Reasons for coating tablets

Masking unpleasant smell or taste of drug

Protecting the drug before ingestion
Protection against light, air & moisture
Ensuring their controlled release
More elegant appearance
Increase mechanical stability
Avoidance of side effects

Types of Coated Tablets

Sugar coated
Hot melts
Film coated
Aqueous Film
Nonaqueous Film

Enteric coated

Characteristics of Cores
Hardness
adequate

strength to withstand the rolling & frictional

processes in pan and the impact stress in fluid-bed
equipment.

Shape : biconvex
to

prevent them sticking together

less material
more uniform

Surface
coarse

for sugar coating

smooth & dust-free for film coating

Size
Heat sensitivity
Interaction between Core and Coating

Interaction between Core and Coating

Hydrophilic swelling substances
cause the core swell
under the influence of moisture
Substances migrating
mottling, discoloration or fading, blooming

Sugar coated
Advantages
Protects drug from air and humidity
Taste and smell barrier
High compliance
Disadvantages
Difficult to manufacture
Irregular coat thickness
Irregular color

Soft
Breakable and chip
Increased size (0.5% per shot)
and weight of tablet (25-50%)

Materials

Sugar (sucrose)
50-60%

(viscosity < 2 Poise)

Fillers (CaCO3, talc, TiO2)

Colorants (dyes, iron oxide, TiO2)
Binders (acacia gum, gelatin, cellulose derivatives, PVA, PVP)
Increase

strength & elasticity

Antiadherent (talc)
Flavors
Surfactants (dispersion aids)
Suspension

stabilizer

Materials

Sugar (sucrose)
50-60%

(viscosity < 2 Poise)

Fillers (CaCO3, talc, TiO2)

Colorants (dyes, iron oxide, TiO2)
Binders (acacia gum, gelatin, cellulose derivatives, PVA, PVP)
Increase

strength & elasticity

Antiadherent (talc)
Flavors
Surfactants (dispersion aids)
Suspension

stabilizer

Process of Sugar Coating

Prime-coating layer
(sealing

& subcoating)
Protecting against moisture, effecting
adhesion, preventing interaction, masking
odor, effecting controlled release

Rounding layer
(dusting

& filler syrup)

Finishing layer
(coloring,

smoothing or polishing,
glossing, protecting)

Uniform coating layers

Requires the services of

highly skilled coating operators

Process of Sugar Coating

Waterproofing and sealing
Shcellacing

Subcoating (40-60C)
3-5 coats which can bond to both the tablet and the sugar
Gelatin or Polyvinylpyrolidone (PVP)

Grossing, Smoothing & Final Rounding

Thick Syrup of 60-70% Sucrose
5-10 coats

Finishing and coloring

mulitple coats of thin sucrose syrup with pigments

Imprinting
Embossed, debossed or engraved

Polishing
Wax

Binder solutions

Gelatin
Gum acacia
Sucrose
Water

3.3-6%
8-8.7%
45-55%
ad 100%

Dusting powder

CaCarbonate
Titanium dioxide
Sucrose powdered
Gum acacia
Talc (asbestos free)

0-40%
1-5%
28-38%
0-2%
25-61%

Uniform coating layers

Sucrose
Gelatin or acacia gum
PEG
Aerosil (colloidal silica)
Titanium dioxide
Dyes, pigments
Water

58-66%
0.5-1%
1-3%
0.5-1%
0.05-0.1%
qs
ad 100%

Process of Sugar Coating

Waterproofing and sealing
Shcellacing

Subcoating (40-60C)
3-5 coats which can bond to both the tablet and the sugar
Gelatin or Polyvinylpyrolidone (PVP)

Grossing, Smoothing & Final Rounding

Thick Syrup of 60-70% Sucrose
5-10 coats

Finishing and coloring

mulitple coats of thin sucrose syrup with pigments

Imprinting
Embossed, debossed or engraved

Polishing
Wax

Problems in sugar coating

Tablet Core Robustness

Shape, hardness

Finished tablets

Chipping: excessive use of insoluble fillers

Cracking: moisture sorption
Nondrying: invert sugar > 5%
Twinning: shape, drying
Uneven color

