AURHOR:- NILESH S.JAWALKAR E-MAIL:-nilesh.jawalkar91@gmail.

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Tablet coating is the application of a coating material to the exterior of a tablet with the intention of conferring benefits and properties to the dosage form over the uncoated variety. Also applicable to modified release dosage forms &also to hard-shell and soft elastic capsules (less extent)

protection particularly from light and moisture. Mechanical strength,reduse cross condamination, dusting prevented, mask tastes,easier to swallow Coloured coating rapid identification, patient compliance, in marketing brand identification Functional film coatings used to impart enteric or controlledrelease properties

Three main types are in use: Film coating Sugar coating Press coating

FEATURES
Appearance

FILM COATING
Retain contour of original core. Usually not as shiny as sugar coat type 2-3%

SUGAR COATING
Rounded with high degree of polish

Weight increase because of coating material Logo or break lines

30-50%

Possible

Not Possible

Process stages Typical batch coating time Functional coatings

Usually single stage 1.5 to 2.0 Hours Easily adaptable for controlled release

Multistage process Eight hours but easily longer Not usually possible apart from enteric coating

Sugar coating
multistage process Increase bulk,mask taste,odour 1. Sealing of the tablet cores 2. Subcoating 3. Smoothing 4. Colouring 5. Polishing 6. Printing. 1. Seal tablet core 2. Sub coating 3. Smoothing 4. Colouring 5. Polishing 6. Printing

1.

2. 3.

Sealing tablet core- application of a water impermeable polymer such as Shellac, cellulose acetate phthalate and polyvinyl acetate phthalate, which protects the core from moisture, increasing its shelf life. Sub coating -by adding bulking agents such as calcium carbonate or talc in combination with sucrose solution. Smoothing process -remove rough layers formed in step 2 with the application of sucrose syrup.

1.

2.

3.

Sealing tablet core- application of a water impermeable polymer such as Shellac, cellulose acetate phthalate and polyvinyl acetate phthalate, which protects the core from moisture, increasing its shelf life. Sub coating -by adding bulking agents such as calcium carbonate or talc in combination with sucrose solution. Smoothing process -remove rough layers formed in step 2 with the application of sucrose syrup.

4. 5.

Colouring - for aesthetic purposes often titanium based pigments are included. Polishing - effectively polished to give characteristic shine, commonly using beeswax, carnauba wax. Printing -indelible characterisation. ink for

6.

Brufen POM Available in 200mg and 400mg strength

Premarin POM Conjugated oestrogens 625mcg (maroon) and 1.25mcg (yellow) Colofac P Mebeverine hydrochloride 100mg Round, white, sugar coated Kalms GSL 45mg Hops powder,90mg Gentian powdered extract, and 135mg Valerian powdered extract

Modern approach to coating tablets, capsules, or pellets by surrounding them with a thin layer of polymeric material. Process: Single stage process, which involves spraying a coating solution containing the following; 1.Polymer 2.Solvent 3.Plasticizer 4.Colourant

Advantages single step process in relatively short period of time. Process enables functional coatings to be incorporated into the dosage form. Disadvantages There are environmental and safety implications of using organic solvents as well as their financial expense.

Ideal characteristics of a film coating polymer Solubility For conventional film coating the polymer should have good solubility in aqueous fluids to facilitate the dissolution of the active ingredient from the finished dosage form. However, where a modified-release action is required then a polymer system of low water solubility or permeability will be chosen.

Viscosity
polymers should have a low viscosity for a given concentration. This will permit the easy, trouble-free spraying of their solutions in industrial film coating equipment.

Permeability Film coating can be used to optimize the shelf-life of a tablet preparation, as some polymers are efficient barriers against the permeability of water vapour or other atmospheric gases. These properties vary widely between the individual polymers.

 Mechanical properties polymer must be one with adequate strength to withstand the impact and abrasion encountered in normal handling. (development of cracks ) comply with the relevant regulatory and pharmacopoeial requirements

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Shellac
Material of natural origin- purified resinous secretion of the insect Laccifer lacca.
Oldest known material used for enteric coatings. Suited for drug targeting in the distal small intestine as soluble at pH 7.0 Its use is now less popular in commercial pharmaceutical applications for enteric coatings. Due to poor batch to batch reproducibility, which is a crucial requirement.

