Generic Drug Formulations With Kollicoat SR 30 D and Kollidon SR

Generic Drug Formulations
with
Kollicoat® SR 30 D
and
Kollidon® SR
® ®
Generic Drug Formulations with Kollicoat SR 30 D and Kollidon SR
Contents
I. Kollicoat® SR 30 D
Coating
1.1 Theophylline sustained-release pellets

(drug-layering process)
2. Caffeine sustained-release pellets
(extrusion process)
3.1 Propranolol HCl sustained-release pellets
(extrusion process)
3.2.1 Propranolol HCl pellet-releasing tablet
4. Acetaminophen – taste masked
5. Ibuprofen sustained-release pellets
6. Ambroxol HCl sustained-release pellets
6.1 Ambroxol HCl pellet-releasing tablet
7. Tramadol HCl sustained-release pellets
8. Acetylsalicylic acid crystals
Page2/51 MEF/EP076 Contents

® ®
Granulation
9. Propranolol HCl sustained-release tablet
10. Theophylline sustained-release tablet
11. Carbamazepine sustained-release tablet

® ®
II. Kollidon® SR
12. Metoprolol tartrate sustained-release tablet

14. Caffeine sustained-release tablet
15. Diclofenac Na sustained-release tablet
16. Ascorbic acid sustained-release tablet
17. Indometacin sustained-release tablet
19. Nifedipine sustained-release tablet
20. Tramadol HCl sustained-release tablet
21. Diltiazem HCl sustained-release tablet
22. Naphtidrofuryl oxalate sustained-release
tablet

® ®
Page5/51 Caffeine sustained-release pellets

® ®
a) Formulation
The formulation is designed for 500g of pure theophylline pellets (Spherofillin [1];
diameter 0.8-1.3mm)
Polymer suspension Kollicoat® SR 30 D [1] 223.67g

Propylene glycol [1] 6.71g
Water 149.86g
Pigment suspension Kollidon® 30 [1] 2.24g

Titanium dioxide [2] 2.24g
Sicovit® Red 30 [1] 2.24g
Talc [3] 15.66g
Water 44.73g
b) Preparation of the spray suspension
Polymer suspension Add propylene glycol followed by Kollicoat® SR

30 D to the given quantity of water with stirring.
Pigment suspension Dissolve Kollidon® 30 in the given quantity of

water. Add Sicovit® Red 30, titanium dioxide and
talc with vigorous stirring and homogenize the
mixture in a corundum disk mill.
Spray suspension Incorporate the pigment suspension into the

polymer suspension with stirring. The suspension
must be stirred during the spraying process to
prevent settling.

® ®
c) Coating
The pellets were coated in an Aeromatic Strea-1 (Aeromatic AG). The suspension
was sprayed continuously onto the fluidized, pre-heated pellets from the top.
Process parameters Inlet air temperature 60°C

Outlet air temperature 37°C
Product temperature 38°C
Air flow 80m³/h
Nozzle diameter 0.8mm
Spraying rate approx. 11.5g/min
Spraying time 39 min
Atomizing pressure 1.0bar
Drying 45°C/ 5min
Coating weight 2mg film former/cm²
The coating weight of 2mg film former / cm² given here was determined from the
surface area of the pellets. Since the particle size distribution and surface structure
influence the polymer quantity required, calculating the surface area is recommended
as a means of estimating the required coating weight in each specific case.
120
method: paddle 50 rpm; 37°C
0-2h: 0.08 M HCl
2-24h: phosphate buffer pH 6.8
100
80
drug release [%]
60
40
20
0.5 mg Kollicoat SR 30 D/cm²
0
0 4 8 12 16 20 24
time [h]

® ®

a) Formulation
The formulation is designed for 800g of pellets manufactured by drug layering of

nonpareilles.

Triethyl citrate (TEC) [4] 16.0g
Water 433.0g
Pigment suspension Talc [3] 56.0g

Water 100.0g
Polymer suspension Add TEC followed by Kollicoat® SR 30 D to the

given quantity of water with stirring.
Pigment suspension Add talc to the given quantity of water with

vigorous stirring.

prevent settling.

