BASF_SR30D配方介绍

1、 Generic Drug FormulationswithKollicoat SR 30 DandKollidon SRContentsI. Kollicoat SR 30 DCoating1.1 Theophylline sustained-release pellets 1.2 Theophylline sustained-release pellets(drug-layering process2. Caffeine sustained-release pellets(extrusion process3.1 Propranolol HCl sustained-release pell

2、ets(extrusion process3.2 Propranolol HCl sustained-release pellets(drug-layering process3.2.1 Propranolol HCl pellet-releasing tablet4. Acetaminophen taste masked5. Ibuprofen sustained-release pellets(drug-layering process6. Ambroxol HCl sustained-release pellets(drug-layering process6.1 Ambroxol HC

3、l pellet-releasing tablet7. Tramadol HCl sustained-release pellets(drug-layering process8. Acetylsalicylic acid crystalsGranulation9. Propranolol HCl sustained-release tablet10. Theophylline sustained-release tablet11. Carbamazepine sustained-release tabletII. Kollidon SR12. Metoprolol tartrate sust

4、ained-release tablet13. Propranolol HCl sustained-release tablet14. Caffeine sustained-release tablet15. Diclofenac Na sustained-release tablet16. Ascorbic acid sustained-release tablet17. Indometacin sustained-release tablet18. Carbamazepine sustained-release tablet19. Nifedipine sustained-release

5、tablet20. Tramadol HCl sustained-release tablet21. Diltiazem HCl sustained-release tablet22. Naphtidrofuryl oxalate sustained-releasetablet23. Theophylline sustained-release tablet1.1 Theophylline sustained-release pelletsa FormulationWater44.73g b Preparation of the spray suspensionPolymer suspensi

6、on Add propylene glycol followed by Kollicoat SR30 D to the given quantity of water with stirring. Pigment suspension Dissolve Kollidon 30 in the given quantity ofwater. Add Sicovit Red 30, titanium dioxide andtalc with vigorous stirring and homogenize themixture in a corundum disk mill.Spray suspen

7、sion Incorporate the pigment suspension into thepolymer suspension with stirring. The suspensionmust be stirred during the spraying process toprevent settling.c CoatingThe pellets were coated in an Aeromatic Strea-1 (Aeromatic AG. The suspension was sprayed continuously onto the fluidized, pre-heate

8、d pellets from the top. Process parameters Inlet air temperature60COutlet air temperature37CProduct temperature38CAir flow80m/hSpraying time39 minDrying45C/ 5minCoating weight2mg film former/cmThe coating weight of 2mg film former / cm given here was determined from the surface area of the pellets.

9、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. 1.2 Theophylline sustained-release pellets(drug-layering processa FormulationThe

10、 formulation is designed for 800g of pellets manufactured by drug layering of nonpareilles.Water100.0g b Preparation of the spray suspensionPolymer suspension Add TEC followed by Kollicoat SR 30 D to thegiven quantity of water with stirring.Pigment suspension Add talc to the given quantity of water

11、withvigorous stirring.Spray suspension Incorporate the pigment suspension into thepolymer suspension with stirring. The suspensionmust be stirred during the spraying process toprevent settling.c CoatingThe pellets were coated in an GPCG1 (Glatt. The suspension was sprayed continuously onto the fluid

12、ized, pre-heated pellets by the Wurster method.Process parameters Machine Glatt GPCG1Method Bottom-spray (WursterInlet air temperature50-55COutlet air temperature29-32CProduct temperature35-40CAir flow90m/hSpraying time260 minSpraying rate approx. 4.5 g/minDrying40C/ 15min20%Coating weight 2. Caffei

13、ne sustained-release pelletsa FormulationThe 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.Water53.89g b Preparation of the spray suspensionPolymer suspen

14、sion Add propylene glycol followed by Kollicoat SR 30 Dto 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 withvigorous stirring and homogenize the mixture in acorundum disk mill.Spray suspe

