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EMCOMPRESSEMCOMPRESS CaHPO * 2 H O

CaHPO4 2

4ANHYDROUS EMCOMPRESS

The ideal flow enhancer from a mineral source.

A fil ler for wet gran ula tion and dire ct comp ress ion.

Great synergistic effect when used in combination

with Microcrystalline Cellulose.

Application in Pharmaceutical Formulations

Both and are used in

solid dosage forms to enhance flow, as a tablet binder or as a capsule

diluent. As a binder, it is used because of its excellent flow properties

and deformation characteristic.

Calciumhydrogenphosphate (Dibasic Calcium Phosphate, DCP),

deforms by brittle fracture during compression.

particles fragment into smaller particles exposing less lubricant

surfaces for improved tablet binding. Hence, Magnesium Stearate has

almost no affect on the hardness and dissolution times of

EMCOMPRESS ANHYDROUS EMCOMPRESS

EMCOMPRESS

EMCOMPRESS

EMCOMPRESS

EMCOMPRESS

EMCOMPRESS

EMCOMPRESS

EMCOMPRESS

,

tablets. Additionally as a consequence of this

behaviour, there are no capping problems in tablets made with

Calciumhydrogenphosphate are reduced. Another

benefit, due to its compaction mechanism, is its reduced sensitivity

to tableting speed. Also, and lactose possess similar

galenic properties; therefore, can be used in place of

lactose during formulation development. is typically

applied in direct compression and is used as a calcium and phospho-

rous source in nutritional supplements.

Issue I/2006

Content page

Appli cations .........................................1

Chemical Nomenclature.........................1

Reg ulatory .............................................1

How does Improve Tablet

Matrices in a Blend with Microcrystalline

Cellulose ? ............................................2

in Combination with a

Swelling Superdisintegrant.....................2

Flo wability .............................................2

Typical Use Level 2

Typical Formulations ......3

Differences between and

..................4Partic le size ...........................................4

Bi nding properties .................................4

Crystal Structure and Application............4

Literature about ............4

Inc ompatibili ties ....................................4

....................................

EMCOMPRESS

EMCOMPRESS

EMCOMPRESSEMCOMPRESS

ANHY DROU S EMCOMPRE SS

EMCOMPRESS

EMCOMPRESS is listed in the Ph.Eur. and USP/NF.

E Classification E 341.

Regulatory:

Chemical Nomenclature:

TechnicalNewsletterTechnicalNewsletter

ANHYDROUS EMCOMPRESS

Calcium Hydrogen Phosphate

Anhydrous Dibasic Calcium Phosphate

Calcium Monohydrogen Phosphate

Dicalcium Orthophosphate Dihydrate

CaHPO

136.1

7757-93-9

4

EMCOMPRESS

Calcium Hydrogen Phosphate Dihydrate

Dibasic Calcium Phosphate Dihydrate

Calcium Monohydrogen Phosphate Dihydrate

Dicalcium Orthophosphate Dihydrate

CaHPO * 2 H O

172.1

7789-77-7

4 2

Chemical name

Synonyms

Formula

Molecular weight

CAS Registry Number

Chemical Nomenclature:

Table 1

Page 1

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EMCOMPRESS

particles(brittle fracture)

A swel ling superdisint egrant requ ires some resi stan ce in the tab-

l et m at ri x t o d eve lo p i ts f ul l d is in te gr at in g f or ce. ,

because it is insoluble and non-elastic, provides such resistance.

Soluble materials, such as lactose, do not offer such resistance

and, consequently, disintegrate much slower.

EMCOMPRESS

Fig. 2 : The swelling disintegrant (blue) deforms a plastic particle (brown) butd is in te gr at es a n on -e la st ic p ar ti cl e ( re d) .EMCOMPRESS

EMCOMPRESS

VIVAPUR

EMCOCEL

is often

blended with or

to create a

synergistic combination. The

combination of brittle fracture

and plastic deformation

properties results in flowabi-lity and compaction, which is

greater than the individual

components.

How does Improve Tablet Matricesin a Blend with Microcrystalline Cellulose ?