® ®
c) Coating
The pellets were coated in an GPCG1 (Glatt). The suspension was sprayed
continuously onto the fluidized, pre-heated pellets by the Wurster method.
Process parameters Machine Glatt GPCG1

Method Bottom-spray (Wurster)
Inlet air temperature 50-55°C
Outlet air temperature 29-32°C
Product temperature 35-40°C
Air flow 90m³/h
Spraying rate approx. 4.5 g/min
Drying 40°C/ 15min
Coating weight 20%
100

0-20h: pH 7.4
80
drug release [%]
60
40
20
0
0 4 8 12 16 20
time [h]

® ®
2. Caffeine sustained-release pellets
a) Formulation
The formulation is designed for 500g of pellets (composition of pellets: 10% caffeine
[1], 43.75% Avicel® PH 101 [5], 43.75% lactose [6], 2.5% Kollidon® VA 64 [1];
diameter 0.7-1.4mm; made by wet extrusion).

Water 188.61g
Pigment suspension Kollidon® 30 [1] 2.7g

Titanium dioxide [2] 2.7g
Sicovit® Red 30 [1] 2.7g
Talc [3] 18.87g
Water 53.89g
Polymer suspension Add propylene glycol followed by Kollicoat® SR 30 D

to the given quantity of water with stirring.
Pigment suspension Dissolve Kollidon® 30 in the given quantity of water.

Add Sicovit® Red 30, titanium dioxide and talc with
vigorous stirring and homogenize the mixture in a
corundum disk mill.
Spray suspension Incorporate the pigment suspension into the polymer

suspension with stirring. The suspension must be
stirred during the spraying process to prevent settling.

® ®
c) Coating

Air flow 80m³/h
Spraying rate approx. 12g/min
Drying 45°C/ 5min
The coating weight of 3mg film former / cm² given here was established for the
pellets by surface area determination. Since the particle size distribution and surface
structure influence the required polymer quantity, calculating the surface area is
recommended as a means of estimating the required coating weight in each specific
case.
100
0-2h: 0.08 M HCl
80
drug release [%]
60
40
20
0
0 4 8 12 16 20 24
time [h]

® ®

(extrusion process)
a) Formulation
The formulation is designed for 500g of pellets (composition of pellets: 20%

propranolol HCl [1], 51.66% Avicel® PH 101 [5], 25.84% lactose [6], 2.5% Kollidon®
VA 64 [1]; diameter 0.4-1.5mm; made by wet extrusion).)

Water 174.59g
Talc suspension Talc [3] 29.94g

Water 44.91g
Polymer suspension Add propylene glycol followed by Kollicoat® SR

30 D to the given quantity of water with stirring.
Talc suspension Add talc with vigorous stirring and homogenize

the mixture in a corundum disk mill.
Spray suspension Incorporate the talc suspension into the polymer

suspension with stirring. The suspension must be
stirred during the spraying process to prevent
settling.
Page12/51 Acetminophen – taste masked

® ®
c) Coating

Air flow 80m³/h
Drying 45°C/ 5min
The coating weight of 3mg film former / cm² given here was established for the
pellets by surface area determination. Since the particle size distribution and surface
structure influence the required polymer quantity, calculating the surface area is
recommended as a means of estimating the required coating weight in each specific
case.
100
0-2h: 0.08 M HCl
80
drug release [%]
60
40
20
0
0 4 8 12 16 20
time [h]

® ®

a) Formulation

nonpareilles.

Water 433.0g

Water 100.0g


vigorous stirring.

prevent settling.

® ®
c) Coating
The pellets were coated in a Glatt GPCG1 coater. The suspension was sprayed
continuously onto the fluidized, pre-heated pellets from the bottom by the Wurster
method. Weight gains of 5, 10, 15 and 20% were tested.