Shellac

Cellulose acetate phthalate (CAP)

Chemical name: Cellulose acetate phthalate Trade name: CAP, Aquateric Application form: organic or aqueous dispersion Functional groups: acetyl, phthalyl Soluble above pH: 6 Additional remarks: sensitive to hydrolysis, 5-30% plasticizer required.

Polyvinyl acetate phthalate (PVAP)

Chemical name: polyvinyl acetate phthalate Trade name: Opadry enteric (aqueous), Coloron Application form: organic solution, aqueous dispersion. Functional groups: acetyl, phthalate, vinylacetat :crotonic acid ratio 90:10. Soluble above pH: 5 Additional remarks: Plasticizer is required.

Acrylic polymers
Chemical name: Methacrylic Trade name: Eudragit Application form: organic solution or aqueous dispersion. Functional groups: methyacrylic acid Soluble above pH: 5 * depends on co- polymers used.

Polymer dissolution
Factors affecting the release of a drug from a polymer: Thickness of the material pH Other excipients Ionic state coating

Plasticizers to modify the physical properties of the polymer to decrease film brittleness. Examples of plasticizers are: polyols, such as polyethylene glycol 400 organic esters, such as diethyl phthalate oils/glycerides, such as fractionated coconut oil. only water-miscible plasticizers can be used for aqueous-based spray systems.
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Colourants water-insoluble colours (pigments). Pigments have certain advantages over water-soluble colours: they tend to be more chemically stable towards light, provide better opacity and covering power, and optimize the impermeability of a given film to water vapour. Examples of colourants are: iron oxide pigments titanium dioxide aluminium Lakes.

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Solvents water is used as polymer solvent The disadvantages of organic solvents for the process: organic solvent vapor into the atmosphere is ecologically unacceptable, and efficient solvent vapor removal from gaseous effluent is expensive. Explosive ,so safety prblem

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Basic process requirements for film coating 1. adequate means of atomizing the spray liquid for application to the tablet cores. 2. adequate mixing and agitation of the tablet bed. 3. sufficient heat input in the form of drying air to Provide the latent heat of evaporation of the solvent. 4-good exhaust facilities to remove dust- and solvent-laden air.

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Functional coatings
Functional coatings are coatings, which perform a pharmaceutical function. These include; Enteric coating Controlled release coating

Enteric coating This technique is used to protect the tablet core from disintegration in the acid environment of the stomach for one or more of the following reasons: 1. Prevention of acid attack on active constituents unstable at low pH 2. To protect the stomach from the irritant effect of certain drugs 3. To facilitate absorption of a drug that is preferentially absorbed distal to the stomach

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Enteric film coating

The enteric polymers (CAP,PVAP, suitable acrylic derivative ) are capable of forming a direct film in a film-coating process. Sufficient weight of enteric polymer must be used to ensure an efficient enteric effect. This is normally two or three times that required for a simple film coating.

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Enteric sugar coating

The sealing coat is modified to comprise one of the enteric polymers in sufficient quantity to pass the enteric test for disintegration. The subcoating and subsequent coating steps are then as for conventional sugar coating.

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Examples of enteric coated OTC products

Enteric coated aspirin E.g. Micropirin 75mg EC tablets

Enteric coated peppermint oil E.g. Colpermin

The ideal properties of enteric coated material

Permeable to intestinal fluid Compatibility with coating solution and drug Formation of continuous film Nontoxic Cheap and ease of application Ability to be readily printed Resistance to gastric fluids

Press coating
process involves compaction of coating material around a preformed core. The technique differs from sugar and film coating process. Advantages:This process enables incompatible materials to be formulated together, such that one chemical or more is placed in the core and the other (s) in the coating material. Disadvantages :Formulation and processing of the coating layer requires some care and relative complexities of the mechanism used in the compressing equipment.

Coating equipments
coating pans

fluid beds
fluid beds

Compression Coating Machines

Accela-Cota: It is a prototype of perforated cylindrical drum providing high drying air capacity. Therefore it is preferred for film coating.

Hi-coater system: The drying air is directed into the drum is passed through the tablet bed, and is exhausted through the perforations in the drum.

Tablet Coating Defetcs

Picking and sticking Bridging Capping Erosion Peeling and frosting Mottled color Chipping Orange peel Twinning

Tablet coating :
Tablet coating is defined as covering the tablets with one or more layers of mixture of various substances such as natural or synthetic resins ,gums ,inactive and insoluble filler, sugar, plasticizer, polyhydric alcohol ,waxes , authorized color and some times flavor .