Enteric Coated

Enteric Coated
Function
Resists dissruption at gastric pH, then disolves
at intestinal pH
Advantages
Protects drugs from acidic hydrolisis
Protects gastric mucosa from irritating drugs
Enhanced drug absorption
Active Agent
Enteric Coats are similar to film coats, but much
thicker or with slightly different constituents
Cellulose Acetate Phthalate is a common coat
constituent
Polymeric Materials with or without Phthalate

Types of Enteric Coats

Solution Dependent Coats
Time dependent
Hydroxyporplymethylcellulose
Ethylcellulose

pH Dependent Coats
Cellulose acetate phthalatate pH 6
HPMC phthalate pH 4-5
Methacrylic acid-methacrylate co-polymer
Polyvinyl Acetate phthalate pH 4-5

Film Coated

Reasons for coating tablets

Masking unpleasant smell or taste of drug

Protecting the drug before ingestion
Protection against light, air & moisture
Ensuring their controlled release
More elegant appearance
Increase mechanical stability
Avoidance of side effects

Types of Coated Tablets

Sugar coated
Hot melts
Film coated
Aqueous Film
Nonaqueous Film

Enteric coated

Characteristics of Cores
Hardness
adequate

strength to withstand the rolling & frictional

processes in pan and the impact stress in fluid-bed
equipment.

Shape : biconvex
to

prevent them sticking together

less material
more uniform

Surface
coarse

for sugar coating

smooth & dust-free for film coating

Size
Heat sensitivity
Interaction between Core and Coating

Film Coating
Types
Water Soluble Film
Water Insoluble Film
Advantages of Film Coats
Less Bulky than Sugar Coated Tablets
Simpler (and cheaper) than Sugar Coated Tablets

One hour for about 10 m and about 1% weight gain

Resistant to chipping
Taste and Smell barrier
Disadvantages of Film Coats In General
Cost
Possible toxicity hazard, esp non polar solvents
Environmental pollution
Increased drying time

Nonaqueous Films Polymeric Materials

Cellulose Acetate Phthalate
Methylcellulose

Plasticizers
Castor Oil, Polyethylene Glycol & Glycerin

Suspending Agents
Colorant & Flavoring
Solvent: isopropyl alcohol, CHCl3
(Water in US)

Polish
Beeswax

Aqueous Films Polymeric Materials

Ethylcellulose
Hydroxymethylcellulose

Plasticizers
Glycerin & Polyethylene Glycol
Colorant & Flavoring
Water as solvent

Solvent
Depending on the solubility of film-formers water,
organic solvents or mixtures of both
Solvent selection:

Empirically
Like is dissolved by like
Quantitatively

The most popular solvents :

water

dichloromethane:ethanol

dichloromethane:methanol

dichloromethane:ethanol

dichloromethane:isopropyl alcohol

acetone

dichloromethane:ethanol:acetone

ethanol:water

Acetone:isopropyl alcohol:water

Processing:
Preheated the tablets
desired temp and dust extracted

Thin sealing coat

Stabilize the core surfaces

The actual film coating

Post drying
Polishing :10%PEG 6000 in water

Variables affecting coat application

Spraying Method

Intermittent spraying
Continuous spraying

Nozzle Distance product temperature

Spray size, rate, pressure
Batch size
Drying time (air inlet)

30-50C for organic solvents

40-60C for aqueous systems

Moisture Content

The coating liquids were as follows:

(1) HPMC 8%(wt/wt), polyethylene glycol 1.6% (wt/wt), and

purified water 90.4% (wt/wt);

(2) HPMC 8% (wt/wt), polyethylene glycol 1.6% (wt/wt), titanium

dioxide 2.4% (wt/wt), and purified water 88% (wt/wt).

