Capsule PDF - PHD 212 Capsules

PHD 212 CAPSULES NURUL ALYAA BINTI IBRAHIM, RPh. DipPharm, BPharm (Hons.), MClinPharm (UiTM) Faculty of Pharmacy, UiTM Pulau Pinang (Bertam Campus)  LEARNING OUTCOME After this lecture, students should be able to : Understand cachets formulation in pharmaceuti...

PHD 212 CAPSULES NURUL ALYAA BINTI IBRAHIM, RPh. DipPharm, BPharm (Hons.), MClinPharm (UiTM) Faculty of Pharmacy, UiTM Pulau Pinang (Bertam Campus)  LEARNING OUTCOME After this lecture, students should be able to : Understand cachets formulation in pharmaceutical preparations Explain advantages, disadvantages, types of capsules and its characteristics Describe quality standard, containers, labeling and storage of capsules Explain general principles involved in manufacturing and dispensing of capsules  LECTURE OUTLINE 1. Cachets 2. Types of capsule 3. Advantages and disadvantages 4. Component of capsules  CACHETS 1. Cachets are solid dosage forms of drugs, also known as wafer capsules. 2. Cachets include 2 plate-shaped rice paper filled with dry powder up to 2g. 3. These cachets are molded from rice flour. Mixture of rice flour + water -> rice paper -> enclosed in between 2 hot, polished cylinders -> water evaporate -> wafer is formed  Quite hard Dipped in water for seconds Swallowed with lots of water Why? -> To prevent the patient from tasting the powder  ADVANTAGES AND DISADVANTAGES Advantages Disadvantages Made easily Easily damaged Disintegrate quickly in the stomach Need to be softened first before swallowing The enclosed cannot be protected from light Large doses of drug can be swallowed and moisture Shell of cachets are fragile hence drug content can be compressed Not suitable for filling of drugs in large scale Cachets occur more space compared with tablets and capsule dosage forms Very RARELY used nowadays!  MAKING CACHETS AT OLD AGE! Putting in the cachets Filing with powder Moistening the lids Pushing out the finished cachets  CAPSULES Capsule is derived from the Latin “capsula” = small box A solid dosage form that is filled with solid, semi-solid, or liquid medications. Unit doses of drugs enclosed within soluble shells of gelatin or similar materials, are intended to be swallowed whole.  TYPES OF CAPSULES Capsules Hard gelatin capsules Soft gelatin capsules  HARD GELATIN CAPSULE Known as hard-shell capsule Capsule shells are made from gelatin and are clear, colourless and tasteless Colourings and markings are added for light protection and to ease identification May be filled with powders, granules and pellets HARD GELATIN CAPSULE The base and body (longer and lesser diameter portion) Hard gelatin capsules (cap and body) Description The cap (shorter and slightly /Properties larger diameter portion. The cap is designed to slide over the base portion and form a snug seal) After filling, these 2 pieces are locked together HARD GELATIN CAPSULE: CAPSULE SIZE Based on capacity of granules, capsule size are numbered and ranges from 000 (largest) to 5 (smallest). SOFT GELATIN CAPSULE Consists of flexible solid shell containing powders, nonaqueous liquids, solutions, emulsions, suspension or paste. Description /Properties Soft gelatin capsules appear swollen -> they are manufactured and filled in one operation that results in the pressure of contents maintaining the capsules shape.  Allow the liquid to be given as solid dosage forms -> improving the bioavailability of delivering a drug. Offer accurate dosage, improved stability, and overcome problems using powder. SOFT GELATIN CAPSULES: SIZE AND SHAPE  HARD VS SOFT GELATIN CAPSULE Mainly both differ in their mechanical properties and in capsule design Hard gelatin capsules Soft gelatin capsules Less flexible More flexible Oblong or cylindrical Spherical, ovoid, or cylindrical Composed of two pieces: Cylindrical body Composed of one-piece capsule shell: and cap formed, filled and sealed in one operation Generally used for solid medicaments Usually, contents are non-aqueous dispersions/oils/solutions, gel and paste  ADVANTAGES OF CAPSULES Easy to swallow Effectively mask the Can be light (suitable shape and odor and taste of resistant (opaque slippery when substances/drugs capsules) moistened) Can be formulated Rapid and uniform to increase oral release of bioavailability of Fewer excipients medication poorly soluble/liquid required drug  DISADVANTAGES OF CAPSULES Disadvantages of capsules Requirement of specialized manufacturing equipment Limited choices of excipients/carriers compatible with gelatin Potential stability problems associated with capsule-containing liquid fills Problems regarding the homogeneity of fill weight and content may be associated with capsule formulations Unable to divide/separate capsule into desirable individual dose  APPLICATION Main use: Oral drugs NOT SUITABLE for drugs: Strongly efflorescent Strongly deliquescent Very soluble salts materials – capsules powder – capsules shell (potassium chloride, tend to soften when water brittle when moisture potassium bromide, is lost from the drugs to extracted from shell into ammonium chloride) capsule shells powder.  