Air flow 90m³/h
Drying 40°C/ 15min
Coating weight 20%
100
0-20h: 0.1M HCl
80
drug release [%]
60
40
20
5% Kollicoat SR 30 D
0
0 4 8 12 16 20
time [h]

® ®
3.2.1 Propranolol HCl pellet-releasing tablet

a) Formulation
The formulation is designed for 500g of tablets:
Propranolol HCl/ Kollicoat® SR pellets 250.0g

Microcrystalline cellulose (Vivapur® 200) [7] 250.0g
Magnesium stearate [8] 2.5g
b) Procedure
Mix the ingredients together, pass through a 0.8mm sieve and compress into tablets
with a force of about 15kN.
Tablet press Korsch EK0, 30 tablets/ min

Compression force 15kN
c) Tablet properties
Weight 400mg
Diameter 10mm
Form biplanar
Hardness 82-112N
100

coating level: 20%
0-20h: 0.1M HCl
80
drug release [%]
60
40
20
Tablets 850 - 1000 µm
Tablets 710 - 850 µm
Pellets 850 - 1000 µm
Pellets 710 - 850 µm
0
0 4 8 12 16 20
time [h]

® ®
4. Acetaminophen - taste masked
a) Formulation
The formulation is designed for 500g of acetaminophen granules [1].
The dispersion is used directly without any additives.
c) Coating
The crystals were coated in an Aeromatic Strea-1 (Aeromatic AG). The dispersion
was sprayed continuously onto the fluidized, pre-heated crystals from the top.

Air flow 80m³/h
Spraying time 9 min
Drying 45°C/ 5min
Coating weight 4%
Crystalline acetaminophen is coated with 4% Kollicoat® SR 30 D.

® ®
100
80
drug release [%]
60
40
20
0.1N HCl
phosphate buffer pH 6.8
0
0 15 30 45 60
time [min]

® ®
5. Ibuprofen sustained-release pellets


nonpareilles.
a) Subcoating
The polymer spray solution for a weight gain of 5%:
Spray solution Mowiol® 4-88 (PVA) [9] 48.0g

Water 432.0g
b) Preparation of the spray solution (subcoating)
Dissolve Mowiol in hot water and cool with stirring.

Inlet air temperature 50°C
Air flow 80m³/h
Spraying rate approx. 3.1g/min
Drying 40°C/ 15min
Subcoating weight 5%
c) Polymer coating
The formulation is designed for 800g of subcoated pellets.

Water 433.0g

Water 100.0g
Page19/51 Ibuprofen sustained-release pellets

® ®
d) Preparation of the spray suspension (polymer coating):


vigorous stirring.

prevent settling.

Air flow 90m³/h
Drying 40°C/ 15min
Spray the suspension continuously onto fluidized pre-heated pellets by the wurster
spray method. Weight gains 5, 10, 15 and 20%.
100

0-20h: pH 7.4
80
drug release [%]
60
40
20
5% Kollicoat SR 30D
10% Kollicoat SR 30D
0
0 4 8 12 16 20
time [h]
Page20/51 Ibuprofen sustained-release pellets

® ®
6. Ambroxol HCl sustained-release pellets

nonpareilles.
a) Formulation

Water 433.0g

Water 100.0g


vigorous stirring.

prevent settling.
c) Coating
Page21/51 Ambroxol HCl sustained-release pellets

® ®

Air flow 90m³/h
Drying 40°C/ 15min
Weight gain 20%
100

0-20h: pH 7.4
80
drug release [%]
60
40
20
5% Kollicoat SR 30D
0
0 4 8 12 16 20
time [h]

® ®
6.1 Ambroxol HCl pellet-releasing tablet
d) Formulation
The formulation is designed for 500g of tablets:
Ambroxol HCl/ Kollicoat® SR pellets 250.0g

Microcrystalline cellulose (Vivapur® 200) [7] 250.0g
Magnesium stearate [8] 2.5g
e) Procedure

Compression force 15kN
f) Tablet properties
Weight 400mg
Diameter 10mm
Form biplanar
Hardness 92-116N
100

0-20h: pH 7.4
80
drug release [%]
60
40
20
5% Kollicoat SR 30D
0
0 4 8 12 16 20
time [h]

® ®
7. Tramadol HCl sustained-release pellets

a) Polymer coating

nonpareilles.