EMCOMPRESS

EMCOMPRESS in with aSwelling Superdisintegrant

Combination

Applications:

Fig. 1 : Tablet matrix after compressionwith MCC and .EMCOMPRESS

To improv e flow ability, the foll owing rati os have been

demonstrated effective:

VIVAPUR 101 EMCOC EL 50M EMCOMPRESS

VIVAPUR 102 EMCOC EL 90M EMCOMPRESS

or :

4 0 : 6 0

or :

5 0 : 5 0

To improv e compa ctio n, the foll owing rati o has been

demonstrated effective:

VIVAPUR 101 VIVAPUR 102 EMCOMPRESS

EMCOCEL 50M EMCOCEL 90M EMCOMPRESS

or :

or :

7 5 : 25

Typical Use Level

In combination with Microcrystalline Cellulose,

use levels depend on Microcrystalline Cellulose grade and total

formulation composition.

EMCOMPRESS

Flowability

EMCOMPRESS is widely used in formulations due to its excellent

flow properties. Angle of repose is one method used to compare

flow properties of different materials.

Angle of repos e

< 33

33 - 38

38 - 44

>44

Relationship between angle of repose and flow:

Flow

excellent flowability

good flow

problematic

not recommended for direct compression

EMCOMPRESS

ANHYDROU S E MCOMPRESS

31

28

Fast Flow Lactose 31

other Lactose 32 - 35

Sugar 31

Ibuprofen 47

CaCO Powder 50

Corn Starch 56

3

as a Tablet binder: 20 - 70 %

as a Diluent: 10 - 80 %

as a Capsule filler: 10 - 50 %


MCC particles(plastic)

Table 2

Table 3

Table 4

Table 5

Table 6

Page 2

disintegrantwater-solublelactose

EMCOMPRESS

(CalciumHydrogenPhosphateDihydrate)

swelling

Dissolve remove

Issue I/2006

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Typical Formulations:EMCOMPRESS

The proposal below is

. gives the non-water soluble, non-elastic

part of the matrix, which in combination with disintegrants reduces

the disintegration time significantly.

EMCOMPRESS a tablet matrix for fast disintegrating

tablets

VIVAPUR / EMCOC EL

EMCOMPRESS

EXPLOTAB / VIVASTAR

PRUV

Microcrystalline Cellulose (Binder) 65.0 %

CaHPO * 2 H 0 (Filler) 33.0 %

Sodium Starch Glycolate (Superdisintegrant) 1.5 %

Sodium Stearyl Fumarate (Lubricant) 0.5 %

4 2

By using (Sodium Stearyl Fumarate), instead of Magnesium

Stearate as a lubricant, the resulting matrix is more hydrophyllic. In

a matrix with , water can penetrate faster than into a

lipophyllic matrix. In combination with , a water-

insoluble, non-elastic material, the disintegration time improves

significantly.

This is a

. improves the flow

and (Microcrystalline Cellulose) provides the hardness.

PRUV

PRUV

EMCOMPRESS

EMCOMPRESS

VIVAPUR

typical combination of Microcrystalline Cellulose and

Calciumhydrogenphosphate

As co rb ic ac id 55 .0 %

( Mi cr ocr yst all ine C ell ulo se) 20 .0 %

(CaHPO * 2 H O) 22.0 %

(Croscarmellose Sodium) 2.0 %

Colloidal Silicone Dioxid 0.5 %

Magnesium Stearate 0.5 %

Results:

Diameter 13 mm

Height 4 mm

Weig ht 80 0 mg

Compression Force 26 kN

Hardness 7 kp

Disintegration time 16 sec

VI VAPU R 10 2

EMCOMPRESS

VI VASO L

4 2

An exam ple of subs tance in comb inat ion with

Microcrystalline Cellulose and :EMCOMPRESS a low dose active

The acti ve ingr edie nt, bind ers and disinte grants were mixed for 15

minutes in a Turbula mixer. The sieved blend of Magnesium

Stearate and Colloidal Silicone Dioxide was added and mixed for

another 5 minutes. The powder was directly compressed on a

Korsch EK0 tablet press.

