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Pharmaceutical composition and preparation method thereof

A composition and drug technology, applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, block delivery, etc., can solve problems such as low bulk density, inappropriate content measurement values, and reduced selectivity

Active Publication Date: 2016-05-04
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] 1. Large changes in the low bulk density caused by the random arrangement and length of the needles,
[0004] 2. Poor fluidity caused by increased resistance of needles aligned in the direction of flow,
[0007] 5. Adhesion of API on surfaces caused by increased static charge which leads to reduced selectivity of API in powder mixtures during processing and thus lack of API in manufactured tablets which would appear inappropriate The measured value of the content
This requires a substantial reduction in standard compression speeds and results in higher variations in compaction force and tablet quality due to incomplete filling of the die
Unable to achieve target tablet quality and acceptable tablet hardness due to extremely high powder volume
In addition, the high pressure force applied during the tableting process can cause capping, while the low pressure force can cause tablet adhesion

Method used

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  • Pharmaceutical composition and preparation method thereof
  • Pharmaceutical composition and preparation method thereof
  • Pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] prescription:

[0036]

[0037] According to the above recipe, take the materials, mix the active substance, lactose, microcrystalline cellulose and crospovidone to obtain an intermediate mixture, then add silicon dioxide and mix with magnesium stearate to obtain the final mixture.

[0038] The static state of each mixture powder in the whole process was directly observed with the naked eye, and it was found that the intermediate mixtures were all electrostatically charged, but the static state of the final mixture of each recipe was different, and the measured particle content was different. The results are shown in Table 1 below.

[0039] Table 1 Example 1 Experiment related results

[0040] combination

A

B

C

D

E

traits

Static electricity

good

good

good

Static electricity

particle content

93.2％

98.7％

99.8％

98.1％

94.9％

[0041] Note: The particle content in this article refer...

Embodiment 2

[0044] Taking the composition C of Example 1 as the object, the influence of different mixing processes on the composition and the final tablet (directly obtained by pressing the composition C) was explored. The process scheme is summarized as follows:

[0045]

[0046] Note: Premix I, premix II, and total mixing are steps performed in sequence, that is, all materials are added to the mixture obtained in the previous step, and then mixed.

[0047] Results: It was observed that the compositions obtained after the total mixing of Schemes 1 and 2 had no static electricity, but the intermediate mixture obtained by the premixing scheme 1 had static electricity, while the intermediate mixtures obtained by the premixing I and the premixing II scheme 2 had no static electricity. Electrostatic; take 6 samples of the mixture obtained in each step, measure its particle content and calculate its deviation RSD, the results are shown in Table 2.1, 2.2.

[0048] Table 2.1 Mixing uniformit...

Embodiment 3

[0067] 1. Prescription

[0068] tablet

Reference preparation

C

Element

mg / tablet

mg / tablet

active substance

59.12

59.12

Lactose

247.72

234

microcrystalline cellulose

36.96

50.68

Crospovidone

7.2

5.4

silica

1.8

3.6

Magnesium stearate

7.2

7.2

[0069] 2. Preparation process

[0070] 2.1 The samples of the reference preparation were prepared by dry granulation process;

[0071] 2.2 Tablet C uses the preparation process of Scheme 2 in Example 2 to prepare samples, and the hardness is controlled at 5-7kg / cm 2 .

[0072] 3. Dissolution

[0073] The dissolution rate of the tablet was determined according to the dissolution method used in the above table 2.3, and the results of the dissolution data are as follows:

[0074] time / min

Reference preparation

tablet C

5

56％

93％

10

96％

98％

15

97％

9...

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Abstract

The present invention discloses a pharmaceutical composition and a preparation method thereof, particularly to a pharmaceutical composition, which comprises an active substance (2E)-N-(4-((3-chloro-4-fluorophenyl)amino)-7-(((3S)-tetrahydro-3-furanyl)oxy)-6-quinazolinyl)-4-(dimethylamino)-2-butenamide dimaleate, a carrier, a disintegrant, a glidant and a lubricant. The composition of the present invention is hardly electrostatically charged, and is suitable for being directly prepared into the solid preparation. The present invention further discloses a solid preparation prepared from the composition.

Description

technical field [0001] The present invention relates to the field of pharmacy, and more particularly, to a pharmaceutical composition and a solid preparation prepared therefrom. Background technique [0002] Drug (2E)-N-(4-((3-Chloro-4-fluorophenyl)amino)-7-(((3S)-tetrahydro-3-furyl)oxy)-6-quinazoline base)-4-(dimethylamino)-2-butenamide dimaleate, the active ingredient (API) usually obtained by direct synthesis is needle-shaped, which results in: [0003] 1. The large change in the low bulk density caused by the random arrangement and length of the needles, [0004] 2. Poor fluidity caused by increased resistance of needles aligned in the direction of flow, [0005] 3. Capping or delamination of tablets during the direct compression process caused by too much air entrapment inside the final blend, [0006] 4. Low compressibility, the active ingredient is also combined with other excipients such as binders or fillers, which results in mechanically weaker granules during t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/517A61K9/20
Inventor 拥青她姆周炳城危军涂炎君
Owner JIANGSU HANSOH PHARMA CO LTD
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