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Pharmaceutical formulations

IP.com Disclosure Number: IPCOM000241326D
Publication Date: 2015-Apr-17
Document File: 9 page(s) / 104K

Publishing Venue

The IP.com Prior Art Database

Abstract

Suitable and stable pharmaceutical formulations are disclosed.

This text was extracted from a Microsoft Word document.
This is the abbreviated version, containing approximately 12% of the total text.

Pharmaceutical formulations

API preparation

The product prepared in example 5 of WO9501338 A1 is milled to the following particle sizes expressed as volume distributions measured by laser diffraction:

Example

d(0.1)

d(0.5)

d(0.9)

API-1

15-25 μm

55-60 μm

100-130 μm

API-2

10-15 μm

30-40 μm

70-80 μm

API-3

7.5-12 μm

25-35 μm

55-70 μm

API-4

5-7.5 μm

20-30 μm

50-60 μm

API-5

2-5 μm

10-20 μm

25-50 μm

API-6

1.5-3 μm

5-10 μm

7-20 μm

API-7

0.75-2 μm

1-4 μm

3-6 μm

API-8

0.5 -1.5 μm

1.5-2 μm

2.5-5 μm

Manufacturing processes

Example M1

1)    Wet granulation of all ingredients except the lubricant with a high shear granulator and drying.

2)    Blend the granulate of step 1 with the lubricant in a bin blender.

3)    Tablet compression with rotary tabletting machine equipped with 5 mm of diameter punches.

Example M2

1)    Sieving: The filler, disintegrant and API were sieved (0.5 to 2.8 mm mesh).

2)    Blending: Raw materials obtained in step 1) were blended until homogeneous into a high shear granulator.

3)    Granulation: Raw materials obtained in step 2) were granulated with the purified water.

4)    Drying: The wet granulate obtained in step 3) was dried until loss on drying ≤ 3%.

5)    Sieving: The granulate and lubricant were sieved and introduced into the blender.

6)    Blending: Raw materials obtained in step 5) were blended until homogeneous.

7)    Tabletting process: The blend of step 6) was pressed in a rotary tablet press.

Example M3

1)    Milling: API and a 30-70 % of the filler were milled (0. 5 to 2.8 mesh).

2)    Sieving: The remaining filler and disintegrant were sieved (0.50 to 2.80 mesh).

3)    Blending: Raw materials obtained in step 1) and 2) were blended until homogeneous into a high shear granulator.

4)    Granulation: Raw materials obtained in step 3) were granulated with the purified water.

5)    Drying: The wet granulate obtained in step 4) was dried until loss on drying ≤ 3%.

6)    Sieving: The granulate and the lubricant were sieved and introduced into the blender.

7)    Blending: Raw materials obtained in step 6) were blended until homogeneous.

8)    Tabletting process: The blend of step 7) was pressed in a rotary tablet press.

Examples depending on the milling in step 1:

Example M3a: Pin mill

Example M3b: cutting mill

Example M3c: hammer mill

Example M3d: loop jet mill

Example M4

1)    Starch paste preparation: A starch paste at 5% (w/w) was prepared with purified water and 30-70% of the disintegrant.

2)    Milling: 30-70% of the filler was milled with the API.

3)    Sieving: The other portion of the filler and the other portion of disintegrant were sieved.

4)    Blending: Raw materials obtained in step 2) and 3) were blended until homogeneous into a high shear granulator.

5)    Granulation: Raw materials obtained in step 4) were granulated with the starch paste obtained in the step 1).

6)    Drying: The wet granulate obtained in step 5) was dried until loss on drying ≤ 3%.

7)    Sieving: The granulate and lubricant were sieved and introduced into the blender.

8)    Blending:...