112 Pharmaceutical Tablet Coating 112.1 History M21 1122 Reasons for Coating Tablets M21 1123. ‘Types of Coating. 1122 The Sugat-Coated Tablet» The Fi-Coated Tabet = Joseph L. Johnson Compression Coating Aqualon Company Bibliography 1123 112.1 History ‘The coating of solid pharmaceutical dosage forms began in the ninth century B.C, with the Egyptians. A that time the primary solid dosage form was the pill, a hand-shaped spherical mass containing drug, sugar, and other diluents. A variety of materials were used to coat pills, such as tale gelatin, and sugar, Gold and silver were also used. Many of these coatings proved to be impervious to chemical attack in the digestive tact; as a result the pill never released its active ingredient and Was thus ineffective ‘The candy-making industry was the first to develop and enhance the art of coating. It is most likely that the pharmaceutical industry adopted sugar coating technology for its own use. The first sugar-coated pills produced in the United States came out of Philadelphia in 1856, Coatings resistant to enteric oF gastric fluids were developed in the 1880s. In 1953 the first compression-coated tablet was introduced, and in 1954 the first flm-coated tablet was marketed. 112.2 Reasons for Coating Tablets ‘There ate many reasons for coating tablets; some aestheti, some functional. One important reason is to enhance drug stability; that is to protect the drug from oxygen, moisture, and light, the three key causes of drug degradation. Coating can also be used to separate reactive components in a tablet formula, ‘Another important reason for tablet coating is identification, Tablet coatings may take on a variety of colors. A coated tablet may also be imprinted with a symbol or word. In the case ofthe film-coated table, the tablet core may be embossed with a symbol or word that remains visible after the coating process. ‘The definitive identification of a coated tablet has saved patients and health care professionals alike, Additionally, coating is used to uniquely identify a branded product. ‘Tablet coating is done for aesthetic reasons as well. Often the appearance ofthe tablet core is mottled or otherwise unattractive. Coating masks this. Many times, too, the drug itself has a bitter taste, Coating. masks this as wel. “Tablet coating can also be used to control the duration and site of drug release. Overall, tablet coating, through an additional step in the manufacturing process, is often vital. 21112.2 Coatings Technology Handbook, Third Edition 112.3. Types of Coating ‘There are two main types of tablet coating done today: sugar coating and film coating; film coating is the more popular. Coated tablets fll into three main subcategories depending on how the drugis released: immediate release, enteric release, and sustained release Immediate-release coating systems, as the name implies, allow immediate release of the drug com- pound to the body. Enteric coatings are soluble only at a pH greater than 5 or 6. Thus, the drug is not released in the stomach but in the small intestine. Enteric coatings are by far the most unreliable because of the wide and unpredictable variance in gastric pH profiles. Gastric pH varies considerably based on stomach content, age of the patient, and disease state. Sustained-release coatings permit drug to dissolve slowly over a period of time. This helps to reduce dosing intervals and improves therapeutic reliability Film coating can be carried out using either an organic solvent system, such as ethanol or methylene chloride, or by using water asa solvent. The solvent film coating systems are fast disappearing because of cost, environmental, and salty concerns, Most film coating carried out today is done with aqueous systems, 112.3.1 The Sugar-Coated Tablet ‘The sugar-coated tablet is the most elegant solid dosage form produced today. Its glossy appearance, slippery feel and sweet taste are unmatched by any other coated tablet. The sugar-coated tablet is also the most difficult and time-consuming to produce. The tablet consists of a core upon which layer after layer of coating material is slowly and carefully built up. In some cases this is done by hand and in other cases automatically. In any event, there is still an art to sugar coating. "To successfully accept a sugar coating, the tablet cores must be robust. They are subjected to wetting rolling in a coating pan with 50 kg or more of other cores. Generally the coating pan is spherical and has a solid exterior surface. Temperature-controlled air is introduced and removed from the pan via external ducts. The following procedure is used for the manual sugar coating of tablets. ‘The first step isto slightly waterproof the tablets by applying a coat of pharmaceutical-grade shellac. ‘This prevents the cores from dissolving prematurely in the presence of the other coating liquids that are to be applied, ‘The second step is subcoating: a solution composed of acacia, gelatin, and sugar is applied to the tablets. The wetted cores are then dusted with dicalcium