15、nsion Incorporate the pigment suspension into the polymersuspension with stirring. The suspension must bestirred during the spraying process to prevent settling.The pellets were coated in an Aeromatic Strea-1 (Aeromatic AG. The suspension was sprayed continuously onto the fluidized, pre-heated pelle

16、ts from the top. Process parameters Inlet air temperature60COutlet air temperature36CProduct temperature37CAir flow80m/hSpraying rate approx. 12g/minSpraying time45 minDrying45C/ 5minCoating weight3mg film former/cmThe coating weight of 3mg film former / cm given here was established for the pellets

17、 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. (extrusion processa FormulationThe formulation i

18、s designed for 500g of pellets (composition of pellets: 20% propranolol HCl 1, 51.66% Avicel PH 101 5, 25.84% lactose 6, 2.5% KollidonVA 64 1; diameter 0.4-1.5mm; made by wet extrusion.Water44.91g b Preparation of the spray suspensionPolymer suspension Add propylene glycol followed by Kollicoat SR30

19、 D to the given quantity of water with stirring. Talc suspension Add talc with vigorous stirring and homogenizethe mixture in a corundum disk mill.Spray suspension Incorporate the talc suspension into the polymersuspension with stirring. The suspension must bestirred during the spraying process to p

20、reventsettling.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 temperature60COutlet air temperature35CProduct temperature36CAir flow80m/hSpraying rate approx. 13g/

21、minSpraying time39 minDrying45C/ 5minCoating weight3mg film former/cmThe coating weight of 3mg film former / cm 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 th

22、e surface area is recommended as a means of estimating the required coating weight in each specific case. (drug-layering processa FormulationThe formulation is designed for 800g of pellets manufactured by drug layering of nonpareilles.Water100.0g b Preparation of the spray suspensionPolymer suspensi

23、on Add TEC followed by Kollicoat SR 30 D to thegiven quantity of water with stirring.Pigment suspension Add talc to the given quantity of water withvigorous stirring.Spray suspension Incorporate the pigment suspension into thepolymer suspension with stirring. The suspensionmust be stirred during the

24、 spraying process toprevent settling.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.Process parameters Machine Glatt GPCG1Method Botto

25、m-spray (WursterInlet air temperature50-55COutlet air temperature29-32CProduct temperature35-40CAir flow90m/hSpraying time220 minSpraying rate approx. 4.5 g/minDrying40C/ 15minCoating weight20% 3.2.1 Propranolol HCl pellet-releasing tableta FormulationThe formulation is designed for 500g of tablets:

26、b ProcedureMix 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/ minCompression force15kNc Tablet propertiesWeight400mgDiameter10mmForm biplanarHardness82-112N 4. Acetaminophen - taste maskeda FormulationThe

27、 formulation is designed for 500g of acetaminophen granules 1.b Preparation of the spray suspensionThe dispersion is used directly without any additives.c CoatingThe crystals were coated in an Aeromatic Strea-1 (Aeromatic AG. The dispersion was sprayed continuously onto the fluidized, pre-heated cry

28、stals from the top. Process parameters Inlet air temperature60COutlet air temperature40CProduct temperature41CAir flow80m/hSpraying rate approx. 9g/minSpraying time9 minDrying45C/ 5minCoating weight4%Crystalline acetaminophen is coated with 4% Kollicoat SR 30 D. pelletssustained-release5. Ibuprofen(

29、drug-layering processThe formulation is designed for 800g of pellets manufactured by drug layering of nonpareilles.a SubcoatingThe polymer spray solution for a weight gain of 5%:Water432.0g b Preparation of the spray solution (subcoatingDissolve Mowiol in hot water and cool with stirring.Process par

30、ameters Machine Glatt GPCG1Method Bottom-spray (WursterInlet air temperature50COutlet air temperature35CProduct temperature40CAir flow80m/hSpraying time56 minDrying40C/ 15minSubcoating weight5% c Polymer coatingThe formulation is designed for 800g of subcoated pellets.d Preparation of the spray susp

31、ension (polymer coating:Polymer suspension Add TEC followed by Kollicoat SR 30 D to thegiven quantity of water with stirring.Pigment suspension Add talc to the given quantity of water withvigorous stirring.Spray suspension Incorporate the pigment suspension into thepolymer suspension with stirring.

