Solid Dosage Forms & Tablets

• Solid oral preparations are also known as Solida peroralia
• Solid oral preparations include, oral powders, capsules and tablets

Application of Solid Dosage Forms (DF)

• Application occurs per os (p.o.)
• Disintegration of the dosage form (DF) occurs
• Active substance (AS) dissolves in the gastrointestinal tract (GIT) fluid
• Absorption into the systemic circulation takes place

Tablets

• Tablets are referred to as Tabulettae
• Tablets are the most widespread and popular oral dosage form
• There has been huge tablet development in the 20th and 21st centuries
• Tablet development has moved from classic conventional moldings to modern next-generation controlled-release dosage forms
• Tablets are solid, mechanically pressed preparations (tablet moldings)
• Tablets are typically cylindrical in shape, and flat or lenticular
• Tablets contain one or more active substances (AS)
• Tablets are intended primarily for oral administration
• They can be swallowed, chewed, dissolved freely in the mouth, or dispersed in water
• Tablets may have a groove for halving or quartering and may have inscriptions or markings
• Excipients (ES) can include fillers, binders, wetting agents, disintegrants, glidants, drug release modifiers, colorants, and flavorings

Tablet Types and Definitions

• TBL. NOB. is Tabuletta (non obductae), which is a non-coated tablet
• TBL. OBD. is T. obductae, which is a coated tablet
• TBL. EFF. is T. effervescentes, which is an effervescent tablet
• TBL. SOL. is T. pro solutione perorali, which is a soluble tablet
• TBL. SUS. is T. pro dispersione, which is a dispersible tablet
• TBL. ENT. is T. enterosolvens, which is a gastro-resistant tablet
• TBL. MRL. is T. cum liberatione modificata, which is a modified-release tablet
• TBL. PRO. is T. cum liberatione prolongata, which is a prolonged-release tablet
• POR. TBL. DIS. is T. pro orodispersione, which is an orodispersible tablet
• TBL. MND. is Tabuletta manducabilis, which is a chewable tablet

Conventional Tablets

• Conventional tablets are sometimes referred to as "1st generation tablets"
• Conventional tablets are simple tablet moldings of various sizes and shapes
• Conventional tablets retain the senses perceivable properties of the original tablet's substances
• After their release, there is a massive one-time release of active substance (AS)
• Conventional tablets are often absorbed from the stomach
• Conventional tablets offer an onset of action that is relatively fast, but typically short

Coated Tablets

• Coated tablets are also known as "2nd generation tablets"
• A core is a conventional tablet, with a single- or multi-layered coating
• Film-coated tablets can be compared with dragees, which possess multiple layers of coating
• More excipients (ES) such as dyes, polishes, and film-forming substances are used compared to conventional tablets

Functions of Coating

• For aesthetic purposes, to improve appearance, mask taste and odor, and facilitate swallowing
• For technological purposes, to protect against external influences, provide mechanical resistance, and separate incompatible substances
• For therapeutic purposes, to target specific areas, such as enteric-coated tablets

Tabulettae Enterosolvens

• Tabulettae enterosolvens, or gastro-resistant tablets, are acid-resistant tablets
• They are a type of controlled-release tablet resistant to gastric fluid
• They release their active substance (AS) in intestinal fluid
• Preparation involves coating granular powders or particles with an acid-resistant cover, or by covering a finished tablet with an acid-resistant cover
• Evaluation involves testing for 2 hours in HCl 0.1 mol/l, then disintegration within 1 hour in a buffer solution with a pH of 6.8

Soluble Tablets

• Soluble tablets dissolve in water before use to form a solution or colloidal solution such as a suspension or gel.

Effervescent Tablets

• Effervescent tablets are also known as T. effervescentes
• These tablets are non-coated
• They contain acids and alkaline components like carbonates or bicarbonates
• In the presence of water these components react violently to form carbon dioxide, mixing the mixture, adjusting the pH, and correcting the taste
• Effervescent tablets are protected from air humidity

Orodispersible tablets

• Orodispersible tablets are soluble in saliva, so no need for drinking
• They are e.g. lyophilized tbl (freeze-dried tablets)

Capsules

• Capsules are also know as Capsulae
• Capsules come in bodies of different volumes and sizes
• Capsules can be hard or soft, depending on the amount of water contained
• Capsules can be swallowed whole or split and have their contents emptied, always according to SPC
• Altering the active substance's (AS) release can be modified
• Controlled release capsules are referred to as Capsulae cum liberatione modificata.
• This directs release to a certain part of the GIT and they are referred to as Capsulae enterosolventes.

Hard Gelatin Capsules

• Hard gelatin capsules are also known as Capsulae durae
• the body and cap fit together exactly
• Contents are powder, granular powder, or pellets
• Contain Raw Materials and Packaging (RMP), and Intermediate Product Processing (IPP)
• Different sizes are available: 5 (smallest) to 000 (largest)

Soft Gelatin Capsules

• Soft gelatin capsules are referred to as Capsulae molles
• Fillings are mostly liquids such as oils with unpleasant taste
• Small capsules = "pearls"
• Soft gelatin capsules are sensitive to moisture

Oral Powders

• Oral powders are known as Pulveres perorales
• They consist of solid, loose, dry particles of varying degrees of fragmentation
• They are administered either by swallowing directly or by dissolving/dispersing in liquid such as water
• A single dose may be split into sachets or gelatin capsules, or multidose is undivided and provided with a measuring cup
• Excipients (ES) are fillers for capsules and sliding agents to improve looseness

Granulates

• Granulates are also known as Grained powders (Granula)
• Granulates are single-dose or multidose undivided preparations for internal use
• Granules are in solid, dry clumps of powder particles sufficiently resistant to mechanical stress
• Must be dissolved or dispersed in liquid before administration
• Types of powders come as effervescent grained powders ( G. effervescentia ), coated grained powders ( G. obducta ), enteric-coated ( G. enterosolventia ) and controlled release ( G. cum liberatione modificata )

Oral Dosage Forms (DF) with Controlled Release

• Tabulettae cum liberatione modificata, are retarded tablets and retardants
• They can be coated or non-coated.
• Selected excipients or processes are used to achieve the desired rate, place or time of active substance (AS) release
• Capsullae cum liberatione modificata have hard or soft capsules with modified packaging, or contents
• This has a specific manufacturing process to speed up, place or time the release of the AS
• Granula cum liberatione modificata are used as drug microforms, for example pellets, microparticles, and nanoparticles

Reservoir Type Release Control System

• Includes a core of active substance (AS) in liquid, semi-solid, or solid form, with a polymer shell (wall and membrane)
• The packaging has a control function to control the release of active substance
• Release can occur through dissolution with a membrane which is soluble at different pH levels
• Release can occur through diffusion using a porous membrane or osmosis

Matrix Type Release Control System

• Does not have a membrane
• The AS is dispersed in the matrix
• The matrix either gradually dissolves (it is biodegradable) or Active Lipids (LL) are released by diffusion and the matrix is excreted unchanged

Common Tablet Designations

• SR = sustained release
• SL = sustained liberation
• XL = extended liberation
• XR = extended release
• MR = modified release
• CR = controlled/continuous release
• PR = pulsatile release