Capsules PDF

CAPSULES Overview Capsules are solid dosage forms in which medicinal agents (API) and/or inert substances are enclosed in a small shell of gelatin. Gelatin capsules may be hard or soft. CAPSULES Overview...

CAPSULES Overview Capsules are solid dosage forms in which medicinal agents (API) and/or inert substances are enclosed in a small shell of gelatin. Gelatin capsules may be hard or soft. CAPSULES Overview TWO TY PES:  HARD GELATIN CAPSULES HARD GELATIN CAPSULE Body Cap HARD GELATIN CAPSULE Hard capsules have a rigid shell in two separate pieces fitted together, hence are also called two-piece capsules. More versatile than soft gels. Empty capsule shell are made up of gelatin, sugar, and water. HARD GELATIN CAPSULE Can be clear, colorless, and essentially tasteless. Colored with FD&C and D&C dyes and made opaque by adding agents such as titanium dioxide. HARD GELATIN CAPSULE Gelatin is obtained by the partial hydrolysis of collagen obtained from the skin, white connective tissue, and bones of animals (bovine, porcine, fish, others). Vegetarian capsules – no known potential health risks and generally consist of hydroxypropyl methylcellulose (HPMC) and purified water. ✓ Fast dissolving and easily digestible ✓ Kosher and Halal certified ✓ GMO free, gluten free, no preservatives HARD GELATIN CAPSULE Stable in air when dry Contains 13% to 16% moisture humidity = moisture absorbed = distorted and lose its rigidity (environment) dryness = moisture/moisture is lost = brittle and crumble (environment) Because moisture may be absorbed by gelatin capsules and may affect hygroscopic agents within, many capsules are packaged along with a small packet or cylinder of a desiccant material to protect against the absorption of atmospheric moisture. HARD GELATIN CAPSULE Gamma Scintigraphy A non-invasive procedure that tracks the passage of capsules and tablets through the gastrointestinal tract to map their transit time and drug release patterns. ✓ Tracking the tablet/capsule – added to the formulation of the tablet/capsule ✓ Gamma camera – detects the gamma rays from the tablet/capsule as it moves through the stomach and intestines HARD GELATIN CAPSULE Manufacture Hard gelatin capsule shells are manufactured in two sections, the capsule body and a shorter cap. HARD GELATIN CAPSULE Manufacture 1. Dipping The shells are produced industrially by the mechanical dipping of pins or pegs of the desired shape and diameter into a temperature-controlled reservoir of melted gelatin mixture. HARD GELATIN CAPSULE Manufacture 2. Spinning After dipping, the pins or pegs are spun rapidly in a spinning machine. Spinning helps to evenly distribute the gelatin coating and remove excess gelatin. This ensures a uniform thickness of the capsule shell and helps in achieving the correct dimensions. HARD GELATIN CAPSULE Manufacture 3. Drying 4. Stripping The gelatin-coated pins or pegs Once dried, the gelatin shells are then placed in a controlled are carefully removed from the environment where they are metal pins or pegs. This step dried. Drying solidifies the separates the now solidified gelatin coating into a firm, rigid gelatin shells from the molds. capsule shell. The drying process must be carefully controlled to ensure the capsules do not become too brittle or too soft. HARD GELATIN CAPSULE Manufacture 4. Cutting and Joining The caps and bodies will be trimmed to an appropriate length and then pre-locked. HARD GELATIN CAPSULE Manufacture HARD GELATIN CAPSULE Capsule Size HARD GELATIN CAPSULE Preparation of Filled Hard Gelatin Capsule The large-scale or small-scale preparation of filled hard gelatin capsules is divided into the following general steps: 1. Developing and preparing the formulation and selecting the capsule size 2. Filling the capsule shells 3. Capsule sealing (optional) 4. Cleaning and polishing the filled capsules HARD GELATIN CAPSULE Preparation of Filled Hard Gelatin Capsule 1. Developing and preparing the formulation and selecting the capsule size GOAL: Accurate dosage, good bioavailability, ease of filling and production, stability and elegance HARD GELATIN CAPSULE Preparation of Filled Hard Gelatin Capsule 1. Developing and preparing the formulation and selecting the capsule size Diluent or filler – may be added to produce the proper capsule fill volume. Examples: lactose, microcrystalline cellulose, starch Disintegrants – assist the breakup and distribution of the capsule’s contents in the stomach Examples: pregelatinized starch, croscarmellose, sodium starch glycolate HARD GELATIN CAPSULE Preparation of Filled Hard Gelatin Capsule 1. Developing and preparing the formulation and selecting the capsule size Lubricant or glidant – enhances flow properties to the powder mix. Examples: fumed silicon dioxide, magnesium stearate, calcium stearate, stearic acid, talc Surface active agent – facilitate wetting by the gastrointestinal fluids Examples: sodium lauryl sulfate HARD GELATIN CAPSULE Preparation of Filled Hard Gelatin Capsule 1. Developing and preparing the formulation and selecting the capsule size HARD GELATIN CAPSULE Preparation of Filled Hard Gelatin Capsule 1. Developing and preparing the formulation and selecting the capsule size HARD GELATIN CAPSULE Preparation of Filled Hard Gelatin Capsule 1. Developing and preparing the formulation and selecting the capsule size An easy method to select the proper capsule is to weigh the ingredients for the required number of capsules to be prepared. Place the powders in a graduated cylinder, and obtain the volume occupied by the powders. HARD GELATIN CAPSULE Preparation of Filled Hard Gelatin Capsule HARD GELATIN CAPSULE Preparation of Filled Hard Gelatin Capsule 2. Filling Hard Capsule Shell Punch method – use when filling a small number of capsules in the pharmacy. 