BASF_SR30D配方介绍
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Generic Drug Formulations
with
Kollicoat® SR 30 D
and
Kollidon® SRGeneric Drug Formulations with Kollicoat® SR 30 D and Kollidon® SR
Page2/51 MEF/EP076
ContentsContents
I. Kollicoat® SR 30 DCoating
1.1 Theophylline sustained-release pellets
1.2 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 Propranolol HCl sustained-release pellets
(drug-layering process)
3.2.1 Propranolol HCl pellet-releasing tablet
4. Acetaminophen – taste masked
5. Ibuprofen sustained-release pellets
(drug-layering process)
6. Ambroxol HCl sustained-release pellets
(drug-layering process)
6.1 Ambroxol HCl pellet-releasing tablet
7. Tramadol HCl sustained-release pellets
(drug-layering process)
8. Acetylsalicylic acid crystalsGeneric Drug Formulations with Kollicoat® SR 30 D and Kollidon® SR
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ContentsGranulation
9. Propranolol HCl sustained-release tablet
10. Theophylline sustained-release tablet
11. Carbamazepine sustained-release tabletGeneric Drug Formulations with Kollicoat® SR 30 D and Kollidon® SR
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ContentsII. Kollidon® SR
12. Metoprolol tartrate sustained-release tablet
13. Propranolol HCl 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
18. Carbamazepine 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
23. Theophylline sustained-release tabletGeneric Drug Formulations with Kollicoat® SR 30 D and Kollidon® SR
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Caffeine sustained-release pellets®Generic Drug Formulations with Kollicoat® SR 30 D and Kollidon® SR
Page6/51
Caffeine sustained-release pellets1.1 Theophylline sustained-release pellets
a) Formulation
The formulation is designed for 500g of pure theophylline pellets (Spherofillin [1];
diameter 0.8-1.3mm)
Polymer suspensionKollicoat® SR 30 D [1]223.67g
Propylene glycol [1]6.71g
Water149.86g
Pigment suspensionKollidon® 30 [1]2.24g
Titanium dioxide [2]2.24g
Sicovit® Red 30 [1]2.24g
Talc [3]15.66g
Water44.73g
b) Preparation of the spray suspension
Polymer suspensionAdd propylene glycol followed by Kollicoat® SR
30 D to the given quantity of water with stirring.
Pigment suspensionDissolve 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 suspensionIncorporate the pigment suspension into the
polymer suspension with stirring. The suspension
must be stirred during the spraying process to
prevent settling.Generic Drug Formulations with Kollicoat® SR 30 D and Kollidon® SR
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Caffeine sustained-release pelletsc) 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 parametersInlet air temperature60°C
Outlet air temperature37°C
Product temperature38°C
Air flow80m³/h
Nozzle diameter0.8mm
Spraying rateapprox. 11.5g/min
Spraying time39 min
Atomizing pressure1.0bar
Drying45°C/ 5min
Coating weight2mg 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.
020406080100120
04812162024
time [h]drug release [%]
0.5 mg Kollicoat SR 30 D/cm² 1.0 mg Kollicoat SR 30 D/cm² 2.0 mg Kollicoat SR 30 D/cm² method: paddle 50 rpm; 37°C0-2h: 0.08 M HCl2-24h: phosphate buffer pH 6.8Generic Drug Formulations with Kollicoat® SR 30 D and Kollidon® SR
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Caffeine sustained-release pellets1.2 Theophylline sustained-release pellets
(drug-layering process)
a) Formulation
The formulation is designed for 800g of pellets manufactured by drug layering of
nonpareilles.
Polymer suspensionKollicoat® SR 30 D [1]533.0g
Triethyl citrate (TEC) [4]16.0g
Water433.0g
Pigment suspensionTalc [3]56.0g
Water100.0g
b) Preparation of the spray suspension
Polymer suspensionAdd TEC followed by Kollicoat® SR 30 D to the
given quantity of water with stirring.
Pigment suspensionAdd talc to the given quantity of water with
vigorous stirring.
Spray suspensionIncorporate the pigment suspension into the
polymer suspension with stirring. The suspension
must be stirred during the spraying process to
prevent settling.