To prepare the coating solution and pigmented dispersion:

added the polymer to the hot water (80-90C) under
magnetic stirring.
after the polymer had been dispersed, the remaining
cold water was added all the polymer was dissolved,
added plasticizer and pigment to obtain a total of 1000 g
of coating liquid.

Defects in Aqueous Film Coats

Picking Little flakes
Reasons
Spray rate too high
Inadequate drying
Slow pan speed
Poor Distribution

Peeling Big flakes

Reasons
Low coating
Poor adhesion
Poor Distribution

Orange Peel Affect

Premature Drying
Film too viscous

Mottling
Lack of Color due to poor mixing of pigments
Bridging: Creases in the film
Erosion of the film or core

Twinning tablets sticking together

Reasons
Spray rate too high
Pan Speed too low
inappropriate shape

Cracking
Inadequate Plasticizers
Excessive pigmentation
Different thermal expansion rate

Kriteria penerimaan uji disolusi berdasarkan nilai Q :

A.

Sediaan kelompok pertama (kapsul, tablet tidak bersalut

dan tablet bersalut bukan enterik) = immediate release

1.

6 unit sediaan : masing-masing unit sediaan tidak < Q +

5%, bila tak terpenuhi, pengujian dilanjutkan ke tahap
kedua.

2.

6 unit sediaan : purata 12 unit sediaan dari tahap pertama

(1) dan kedua (2) tidak < nilai Q; tidak satu unitpun yang
< Q -15%; bila syarat tak terpenuhi, pengujian dilanjutkan
ke tahap ketiga.

3.

12 unit sediaan : purata 24 unit dari tahap pertama (1),

tahap kedua (2) dan tahap ketiga(3) tidak < nilai Q; tidak
lebih 2 unit sediaan dengan nilai < Q 15% dan tidak
boleh satu unit sediaan dengan nilai < Q -25%

B. Sediaan salut enterik (delayed release)

a.

Tahap asam : 750 ml 0,1 N HCl, selama 2 Jam + 2%

1.

6 unit sediaan : masing-masing unit sediaan tidak > 10%

Q, bila tak terpenuhi, pengujian dilanjutkan ke tahap
kedua.

2.

6 unit sediaan : purata 12 unit sediaan dari tahap pertama

(1) dan kedua (2) tidak > 10% Q; tidak satu unitpun yang
terdisolusi > 25% Q; bila syarat tak terpenuhi, pengujian
dilanjutkan ke tahap ketiga.

3.

12 unit sediaan : purata 24 unit dari tahap pertama (1),

tahap kedua (2) dan tahap ketiga(3) tidak > 10% Q; dan
tidak satu unitpun yang terdisolusi > 25% Q

b. Tahap dapar
dalam waktu 5 menit hilangkan tahap asam, pada alikot
sampel tambahkan 250 ml 0,20 M natrium trifosfat, atur
pH sampai 6,8+0,05 pada 370C dengan pengadukan
pada kecepatan spesifik. Uji disolusi dilanjutkan selama
45 menit atau sesuai dengan monografi. Alikot sampel
kemudian dianalisis, dimana Q adalah perhitungan total
dari tahap asam dan dapar.

salut enterik

6 unit sediaan : masing-masing unit sediaan tidak < Q + 5%,

bila tak terpenuhi, pengujian dilanjutkan ke tahap kedua.

6 unit sediaan : purata 12 unit sediaan dari tahap pertama

(1) dan kedua (2) tidak < nilai Q; tidak satu unitpun yang <
Q -15%; bila syarat tak terpenuhi, pengujian dilanjutkan ke
tahap ketiga.

12 unit sediaan : purata 24 unit dari tahap pertama (1),

tahap kedua (2) dan tahap ketiga(3) tidak < nilai Q; tidak
lebih 2 unit sediaan dengan nilai < Q 15% dan tidak boleh
satu unit sediaan dengan nilai < Q -25%