ABSTRACT
LD50 3000 mg/ kg oral rat
Maize starch 3 PVP-K-30 2 Magnesium stearate
Avicel PH-102 7 Primogel 6
Prednisolone 20 mg tablets
750,000 tablets (187.5 kg)
Prednisolone Magnesium stearate
20 mg 200 mg 6 7
LD50 1680 mg/kg oral mouse
Lactose 2 Avicel 7
Promethasone 25 mg F/C
600,000 tablets (20 kg)
Promethasone
Lactose monohydrates
25 mg 50 mg 1
LD50 255 mg/kg oral rat
Maize starch 3 PVP-K-30 2 Magnesium stearate
Sodium disulfate Indapamide 2.5 mg F/C tablets
1,000,000 tablets (95 kg)
Indapamide
Lactose monohydrates
2.5 mg 2.5 mg 7
LD50 >3000 mg/kg oral rat
PVP-K-30 2 Maize starch 3 Magnesium stearate
Sodium lauryl sulfate
Diphenoxylate 1,000, 000 tablets
Diphenoxylate HCl 2.5 mg 30 mg 4 LD50 600 mg/kg oral rat
Atropine tabs Atropine sulfate 0.025 mg 0.3 mg Lactose monohydrates
continued
Product Batch Size Ingredients Therapeutic
Dose
Usage per
Day Solubility Toxicity Level LD50
Maize starch 3 Magnesium stearate
Levofl oxacin F/C tablets
160,000 tablets (105.6 kg)
Levofl oxacin 500 mg 1000 mg LD50 35,900 mg/kg oral rat; LD50 3366 mg/kg oral mouse
Avicel PH-102 7 PVP-K-30 2 Hypromellose
Paracetamol caplet 500
1,000,000 tablets (640 kg)
Paracetamol
Maize starch PVP-K-30
500 mg 2000 mg 3
3 2
LD50 2404 mg/kg oral rat
Magnesium stearate
Gelatin 7 Glycerol 5 Primogel 6 Aerosil 200 7
Aspirin 81 mg E/C tablets
2,000,000 tablets (230 kg)
Aspirin Avicel PH-102
81 mg 4 g/day 5 7
LD50 200 mg/kg oral rat
Magnesium stearate
Aspirin 300 mg E/C tablets
2,000,000 tablets
Aspirin 300 mg 5 LD50 200 mg/kg oral rat
Avicel PH-102 7 Magnesium stearate
Attapulgite tablets 120,000 tablets (120 kg)
Attapulgite regular
Attapulgite colloidal
19 kg
11 kg
750 mg 1500 mg
880 mg
Nontoxic
Klucel Sucrose Magnesium stearate
PVP-K-30 Lamotrigine 100 mg tablets
150,000 tablets (45 kg)
Lamotrigine 100 mg 200 mg 6 LD50 185 mg/kg oral rat; LD50 269 mg/kg oral mouse
Product Batch Size Ingredients Therapeutic
Dose
Usage per
Day Solubility Toxicity Level LD50
Avicel PH-102 7 Lactose monohydrates
Primogel 6 PVP-K-30 2 Iron oxide yellow 7
Sennosides 12 mg S/C tablets
1,300,000 tablets (178.75 kg)
Sennosides 12 mg 72 mg/ day
Avicel PH-102 7 Magnesium stearate
Lactose dried 2 Starch 1500 Aerosil 200 7
Bisacodyl 5 mg tablets
650,000 tablets (48.75 kg)
Bisacodyl
Lactose Avicel
5 mg 20 mg 6
2 7
LD50 4320 mg/kg oral rat
Maize starch 3 Magnesium stearate
Benzafi brate 200 mg tablets
3,000,000 tablets (111 kg)
Benzafi brate
Maize starch Magnesium stearate
200 mg 600 mg 7
3 7
LD50 1082.0 mg/kg oral rat
Methocel 3 Avicel 7 Primogel 6 Lactose monohydrates
Lomefl oxacin 400 mg tablets
150,000 tablets (102.6 kg)
Lomefl oxacin HCl
Lactose monohydrates
400 mg 400 mg 5
LD50 1556 mg/kg oral rat
CMC calcium 3 Klucel EF 3 Magnesium stearate 7 Avicel PH-102 7
continued
Product Batch Size Ingredients Therapeutic
Dose
Usage per
