Professional Documents
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qxd
07.06.2005
10:57 Uhr
5 Granules,
powders, dry
syrups and
lyophilisates
Seite 457
5.4
Formulations
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Seite 459
1. Formulation (granules)
I.
II.
Aceclofenac .............................................1.3
Orange flavour .........................................4.3
Sorbitol ..................................................85.6
Lutrol F 68 [1]...........................................4.4
Cremophor RH 40 [1] ...............................4.4
Water ..............................................about 50
g
g
g
g
g
g
2. Manufacturing
Granulate mixture I with solution II, pass through a 0.8 mm screen,
dry and sieve again. Fill 3.9 g in sachets corresponding to 50 mg
aceclofenac.
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Seite 460
1. Formulation
I.
II.
Albendazole ................................................4
Citric acid ...................................................3
Sodium citrate.............................................3
Sorbitol, crystalline [10]..............................88
Ethanol 96 % ............................................22
Lutrol F 68 [1] .............................................2
g
g
g
g
g
g
2. Manufacturing
Granulate mixture I with solution II, pass through a 0.8 mm screen, dry
and sieve again.
Fill 50 g of the granules in a 100 ml flask (= dry syrup) or 5 g in sachets
(= instant granules)
3. Administration forms
Dry syrup (200 mg albendazole /10 ml):
Fill the flask containing 50 g of granules with water to the 100 ml mark.
The obtained suspension has no bitter taste.
Instant granules (200 mg albendazole sachet):
Suspend 5 g of the granules (= 200 mg albendazol) in a glass of water.
The suspension has no bitter taste.
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Seite 461
II.
g
g
g
g
g
g
g
g
g
g
g
2. Manufacturing
Granulate mixture I with solution II, pass through a sieve and dry.
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page 2
4
8
Kollidon CL-M in the administration form [%]
12
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Seite 463
1. Formulation
Amoxicillin trihydrate.................................5.0
Sodium citrate..........................................5.0
Citric acid, crystalline ................................2.1
Sodium gluconate ....................................5.0
Sorbitol crystalline [10] ............................40.0
Kollidon CL-M [1] .....................................6.0
Orange flavour .........................................1.5
Lemon flavour ..........................................0.5
Saccharin sodium.....................................0.4
g
g
g
g
g
g
g
g
g
2. Manufacturing
Mix all components and fill in a flask.
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page 2
4
6
2
Kollidon CL-M in the administration form [%]
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1. Formulation
Amoxicillin sodium ..................................6.25 g
Kollidon 12 PF [1] ...................................7.50 g
Water for injections .....................add 100.00 ml
2. Manufacturing
Dissolve the active ingredient in the well stirred solution of Kollidon 12 PF
and after freeze-drying, fill 500-mg-portions of the dry lyophilisate into
ampoules.
3. Administration
Prior to administration, the dry content of an ampoule is mixed with
1.9 ml of water to give a clear injection solution.
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Seite 467
1. Formulation
Ampicillin trihydrate ..................................5.0
Sodium citrate..........................................5.0
Citric acid, crystalline ................................2.1
Sodium gluconate ....................................5.0
Sorbitol crystalline [10] ............................40.0
Kollidon CL-M [1] .....................................6.0
Orange flavour .........................................1.5
Lemon flavour ..........................................0.5
Saccharin sodium.....................................0.4
g
g
g
g
g
g
g
g
g
2. Manufacturing
Mix all components and fill in a flask.
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page 2
Viscosity [mPas]
60
40
20
0
0
4
6
Kollidon CL-M in the suspension [g/100 ml]
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Seite 469
1. Formulation
I.
II.
g
g
g
g
g
g
g
g
g
2. Manufacturing
The mixture I is granulated with the solution II. The obtained granules are
passed through a 1.0 mm sieve and dried at room temperature. Fill 83 g
of the granules in a 100 ml flask.
3. Remark
See also Sustained Release Coating of Diclofenac Pellets
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Seite 470
1. Formulation
I.
II.
g
g
g
g
g
2. Manufacturing
Granulate the mixture (I) in a Diosna granulator with water (II) and press
the humid granules through a sieve of 1.5 mm. Form pellets in a spheronizer during 10 min with the rotation speed of 380-420 rpm. Dry the pellets in a fluidizedd bed at 70C.
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Seite 471
1. Formulation
Indomethacin ..........................................160 g
Kollidon CL [1].........................................320 g
Aerosil 200 [4] ............................................q.s.
2. Manufacturing
Mix the components for about 10 min and fill in hard gelatin capsules to
obtain 160 mg indomethacin in each capsule.
3. Dissolution
100
80
with Kollidon CL
60
40
20
without Kollidon CL
0
0
15
30
45
60
75
Minutes
90
105
120
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Seite 472
1. Formulation
I.
II.
2. Manufacturing
Granulate mixture I with solution II and pass through a 0.8 mm sieve to
obtain free-flowing granules. Fill 2 g in sachets or 20 g in a 100 ml flask.
3. Administration
Instant granules in sachets:
Suspend 2 g (= 1 sachet) in a glass of water (= 800 mg Magaldrate)
Dry syrup:
Fill the flask with drinking water until the mark of 100 ml and shake
well. 10 ml of the suspension correspond to 800 mg Magaldrate.
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Seite 473
1. Formulation
I.
g
g
g
g
g
g
g
g
g
g
g
g
g
g
g
g
g
g
g
g
2. Manufacturing
Granulate mixture I with solution II, pass through a 0.8 mm sieve, dry
well and mix with III.
Fill 3 4 g in sachets.
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Yellow granules
Very good
4 g disperse homogeneously in water
after about 40 seconds.