32、The suspensionmust be stirred during the spraying process toprevent settling.Process parameters Machine Glatt GPCG1Method Bottom-spray (WursterInlet air temperature50-55COutlet air temperature29-32CProduct temperature35-40CAir flow90m/hSpraying time230 minSpraying rate approx. 4.5 g/minDrying40C/ 15

33、min Spray the suspension continuously onto fluidized pre-heated pellets by the wurster spray method. Weight gains 5, 10, 15 and 20%. 6. Ambroxol HCl sustained-release pellets(drug-layering processThe formulation is designed for 800g of pellets manufactured by drug layering of nonpareilles.a Formulat

34、ionWater100.0g b Preparation of the spray suspensionPolymer suspension Add TEC followed by Kollicoat SR 30 D to thegiven quantity of water with stirring.Pigment suspension Add talc to the given quantity of water withvigorous stirring.Spray suspension Incorporate the pigment suspension into thepolyme

35、r suspension with stirring. The suspensionmust be stirred during the spraying process toprevent settling.c CoatingThe 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 GPCG1Met

36、hod Bottom-spray (WursterInlet air temperature50-55COutlet air temperature29-32CProduct temperature35-40CAir flow90m/hSpraying time220 minSpraying rate approx. 4.5 g/minDrying40C/ 15minWeight gain20% 6.1 Ambroxol HCl pellet-releasing tabletd FormulationThe formulation is designed for 500g of tablets

37、:e ProcedureMix 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/ minCompression force15kNf Tablet propertiesWeight400mgDiameter10mmForm biplanarHardness92-116N 7. Tramadol HCl sustained-release pellets(drug

38、-layering processa Polymer coatingThe formulation is designed for 800g of pellets manufactured by drug layering of nonpareilles.Water100.0g b Preparation of the spray suspensionPolymer suspension Add TEC followed by Kollicoat SR 30 D to thegiven quantity of water with stirring.Pigment suspension Add

39、 talc to the given quantity of water withvigorous stirring.Spray suspension Incorporate the pigment suspension into thepolymer suspension with stirring. The suspensionmust be stirred during the spraying process toprevent settling.c CoatingThe pellets were coated in an GPCG1 (Glatt. The suspension wa

40、s sprayed continuously onto the fluidized, pre-heated pellets by the Wurster method.Process parameters Machine Glatt GPCG1Method Bottom-spray (WursterInlet air temperature50-55COutlet air temperature29-32CProduct temperature35-40CAir flow90m/hSpraying time225 minSpraying rate approx. 4.5 g/minDrying

41、40C/ 15minWeight gain20% 8. Acetylsalicylic acid crystalsa FormulationThe formulation is designed for 800g of acetylicsalicylic acid crystals 12.b Preparation of the spray suspensionAdd talk to the given amount of water with vigorous stirring.Then add Kollicoat SR 30 D with slow stirring.c CoatingTh

42、e 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.Process parameters Machine Glatt GPCG1Method Bottom-spray (WursterInlet air temperature50-55COutlet air

43、temperature29-32CProduct temperature35-40CAir flow90m/hSpraying time166 minSpraying rate approx. 8.9 g/minDrying40C/ 15minCoating weight20% 9. Propranolol HCl sustained-release tableta Formulation of the granulesb Manufacture of the granulesThe active ingredient and excipient were granulated in an A

44、eromatic Strea-1 (Aeromatic AG. The polymer dispersion was sprayed into the fluid bed from the top. Process parameters Inlet air temperature55COutlet air temperature22 27CSpraying rate approx. 10g/minAtomizing pressure 2.0bar c Formulation of the tabletsd TabletingThe granules were passed together w

