sta Rx 1500

wet

FORMULATION COMPONENTS

USP grade starch is for ______ granulation

dry

FORMULATION COMPONENTS

modified starches for ______ granulation

maillard’s reaction (browning of sugar)

FORMULATION COMPONENTS

rxn when lactose, sucrose or dextrose is added to strong oxidizers, amine drugs and alkali lubricants

sugar alcohol

FORMULATION COMPONENTS

diluent with a slightly sweet taste and impart a cool sensation in the mouth due to its negative heat of solution 

sugar alcohols

FORMULATION COMPONENTS

widely used diluent in chewable tablets

sugar alcohols

FORMULATION COMPONENTS

classification of diluents: mannitol, xylitol, sorbitol

microcrystalline cellulose

FORMULATION COMPONENTS: DILUENTS

Avicel classification

direct compression

FORMULATION COMPONENTS: DILUENTS

microcrystalline cellulose suitable for __________

inorganic

FORMULATION COMPONENTS:

________ calcium salts used as diluent

acidic

FORMULATION COMPONENTS: DILUENT

incompatible with ______ drugs

lactose

sucrose

dextrose

FORMULATION COMPONENTS

calcium salt is incompatible with diluents (3)

calcium salts

FORMULATION COMPONENTS: DILUENT

ex: dibasic CaHBO4, CaCO3, CaSO4

Kaolin

FORMULATION COMPONENTS: DILUENT

hydrated Al silicate having a layer structure

diluent

FORMULATION COMPONENTS

use of kaolin

diluent

FORMULATION COMPONENTS

use of microcrystalline cellulose

diluent

FORMULATION COMPONENTS

use of Ca salts

diluent

FORMULATION COMPONENTS

use of sugar alcohols

diluent

FORMULATION COMPONENTS

use of starch

diluent

FORMULATION COMPONENTS

use of sugar alcohols

diluent

FORMULATION COMPONENTS

use of dextrose

diluent

FORMULATION COMPONENTS

use of sucrose

diluent

FORMULATION COMPONENTS

use of lactose

binder

FORMULATION COMPONENTS

imparts cohesiveness to powders causing them to form granules

binder

FORMULATION COMPONENTS

commonly used in wet granulation as binder solutions

31-35%

FORMULATION COMPONENTS

granules moisture content

FORMULATION COMPONENTS: PROBLEMS

amount of binder is too low or inadequate results to vert soft granules which can easily crumble

starch paste

FORMULATION COMPONENTS

binder of choice for wet granulation

natural gums

FORMULATION COMPONENTS

** for familiarization

binder classification which includes acacia, tragacanth, alginic acid, guar gum

binder

FORMULATION COMPONENTS
gelatin as an excipient in solid DF

binder

FORMULATION COMPONENTS

sucrose as an excipient in solid DF

EC

FORMULATION COMPONENTS: BINDERS

preferred cellulose der binder for powders/granules

binder

FORMULATION COMPONENTS

methylcellulose, ethylcellulose, hydroxypropylmethylcellulose and carboxymethylcellulose (cellulose dev) use

polyvinylpyrrolidone (PVP)

FORMULATION COMPONENTS

binder for chewable tabs

binder

FORMULATION COMPONENTS

PVP use

starch paste

natural gum

gelatin

sucrose

FORMULATION COMPONENTS

Binders used in wet granilation

diluent, disnintegrant

FORMULATION COMPONENTS

avicel uses (2)

disintegrant

FORMULATION COMPONENTS

facilitates breakup of a tablet when in contact with aqueous medium, such as gastric fluids

disintegrant (double disintegration)

FORMULATION COMPONENTS

commonly added in 2 portions

internal (intragranular)

FORMULATION COMPONENTS: DISINTEGRANT

added during the dry mixing step prior granulation

external (extragranular)

FORMULATION COMPONENTS: DISINTEGRANT

added during the lubrication step prior compression

starch

FORMULATION COMPONENTS: DISINTEGRANT

mechanism is thru swelling (absorbs inc amount of water)

natural starch

FORMULATION COMPONENTS: DISINTEGRANTS

most common type of starch used as disintegrant

natural starch

FORMULATION COMPONENTS: DISINTEGRANT

ex: corn starch, potato starch

modified starch

FORMULATION COMPONENTS: DISINTEGRANT

Sta Rx 1500

Clays

FORMULATION COMPONENTS: DISINTEGRANTS

classify bentonite and veegum

veegum

FORMULATION COMPONENTS: DISINTEGRANT

MgAl Silicate

FORMULATION COMPONENTS: DISNINTEGRANTS

cellulose dev not widely accpeted

MCC

FORMULATION COMPONENTS: DISINTEGRANTS

cellulose dev which is an excellent disintegrant in almost all preparations

cellulose derivatives (MCC)

