Replies to post #27434 on Intellipharmaceutics International Inc. (IPCI)

[WeeZuhl]

WeeZuhl, your whole reasoning is irrelevant as you don't know the Rexista formula. So you're posting lots of articles but don't know the core of Rexista.

Of course I know. Dr. Odidi told me. He gave me 5 different examples, and they all have a minimum 12mg of blue dye #1 and one has 18mg of blue dye #1. This is a concentrated dose- well-beyond typical color additives. A brand new use as "stigmatizing dye," never done before, and not established as safe. As always, please let me know if there are additional information gaps I can help you fill. (And, yes, I am posting lots of articles, thanks for noticing. One would be well-advised to pay close attention to what they say.)











http://www.freepatentsonline.com/9522119.html

Example 29
Oxycodone Sustained Action (SA) 80 mg ODR Tablets (Each Tablet Contain 70 mg in the Core and 10 mg External to the Core)
Formula for core
Ingredients % w/w
Oxycodone HCl 18.34
Polyethylene Oxide 65.00
Aluminum lake Blue#1 4.00
Crospovidone 2.00
Microcrystalline cellulose 11.66
Eudragit RL 2.00
Magnesium stearate 0.50
Formula for Loading Dose
Ingredients % w/w
Opadry White 13.09
Oxycodone HCl 9.53
Water 77.38
Formula for Acid labile coat
Ingredients % w/w
Eudragit E (milled) 9.73
Sodium Lauryl sulfate 0.974
Stearic acid (milled) 1.46
Talc 3.40
Simethicone 0.84
Water QS
Formula for Alkalinizing Coat
Ingredients % w/w
Opadry White 16.132
Magnesium Hydroxide 16.592
Water 67.276

Processing Techniques
Step 1a. Preparation of Granules for the Core:
All the ingredients with the exception of the magnesium stearate from the core formula were charged into a high shear granulator and dry mixed for less than 10 minutes. The dry mixed granules were discharged into a Paterson Kelly V-Blender. The magnesium stearate was then added to the V-Blender. The granules were blended for less than 10 minutes.

Step 1b. Preparation of the Core (Extended Release Tablets):

The cores are tablets made from the granules prepared in Step 1a. A rotary press was set-up to produce capsule shaped tablets each weighing about 400 mg (a Manesty tablet press with 16 stations was used). Granules from Step 1a were charged into a feed hopper and the tablet was produced from the double rotary press by applying suitable compression force to give tablets of required thickness, hardness and friability.

Step 2. Preparation of a Coating Suspension of the Ingredients for the Loading Dose to be Applied to the Tablet from Step 1 b:

(I) Water was added into a stainless steel vessel. (II) Opadry was added while stirring with a propeller mixer until all ingredients are finely dispersed in a suspension. (III) Oxycodone HCl was added to the Opadry water mixture while stirring using a propeller mixer.

Step 3. Application of the Coating Suspension from Step 2 to Form Part of the Loading Dose Surrounding the Tablet from Step 1b:

Tablets from step 1b were charged into a rotating drum of a side vented automated Tablet coater (Rama Cota Tablet Film Coater was used). The suspension from Step 2 was applied to the tablets obtained from Step 1 b, using a peristaltic pump and spray gun. The suspension was dried as a film onto the tablets, using heated air drawn through the tablet bed from an inlet fan. The suspension is applied to form a coat surrounding the tablet.

Step 4. Preparation of Acid Labile Coating Suspension to be Applied to the Tablet from Step 3:

(I) Water was added into a stainless steel vessel followed by Sodium lauryl sulfate and stearic acid, step-by-step, while stirring vigorously with a high shear mixer until all ingredients are dissolved. (II) Eudragit E was added, step-by-step, while stirring vigorously with a high shear mixer until all ingredients were dissolved. (III) Talc was added, followed by simethicone while stirring using a high shear mixer until finely dispersed in the solution.