Water 433.0g

Water 100.0g


vigorous stirring.

prevent settling.
c) Coating
Page24/51 Tramadol HCl sustained-release pellets

® ®

Air flow 90m³/h
Drying 40°C/ 15min
Weight gain 20%
100

0-20h: pH 7.4
80
drug release [%]
60
40
20
tablets, 15% Kollicoat SR 30 D
tablets, 20% Kollicoat SR 30 D
pellets, 15% Kollicoat SR 30 D
pellets, 20% Kollicoat SR 30 D
0
0 4 8 12 16 20
time [h]
Page25/51 Tramadol HCl sustained-release pellets

® ®
8. Acetylsalicylic acid crystals

a) Formulation
The formulation is designed for 800g of acetylicsalicylic acid crystals [12].
Spray suspension Kollicoat® SR 30 D [1] 666.25g

Talc [3] 70.00g
Water 666.25g
Add talk to the given amount of water with vigorous stirring.

Then add Kollicoat SR 30 D with slow stirring.
c) Coating
The crystals were coated in a Glatt GPCG1 coater. The suspension was sprayed
continously onto the fluidized, pre-heated crystals by the Wurster method. Weight
gains of 5, 10, 15 and 20% were tested.

Air flow 90m³/h
Drying 40°C/ 15min
Coating weight 20%
Page26/51 Acetylsalicylic acid crystals

® ®
120
100
0-20h: pH 7.4
no plasticizer
80
drug release [%]
60
40
crystals
20 15% Kollicoat SR 30D
0
0 4 8 12 16 20
time [h]
Page27/51 Acetylsalicylic acid crystals

® ®
®
Page28/51 Kollicoat SR 30 D - Granulation
® ®

a) Formulation of the granules
Propranolol HCl Powder 80 [1] 250.0g

Granulac® 140 (lactose) [6] 100.0g
Kollicoat® SR 30 D [1] 525.0g
b) Manufacture of the granules
The active ingredient and excipient were granulated in an Aeromatic Strea-1

(Aeromatic AG). The polymer dispersion was sprayed into the fluid bed from the top.

Outlet air temperature 22 – 27°C
c) Formulation of the tablets
Propranolol HCl powder 80 [1] 160.0mg

Kollicoat® SR 30 D [1] 96.0mg
Granulac® 140 [6] 64.0mg
Aerosil® 200 [13] 1.6mg
Magnesium stearate [8] 1.6mg
d) Tableting
The granules were passed together with magnesium stearate (0.5%) and Aerosil®
200 (0.5%) through an 800µm sieve, blended for 10 min in a Turbula mixer and
compressed into tablets with a force of about 18kN.

Compression force 17.7kN
Page29/51 Propranolol HCl sustained-release tablet

® ®
e) Tablet properties
Weight 323.0mg
Diameter 10mm
Form biplanar
Hardness 260N
100
0-2h: 0.08 M HCl
80
drug release [%]
60
40
20
0
0 4 8 12 16 20
time [h]

® ®
Theophylline powder [1] 250.0g

Granulac® 140 [6] 212.5g
The active ingredient and excipient was granulated in an Aeromatic Strea-1


Theophylline pdr [1] 400.0mg

Aerosil® 200 [13] 4.0mg
d) Tableting
Tablet press Korsch PH 106, 30 rpm

Page31/51 Theophylline sustained-release tablet

® ®
Weight 808.0mg
Diameter football shape 19.0x8.5mm
Hardness 276N
100
0-2h: 0.08 M HCl
80
drug release [%]
60
40
20
0
0 2 4 6 8 10 12 14 16 18 20 22 24
time [h]