Day Solubility Toxicity Level LD50
Acyclovir 800 mg tablets
90,000 tablets (97.65 kg)
Acyclovir
Avicel PH-102 Primogel
800 mg 2400 mg 3
7 6
LD50 >20.0 g/kg oral rat
Maize starch 3 Magnesium stearate
Loratadine 10 mg tablets
1,000,000 tablets (115 kg)
Loratadine
Lactose monohydrates
10 mg 10 mg 7
Nontoxic
Maize starch 3 Magnesium stearate
Mebendazole 100 mg tablets
150,000 tablets (43. 05 kg)
Mebendazole
Maize starch Avicel PH-102
100 mg 100 mg 7
3 7
LD50 714 mg/kg oral rat
PVP-K-30 2 Methyldopa 250 mg F/C tablets
285,000 tablets (101.175)
Methyldopa anhydrous
Guar gum
7 Avicel PH-102 Aerosil 200 7 Ethyl cellulose Magnesium stearate
Glibenclamide tablets
500,000 tablets (80 kg)
Glibenclamide
Lactose monohydrates
2.5 mg 20 mg/ day
LD50 >20,000 mg/kg oral rat
Maize starch 3 Magnesium stearate
Aerosil 200 7 Talc fi ne powder 7
Multivitamin M tablets
1,300,000 tablets (240 kg)
Thiamine 2 mg 6 mg/ day
2 LD50 >1000 mg/kg oral rat
Ribofl avin 1 mg 3 mg/ day
2 LD50 >20,000 mg/kg oral rat
Product Batch Size Ingredients Therapeutic
Dose
Usage per
Day Solubility Toxicity Level LD50
Nicotinamide 15 mg 45 mg/ day
2 LD50 3500 mg/kg oral rat
Vitamin D3 300 IU 900 IU/ day
7 LD50 >2000 mg/kg oral rat
Vitamin A palmitate
3000 IU 9000 IU/ day
7 LD50 7910 mg/kg oral rat
PVP-K-30 2 Avicel PH-102 7 Magnesium stearate
Lactose monohydrates
Magnesium oxide 7 Zinc sulfate 7
Bromhexine 8 mg tablets
2,000,000 tablets (240 kg)
Bromhexine HCl
Lactose monohydrates
8 mg 48 mg 6
LD50 1226 mg/kg oral mouse
Maize starch 3 Gelatin powder 7 Magnesium stearate
Ambroxol 30 mg tablets
350,000 tablets (84 kg)
Ambroxol HCl
Lactose monohydrates
30 mg 60 mg 4
LD50 13,400.0 mg/ kg oral rat
Maize starch 3 Aerosil 200/ AC-DI-So1
7-7
Magnesium stearate
Orphenadrine tablets
1,000,000 tablets (660 kg)
Paracetamol 450 mg 3600 mg 3 LD50 2404 mg/kg oral rat
Orphenadrine citrate
35 mg 4 LD50 150 mg/kg oral mouse
Maize starch 3 PVP-K-30 2 Primogel 6 Glycerol 5
Enalapril 20 mg tablets
200,000 tablets (40 kg)
Enalapril maleate
Lactose monohydrates
20 mg 20 mg 3
LD50 2973 mg/kg oral rat
continued
Product Batch Size Ingredients Therapeutic
Dose
Usage per
Day Solubility Toxicity Level LD50
Magnesium stearate
Maize starch 3 Starch 1500 5
Metronidazole 500 mg tablets
625,000 tablets (593.75 kg)
Metronidazole
Lactose monohydrates
500 mg 2000 mg 4
LD50 3000 mg/kg oral rat
Avicel PH-102 7 Maize starch 3 PVP-K-30 2 Magnesium stearate
Primogel 6 Mebendazole 100 mg tablets
400,000 tablets (116 kg)
Mebendazole 100 mg 200 mg 7 LD50 714 mg/kg oral rat; LD50 620mg/kg oral mouse
Avicel PH-102 7 PVP-K-30 2 Primogel 6 Magnesium stearate
Sodium saccharin 2 Sodium lauryl sulfate
Ibuprofen 600 mg tablets
650,000 tablets (562.25 kg)
Ibuprofen
Maize starch
600 mg 2400 mg 7
LD50 636 mg/kg oral rat
Magnesium stearate