Step 5. Application of a Coating Suspension from Step 4 to Form an Acid Labile Coat Surrounding the Tablet from Step 3:

Tablets from step 3 were charged into the rotating drum of a side vented automated Tablet coater (Rama Cota Tablet Film Coater was used). The suspension from Step 4 was applied to the tablets obtained from Step 3, using a peristaltic pump and spray gun. The suspension was dried as a film onto the tablets, using heated air drawn through the tablet bed from an inlet fan. A sufficient amount of the suspension was applied to form about 4 mg/cm2 to about 20 mg/cm2 of the coat surrounding the tablet.

Step 6. Preparation of a Coating Suspension of the Ingredients of the Alkalinizing Coat:

(I) Water was added into a stainless steel vessel followed by Opadry White until no lumps are seen in the resulting suspension. (II) To a vortex of this suspension was added magnesium hydroxide until finely dispersed.

Step 7. Application of the Coating Suspension from Step 6 to Form an Alkalinizing Coat Surrounding the Coated Tablets from Step 5:

Tablets from Step 5 were charged into the rotating drum of a side vented automated Tablet coater (Rama Cota Tablet Film Coater was used). The suspension from Step 6 was applied to the tablets obtained from Step 5, using a peristaltic pump and spray gun. The suspension was dried as a film onto the tablets, using heated air drawn through the tablet bed from an inlet fan. A sufficient amount of the suspension was applied to form coat containing about 20 mg to 24 mg of magnesium hydroxide per coated tablet.

FIGS. 18 to 26 below show the results of the various tests for this example.

Example 30
Same as Example 29 except that each Tablet contain 52.5 mg in the core and 7.5 mg external to the core

Formula for core
Ingredients % w/w
Oxycodone HCl 13.755
Polyethylene Oxide 61.00
Aluminum lake Blue#1 4.00
Crospovidone 4.00
Microcrystalline cellulose 14.24
Eudragit RL 2.00
Magnesium stearate 1.00
Formula for Loading Dose
Ingredients % w/w
Opadry White 12.73
Oxycodone HCl 7.86
Water 79.41

Example 31
Same as Example 29 except that each Tablet contain 7.5 mg in the core and 2.5 mg external to the core

Formula for core
Ingredients % w/w
Oxycodone HCl 1.973
Polyethylene Oxide 80.21
Aluminum lake Blue#1 4.00
Crospovidone 5.00
Microcrystalline cellulose 4.00
Eudragit RL 2.38
Magnesium stearate 0.44
Formula for Loading Dose
Ingredients % w/w
Opadry White 12.63
Oxycodone HCl 2.37
Water 85.00

Example 32
Same as Example 29 except that each Tablet contain 8.75 mg in the core and 1.25 mg external to the core

Formula for core
Ingredients % w/w
Oxycodone HCl 2.822
Polyethylene Oxide 67.69
Aluminum lake Blue#1 6.00
Crospovidone 2.00
Microcrystalline cellulose 18.99
Eudragit RL 2.00
Magnesium stearate 0.50
Formula for Loading Dose
Ingredients % w/w
Opadry White 15.091
Oxycodone HCl 1.612
Water 83.297

Example 33
Same as Example 29 except that each Tablet contain 13.125 mg in the core and 1.875 mg external to the core

Formula for core
Ingredients % w/w
Oxycodone HCl 4.232
Polyethylene Oxide 73.69
Aluminum lake Blue#1 4.00
Crospovidone 2.00
Microcrystalline cellulose 13.58
Eudragit RL 2.00
Magnesium stearate 0.50
Formula for Loading Dose
Ingredients % w/w
Opadry White 13.091
Oxycodone HCl 2.418
Water 84.490

Example 34
Same as Example 29 except that each Tablet contain Oxymorphone HCl as active substance i.e., 35 mg in the core and 5 mg external to the core

Formula for core
Ingredients % w/w
Oxymorphone HCl 11.507
Polyethylene Oxide 64.27
Aluminum lake Blue#1 4.00
Crospovidone 2.00
Microcrystalline cellulose 15.72
Eudragit RL 2.00
Magnesium stearate 0.50
Formula for Loading Dose
Ingredients % w/w
Opadry White 14.216
Oxycodone HCl 6.575
Water 79.461