COMPONENTS OF CAPSULE What we use to make capsules? Gelatin Preservatives Plasticizer Wetting Colorants agents  GELATIN non-toxic (widely used in foodstuffs. readily soluble in biological fluids at body temperature Basic properties forms a good film a solution in water undergoes a reversible phase change from a colloidal dispersion (mobile liquid) to a gel (rigid state) at temperatures only a few degrees above ambient temperature  GELATIN #2 Gelatin is a substance of natural origin. However, it does not occur as such in nature. It is prepared by hydrolysis of collagen which is the main protein constituent of connective tissues or collagen (animal bone and skin is main raw material used for manufacture) There are two types of gelatin Type A produced by acid hydrolysis (manufactured mainly from skins) Type B is produced by basic hydrolysis (manufactured mainly from bones) - typically used for soft gelatin capsules  GELATIN #3 Two key properties of gelatin that are relevant for manufacturing capsule/ quality control of raw material Bloom strength Measure of gel rigidity Viscosity To control the thickness of of gelatin solution the films or sheets  MANUFACTURING OF HARD GELATIN CAPSULES FROM GELATIN Capsule molds Once dipped, Capsule Finished (pin) are they are raised Capsules are bodies and capsules are dipped into to let bodies stripped from caps are pushed into gelatin and caps to the pins joined conveyer belt solution set and dry automatically to be collected  WATER CONTENT IN GELATIN CAPSULE SHELL When forming the hard gelatin Water in the gelatin capsule capsule shells, the water content shell helps of capsule is between 14-16%. After filling of the capsules with To ensure the mechanical properties of the capsule are sufficiently robust a drug, a final drying to 13% so that the capsule does not either crack or permanently deform w/w of water content. Soft gelatin capsule sheet is 30- To ensure the capsule is flexible during manufacturing, following 40% w/w but a final soft capsule formation, the capsule are drying but not overdried, not brittle. water content is 5-14% w/w.  PRESERVATIVES Preservatives are sometimes added to capsule gelatin to prevent microbial contamination during manufacture Commonly in finished capsules, moisture levels are low enough so that capsules will not support bacterial growth Soft gelatin capsules sometimes have antifungal agents added to prevent surface growth when stored in non-protective packages Examples Parabens Benzoic acid  PLASTICISER Added to increase the pliability/flexibility Examples: Glycerol, sorbitol, propylene glycol, sucrose and acacia Soft gelatin capsules are softer and more flexible because they contain a large proportion of plasticiser (plasticiser: gelatin = 0.8:1) Hard gelatin capsules are firm and rigid (plasticiser: gelatin= 0.4:1) Glycerol plasticised gelatin films  COLOURANTS Mainly synthetic in To enhance the origin and by using Soluble dyes mixtures, capsules can aesthetic (beauty) be made in most colours Colourants properties Titanium dioxide which As a means is white and is used as an opacifying agent of identifying Insoluble pigments the product Iron oxides which are available as black, red and yellow  WETTING AGENT Added to the gelatin solution during the Example: Sodium lauryl sulphate preparation stage. The stainless-steel molds are lubricated prior to dipping into the gelatin solution to reduce the surface tension of the mix and cause the mold pins to wet more uniformly Enhance the wetting of the gelatin solution on the metal pins (moulds) during the manufacturing process, thus production of the uniform thickness gelatin  WHAT NEED TO GO INSIDE CAPSULES? Powder filling Contents of capsule Non-powder filling  POWDER FILLING Consists of the active ingredients, diluents, additives The most significant factor about a uniformly filled capsule is powder flow Free-flowing excipient (lubricant/glidant: magnesium stearate) are used to improve flow, thus powders are homogeneous and reproducibly packed into capsules Like tablet dosage forms, to achieve good drug release, the contents should be readily wetted and dispersed by biological fluids. Thus, the powders are added with other excipients (wetting and disintegrating agents) to increase drug release.  NON-POWDER FILLING Liquids, granules, pellets and semisolids may be incorporated into capsules 1. Liquids: Water cannot be used as a liquid fill Fill materials for hard gelatin capsules must be nonaqueous in nature. Water-miscible liquids: Oils: polyethylene glycols vegetable oils, fatty (solid at room acid esters temperature but liquify upon heating)  NON-POWDER FILLING #2 2. Granules and pellets should be as near to spherical as possible Like powders, uniform filling depends on granules being free flowing, regular in shape and size Both granules and pellets are often formulated  NON-POWDER FILLING #3 3. Semi solid Semi solid may be incorporated into hard and soft gelatin capsules Mixture for filling need only be ‘liquid’ when filled into capsule while hot and ‘solid’ when inside at room temperature This can be achieved by using thermosoftening or thixotropic materials and are liquefied by using either heat or shearing forces respectively which revert to the solid state once in the capsule  HARD VS SOFT CAPSULE Hard gelatin capsule Soft gelatin capsule Fill mainly solids: powder, Fill mainly liquid and semi-solids: granules oily solution, suspension, paste Capsule shell? THANK YOU [email protected] Level 4, Room 77