Starch 1500 5 Aerosil 200 7 Stearic acid 7
Metoclopramide 10 mg tablets
1,000,000 tablets (125 kg)
Metoclopramide 10 mg 30 mg/ day
1 LD50 280 mg/kg oral mouse
Lactose monohydrates
Maize starch 3 Microcrystalline cellulose
Product Batch Size Ingredients Therapeutic
Dose
Usage per
Day Solubility Toxicity Level LD50
Pyridoxine 40 mg tablets
2,000,000 tablets (240 kg)
Pyridoxine HCl
Microcrystalline cellulose
40 mg 1200 mg 2
LD50 5500 mg/kg oral mouse
Magnesium stearate
Aerosil 200 7 Ranitidine 300 mg F/C tablets
250,000 tablets (120 kg)
Ranitidine HCl
Magnesium stearate
300 mg 600 mg 1
LD50 >5 mg/kg oral rat; LD50 884 mg/kg
Avicel PH-102 7 Clarithromycin 500 tablets
125,000 tablets (112.5 kg)
Clarithromycin
Avicel PH-102 PVP-K-30
500 mg 1500 mg 7
7 2
Aerosil 200 7 AC-DI-So1 7 Magnesium stearate
Stearic acid 7 Simethicone tablets
400,000 tablets (252 kg)
Simethicone
Magnesium stearate
Dextrates
42 mg 336 mg 7
LD50 >2000 mg/kg oral rat
Furosemide 40 mg tablets
500,000 tablets (100 kg)
Furosemide 40 mg 40 mg 4 LD50 2600 mg/kg oral rat
Maize starch 3 Lactose monohydrates
Starch 1500 5 Stearic acid 7 Aerosil 200 7 Magnesium stearate
Ciprofl oxacin 500 F/C tablets
150,000 tablets (115.5 kg)
Ciprofl oxacin HCl
Kolidone
500 mg 1500 mg 7
LD50 >500 mg/kg oral rat
Primogel 6
continued
Product Batch Size Ingredients Therapeutic
Dose
Usage per
Day Solubility Toxicity Level LD50
PVP-K-30 2 Aerosil 200 7 Magnesium stearate
Avicel PH-102 7 Hyoscine butyl S/C tablets
2,600,000 tablets (202.8 kg)
Hyoscine butyl
Lactose monohydrates
10 mg 100 mg 2
LD50 1040 mg/kg oral rat
Magnesium stearate
Maize starch 3 Starch 1500 PVP-K-30 2
Pseudoephedrine tablets
500,000 tablets
Triprolidine HCl 2.5 mg 7.5 mg 3 LD50 840 mg/kg oral rat
Pseudoephedrine HCl
60 mg 180 mg 2 LD50 202 mg/kg IP mouse
Lactose monohydrates
Maize starch 3 PVP-K-30 2 Magnesium stearate
Simvastatin 20 mg tablets
500,000 tablets (100 kg)
Simvastatin sodium 20 mg 40 mg 7 LD50 4438 mg/kg oral rat; LD50 3.0 g/kg oral mouse
Lactose monohydrates
Starch 1500 5 Avicel PH-102 7 Ascorbic acid Aerosil 200 7 Magnesium stearate
Tamoxifen 10 mg tablets
500,000 tablets (87.5 kg)
Tamoxifen citrate 10 mg 20 mg 5 LD50 1190 g/kg oral rat
Lactose monohydrates
Maize starch 3 Magnesium stearate
Product Batch Size Ingredients Therapeutic
Dose
Usage per
Day Solubility Toxicity Level LD50
PVP-K-30 2 AC-DI-So1 7
Atenolol 100 mg F/C tablets
250,000 tablets (100 kg)
Atenolol Maize starch
50 mg 100 mg 4 3
LD50 2000.0 mg/kg oral mouse/rat
Magnesium carbonate
Sodium lauryl sulfate
Avicel PH-102 7 Magnesium stearate 7 Primogel 6
Thiamine 100 mg tablets
375,000 tablets (78.75 kg)
Thiamine HCl
Lactose monohydrates
100 mg 100 mg 4
LD50 >10,000 mg/kg oral rat
Kollidone CL 7 PVP-K-90 2 Magnesium stearate
Avicel PH-112 7 Trimethoprim DS tablets
750,000 tablets (825 kg)
