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Medicament composition containing aripiprazole and preparation thereof

A technology of aripiprazole and composition, applied in the field of pharmaceutical composition containing aripiprazole and its preparation, to achieve the effect of reducing production cost

Active Publication Date: 2011-03-02
CHENGDU KANGHONG PHARMA GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The composition has a simple formula and a mature preparation process. Under the condition that the disintegration time limit meets the quality requirements of orally disintegrating tablets, the hardness of aripiprazole orally disintegrating tablets prepared by ordinary tablet production equipment reaches 8-10 kg, successfully Solved the problem that orally disintegrating tablets cannot be packaged by general packaging equipment, and realized industrialized mass production

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1- Embodiment 9

[0146] Embodiment 1-embodiment 9, see table 13: (by weight)

[0147] Table 13 Examples 1-9

[0148] Component\Recipe

1

2

3

4

5

6

7

8

9

Aripiprazole

2.50

1.25

5.00

5.00

3.00

2.00

4.50

3.00

4.50

Crospovidone

5.17

8.00

2.00

5.17

5.17

4.00

7.00

6.00

4.00

microcrystalline cellulose

50.00

63.43

46.92

50.00

55.00

49.90

60.00

45.00

49.90

Mannitol

36.00

21.12

39.08

33.50

30.00

41.60

20.00

37.50

41.60

aspartame

0.33

0.20

1.00

0.33

0.33

-

0.50

1.00

-

Micropowder silica gel

4.00

4.00

4.00

4.00

5.00

2.00

5.00

4.50

-

Magnesium stearate

2.00

2.00

2.00

2.00

1.50

0.50

3.00

3.00

-

[0149] The preparation method is:

[0150] Take aripiprazole and pulverize, sieve, and set aside; weigh the formula amount of crospovidone...

Embodiment 10- Embodiment 18

[0155] Embodiment 10-embodiment 18, see table 14: (by weight)

[0156] Table 14 Examples 10 to 18

[0157] Component\Recipe

10

11

12

13

14

15

16

17

18

Aripiprazole

2.50

1.25

5.00

5.00

3.00

2.00

5.00

3.00

4.50

Croscarmell Starch Sodium

5.17

8.00

2.00

5.17

5.17

4.00

8.00

6.00

4.00

microcrystalline cellulose

50.00

63.43

46.92

50.00

55.00

49.90

60.00

45.00

49.90

Mannitol

36.00

21.12

39.08

33.50

30.00

41.60

20.00

37.50

41.60

aspartame

0.33

0.20

-

0.33

0.33

0.5

2.00

1.00

-

Micropowder silica gel

4.00

4.00

5.00

4.00

5.00

-

5.00

4.50

-

Magnesium stearate

2.00

2.00

2.00

2.00

1.50

2.00

-

3.00

-

[0158] The preparation method is:

[0159] Take aripiprazole and pulverize, sieve, and set aside; weigh the formula ...

Embodiment 19 Embodiment 27

[0164] Embodiment 19 Embodiment 27, see table 15: (by weight)

[0165] Table 15 Examples 19 to 27

[0166] Component\Recipe

19

20

21

22

23

24

25

26

27

Aripiprazole

2.50

1.25

5.00

5.00

3.00

2.00

5.00

3.00

4.50

Croscarmellose Sodium

5.17

8.00

2.00

5.17

5.17

4.00

8.00

6.00

4.00

microcrystalline cellulose

50.00

63.43

46.92

50.00

55.00

49.90

60.00

45.00

49.90

[0167] Mannitol

36.00

21.12

39.08

33.50

30.00

41.60

20.00

37.50

41.60

aspartame

0.33

0.20

1.00

0.33

0.33

-

2.00

1.00

-

Micropowder silica gel

4.00

4.00

4.00

4.00

5.00

2.00

5.00

4.50

-

Magnesium stearate

2.00

2.00

2.00

2.00

1.50

0.50

-

3.00

-

[0168] The preparation method is:

[0169] Take aripiprazole and pulverize, sieve, and set aside;...

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Abstract

The invention discloses a pharmaceutical composition containing aripiprazole and a preparation method thereof. The formula which is suitable for preparing oral disintegrating tablets provided by the invention comprises an active component, a disintegrating agent, a diluent agent and a latent solvent, a proper amount of a corrective, a lubricant and a glidant. The composition has simple formula, mature preparation process, and successfully solves the problem that oral disintegrating tablets can not be packed by using the common equipment in a way of choosing adjuvants and the proportions of adjuvants by adopting the common tablet production equipment under the condition that the disintegration time limit is guaranteed. The preparation method of the pharmaceutical composition comprises the steps: the aripiprazole is crushed and sieved for use, the adjuvants are weighed up based on the formula and mixed thoroughly to obtain adjuvant mixture; the aripiprazole is weighed up based on the formula and evenly mixed with the adjuvant mixture based on the principle of progressively adding in equal amount to make into a mixture; the pharmaceutical content of the mixture is determined, the weight of a tablet is calculated, a tablet is obtained by being pressed directly, and the hardness of medicine tablet is 8-10kg.

Description

field of invention [0001] The invention relates to the field of pharmaceutical preparations, in particular to a pharmaceutical composition containing aripiprazole and a preparation method thereof. Background technique [0002] Aripiprazole, 7-[4-[4-(2,3-dichlorophenyl)-1-piperazine]butoxy]-3,4-dihydro-2(1)-quinolone , is an atypical antipsychotic drug developed by Otsuka Pharmaceutical Company, see EP367141A, US4234585, CN1028104C, etc. Aripiprazole is a quinolinone derivative and belongs to the third generation of atypical antipsychotic drugs with unique mechanism of action and pharmacological properties. Basic pharmacological research shows that this product has strong affinity to D2 and D3 and 5-HT1A and 5-HT2A receptors (Ki values ​​are 0.34, 0.8, 1.7, 3.4nmol / L), and has strong affinity to D4, 5-HT2C and 5-HT2A receptors. 5-HT7, α1-receptor and H1 receptor have strong affinity (Ki values ​​are 44, 15, 39, 57 and 61nmol / L, respectively), and have strong affinity for th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/496A61K9/20A61P25/00A61P25/18
Inventor 郭礼新杨旗明
Owner CHENGDU KANGHONG PHARMA GRP