part 3: GRANULES, TABLETS, AND CAPSULES

Granules

Granules

Agglomerates of smaller particles of powders

0.2mm to 4mm

Size range of Pharmaceutical granules

#4 to #12

Pharmaceutical granules pass through mesh size sieve #___ to #___

1. To prevent segregation or demixing of the constituents of the powder mix

2. To improve the flow properties of the mix

3. To improve the compaction characteristics of the mix

Enumerate the reasons why we do the process of Granulation

1. Dry Granulation

2. Wet Granulation

Methods of Granulation

Pre-Compression or Double Compression

Dry granulation is also known as?

Dry Granulation

• The primary powder particles are aggregated under high pressure

• Used for drugs that do not compress well after wet granulation, or those which are sensitive to heat and moisture

1. Slugging

2. Roller Compaction

Dry Granulation Methods

Rotary Compaction

Slugging is also known as?

Slugging

A large tablet (known as Slugs) is produced which is broken via Milling to produce granular materials

Ribbon Technique

Roller Compaction is also known as?

Roller Compaction

The powder is squeezed between two rollers to produce a sheet of material

Wet Granulation

• Most widely used Granulation technique

• Involves the massing of a mix of dry primary powder particles using a granulating fluid, the wet mass is forced through a sieve to produce wet granules which are then dried. A subsequent screening stage breaks agglomerates of granules

Tablets

• Solid pharmaceutical dosage forms containing drug substances with or without suitable diluents and have been prepared by either Compression or Molding

• MOST COMMON SDF

• MOST STABLE ODF

• MOST TAMPER PROOF ODF

Hard Tablets

Tablets produced through Compression

Soft Tablets

Tablets produced through Molding

1. Precision and low content variability

2. Low manufacturing cost

3. Easy to package and ship

4. Appropriate for special release form

5. Simple to identify

6. Essentially tamper proof

Advantages of Tablets

1. Good compatibility is required

2. Resist compression

3. Require encapsulation before compression

Disadvantages of Tablets

1. Tablets for Oral Ingestion

2. Tablets used in Oral Cavity

3. Tablet used to Prepare Solutions

Types and classes of Tablets

1. Conventional Compressed Tablets

2. Multiple Compressed Tablets

3. Sugar Coated Tablets

4. Film Coated Tablets

5. Enteric Coated Tablets

6. Chewable Tablets

Tablets for Oral Ingestion

Conventional Compressed Tablets

Tablets formed by Compression and in their simplest form, contain no special coating

1. Layered Tablets

2. Press Coated Tablets

Types of Multiple Compressed Tablets

Layered Tablets

Compressing additional tablet granulation on previously compressed granulation

Significance:

1. To separate incompatible ingredients

2. To produced prolonged or repeated release profile

Compression Coated Tablets or Dry Coated

Press Coated Tablets are also known as?

Press Coated Tablets

Compressing another granulation outershell around the preformed tablet

Significance:

1. To separate incompatible ingredients

2. To produced prolonged or repeated release profile

Sugar Coated Tablets

• Compressed tablets coated by Sugar solution

• Most elegant solid dosage form produced today

• Most difficult and time consuming to produce

• 50-100% increase in size and weight

Significance:

1. To improve appearance

2. To mask unpleasant taste or smell

3. To protect from oxidation

Film Coated Tablets

• Compressed tablets coated with a thin layer of water insoluble or soluble Polymer

• 2-3% increase in weight

Significance:

1. To protect the drug from atmospheric conditions

Enteric Coated Tablets

• Compressed tablets coated with substances that RESIST solution in gastric fluid but disintegrate in the intestine

• Also known as Delayed Action Tablet

• Enteric coating: Shellac and Cellulose Acetate Phthalate

Significance:

1. To protect the drug which are inactivated destroyed in stomach

Chewable Tablets

• Tablets that are intended to be chewed and swallowed

• Diluent used: Mannitol

• Commonly used for multivitamin tablets and are used for some antacids and antibiotics

Significance:

1. Useful for children and elderly who is having difficulty in swallowing

1. Sublingual Tablets

2. Buccal Tablets

3. Lozenges and Troches

Tablets used in the Oral Cavity

Sublingual Tablets

Tablets are placed under the tongue and dissolve rapidly

Significance:

1. Suitable for drugs that does not absorb very well in the stomach

2. Avoid first pass metabolism

Buccal Tablets

Tablets designed to dissolve slowly in the mouth between the cheek (buccal) and gingiva

Significance:

1. Suitable for drugs that does not absorb very well in the stomach

2. Avoid first pass metabolism

Lozenges and Troches

These are slow dissolving tablet prepared by Molding or Compression (to produce local (primary) or systemic effect

Significance:

1. Better patient compliance

2. Avoid first past metabolism

Lollipop

Lozenge + Stick = ?

Pastilles

Molded Lozenge is called what?

Troches

Compressed Lozenge is called what?