Sulfamethoxazole 400 mg 3 g/day 2
Trimethoprim 80 mg 6 LD50 >5300 mg/kg oral rat; LD50 2764 mg/kg oral mouse
Maize starch 3 Magnesium stearate
Gelatin 7 Guar gum Sodium lauryl sulfate
Norfl oxacin 400 mg F/C tablets
200,000 tablets (104 kg)
Norfl oxacin
Avicel PH-102 AC-DI-So1
400 mg 800 mg 5
7 7
LD50 >4000 mg/kg oral rat
Magnesium stearate
Valproate 500 mg E/C tablets
200,000 tablets (200 kg)
Sodium valproate LD50 870 mg/kg oral rat
continued
Product Batch Size Ingredients Therapeutic Dose (mg)
Maximum Usage per
Day Solubility Toxicity Level
LD50
Indomethacin 25 mg tablets
500,000 capsules (125 kg)
Indomethacin
AC-DI-So1
25 200 mg 1
LD50 2.42 mg/kg oral rat
Lactose monohydrates
Magnesium stearate 7 Aerosil 200 7 Sodium lauryl sulfate 2
Product Batch Size Ingredients Therapeutic
Dose
Usage per
Day Solubility Toxicity Level LD50
Magnesium stearate 7 Avicel PH-112 7 Maize starch 3 AC-DI-So1 7 Aerosil 200 7
B-complex tablets 7,500,000 tablets (682.8 kg)
Calcium pantothenate
3 mg 150 mg 2 LD50 10 g/kg oral rat
Pyridoxine 2 mg 60 mg 2 LD50 5500 mg/kg oral mouse
Ribofl avin base 2 mg 60 mg 2 LD50 >40,000 mg/kg oral mouse
Magnesium stearate 7 Aerosil 200 7 Thiamine mononitrate
2 mg 120 mg 2 LD50 >10,000 mg/kg oral rat
Vitamin C 500 mg tablets
300,000 tablets (390 kg)
Ascorbic acid 170 mg 340 mg 2 LD50 1190 mg/kg oral rat
Sodium ascorbate 776 mg 2
Magnesium stearate
Sorbitol 4 Dextrates 2
Product Batch Size Ingredients Therapeutic Dose (mg)
Usage per
Day Solubility Toxicity Level
LD50
Tetracycline HCl 250 mg
750,000 capsules (243.75 kg)
Tetracycline HCl
Lactose monohydrates
250 4 g 3
LD50 6443 mg/kg oral rat
Aerosil 200 7 Magnesium stearate 7
Oxytetracycline HCl 250 mg
750,000 capsules (234 kg)
Oxytetracycline HCl
Maize starch
250 2 g/day 2
LD50 4700 mg/kg oral rat
Aerosil 200 7 Talc fi ne 7 Magnesium stearate 7
Doxycycline 100 mg
150,000 capsules (23.25 kg)
Doxycycline hyclate
Avicel PH-102
100 200 mg 3
LD50 1900.0 g/kg oral mouse
Maize starch 3 Sodium lauryl sulfate 2 Magnesium stearate 7 Aerosil 200 7
Carbinoxamine 50,000 capsules
Carbinoxamine maleate
10 10 mg 2 LD50 162 mg/kg oral mouse
Phynyle propanolamine HCl
Fluoxetine 20 mg capsule
500,000 capsules (77.5 kg)
Fluoxetine HCl
Maize starch Aerosil 200
20 20 mg 5
3 7
LD50 452 mg/kg oral rat
Simethicone 7 Azithromycin 250 mg
100,000 capsules (52 kg)
Azithromycin
Maize starch
250 500 mg 5
LD50 >3.0 g/kg oral rat
Sodium lauryl sulfate 2 Anhydrous lactose 2
In the preceding chapters, we have presented matrices for equipment details, solubility, and toxicity of active materials as well as products grouping with the concentration and daily maximum dosage of the actives in the table above. After having all these information, it is important for the validation professional to build the equipment train for the different dosage forms.
