Solid Oral Dosage Forms

• Solid Oral Dosage Forms

Solid Oral Dosage Forms

• Solid oral dosage forms are widely used for medication due to their simplicity, safety, and convenience in administration.

Advantages of Solid Oral Dosage Forms

• They offer great physical, chemical, and biological stability.
• Dosing is accurate.
• Controlling drug release is achievable, and production costs are low.
• They are simple and practical to administer.

Powders for Oral Use

• Powders are solid, free, and dry particles with varying degrees of fineness.
• They contain single or multiple active ingredients, with or without excipients.
• Effervescent powders are a type of powder formulation.

Advantages of Solid Dosage Forms

• Solids are more stable than liquids; reactions are slower.
• They have a longer shelf life.
• They are suitable for high-dose medications because they can accommodate large amounts of active ingredients.
• Powders dissolve faster than tablets or capsules.

Disadvantages of Solid Dosage Forms

• They are less convenient to carry, lacking the discretion of capsules.
• Masking unpleasant tastes is challenging.
• They are unsuitable for low-dose drugs or those inactivated or harmful to the stomach.

Solid Forms Derived From Powders

• Powder can be presented in several forms, including compacted, granulated, or with excipients.
• Different forms: paper packets, sachets, wafers, gelatin capsules, pills, granules, tablets, and gum pastilles

Granules

• Granules consist of solid and dry aggregates of powder particles, strong enough for handling.
• They are meant for oral administration.

Granule Presentations

• They can be presented in single-dose or multiple-dose forms.
• Different types include effervescent, coated, gastro-resistant, and modified-release granules.

Objectives of Granulation

• Prevents the segregation of mixed ingredients.
• Improves flow and gliding properties.
• Facilitates homogeneous filling of containers and compression machines.
• Enhances compaction characteristics, reducing friction and electrical charge effects.
• Improves tablet characteristics like hardness, friability, and weight.
• Reduces toxicity risks associated with handling solid particles.
• Minimizes paste formation with hygroscopic materials.
• Reduces volume for easier storage and transport.

Dry Granulation Method

• Dry granulation involves compression at high pressures, creating bonds on the particle surfaces.
• Steps: mixing, compacting, fragmenting, and sieving.

Equipment used in Dry Granulation

• Briquetting machines produce briquettes.
• Compaction with rollers produces a sheet of product.

Wet Granulation Method

• Wet granulation involves wetting the drug.
• It requires drying.
• Phases: nucleation, transition, and ball growth.

Wet Granulation Equipment

• Mixers: Drugs are mixed with a diluent.
• Fluid bed: Drying occurs in the same machine.
• Super-cutter mixer granulator: Has a wetting system.

Pelletization

• It attempts to create spherical aggregates from fine powders.
• Spherical shapes facilitate better flow.
• Pellets can be coated for sustained release, compressed into tablets, or dosed in capsules.

Capsules

• Capsules are solid dosage forms for oral use.
• They consist of a gelatin container filled with a quantity of drug and excipients.

Advantages of Capsules

• They protect the drug from external agents.
• They mask unpleasant organoleptic characteristics.
• They provide stability to the drug.
• They offer good bioavailability.

Disadvantages of Capsules

• Production costs are higher.
• Achieving uniform weight in hard capsules can be difficult.
• They are sensitive to temperature and humidity.
• They cannot be split or used by patients with swallowing issues.

Raw Materials used in Capsule Production

• Gelatin: A film-forming material.
• Plasticizers: For making soft capsules.
• Colorants: To color the gelatin.
• Preservatives: To prevent microbial growth.
• Humectants: To aid capsule wetting and disintegration.
• Gastro-resistant materials: For capsules resistant to gastric fluids.

Soft Gelatin Capsules

• Soft gelatin capsules, or "elastic" capsules, consist of a continuous gelatin cover enclosing a liquid fill material.

Soft Gelatin Capsule Composition

• Gelatin mass preparation involves maceration in demineralized water.
• The suspension uses agents to prevent deposition and maintain homogeneity.
• Humectants help with the wetting of components.
• Then gelatin is immersed in the aqueous agent, and heated in a water bath until dissolved.
• Coadjutants are added.
• Filtration through a sieve gives a ready-to-use preparation.

Capsules: Production Methods

• Plate method: Gelatin layer is deposited on a mold plate, filled, and then sealed with another gelatin layer.
• Rotary die process: Gelatin flows over lubricated cylinders to form continuous films.
• These films are then shaped, filled, and sealed by rotating dies.

Storage Conditions for Capsules

• Capsules are typically packaged in plastic or aluminum blisters for protection.
• Hygroscopic liquids should be protected from moisture using glass bottles or airtight blisters.
• Capsules should be stored in cool, dry places below 30°C.

Hard Gelatin Capsules

• Hard gelatin capsules are made using high-speed machines.
• Manufacturing steps include preparing the gelatin solution, forming capsules by immersion, drying.
• The shell is dried in a temperature controlled environment, then its extracted.

Hard Gelatin Capsules controls

• Tests include odor, humidity, dimensions, solubility, fracture resistance, and defect inspection.

Filling Materials for Capsules

• Fill materials consist of active ingredients mixed with auxiliary substances.

Types of Fill Materials

• Powders must have good flow properties.
• Granules pellets, and microcapsules have a spherical shape.
• Tablets release by control and separate components.
• Semi-solids use drug safe and powerful.

Filling the Hard Gelatin Capsules

• The correct capsule size must get selected.
• Filling can be done manually or industrially.

Post-Filling Operations

• Capsules fill can be sealed.

Capsules: Capsule Controls

• Weight variation: Estimates drug content assuming homogeneous distribution.
• Content uniformity: Ensures each capsule contains the specified amount of active ingredient.
• Disintegration test: Assesses the time needed for the capsule to release its contents in the stomach.
• Dissolution test: Determines the rate at which the active ingredient dissolves.

Tablets

Tablets Definition

• Tablets are solid dosage forms with a unit dose.
• Obtained by compressing granules or powder mixtures of one or more active ingredients and various excipients.

Types of Tablets and Applications

• Oral tablets for ingestion.
• Sustained in the oral cavity.
• Administered via other routes and intended to disperse or dissolve before administration.

Tablets Types

• Conventional tablets.
• Chewable tablets.
• Multi-layered tablets.
• Coated tablets.
• Etc.

Tablets Via Compression

• The tablet obtains pre-processing and mixing.
• The process makes it very simple to make a tablet, reduces costs, and presents various restrictions.
• Differences in size are created.
• If drugs do not compress well, there will be a problem

Tablets of a Granulated Compression

• Tablet mixture causes the segregation of products.

Reasons for resorting to granulation

• Prevent component segregation as well as improve its features.
• Improve flow properties.
• Increase compression characteristics.
• It favors the air expulsion and reduces the hygroscopicity of the mixture.

Compression tablet by wet granulation

• Wet granulation is the pulverization and hydration of powder.
• This method results in good cohesion between molecules.

Pellelization Tablet method

• A pellet is a process of agglomeration.
• It converts powder into a smaller package.

Compression Table by Dry Granulation

• Dry granulation known as double compression.
• This method is great because it avoids humidification.