1. Spread the powder on a clean paper or plate. 2. Use a spatula to form the powder into a flat layer. 3. Hold an empty capsule body and press it down into the powder layer repeatedly to fill it. HARD GELATIN CAPSULE Preparation of Filled Hard Gelatin Capsule 2. Filling Hard Capsule Shell Punch method HARD GELATIN CAPSULE Preparation of Filled Hard Gelatin Capsule 2. Filling Hard Capsule Shell Non-potent materials, the first filled capsule should be weighed (using an empty capsule of the same size on the opposite balance pan to counter the weight of the shell) to determine the capsule size to use and the degree of compaction to be used. After this determination, the other capsules should be prepared and weighed periodically to check the uniformity of the process. HARD GELATIN CAPSULE Preparation of Filled Hard Gelatin Capsule 2. Filling Hard Capsule Shell Potent materials, each capsule should be weighed after filling to ensure accuracy. HARD GELATIN CAPSULE Preparation of Filled Hard Gelatin Capsule 3. Capsule Sealing Banding - sealing them with a colored band of gelatin (tamper- evident seal) Heat welding - The heat causes the gelatin of the capsule cap and body to soften and melt slightly. The softened gelatin from the cap and body then merges together when pressure is applied. This forms a secure seal around the capsule, closing it tightly. HARD GELATIN CAPSULE Preparation of Filled Hard Gelatin Capsule 4. Cleaning and Polishing On a small scale, capsules may be cleaned individually or in small numbers by rubbing them with a clean gauze or cloth. On a large scale, many capsule-filling machines are affixed with a cleaning vacuum that removes any extraneous material from the capsules as they exit the equipment.  SOFT GELATIN CAPSULES SOFT GELATIN CAPSULE Made of gelatin to which glycerin or polyhydric alcohol such as sorbitol has been added. Contain more moisture than hard capsules. May be oblong, oval, or round. Encapsulate and hermetically seal liquids, suspensions, pasty, materials, dry powders and preformed tablets. SOFT GELATIN CAPSULE Preparation of SOFT Gelatin Capsule Rotary Die Process Liquid gelatin flowing from an overhead tank is formed into two continuous ribbons by the rotary die machine and brought together between twin rotating dies SOFT GELATIN CAPSULE Preparation of SOFT Gelatin Capsule Rotary Die Process At the same time, metered fill material is injected between the ribbons precisely at the moment that the dies form pockets of the gelatin ribbons. These pockets of fill- containing gelatin are sealed by pressure and heat and then severed from the ribbon. Use of ribbons of two different colors results in bicolored capsules. SOFT GELATIN CAPSULE Use of SOFT Gelatin Capsules Soft gelatin capsules are prepared to contain a variety of liquid, paste, and dry fills. Liquids that may be encapsulated into soft gelatin capsules include the following: 1. Water-immiscible volatile and nonvolatile liquids such as vegetable and aromatic oils, aromatic and aliphatic hydrocarbons, chlorinated hydrocarbons, ethers, esters, alcohols, and organic acids SOFT GELATIN CAPSULE Use of SOFT Gelatin Capsules 2. Water-miscible nonvolatile liquids, such as polyethylene glycols, and nonionic surface-active agents, such as polysorbate 80 3. Water-miscible and relatively nonvolatile compounds such as propylene glycol and isopropyl alcohol, depending on factors such as concentration used and packaging conditions  Compendial Requirements for Capsules Added Substances ✓Are harmless in the quantities used ✓Do not exceed the minimum amounts required to provide their intended effect ✓Do not impair the product's bioavailability, therapeutic efficacy, or safety ✓Do not interfere with requisite compendial assays and tests  Compendial Requirements for Capsules Containers ✓tight, well closed, light resistant, and/or a combination of these  Compendial Requirements for Capsules Disintegration Test for Capsules ✓The capsules are placed in a device called a basket rack assembly. This device is designed to hold and move the capsules through a testing medium. The basket rack assembly is immersed into a fluid (usually a simulated digestive fluid or a similar medium) at a controlled temperature of 37°C, which is roughly the temperature of the human body. The fluid simulates the conditions in the digestive system where the capsules will be broken down. Compendial Requirements for Capsules Basket rack assembly Compendial Requirements for Capsules Dissolution Test for Capsules Weight and Content Uniformity Content Labeling Requirement Stability Testing Moisture Permeation Test Official and Commercially Available Capsules Official and Commercially Available Capsules Next Meeting: TABLETS