® ®
Carbamazepine [14] 250.0g

Granulac® 140 [6] 185.3g
Kollidon® CL-M [1] 25.3g
The active ingredient and excipients were granulated in an Aeromatic Strea-1


Carbamazepine [14] 200.0mg

Kollidon® CL-M [1] 20.2mg
Aerosil® 200 [13] 2.0mg
d) Tableting

Page33/51 Carbamazepine sustained-release tablet

® ®
Weight 404.0mg
Diameter 11mm
Form biconvex
Hardness 136N
100

0-16h: SDS-solution (1%; water)
80
drug release [%]
60
40
20
0
0 4 8 12 16
time [h]

® ®
Page35/51 Kollidon SR
® ®
12. Metoprolol tartrate sustained-release tablet
Metoprolol tartrate [15] 454.5g

The active ingredient was granulated in an Aeromatic Strea-1 (Aeromatic AG). The
polymer dispersion was sprayed into the fluid bed from the top.

Metoprolol tartrate [15] 200.0mg

Kollicoat® SR 30 D solid polymer 6.0mg
Kollidon® SR [1] 250.0mg
d) Tableting
The granules were passed together with magnesium stearate (0.5%) and Kollidon®
SR (54.5%) through an 800µm sieve, blended for 10 min in a Turbula mixer and

Compression force 9,3kN
Page36/51 Metoprolol tartrate sustained-release tablet

® ®
Weight 458.5mg
Diameter 12mm
Form biplanar
Hardness 220N
120
100
80
60
40
20
0-2h: 0.08 M HCl
0
0 2 4 6 8 10 12
time [h]
Page37/51 Metoprolol tartrate sustained-release tablet

® ®
a) Formulation
Propranolol HCl [1] 160.0mg

Aerosil® 200 [13] 3.4mg
b) Procedure
Mix the ingredients together, pass through a 0.8mm sieve and compress into
tablets with a force of about 10kN.
Tablet press Korsch PH 100/6 30 rpm

Compression force 9,9kN
Weight 325.0mg
Diameter 10mm
Form biplanar
Hardness 172N
100
80
drug release [%]
60
40
20

0-2h: 0.08 M HCl
0
0 2 4 6 8 10 12 14 16
time [h]

® ®
14. Caffeine sustained-release tablet
a) Formulation
Caffeine gran. 0,2/0,5 [1] 160.0mg 160.0mg 160.0mg

Kollidon® SR [1] 160.0mg 120.0mg 80.0mg
Avicel® PH 102 [5] -- 40.0mg 80.0mg
Magnesium stearate [8] 1.6mg 1.6mg 1.6mg
b) Procedure
Tablet press Korsch PH100/6, 30 rpm

Compression force 9.6kN 9.8kN 10.1kN
Weight 322.0mg 322.0mg 322.0mg

Diameter 10mm 10mm 10mm
Form biplanar
Hardness 213N 201N 193N
Friability <0.1% <0.1% <0.1%
100
80
drug release [%]
60
caffeine/ Kollidon SR (160mg/ 80mg)

40 caffeine/ Kollidon SR (160mg/ 120mg)
caffeine/ Kollidon SR (160mg/ 160mg)
20
0-2h: 0.08 M HCl
0
0 2 4 6 8 10 12 14 16 18 20 22 24
time [h]
Page39/51 Caffeine sustained-release tablet

® ®
15. Diclofenac Na sustained-release tablet
a) Formulation
Diclofenac Na [16] 100.0mg 100.0mg

Kollidon® SR [1] 100.0mg 150.0mg
Aerosil® 200 [13] 3.4mg 3.4mg
Magnesium stearate [8] 3.0mg 3.0mg
b) Procedure

