Pramipexole dihydrochloride sustained-release preparation and preparing method thereof

A technology for pramipexole hydrochloride and sustained-release preparations, which is applied in the field of pramipexole hydrochloride sustained-release preparations and its preparation, which can solve the problems of insufficiently stable release and too fast release, achieve uniform and stable content, and avoid different release amounts.

Active Publication Date: 2018-06-15
CHENGDU BAIYU PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Most of the pramipexole hydrochloride sustained-release tablets currently on the market are three times a day, which brings great inconvenience to Parkinson's patients with limited mobility
Chinese patent CN104606162A discloses a sustained-release preparatio

Method used

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  • Pramipexole dihydrochloride sustained-release preparation and preparing method thereof
  • Pramipexole dihydrochloride sustained-release preparation and preparing method thereof
  • Pramipexole dihydrochloride sustained-release preparation and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Embodiment 1 The preparation of pramipexole hydrochloride sustained-release preparation of the present invention

[0044] 1. The dosage of each component of pramipexole hydrochloride sustained-release preparation

[0045] The components and dosages of pramipexole hydrochloride sustained-release preparations in Example 1 are shown in Table 1.

[0046] Components of pramipexole hydrochloride sustained-release preparation in table 1 embodiment 1

[0047] Name of raw material

Dosage per tablet / mg

Weight percentage / %

Dosage / g

pramipexole hydrochloride

0.375

0.15%

0.5625

Hypromellose K15

60

24.00%

90

Eudragit RS

20

8.00%

30

pregelatinized starch

122.125

48.85%

183.1875

Microcrystalline Cellulose KG802

40

16.00%

60

Magnesium stearate

2.5

1.00%

3.75

silica

5

2.00%

7.5

total

250

100.00%

375

[0048] 2. Preparation of Pramipexo...

Embodiment 2

[0055] Embodiment 2 Preparation of pramipexole hydrochloride sustained-release preparation of the present invention

[0056] 1. The dosage of each component of pramipexole hydrochloride sustained-release preparation

[0057] The components and dosages of pramipexole hydrochloride sustained-release preparations in Example 2 are shown in Table 2.

[0058] Components of pramipexole hydrochloride sustained-release preparation in table 2 embodiment 2

[0059] Name of raw material

Dosage per tablet / mg

Percent content / %

Dosage / g

pramipexole hydrochloride

0.375

0.15%

0.5625

Hydroxypropyl Cellulose-H

40

26.00%

97.5

Carbomer 934P

35

14.00%

52.5

Ethylcellulose-N

25

10.00%

37.5

pregelatinized starch

77.125

30.85%

115.6875

Microcrystalline Cellulose KG802

40

16.00%

60

Magnesium stearate

2.5

1.00%

3.75

silica

5

2.00%

7.5

total

250

...

Embodiment 3

[0067] Embodiment 3 Preparation of pramipexole hydrochloride sustained-release preparation of the present invention

[0068] 1. The dosage of each component of pramipexole hydrochloride sustained-release preparation

[0069] The components and dosages of pramipexole hydrochloride sustained-release preparations in Example 3 are shown in Table 3.

[0070] Components of pramipexole hydrochloride sustained-release preparation in table 3 embodiment 3

[0071] Name of raw material

Dosage per tablet / mg

Percent content / %

Dosage / g

pramipexole hydrochloride

0.375

0.15%

0.5625

Hypromellose K100

25

10.00%

37.5

Eudragit RL100

20

8.00%

30

Ethylcellulose-N

77.125

30.85%

115.6875

Microcrystalline Cellulose PH302

120

48.00%

180

Sodium stearate fumarate

2.5

1.00%

3.75

silica

5

2.00%

7.5

total

250

100.00%

375

[0072] 2. Preparation of Pramipe...

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Abstract

The invention discloses a pramipexole dihydrochloride sustained-release preparation and a preparing method thereof, and belongs to the field of pharmaceutical preparations. The invention provides thepramipexole dihydrochloride sustained-release preparation which is prepared from the following raw and auxiliary materials by weight: 1-5 parts of pramipexole dihydrochloride, 35-140 parts of a sustained-release material, 130-400 parts of a skeleton material, 300-750 parts of a diluent, 10-20 parts of a flow aid, and 5-15 parts of a lubricant. The invention also provides the preparing method of the sustained-release preparation, wherein the preparing method includes the following steps: (1) taking pramipexole dihydrochloride, and crushing; (2) mixing the sustained-release material and pramipexole dihydrochloride evenly; (3) adding the skeleton material and the diluent, and mixing evenly; (4) making the mixture obtained in the step (3) into dry particles; (5) mixing the dry particles with the lubricant and the flow aid, to obtain an intermediate; and (6) tabletting. Under the specific ratio and granulating process, the sustained-release preparation has the advantages of uniform content,stable release and reliable quality, can be released evenly in various dissolving media with different pH, and is suitable for oral administration once a day.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a pramipexole hydrochloride sustained-release preparation and a preparation method thereof. Background technique [0002] Parkinson's disease (PD) is a common neurodegenerative disease. The main pathological change of Parkinson's disease is the degeneration and death of dopamine (DA) neurons in the substantia nigra of the midbrain, which leads to a significant decrease in the content of DA in the striatum and causes the disease. The exact cause of this pathological change is still unclear. Genetic factors, environmental factors, aging, oxidative stress, etc. may all be involved in the degeneration and death process of PD dopaminergic neurons. [0003] Pramipexole is a synthetic derivative of aminobenzothiazole. Pramipexole hydrochloride in the present invention refers to pramipexole dihydrochloride monohydrate, chemical name: monohydrate dihydrochloride (S)-2-amino-6-...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/428A61K47/32A61K47/10A61K47/38A61P25/16
CPCA61K9/2027A61K9/2031A61K9/2054A61K31/428
Inventor 陈彦杨勇
Owner CHENGDU BAIYU PHARMA CO LTD
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