1. Effervescent Tablets

2. Dispensing Tablets

3. Hypodermic Tablets

4. Molded Tablets

Tablets used to prepare Solutions

Effervescent Tablets

Tablets containing an organic acid and a carbonate salt along with API, which is dissolved in water to produce Effervescence

Significance:

1. Improves the palatability

2. Acts faster absorption

Compounding Tablets

Dispensing Tablets are also known as?

Dispensing Tablets

Tablets containing large amounts of highly potent drug substances and supplied primarily for EXTEMPORANEOUS COMPOUNDING of the Pharmacist

Significance:

1. It can be extemporaneously prepared according to the requirement of the patient

Hypodermic Tablets

Soft, readily soluble tablets, originally used by Physicians in preparation of Parenteral Solutions

Significance:

1. Preparation of parenteral solutions

Tablet Triturates

Molded Tablets are also known as?

Molded Tablets

Tablets prepared by Molding and are very soft and disintegrate quickly

Significance:

1. It can be extemporaneously prepared according to the requirement of the patient

Modified Release Dosage Forms

Drug product that alter the rate or timing of drug release

Dose Dumping

Abrupt, uncontrolled release of a large amount of drug is a problem for Modified Release Dosage Forms

1. Extended Release

2. Delayed Release

3. Repeat Action

4. Targeted Release

Types of Modified Release Dosage Forms

Extended Release

any dosage form that maintains therapeutic blood or tissue levels of the drug for a prolonged period (usually between 8 and 12h)

1. Controlled-release

2. Sustained-release

Types of Extended Release

Controlled-release

• Releases the drug at a constant rate and provide plasma concentrations that remain invariant with time

• Rate of release is largely determined by the design of the device itself (which could be a polymer or pump) and is not dependent on environmental conditions (pH)

Zero Order Release Kinetics

Controlled-release follows what release kinetics?

Sustained-release

• Releases an initial release of drug sufficient to provide a therapeutic a therapeutic dose soon after administration, and then a gradual release over an extended period

• Affected by environmental conditions

First Order Release Kinetics

Sustained-release follows what release kinetics?

Delayed Release

Drug is not being released immediately following administration, but a later time

Repeat Action

An individual dose is released fairly soon after administration, and second or third doses are subsequently released at intermittent intervals

Immediate release

Under Repeat Action, 1st dose = _______________

Delayed release

Under Repeat Action, 2nd dose = _______________

Targeted Release

• Drug release direct toward isolating or concentrating a drug in a body region, tissue, or site for absorption or for drug action

• Examples: Monoclonal Antibodies

Capsules

Solid dosage forms in which medicinal agents and/or inert substances are enclosed in small shell of Gelatin

Gelatin

It obtained by the partial hydrolysis of Collagen obtained from the skin, white connective tissue, and bones of animals

1. Type A - Acid Hydrolysis

2. Type B - Alkali Hydrolysis

Two types of Gelatin

Bloom Strength

Gelatin grade is specified by what?

Bloom Strength

• Measurement of gel rigidity or strength

• Force expressed in grams used to depress the gel surface by 4mm using a standard plunger

200-250g

HGC = _______________

150g

SGC = _______________

Hydroxypropyl methylcellulose

Hard gelatin capsule is considered vegetarian and can be used by people with restriction on consuming animal- based product

10 degrees C to 25 degrees C, and 35% - 45% RH

or

15 degrees C to 30 degrees C, and <70% RH

Capsules storage condition

1. Hard Gelatin Capsules

2. Soft Gelatin Capsules

Two types of Capsules

Dry Filled Capsules

Hard Gelatin Capsules are also referred as?

1. Gelatin

2. Sugar

3. Water

Main components of Hard Gelatin Capsules

1. Colorant

2. Opacifying agent

3. Preservative

Other components of Hard Gelatin Capsules

Titanium dioxide

Opacifying agent that is commonly used for Hard Gelatin Capsules

Sulfur dioxide

Preservative that is commonly used for Hard Gelatin Capsules

12-16% or 13-16%

Moisture content of Hard Gelatin Capsules

Punch Method

Method of Preparation (Extemporaneous) of Hard Gelatin Capsules

TRUE

True or False: In Hard Gelatin Capsules, empty capsules are supplied in a varied of sizes from 000 to 5

5

Smallest capsule size

000

Largest capsule size

Soft Elastic Capsules

Soft Gelatin Capsules are also known as?

Soft Gelatin Capsules

• One-piece capsule

• Used to contain a nonaqueous solution, a powder, or a drug suspension

1. Gelatin

2. Water

3. Plasticizer

Main components of Soft Gelatin Capsules

1. Preservative

2. Opacifying agent

3. Colorant, flavoring, and sweetening agent

Other components of Soft Gelatin Capsules

4-10%

Moisture content of Soft Gelatin Capsules

1. Plate Process

2. Rotary Die Process

Method of preparation of Soft Gelatin Capsules

Plate Process

Old method of preparation of Soft Gelatin Capsules

Rotary Die Process

New method of preparation of Soft Gelatin Capsules