FORMULATION COMPONENTS: DISINTEGRANTS 

MOA: wicking, capillary action

alginate

FORMULATION COMPONENTS: DISINTEGRANT

hydrophillic colloid from kelp

ion exchange resin

FORMULATION COMPONENTS: DISINTEGRANTS

Polacrallin K classification

Polacrallin K (ion exchange resis)

FORMULATION COMPONENTS: DISINTEGRANTS

amberlife

disintegrant

FORMULATION COMPONENTS

starch

clays

cellulose derivatives

alginates

gums

ion exchange resin

anti-frictional agents/flow activators

FORMULATION COMPONENTS

stearates (Mg, Ca, Na)

Purified Talc

Colloidal Talc

Colloidal SiO2

Silicates (Ca, Mg)

PEG & SLS

superdisintegrants

FORMULATION COMPONENTS

newer class of disintegrants which are effective at much lower levels; have the capability to swell faster and greater when absorbing water

hygroscopic and readily absorb moisture

FORMULATION COMPONENTS

disadvantage of disintegrants

superdisintegrant (cross-linked polymers)

FORMULATION COMPONENTS

sodium starch glycolate

crospovidone

croscarmellose Na

superdisintegrant

Na starch glycolate

FORMULATION COMPONENTS

explotab

superdisintegrant

Na starch glycolate; gelling agent

FORMULATION COMPONENTS

primojel

anti-frictional agents/flow activators

FORMULATION COMPONENTS

• fine powders added to reduce friction and improve flow properties

• mostly hydrophobic (<1% moisture)

• added at low conc prior to tablet compression

lubricant + external disintegrant

FORMULATION COMPONENTS: ANTI-FRICTIONAL AGENTS/FLOW ACTIVATORS

running powder components: ______ + _______

lubricant

BEQ

FORMULATION COMPONENTS: Role/Types of Flow Activators

reduces friction between the tablet and the inner die walls to facilitate ejection from die cavity

anti-adherent

BEQ

FORMULATION COMPONENTS: Role/Types of Flow Activators

reduces sticking to die walls and picking by punches

glidant

BEQ

FORMULATION COMPONENTS: Role/Types of Flow Activators

reduces friction among particles to enhance the flow

stearates (Mg, Ca, Na)

FORMULATION COMPONENTS

most widely used flow activator (used as lubricant, anti-adherent, glidant)

lubricant, anti-adherent

FORMULATION COMPONENTS

purified talc use as flow activator

glidant

FORMULATION COMPONENTS

colloidal tacl use as flow activator

colloidal SiO2

FORMULATION COMPONENTS

Cab-O-Sil

glidant

FORMULATION COMPONENTS

Colloidal SiO2 (Cab-O-Sil) use as flow activator

glidant

FORMULATION COMPONENTS

silicates (Ca, Mg) use as flow activator

PEGs and SLS

FORMULATION COMPONENTS

hydrophilic lubricants; not as effective

PEG and SLS

FORMULATION COMPONENTS: Flow Activators

polymers of ethylene oxide in H2O

colorant

FORMULATION COMPONENTS

• disguises off-color drugs and improves appearance

• provides identification for similar-looking products within a product line to minimize mix-ups during production

dyes

FORMULATION COMPONENTS

aka FD&C

lakes

FORMULATION COMPONENTS

aka D&C

dyes

FORMULATION COMPONENTS: Colorant

synthetic organic colorants

dyes

FORMULATION COMPONENTS: Colorant

added together with the binder in solution form; used in liquid products

dyes

FORMULATION COMPONENTS: Colorant

water soluble —> easily excreted

lakes

FORMULATION COMPONENTS: Colorant

dyes adsorbed on an inorganic oxide

lakes

FORMULATION COMPONENTS: Colorant

blended in dry chewable products and coating solutions

lakes

FORMULATION COMPONENTS: Colorant

water insoluble —> not easily excreted

brilliant blue

FORMULATION COMPONENTS: FDA-approved FD&C colorants

Blue No 1

Indigotine

FORMULATION COMPONENTS: FDA-approved FD&C colorants

Blue No 2

Fast Green

FORMULATION COMPONENTS: FDA-approved FD&C colorants

Green No 3

Erythrosine

FORMULATION COMPONENTS: FDA-approved FD&C colorants

Red No 3

Allura Red

FORMULATION COMPONENTS: FDA-approved FD&C colorants

Red No 40

Tartrazine

FORMULATION COMPONENTS: FDA-approved FD&C colorants

Yellow No 5

Sunset Yellow

FORMULATION COMPONENTS: FDA-approved FD&C colorants

Yellow No 6