Compression force 7.9kN 7.0kN
Weight 206.0mg 256.0mg

Diameter 8mm
Form biplanar
Hardness 195N 229N
Friability <0.1% <0.1%
120
100
80
drug release [%]
60
40
20
diclofenac Na/ Kollidon SR (100mg/ 100mg)
diclofenac Na/ Kollidon SR (100mg/ 150mg)
0
0 2 4 6 8 10 12 14 16
time [h]
Page40/51 Caffeine sustained-release tablet

® ®
16. Ascorbic acid sustained-release tablet
a) Formulation
Ascorbic acid cryst. [1] -- 200.0mg 200.0mg

Ascorbic acid pdr. [1] 200.0mg -- --
Kollidon® SR [1] 200.0mg 200.0mg 280.0mg
Ludipress® LCE [1] 75.0mg 80.0mg --
Aerosil® 200 [13] 5.0mg -- --
Magnesium stearate [8] 9.0mg 9.0mg 9.0mg
b) Procedure

Compression force 17.1kN 20.0kN 18.6kN
Weight 489.0mg 489.0mg 489.0mg

Diameter 12mm
Form biplanar
Hardness 164N 140N 151N
Friability 0.1% 0.1% 0.2%
100
80
drug release [%]
60

(1% cysteine HCl-solution)
40
20
ascorbic acid plv./ K.SR/ L.LCE (200mg/ 200mg/ 75mg)
ascorbic acid cryst./ K.SR/ L.LCE (200mg/ 200mg/ 80mg)
ascorbic acid cryst./ K.SR/ L.LCE (200mg/ 200mg/ 80mg)
0
0 2 4 6 8 10 12 14 16 18 20 22 24
time [h]

® ®
17. Indometacin sustained-release tablet
a) Formulation
Indometacin [12] 75.0mg 75.0mg

Ludipress® LCE [1] 100.0mg --
Aerosil® 200 [13] 1.5mg 4.0mg
b) Procedure


Diameter 10mm
Form biplanar
Hardness 163N 133N
Friability <0.1% 0.1%
100

80
drug release [%]
60
40
20
indometacin/ K.SR (75mg/ 125 mg)
indometacin/ K.SR/L.LCE (75mg/ 125mg/100mg)
0
0 2 4 6 8 10 12 14 16
time [h]

® ®
a) Formulation
Carbamazepine [14] 200.0mg 200.0mg

Ludipress® LCE [1] 200.0mg 150.0mg
Kollidon® CL-M [13] -- 20.0mg
b) Procedure


Diameter 12mm
Form biplanar
Hardness 146N 164N
Friability 0.1% <0.1%
120
0-16h: SDS-solution (1%; water)
100
80
drug release [%]
60
40
20
carbamazepine/ K. SR/ L. LCE (200mg/ 100mg/ 200mg)
carbamazepine/ K. SR/ L. LCE/ K. CL-M (200mg/ 100mg/ 150mg/ 20mg)

0
0 2 4 6 8 10 12 14 16
time [h]

® ®
19. Nifedipine sustained-release tablet
a) Formulation
Nifedipine [17] 20.0mg

Ludipress® LCE [1] 100.0mg
b) Procedure

Weight 221.0mg
Diameter 8mm
Form biplanar
Hardness 193N
Friability <0.1%
100

0-24h: phosphate buffer 6.8/0.5% SDS
80
drug release [%]
60
40
20
0
0 4 8 12 16 20 24
time [h]
Page44/51 Nifedipine sustained-release tablet

® ®
20. Tramadol HCl sustained-release tablet
a) Formulation
Tramadol HCl [11] 100.0mg

Aerosil® 200 [13] 2.5mg
b) Procedure

Weight 254.0mg
Diameter 10mm
Form biplanar
Hardness 211N
Friability <0.1%
100
0-2h: 0.08 M HCl
80
drug release [%]
60
40
20
0
0 2 4 6 8 10 12 14 16
time [h]
Page45/51 Tramadol HCl sustained-release tablet

® ®
21. Diltiazem HCl sustained-release tablet
a) Formulation
Diltiazem HCl [18] 120.0mg