45、ith magnesium stearate (0.5% and Aerosil200 (0.5% through an 800m sieve, blended for 10 min in a Turbula mixer and compressed into tablets with a force of about 18kN.Tablet press Korsch EK0, 30 tablets/ mine Tablet propertiesDiameter10mmForm biplanarHardness260N 10. Theophyllinetabletsustained-relea

46、sea Formulation of the granulesb Manufacture of the granulesThe active ingredient and excipient was granulated in an Aeromatic Strea-1 (Aeromatic AG. The polymer dispersion was sprayed into the fluid bed from the top.Process parameters Inlet air temperature55COutlet air temperature22 27CSpraying rat

47、e approx. 10g/minAtomizing pressure 2.0bar c Formulation of the tabletsMagnesium stearate 8 4.0mg d TabletingThe granules were passed together with magnesium stearate (0.5% and Aerosil200 (0.5% through an 800m sieve, blended for 10 min in a Turbula mixer and compressed into tablets with a force of a

48、bout 18kN.Tablet press Korsch PH 106, 30 rpme Tablet propertiesHardness276N 11. Carbamazepinetabletsustained-releasea Formulation of the granulesKollicoat SR 30 D 1131.25g b Manufacture of the granulesThe active ingredient and excipients were granulated in an Aeromatic Strea-1 (Aeromatic AG. The pol

49、ymer dispersion was sprayed into the fluid bed from the top.Process parameters Inlet air temperature55COutlet air temperature22 27CSpraying rate approx. 10g/minAtomizing pressure 2.0bar c Formulation of the tabletsMagnesium stearate 8 2.0mg d TabletingThe granules were passed together with magnesium

50、 stearate (0.5% and Aerosil200 (0.5% through an 800m sieve, blended for 10 min in a Turbula mixer and compressed into tablets with a force of about 18kN.Tablet press Korsch EK0, 30 tablets/ mine Tablet propertiesDiameter11mmForm biconvexHardness136N 12. Metoprolol tartrate sustained-release tableta

51、Formulation of the granulesb Manufacture of the granulesThe active ingredient was granulated in an Aeromatic Strea-1 (Aeromatic AG. The polymer dispersion was sprayed into the fluid bed from the top.Process parameters Inlet air temperature50COutlet air temperature24 28CSpraying rate approx. 10g/minc

52、 Formulation of the tabletsd TabletingThe granules were passed together with magnesium stearate (0.5% and KollidonSR (54.5% through an 800m sieve, blended for 10 min in a Turbula mixer and compressed into tablets with a force of about 10kN.Tablet press Korsch EK0, 30 tablets/ minCompression force9,3

53、kNe Tablet propertiesDiameter12mmForm biplanarHardness220N 13. Propranolol HCl sustained-release tableta Formulationb ProcedureMix the ingredients together, pass through a 0.8mm sieve and compress intotablets with a force of about 10kN.Tablet press Korsch PH 100/6 30 rpmCompression force9,9kNc Table

54、t propertiesDiameter10mmForm biplanar172NHardness 14. Caffeine sustained-release tableta Formulationb ProcedureMix the ingredients together, pass through a 0.8mm sieve and compress into tablets with a force of about 10kN.Tablet press Korsch PH100/6, 30 rpmCompression force9.6kN9.8kN10.1kN c Tablet p

55、ropertiesDiameter10mm10mm10mmForm biplanarHardness213N201N193NFriability0.1%0.1%0.1% 15. Diclofenac Na sustained-release tableta Formulationb ProcedureMix the ingredients together, pass through a 0.8mm sieve and compress into tablets with a force of about 8kN.Tablet press Korsch EK0, 30 tablets/ minc Tablet propertiesDiameter8mmForm biplanarHardness195N229NFriability0.1%0.1% 16. Ascorbic acid sustained-release tableta Formulationb ProcedureMix the ingredients together, pass through a