1. TABLET DILUENTS
(LACTOSE AND CALCIUM PHOSPHATE)
MD.JAKIUL ISLAM
ID:UG08-20-12-066

2. CONTENTS
 Definition
 Properties of diluents
 Purpose of diluents
 classification

3. What is diluent ?????
 Diluents are fillers used to increase the bulk volume of a tablet
diluent
active pharmaceutical ingredients
product adequate weight and size
 Purpose of
diluents :• to enhance bulkiness
• to provide improved cohesion
• to enhance flow
• to allow direct compression manufacturing

4. Properties of diluents:
• inert
• nontoxic
• biocompatible
• stable
• acceptable
• non-hygroscopic
• non-conducive to microbiological
• commercially available in acceptable grades
• color-compatible
• no deleterious effect on bioavailability of
drugs.

5. Classification :
Diluents
Chemical nature Solubility
Organic materials Inorganic materials Insoluble Soluble
Dextrose
Lactose
Mannitol
Sorbitol
Starch
sucrose
Calcium phosphate (II)
Calcium phosphate (III)
Calcium sulphate
Calcium carbonate
Dextrose
Lactose
Mannitol
Sorbitol
sucrose
Calcium phosphate (II)
Calcium phosphate (III)
Calcium sulphate
Calcium carbonate
Starch

6.  Compatibility
 Flowability
 Solubility
 disintegration qualities
 hygroscopicity
 lubricity
 stability
SELECTION OF DILUENT

7.  EFFECTS OF DILUENTS:
• Degradation of API (hydrolysis)
• Mannitol - punch filming/ picking
• Sucrose – tablet hardness-poor disintegration
• Capping – low moisture
• complex formation

8.  LACTOSE :
• solubility – water soluble
Forms
Hydrous
Anhydrous
used in wet granulation
shows fast disintegration, good friability,
practically no sticking, binding and
capping
• most widely used diluent
hydrous form undergoes maillard reaction discoloration of certain drugs
( amine drug )
●
Problem of browning due to contamination of 5-hydroxyfurfural which was
accelerated in the presence of basic amine drugs and catalyzed by tartarate, citrate
and acetate ions

9.  Inorganic calcium salts
• Dicalcium phosphate (Emcompress or DiTab)
Free flowing aggregates of small microcrystals that shatter upon compaction
Inexpensive and possesses a high degree of physical and chemical stability
Non hygroscopic at a RH of up to 80%
Good fluidity
Slightly alkaline with a pH of 7.0 to 7.3
• Tricalcium phosphate (TriTab) is less compressible and less soluble, higher ratio of calcium ions

10. Tribasic Calcium Phosphate
As with dibasic calcium phosphate, a lubricant and a disintegrant should usually be
incorporated in capsule or tablet formulations that include tribasic calcium phosphate.
In some cases tribasic calcium phosphate has been used as a disintegrant. It is most
widely used in vitamin and mineral preparations as a filler and as a binder. It is a
source of both calcium and phosphorus, the two main osteogenic minerals for bone
health.
Trade name:
• Dibasic calcium phosphate : Di-Tab and Emcompress
• Anhydrous dibasic calcium phosphate : A-Tab, Fujicalin, Emcompress Anhydrous
• Tribasic calcium phosphate : Tri-Tab.

11. Lactose monohydrate, spray dried lactose and anhydrate lactose are
widely used as diluents:
 Spray dried lactose :
●
Lactose is placed in aqueous solution, removed impurities and spray dried
●
Mixture of large alpha monohydrate crystals and spherical aggregates of smaller crystals
●
Good flow ability but less compressibility
●
Poor dilution potential
●
Trade name: Spray Process 315; Flow Lac; Lacto press; Super Tab 11SD,14SD etc.
Fast-Flo lactose (early 1970s)
●Spherical aggregates of microcrystals lactose monohydrate
●Much more compressible
●Non hygroscopic
●Tablets are three to four times harder than regular spray dried

12. SuperTab® 11SD
SuperTab® 11SD is a DFE Pharma key range product.
Lactose monohydrate - SuperTab® 11SD (EU)
• Complies with the latest editions of USP-NF, Ph. Eur & JP.
• Production location: DMV-Fonterra Excipients GmbH & Co.KG, Nörten
Hardenberg, Germany.
• Standard packaging size: 40 kg HDPE drum with PE inner liner.
• Shelf life: 2 years.
Lactose monohydrate - SuperTab® 11SD (NZ)
• Complies with the latest editions of USP-NF, Ph. Eur &JP.
• Production location: Fonterra Limited, Kapuni, New Zealand.
• Standard packaging size: 30 kg carton box with PE inner liner.
• Shelf life: 2 years.

13. What is Lactose Monohydrate?
Lactose (C12H22O11) is milk sugar. It is a disaccharide
composed of one galactose and one glucose molecule. In the
pharmaceutical industry, lactose is used to help form tablets
because it has excellent compressibility properties. It is also
used to form a diluents powder for dry-powder inhalations.
Lactose may be listed as lactose hydrous, lactose anhydrous,
lactose monohydrate, or lactose spray-dried.

14. Characteristics of a –Lactose monohydrate
(hydrous)
• Lactose monohydrate is not directly compressible and therefore it is
suitable for use in wet granulation.
• It has poor flow properties and water soluble
• Lactose is odorless and slightly sweet-tasting; a-lactose is approximately
20% as sweet as sucrose
• It produces a hard tablet and the tablet hardness increases on storage,
disintegrant is needed in formulation.
• Drug release rate is usually not affected.
• Occurs discoloration with amines and alkaline materials.
• It contains approximately 5% moisture and hence is a potential source of
instability especially with moisture sensitive drugs.
• Trade name: Pharmatose and Respitose®

15. Pharmatose® 90M
Lactose monohydrate:
• Complies with the latest editions of USP-NF, Ph. Eur & JP.
• Production location: Friesland Campina DMV BV, Veghel, The
Netherlands.
• Standard packaging size: 25 kg paper bag with PE inner liner.
• Shelf life: 3 years.

16. Anhydrous Lactose
A solution of lactose is rapidly dried at high temperature to form
anhydrous lactose which is then milled and sieved to the required
particle size distribution. Anhydrous lactose offers the best
compact ability of all grades of lactose, and it is well suited to
direct compression applications. Anhydrous lactose is also well
suited for formulations containing moisture sensitive drugs, due
to the absence of crystal water. It is the recommended form of
lactose for dry granulation because its brittle nature allows re-
compaction without loss of tablet ability. DFE Pharma offers
anhydrous lactose under the brand names Lacto
press® Anhydrous and Super Tab® AN. The specialty range
products offer a selection of particle size distributions for
improved flow or low dusting.

17. Characteristics of Lactose anhydrous
• Lactose anhydrous is a directly compressible diluents.
• It does not exhibit free flowing property.
• It can pick up moisture at elevated humidity as a result of which
changes in tablet dimensions may occur.
• Anhydrous lactose can be used with moisture-sensitive drugs due to
its low moisture content.
• Anhydrous lactose typically contains 70–80% anhydrous b-lactose
and 20–30% anhydrous a-lactose.
• It is inexpensive.
• Trade name : Pharmatose® DCL 21, Super Tab 21AN

18. Super Tab® 21AN
Super Tab® 21AN is a DFE Pharma key range product.
1.Complies with the latest editions of USP-NF, Ph. Eur. & JP.
2.Production location: DMV-Fonterra Excipients GmbH & Co.KG,
Nörten Hardenberg, Germany.
3.Standard packaging size: 50 kg HDPE drum with PE inner liner.
4.Shelf life: 2 years.
Anhydrous lactose