Aspects of tablet coating :

Avoid irritation of stomach Avoid bad taste Avoid inactivation of drug in the stomach Improve drug effectiveness Reduce influence of moisture Improve drug stability Improve product identity Improve appearance and acceptability

Coating defects :
An ideal coated tablet should be free from any visual defect or functional defect. But some imperfections are seen in the tablet coating for different kinds of reasons . The imperfections found in tablets coating are known as tablet coating defects .

Some coating defects Twinning Color variation Orange peel Roughness Agglomeration Chipping

Blistering Bridging Cracking Picking Capping Pitting

Splitting Flaking Mottled color Erosion Blushing

Twinning
Two tablets stick together. Most common in capsule shaped tablets .

Cause
Coating suspension can not be evaporated.

Remedy
Reducing spray rate Increasing pan speed

Cracking
Small, fine cracks observed on the upper and lower central surface of tablets, or very rarely on the sidewall are referred to as Cracks.

Cause
Use of higher molecular weight polymers or polymeric blends Higher internal stresses in the film ( more than tensile strength of the film )

Remedy
Use low molecular weight polymer Adjust the plasticizer & pigment types and concentration to minimize internal stresses

Sticking & picking

It is defect where isolated areas of film are pulled away from the surface when the tablet sticks together and then part. Picking does not occur alone it must have another tablet to be stuck with which called sticking .
Sticking Picking

Sticking & picking

Cause :
Inefficient drying. Higher rate of application of coating solution Over wetting Excessive film thickness

Remedy :
Reduce liquid application rate. Increase in drying air temperature and air volume.

Blistering
It is local detachment of film from the substrate forming a blister .

Cause :
Over heating during spraying coating solution

Remedy : use mild drying

condition .

Chipping
o It is the defect where film become chipped and dented ,
usually at the edges of tablet .

Cause :
Excessive attrition during coating process

Remedy :
Increase hardness of the film .

Orange peel effects

It refers to a coating texture that resembles the surface of an orange .
Cause :
Rapid Drying High solution viscosity

Remedy :
Use mild drying conditions Use additional solvents to decrease viscosity of solution.

Roughness :
The surface becomes rough and no glossy .

Remedy:
Reduce the degree of atomization

Bridging
Coating fills in the letter or logo on the tablet .
Cause :
Improper formulation Poor logo design Improper application of coating solution Improper atomization pressure High percentage of solid in coating solution High coating viscosity

Remedy :
Increase plasticizer contents or change plasticizer concentration Reduce viscosity of coating solution

Filling
The monogram or bisect is filled and become narrow . Cause :
Applying too much solution Higher solution applying rate

Remedy -

Control fluid application rate

Blooming (Hazing/dull film)

Coating becomes dull immediately or after a prolonged storage . Normally it occurs together with surface roughness. Cause - using low molecular weight plastisizer .

Remedy -

increase MW & concentration of plastisizer .

Erosion
Cause :
Over-wetted tablet surface Inadequate drying Lack of tablet surface strength

Remedy Control drying rate & temparature

Pitting
It is defect whereby pits occur in the surface of tablet core

Cause
Incontinuous spreading of film temperature of the tablet core is greater than the melting point of the materials used in tablet formulation

Remedy -

control drying temperature

Color variation
Two types of color variation
Individual Tablet Color variation, Whole Batch Color Variation

Cause :
improper mixing, uneven spray pattern, insufficient coating migration of soluble dyes , plasticizer and other additives during drying.

Remedy :
Use of lake dyes eliminates dye migration. A reformulation with different plasticizer and additives is the best way to solve film instability.

Cratering
It is the defect of film coating whereby volcanic-like craters appears exposing the tablet surface .
Cause
Penetration of the coating solution into the surface of the tablet

Remedy
Decrease in spray application rate Use of optimum and efficient drying

Blushing (whitish specks)

The defect best described as whitish specks or haziness of the film . It is characterized by precipitation of polymer exacerbated by the use of high coating temperature at or above the thermal gelation temperature of the polymers.

Agglomeration
Agglomeration caused by coating suspension cannot be evaporated as soon as it reach the tablet which may be caused from too much inlet coating suspension or too less inlet heat and the unevaporated suspension glue the tablets together. The amount of excess unevaporated suspension is much more than twinning.

Sometimes it can cause by the leaking of coating suspension into the chamber, or too close spraying distance or too low atomizing pressure.