PhD212 L4 Granules PDF

N u r u l Al ya a b i n t i I b ra h i m , R P h. DipPharm, BPharm, MClinPharm (UiTM) Fa c u l t y o f P h a r m a c y UiTM Pulau Pinang (Bertam Campus) At the end of this lecture, you should be able to: 1) Define granules and their properties 2) Identify the reason for using granu...

N u r u l Al ya a b i n t i I b ra h i m , R P h. DipPharm, BPharm, MClinPharm (UiTM) Fa c u l t y o f P h a r m a c y UiTM Pulau Pinang (Bertam Campus) At the end of this lecture, you should be able to: 1) Define granules and their properties 2) Identify the reason for using granules as dosage forms 3) Describe the granulation process 4) Discuss the advantages of granules 5) Identify the suitable container, labeling, and storage 1. Granules and their properties 2. Granulation process 3. Advantages of granules 4. Overview on method of preparation 5. Containers, labelling and storage Prepared agglomerates of smaller particles of powder/ Prepared agglomerates to produce larger free-flowing properties. Granules; comprise powder particles that have been aggregated to form larger particles sufficiently robust to withstand handling. Pharmaceutical uses?  It has its medicinal value in their content  Can be used for other pharmaceutical purposes (i.e., forming tablets or capsules)  Size Shape Typically fall within the range of 4-sieve (4.75mm) to 12- Irregular in shape sieve (1.7mm) size. ‒ Depends on the use of granules. ‒ If to be used for manufacturing of tablets: granulation of powder can be prepared in the 12 to 20-sieve  Prepared for solid: Prepared for large which are to be doses: Unable to administered orally in formulate as capsules large quantities or tablets Difficult to dispense Difficult to convert as such in powder into liquid because of form because of bitter stability problem and nauseous taste  Process in which primary powder particles are made adhere to form larger multiparticle entities. Also, a process of collecting particles together by creating bonds between them; whereby bonds are formed by compression or by using a binding agent. Advantages of granulation: To prevent segregation of the constituents of the powder mix To improve the flow properties of the powder mix To improve compaction characteristics of powder mix  Screening Drying in air or Purpose: To in oven obtain optimal Granulation sized granules Purpose: To Can be done by passing Wetting/moiste obtain desired through wet and through sieve ning the mixture granule First, blending dry methods Purpose: To bind moisture level the powders the ingredients (for wet together together. granulation) Mix the API and excipients uniformly  Form granules by binding the powder together with an adhesive.  Wet granulation Fluidized bed granulation Fluidized bed Mixer granulation granulators Mixer granulators Particles are placed in a conical piece of equipment and vigorously dispersed and suspended while a liquid excipient is sprayed on them and the product dried forming granules or pellets of defined particle size  Moist the powder or powder mixture then the paste are passed through the mesh to get desired size of granules. The granules are dried by air or under heat. Periodically move out the granules to prevent adhesion into large Mixer granulators Granule screener mass  Dry methods/granulation form granules by compacting large masses of the mixture and subsequently crushing and sizing these pieces into smaller granules Why dry methods? This method applicable to the materials that cannot be prepared by the wet granulation method due to the degradation by moisture OR the elevated temperature required for drying  Dry granulation Roller Slugging compaction Powder is squeezed Large tablets between two rollers produce in heavy Roller compactor to produce sheet of material duty tablet press  Granules flow well more smoothly and predictably than the small powder particles. Hence, commonly used as intermediates in the preparation of capsules and tablets Due to its flow properties, granulations commonly used in the tablet making to facilitate the free flow of material from the feeding container into the tableting presses. Granules usually more stable due to less surface exposure to the effects of atmospheric humidity and are less likely to cake/harden upon standing as the surface area is less than a comparable volume of powder; hence convenience for packaging Granules more easily “wetted” by liquid than certain light and fluffy powders Flow better than powders More stable; convenience for packaging Advantages of granules More easily wetted Produce particle size by a solvent/liquid uniformity  Erythromycin Antibiotics /Antifungals Terbinafine oral Erythromycin Terbinafine granules oral granules GRANULATED CO MMERCI A L PRODUCTS Anti- asthmatics Montelukast granules Montelukast granules  GRANULATED COMMERCIAL PRODUCTS Laxative Senokot Senokot granules granules  EXAMPLES OF GRANULE PREPARATION Ingredients Master formula Methods of Compounding Methylcellulose 64g 1.Mix the powder in a mortar until homogenous. Amaranth 20mg 2.Add sufficient water to form a coherent mass, 3.Press the mass through a 2.8 mm sieve and collect Aspartame 100mg the resulting granules on the mesh of a 710 μm Vanilla 200mg sieve Tragacanth 5g 4.Fine granules and powder will fall through the lower sieve leaving the uniform granules on its Lactose sufficient to 100g surface. 5.Spread the granules to dry on a tray in a drying oven at a temperature of 60 ˚C. Methylcellulose: Bulk laxative use to relieve constipation Others: Psyllium or ispaghula husk 6.Once cool down, pack in a plastic jars with screw- cappedjar  Bulk granules should be packed in plain glass or plastic jars with close- fitting/ airtight closures; a measuring spoon should be supplied. Granules may be dispersed in water or placed on the back of the tongue before swallowing. Effervescent granules should be dissolved in water before taking. Shelf life of granules about 2-3 weeks