Dissolution profile:

Diclofenac 10.0 mg

( Mic ro cr yst al lin e C el lul os e) 31 .3 m g

(CaHPO * 2 H 0) 77.2 mg

(Sodium Starch Glycolate) 5.3 mg

Colloidal Silicone Dioxid 0.6 mg

Magnesium Stearate 0.6 mg

Results:

7 mm

125 mg

6.8 kp

0.4 %

Disintegration time 103 sec

VIVAPUR 102

EMCOMPRESS

VIVASTAR

4 2

Diameter

Weight

Hardness

Friability

0 80

100

80

60

40

20

0

10 20 30 40 50 60 70

Diclofenac

Tabletdisso

lve

d(%)

time (min)


Table 7

Table 8

Fig. 3

Table 9

Page 3

Issue I/2006


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Literature about EMCOMPRESS :

Schmidt , P.C., Her zog, R.,

(3), 105 and 116 (1993)

Carstensen, J.T., Ertell,C.

Drug Dev. (7), 1121 (1990)

Pharm.World Sci. 15

Ind.Pharm. 16

Disclaimer:

The information provided in this brochure is based on thorough research and is believed

to be completely reliable. Application suggestions are given to assist our customers, but

are for guidance only. Circumstances in which our material is used vary and are beyond

our control. Therefore, we cannot assume any responsibility for risks or liabilities, which

may result from the use of this technical advice.

Differences Betweenand

EMCOMPRESSANHYDROUS EMCOMPRESS

Fig. 4: Magnification: 200xSEM ofEMCOMPRESS

Fig. 5: Magnification: 200xSEM ofANHYDROUSEMCOMPRESS

Both materials have a median particle size ranging from 130 m

to 150 m. As illustrated by the SEMs lower case.Both materials

exhibit excellent crystallinity. Monoclinic crystal habit

EMCOMPRESS Triclinic crystal habit


Fig. 7:

Fig. 6: Compaction force vs. tensile strength.Formulation: (99 % Calciumhydrogenphosphate + 1 % MagnesiumStearate).

As can be seen, is sligh tly more compr essi blethan

ANHYDR OUS EMCOM PRESSEMCOMPRESS

AC

B

A

C

B

Tensile Strength as a Funct ion of Compa ctio n force

Particle Size

Binding Properties

0 20.0

2.5

2.0

1.5

1.0

0.5

0

2.5 5.0 7.5 10 12.5 15 17.5


EMCOMPRESS

Tens

ile

Stre

ng

th(MPA)

Compaction Force (kN)

EMCOMPRESS ANHYDROUS EMCOMPRESS

ANHYDROUS

EMCOMPRESS

is denser, while

possesses a higher specific surface area. As a result,

produces harder compacts at equivalent forces.

Crystal Structure and Application



, which has no water, of crystalization is

less sensitive to interactions with gelatine capsules. Because of is

excellent flow, is an ideal flow enhancer

for capsule filling.

TechnicalNewsletterTechnicalNewsletterPage 4

WORLDWIDE HEADQUARTERS USA+Canada

JRS PHARMA GMBH+CO.KG JRS PHARMA LP, USA

JRS PHARMALEADINGTHE WORLDIN EXCIPIENTSA Member of the JRS Group

2981 Route 22, Suite 1Patterson, NY 12563-2359

Toll-Fr ee: (800 ) 431- 2457Phone: (845) 878-3414F ax: (84 5) 8 78 -3 48 4E-mail: [email protected], www.jrs.de

Holzmhle 1D-73494 Rosenberg (Germany)Phone: + 49 (0) 79 67 / 1 52-0Fax: + 49 (0) 79 67 / 1 52-345E-mail: [email protected],www.jrs.de

Customer Service:Customer Service: ++49 (0) 7967 / 152-312 (845) 878 3414

Incompatibilities :

Calciumhydrogenphosphate is incompatible with tetra-cyclineantibiotics and indomethacin. Due to its alkaline nature

Calciumhydrogenphosphate should also not be used with active

ingredients that are sensitive to a pH of 7.3 or above.

Issue I/2006

E-Version, Stand: 08.12.2005

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