4. Administration
3 4 g of the granules (= 1 sachet) correspond to about 1 RDA of the
vitamins
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Seite 475
1. Formulation
I.
II.
2. Manufacturing
Pass mixture through a 0.8 mm sieve and granulate with solution II in the
fluidized bed. Fill 6 12 g of the granules in sachets.
If the technology of a fluidized bed is not available, the dry powders of
vitamin A, E and B 12 should be added after the granulation of the other
components.
3. Administration
Suspend 6 12 g (= 1 sachet) in a glass of water corresponding to 2 4
RDA of vitamins.
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page 2
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Seite 477
Paracetamol (= Acetaminophen) +
Doxylamine + Caffeine Effervescent
Granules (500 mg + 5 mg + 33 mg/2.1 g)
1. Formulation
I.
Paracetamol, powder...............................500 g
Doxylamine succinate ..................................5 g
Caffeine (BASF) .........................................33 g
Tartaric acid ............................................391 g
Sodium hydrogen carbonate ....................417 g
II. Kollidon 30 [1] .............................................6 g
Isopropanol (or Ethanol) ..............................q.s.
III. Sodium citrate...........................................30 g
Sugar .....................................................707 g
2. Manufacturing
Granulate mixture I with solution II, dry at 60C under vacuum conditions, sieve and mix with III.
Fill 2.1 g in sachets at maximum 30 % of relative atmospheric humidity.
3. Properties
Free flowing granules.
4. Remark
If the solvent insopropanol is replaced by water the granulation should
be done in a fluidized bed.
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Seite 479
1. Formulations
I.
II.
No. 1
No. 2
50 g
130 g
50 g
7g
5g
5g
3g
3g
8g
50 g
4. Administration
Formulation No. 1: Suspend 1.5 g
500 mg paracetamol) in a glass of
Formulation No. 2: Suspend 1.3 g
500 mg paracetamol) in a glass of
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page 2
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Seite 481
1. Formulation
I.
g
g
g
g
g
g
2. Manufacturing
Suspend PVP-Iodine and Maize-PO4-Aerosol (I) in the liquid mixture II
and fill in aerosol cans with the propellants III.
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Seite 482
Propanolol Spheronized Pellets for Sustained Release Coating (20% and 30%)
1. Formulations
20% Pellets
I
II
Propanolol HCI.............................................200
Avicel PH101 [5] ...........................................517
Granulac 230 [8] ..........................................258
Kollidon VA64 [1] ............................................25
Water .................................................about 500
30% Pellets
g
g
g
g
g
300
467
208
25
540
g
g
g
g
g
2. Manufacturing
Granulate the mixture (I) in a Diosna granulator with water (II) and press
the humid granules through a sieve of 1.5 mm. Form pellets in a spheronizer with the rotation speed of 200-400 rpm. Dry the pellets in a fluizid
bed and sieve through a 0.7 mm sieve to eliminate the fine particles.
3. Remark
See also Sustained Release Coating of Propanolol Pellets
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1. Formulation
Simethicone (Abil 200, Goldschmidt) .....10.0
Cremophor RH 40 [1] ...............................5.0
II. Kollidon VA 64 [1] .....................................3.0
Ethanol ..................................................40.0
III. Sorbitol, crystalline (Merck) .....................50.0
Fructose (Merck) ....................................50.0
Kollidon CL-M [1]....................................50.0
Orange flavour (Dragoco) ..........................0.5
I.
g
g
g
g
g
g
g
g
2. Manufacturing
Introduce solution II into the mixture I. Granulate the powder mixture III
with the well stirred mixture I/II, dry and pass through a 1 mm sieve.
Fill 1 or 2 g in sachets.
4. Administration
Take the content of one sachet (1 g = 60 mg simethicone or 2 g = 120 mg
simethicone) as powder or disperse the recommended amount (e.g. 1 to
2 g) in 100 ml of drinking water.
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Seite 484
g
g
g
g
g
g
g
g
g
g
2. Manufacturing
Mix all components and sieve for administration. Fill 55 g of the mixture
in a 100 ml flask.
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Seite 485
g
g
g
g
g
II
Water......................................................400 g
2. Manufacturing
Granulate the mixture (I) in a Diosna granulator with water (II) and pass
the humid granules through a sieve of 1.5 mm. Form pellets in a spheronizer with the rotation speed of 300-400 rpm. Dry the pellets in a fluidized bed and sieve through a 0.7 mm sieve to eliminate the fine particles.
3. Remark
See also Sustained Release Coating of Verapamil Pellets
129738_Rezeptblaetter.qxd
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Seite 486
I.
2. Manufacturing
Mix the components I, add the mixture II, granulate mixture I+II with the
liquid III, pass through a 0.8 mm sieve, dry well and mix with III.
Fill 2.1 g of the granules in sachets.
Yellow granules
Very good
2.1 g disperse homogeneously in 100 ml of water in
about 60 seconds.
4. Administration
2.1 g of the granules correspond to about 1 RDA of the vitamins and
500 mg of carnitine and 20 mg of glutamine.
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Seite 487
II.
2. Manufacturing
Mix the components I, granulate with soluiton II, dry and pass through a
0.8 mm sieve.
Fill 1 g of the granules in sachets, (or 10 g in 100 ml flaks as dry syrup).
4. Administration
About 1 g of the granules (= 1 sachet) correspond to two daily vitamin B
and vitamin C requirements of adults.
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page 2
6 Months
B1
B2
B3
B6
B 12
C
100 %
100 %
100 %
100 %
100 %
100 %
93 %
80 %
98 %
97 %
100 %
97 %
100 %
93 %
100 %
100 %
100 %
100 %
6. Remark
Due to the high loss of riboflavin phosphate sodium it should be substituted by riboflavin.