Tablet Pharmaceutical Industry Lecture 1 PDF

PHARMACEUTICAL INDUSTRY Lecture 1 Tablet Solid dosage form containing one or more active ingredients produced by compressing uniform volumes of granules. Pharmacopoeia Phar·ma·co·pe·ia was created from two Greek words: pharmakon (medicine or charm) and poiein (to make)....

PHARMACEUTICAL INDUSTRY Lecture 1 Tablet Solid dosage form containing one or more active ingredients produced by compressing uniform volumes of granules. Pharmacopoeia Phar·ma·co·pe·ia was created from two Greek words: pharmakon (medicine or charm) and poiein (to make). A book containing directions for the identification of compound medicines, and published by the authority of a government or a medical or pharmaceutical society USP BP EP Tablet material Drug Excipients Drug (API) A pharmaceutical drug is a chemical substance used to treat, cure, prevent, or diagnose a disease or to promote well-being. Active pharmaceutical ingredient (API) against disease. Excipients The word excipient is derived from the Latin excipere, meaning ‘to except’, which is simply explained as ‘other than‘. Pharmaceutical excipients are substances other than the active pharmaceutical ingredient (API) that have been appropriately evaluated for safety and are intentionally included in a drug delivery system. the excipients enable the drug substance to be applied to the patient in the right form and supports the way and place of action without being active themselves. Tablet administration Whole swallowed After being chewed Dissolved or dispersed in water before administration Retained in mouth Tablet ---A commonly used product Oral route----- safe and convenient way of drug administration Physically and chemically more stable than liquid dosage forms Preparation procedures provide accurate dosing of drug Convenient to handle, low in price Quality attributes It must fulfil following quality attributes: Contain correct dose of drug Weight, size and appearance consistent Controlled and reproducible release of drug High mechanical strength to withstand abrasion, fracture and erosion during handling and transport Chemically, physically, microbiologically stable Packed in safe manner Tablet Excipients Diluents/ Filler Disintegrant Binder Glidant Lubricant Antiadherent Sorbent Flavor Color Diluent/ Filler It is added to increase the size of tablet or to increase powder volume when drug is present in small amount. It should be Chemically inert Non hygroscopic Hydrophilic Inexpensive Acceptable in taste E.g. carbohydrates, cellulose derivatives (multifunctional), inorganic salts Sorbitol, mannitol, glucose, sucrose, calcium phosphate, di calcium phosphate etc. Lactose is common due to high dissolution rate, inert, nonhygroscopic nature and pleasant taste. Disintegrant It helps in rapid break down of tablet into primary particles thereby facilitate the dissolution or release of active ingredient. Disintegration time Dissolution time Disintegration time is the time required for a dosage form to break up in to granules of specified size (or smaller) under carefully specified conditions. Dissolution is a process by which solid substance enters in the solvent to yield a solution. Disintegration After the liquid wets the tablet surface and penetrates the pores, disintegration takes place in two steps: first, tablet disintegrates into small granules, and second, deaggregation or granule disintegration Mechanism of Disintegration 1. Disintegration by capillary action (Wicking)----When we put the tablet into suitable aqueous medium, the medium penetrates into the tablet and replaces the air adsorbed on the particles, which weakens the intermolecular bond and breaks the tablet into fine particles., usually surfactants 2. Disintegrant follows swelling mechanism ----- these swell by water absorption and causes rupture of tablet. E.g. corn/ potato starch 3. Disintegrant functions by release of gas ----- acid and base in the solid form added and release carbon dioxide when contact with water. E.g. Bicarbonates with citric/ tartaric acid. Wicking Mechanism Swelling Mechanism Disintegration by release of gas Binder To ensure the making of tablet with good mechanical strength. Binders or adhesives are the substances that promotes cohesiveness. A binder is therefore used for transforming powder into granules through a process known as granulation. In tablet making, granulation is the process by which small powdery particles are agglomerated into larger entities called granules. In the agglomeration, the active ingredient and excipients are bound together by the binder which gives the granule strength. Types of Binder Binders can also form intergranular bonds that fuse the granules together, forming bridges between adjacent granules. The bridges may result from the melting or softening of the binder during the compression process. Rather than add the binder to the powder before the granulation process, a relatively recent innovation is to mix a dry binder directly with the powder before the tablet compression step. Solution binder added in wet granulation in which the binder is added in the form of a solution or suspension. Dry binder added in dry granulation/slugging in which the binder is added as a dry powder. Solution Binder Dry Binder Glidant A Glidant is a substance that is added to a powder to improve its flow ability. In tablet manufacture, glidant are usually added just prior to compression. It improves the flow ability of granules or powder from hopper to die and helps in making of a tablet with consistent weight and shape. It reduces interparticles friction, cohesion. E.g. magnesium stearate, Aerosil ( colloidal silica), talc, starch etc. Glidant Lubricant These are added to ensure smooth surface of tablet These reduce friction between tablet solid surface and die walls. In their absence tablet with uneven surface may form due to erosion and vertical scratches. These reduce force needed for ejection of tablet and tablet without any breakage or cracking is ejected. These should be added in limited concentration, their excess may reduce the mechanical strength of tablet and decrease dissolution rate due to hydrophobic nature. Recommended limit is ≤1 % by wt. Stearic acid and its salts are commonly used lubricants. Starch, talc and hydrogenated vegetable oil are also used. Types of lubrication Boundary lubrication: Solid lubricants act by a boundary mechanism that is the result of the adherence of the polar portions of molecules with long carbon chains to the metal surfaces of the die wall. Magnesium stearate is an example of a commonly used boundary lubricant for tablets. Fluid lubrication: These lubricants, on the other hand, operate by a hydrodynamic mechanism. In this the fluid forms a continuous layer of lubricant between solid particles. Since solid lubricants adhere better to the die walls than fluid lubricants, solid lubricants are more effective and more frequently used. Types of lubrication Antiadherent These reduce adhesion of powder (sticking or picking) of tablet on to the faces of punches or die walls, particularly when powder contains moisture or punches have markings or symbols (engraved/ embossed type). E.g. talc, starch, magnesium stearate Sorbent These are capable of absorbing some quantities of fluids in an apparently dry state. Thus oil or oil-drug solution can be incorporated in a powder mixture of tablet. E.g. microcrystalline cellulose and silica Colorants These are added to impart distinctive appearance to a tablet, to aid its identification and for patient compliance. These are added as dry powder form or in granulation liquid or in coating solution. E.g. water soluble dyes, water insoluble pigments Flavor These are added to mask unpleasant taste of tablet, particularly when made for children or chewable type e.g. antacid or vitamin tablet. These are added either in dry form or as liquid in coating solution. THANK YOU