Aerosil® 200 [13] 3.0mg
b) Procedure

Weight 305.0mg
Diameter 10mm
Form biplanar
Hardness 217N
Friability <0.1%
100

0-16h: deionized water
80
drug release [%]
60
40
20
0
0 2 4 6 8 10 12 14 16
time [h]
Page46/51 Diltiazem HCl sustained-release tablet

® ®
22. Naphtidrofuryl oxalate sustained-release tablet
a) Formulation
Naphtidrofuryl oxalate [18] 100.0mg

Talc [3] 25.0mg
Aerosil® 200 [13] 5.4mg
b) Procedure
Tablet press Korsch PH106, 30 rpm

Weight 283.0mg
Diameter 10mm
Form biplanar
Hardness 197N
Friability <0.1%
100
0-2h: 0.08 M HCl
80
60
40
20
0
0 4 8 12 16 20 24
time [h]
Page47/51 Naphtidrofuryl oxalate sustained-release tablet

® ®
a) Formulation
Theophylline pdr. [1] 500.0mg

Ludipress® LCE [1] 225.0mg
b) Procedure
Tablet press Korsch PH 106, 30 rpm

Weight 928.0mg
Diameter 19.0x8.5mm
Form football shape
Hardness 172N
Friability <0.1%
100
0-2h: 0.08 M HCl
80
drug release [%]
60
40
20
0
0 2 4 6 8 10 12 14 16 18 20 22 24
time [h]

® ®
Substances
[1] BASF Aktiengesellschaft Excipients
Carl-Bosch Str. 38 Kollicoat® SR 30 D
67056 Ludwigshafen, Germany Kollidon® 30
Kollidon® CL
Kollidon® CL-M
Kollidon® SR
Kollidon® VA 64
Ludipress® LCE
Propylene glycol
Sicovit® Red 30
Actives
Acetaminophen gran.
Ascorbic acid cryst.
Ascorbic acid powder
Caffeine gran. 0.2/0.5
Ibuprofen
Propranolol HCl powder 80
Theophylline powder
Spherofillin
[2] Kronos Titan GmbH Titanium dioxide

Postfach 100720
51307 Leverkusen, Germany
[3] Riedel-de-Haën AG Talc

Wunstdorferstr. 40
30926 Seelze, Germany
[4] Merck-Schuchardt Triethyl citrate

85662 Hohenbrunn, Germany
[5] FMC Corp. Food + Pharmaceutical Avicel® PH 101

Products Avicel® PH 102
735 Market Street
Philadelphia, PA 19103, USA
[6] Meggle Milchindustrie Granulac® 140

Postfach 40 Granulac® 230
83512 Wasserburg, Germany
[7] J. Rettenmaier & Söhne Vivapur® 200

Holzmühle 1
73494 Rosenberg, Germany
[8] Bärlocher GmbH Magnesium stearate

80992 Munich, Germany
Page49/51 Substances
® ®
[9] Clariant GmbH Mowiol® 4-88 PVA

Division CP/TQM-QP
65926 Frankfurt am Main, Germany
[10] Heumann Pharma GmbH Ambroxol HCl

Postfach 2260
90008 Nuremberg, Germany
[11] Chemagis Ltd. Tramadol HCl

P.O. Box 9091
Tel Aviv 61090, Israel
[12] Synopharm GmbH Acetylicsalicylic acid crystals

Postfach 1205 Indometacin
22882 Barsbüttel, Germany
[13] Degussa-Hüls AG Aerosil® 200

Weissfrauenstr. 9
60287 Frankfurt, Germany
[14] Fabbrica Italiana Sintetici S.p.A. Carbamazepine

Viale Milano, 26
36041 Alte di Montecclio Maggiore,
Italy
[15] Moehs S.A. Metoprolol tartrate

Apartado 59
08191 Rubi, Spain
[16] Irotec Laboratories Diclofenac Na

Little Island, Cork, Ireland
[17] Prosintex Industrie Chimiche Nifedipine

Italiano
Via E. Ferm, 20/26
20019 Seltimo Milanese (Mi), Italy
[18] Farmak a.s. Diltiazem HCl

