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Displacing and change of materials in order to simplify component functions in one only excipient for a sugar coated tablet

IP.com Disclosure Number: IPCOM000182430D
Publication Date: 2009-Apr-30
Document File: 6 page(s) / 36K

Publishing Venue

The IP.com Prior Art Database

Abstract

This article shows the composition changes in a granulate undergoing tableting for different compositions. By all the investigated changes it is possible to obtain the same in vitro performance by dissolution test, without using the same quali-quantitative composition of originary formula.

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Page 1 of 6

Fig 1 - Exemestane 25 mg Coated tablets vs Aromasin DISSOLUTION TEST

Dissolution test of three different

Aromasin batches

120

100

80

% dissolved

60

40

20

batch H627A batch G757A batch H116B

0

0 10 20 30 40

elapsed time (min)

Dissolution test of A, B and C compositions

120

100

80

% dissolved

60

40

A

B

C

20

0

0 10 20 30 40 elapsed time (min)

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Equipment list

High shear mixer granulator Roto P50 - Zanchetta
Vented oven Mandelli static oven
Oscillating granulator Erweka with 0.6 mm and 1.00 mm nets opening 30 liters Biconical mixer Cosmec
Rotary press Ronchi PA20
High shear homogenizer Ultra Turrax
Coating pan GS T10
Spraying System Schlick nozzle
Stainless steel containers
Stirrers

Table 2 - Exemestane tablet controls and Dissolution results

Exemestane 25 mg

Tablet
characteristics COMPOSITION

A

COMPOSITION B

COMPOSITION C

Weight (mg) 62.9 ± 3.6 62.4 ± 0.9 61.9 ± 2.3

Thickness (mm) 3.440 ± 0.024 3.437 ± 0.021 3.425 ± 0.019

Hardness (kp) 5.20 ± 0.60 5.40 ± 0.40 5.10 ± 0.90

Friability (%) 0.488 0.240 0.243

5. CONCLUSIONS

By all the investigated changes, like shown by dissolution tests reported in Fig 1, it is possible to obtain the same performance of Exemestane to the dissolution media without using the same quali-quantitative composition of Aromasin®.

Page 3 of 6

3.3 Changes in the seal coating

Being the size of the batches very small and the deposition of this protective coating onto the cores much efficient, halved quantities have been evaluated as enough to prevent disintegration of core surface in the next sugar coating step.

Testing of a reduced amount of this layer and different compositions

COMPOSITION A: halved amounts of this layer
Components mg/tab mg/tab Function Hypromellose E5 GRADE 1.810 0.900 coating agent Simeticon emulsion 0.009 0.05 antifoam Polyethylenglycol 0.181 0.090 plasticizer Sucrose 1.000 0.5 filler

COMPOSITION B: Reintroduction of Crospovidone instead of Polyethilenglycol Components mg/tab mg/tab Function Hypromellose E5 GRADE 1.810 0.900 coating agent Simeticon emulsion 0.009 0.05 antifoam Polyethylenglycol 0.181 0.090 plasticizer Sucrose 1.000 0.5 filler Crospovidone 2.125 water penetration enhancer

COMPOSITION C: halved amounts of this layer with a different Methocel grade Components mg/tab mg/tab Function Hypromellose E3 GRADE 1.810 0.900 coating agent Simeticon emulsion 0.009 0.05 antifoam Polyethylenglycol 0.181 0.090 plasticizer Sucrose 1.000 0.5 filler

4. MANUFACTURING METHOD FOR 100.000 SUGAR COATED TABLETS

The process consists of wet granulation, where the binder is hypromellose (Methocel
E5) added with polysorbate (Tween 80) to a mixture of Exemestane, mannitol and crospovidone into the high shear mixer. The binding solution was added trickling it
into the powder bed under stirring and then the mass was kneaded for few minutes.

The product, discharged from the high shear mixer (HSM) and distributed on trays,
was dried in a vented oven at 55°C. The d...