phosphate or calcium sulfate and allowed to dry. This step is repeated many times until a smooth rounded tablet form has been achieved, “The third step isthe grossing coat. The cores are wetted with a sugar solution and dusted with titanium dioxide powder. This creates a very white base coat on which color may be applied, ‘The fourth step isthe color coat. In this instance an insoluble opaque color solid is suspended in sugar syrup and applied tothe tablet. No dusting ofthe cores takes place. The tablets are simply ait dried, "The fifth step isthe shutdown coat. In this step diluted sugar syrup is applied to the tablet and allowed to dry. This produces a very smooth finish in preparation for the last step. ‘The last step is polishing of the tablets. The tablets are placed in a canvas-lined drum, Beeswax or carnauba wax is dissolved in methylene chloride, and the solution is applied to the tablets, which are tumbled until the solvent evaporates and tablets achieve a very high shine. In all, 40 or more separate layers are applied during the manual sugar coating process, The process takes between five and eight 8-houe shifts to complete. ‘Automated sugar coating is generally faster. For example, the various syrups used inthe coating process have the dusting powders suspended in them. The syrups are applied by spray. This process can be automated to reduce the number of operators required. Perforated coating pans, which greatly enhancePharmaceutical Tablet Coating 112.3 air throughput, are used almost exclusively. With greater air throughput, water evaporates more quickly, thus speeding the process, Using automated techniques, tablets can be sugar coated in about 16 hours. 112.3.2. The Film-Coated Tablet ‘The film-coated tablet consists of a core around which a thin, colored polymer film is deposited. Thus, afilm-coated tablet gains about 3% of total tablet weight upon coating, The sugar-coated tablet undergoes 10006 weight gain. Overall, film coating is a much faster procedure, and much less prone to error. ‘The basic film coating formula consists of a film former, a pigment dispersion, a plasticizer, and a solvent. A variety of polymeric film formers can be used to coat tablets. By selecting the solubility properties of the polymer, one can produce an immediate-release, an enteric-release, or a sustained- release tablet ‘The most popular immediate-release film formers are the water-soluble cellulose ether polymers. The {wo most common are hydroxypropylcellulose (HPC) and hydroxypropylmethycellulose (HPMC). The low viscosity grades of these polymers are employed in the coating formula to maximize polymer solids concentration. Both these polymers are water soluble. ‘Water-insoluble film formers can also be used to prepare immediate-release coatings. These products fall into two categories: cellulose ethers and acrylate derivatives. The most common cellulose ether is ethylcellulose. This material is commercially available in two forms: as pure polymer and as an aqueous dispersion. The pure polymer is generally dissolved in an organic solvent; the dispersion is delivered out of an aqueous media. In both cases, a certain amount of water-soluble component (up to 509% of the total polymer solids) is included in the coating formula, to provide immediate drug release. ‘The ethylcellulose and acrylate compounds are also used to formulate sustained-release products Again, a water-soluble component is included in the coating formula. However, the level is very low: usually about 396 of total polymer solids. When the coated dosage form is exposed to water, the water- soluble component dissolves. Ths leaves a porous film surface through which drug diffuses. ‘The third class of coatings, the enterics, resist the attack of gastric ids. As a result, drug is released only in the small intestine, Enteric coatings ate prepared by using a polymer with pH-dependent solubility properties. Cellulose estes, substituted with phthalate groups, are the primary polymers used in this application, especialy cellulose acetate phthalate. Polyvinyl acetate phthalate is also used. Acrylate deriv. aves are also capable of providing enteric release 112.33 Compression Coating Compression coating isa technique wherein a large tablet either completely or partially surrounds a smaller tablet. Essentially, a small tablet is compressed first and is then surrounded by powder, which undergoes compression. This type of coating technique requires the use of special tableting machinery and itis used to produce sustained-release tablets. Bibliography Florence, A. Ty Ed, Criial Reports on Applied Chemistry, Vol. 6, Materials Used in Pharmaceutical Formulation. London: Blackwell Scientific Publications, 1984 Lachman, L, H. A. Leiberman, and J. I. Kanig, Eds, The Theory and Practice of dustrial Pharmacy, Philadelphia: Lea & Febiger, Ist ed, 1970; 2nd ed, 1976; 3rd ed, 1986 Oso, Arthur, Ed, Remington's Pharmaceutical Sciences, Eston, PA: Mack Publishing Company, Lith ed, 1970; 15th ed, 1975; 16th ed, 1980; 17h ed, 1985 ©2009 Tyr Ar Gap.