Na Vlcinci 3 Naphtidrofuryl oxalate
77117 Olomouc, Czech Republic
Page50/51 Substances
® ®
Note
The data submitted in this publication are based on our current knowledge and
experience. They do not constitute a guarantee in the legal sense of the term and, in
view of the mainfold factors that may effect processing and application, do not relieve
processors from the responsibility of carrying out their own tests and experiments.
Any relevant patent rights and existing legislation and regulations must be observed.
BASF Aktiengesellschaft
Unternehmensbereich Fine Chemicals
67056 Ludwigshafen, Germany
Page51/51

Generic Drug Formulations With Kollicoat SR 30 D and Kollidon SR

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Generic Drug Formulations With Kollicoat SR 30 D and Kollidon SR

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Generic Drug Formulations

1.1 Theophylline sustained-release pellets

Page2/51 MEF/EP076 Contents

9. Propranolol HCl sustained-release tablet

10. Theophylline sustained-release tablet

11. Carbamazepine sustained-release tablet

Page3/51 MEF/EP076 Contents

12. Metoprolol tartrate sustained-release tablet

Page4/51 MEF/EP076 Contents

Page5/51 Caffeine sustained-release pellets

1.1 Theophylline sustained-release pellets

Polymer suspension Kollicoat® SR 30 D [1] 223.67g

Pigment suspension Kollidon® 30 [1] 2.24g

b) Preparation of the spray suspension

Polymer suspension Add propylene glycol followed by Kollicoat® SR

Pigment suspension Dissolve Kollidon® 30 in the given quantity of

Spray suspension Incorporate the pigment suspension into the

Page6/51 Caffeine sustained-release pellets

Process parameters Inlet air temperature 60°C

Page7/51 Caffeine sustained-release pellets

1.2 Theophylline sustained-release pellets

The formulation is designed for 800g of pellets manufactured by drug layering of

Polymer suspension Kollicoat® SR 30 D [1] 533.0g

Pigment suspension Talc [3] 56.0g

b) Preparation of the spray suspension

Polymer suspension Add TEC followed by Kollicoat® SR 30 D to the

Pigment suspension Add talc to the given quantity of water with

Spray suspension Incorporate the pigment suspension into the

Page8/51 Caffeine sustained-release pellets

Process parameters Machine Glatt GPCG1

method: paddle 100 rpm; 37°C

Page9/51 Caffeine sustained-release pellets

2. Caffeine sustained-release pellets

Polymer suspension Kollicoat® SR 30 D [1] 269.44g

Pigment suspension Kollidon® 30 [1] 2.7g

b) Preparation of the spray suspension

Polymer suspension Add propylene glycol followed by Kollicoat® SR 30 D

Pigment suspension Dissolve Kollidon® 30 in the given quantity of water.

Spray suspension Incorporate the pigment suspension into the polymer

Page10/51 Caffeine sustained-release pellets

Process parameters Inlet air temperature 60°C

Page11/51 Caffeine sustained-release pellets

3.1 Propranolol HCl sustained-release pellets

The formulation is designed for 500g of pellets (composition of pellets: 20%

Polymer suspension Kollicoat® SR 30 D [1] 249.41g

Talc suspension Talc [3] 29.94g

b) Preparation of the spray suspension

Polymer suspension Add propylene glycol followed by Kollicoat® SR

Talc suspension Add talc with vigorous stirring and homogenize

Spray suspension Incorporate the talc suspension into the polymer

Page12/51 Acetminophen – taste masked

Process parameters Inlet air temperature 60°C

Page13/51 Acetminophen – taste masked

3.2 Propranolol HCl sustained-release pellets

The formulation is designed for 800g of pellets manufactured by drug layering of

Polymer suspension Kollicoat® SR 30 D [1] 533.0g

Pigment suspension Talc [3] 56.0g

b) Preparation of the spray suspension