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A kind of 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 poor fluidity, lack of API, and reduced standard tableting speed

Active Publication Date: 2020-07-10
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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  • A kind of pharmaceutical composition and preparation method thereof
  • A kind of pharmaceutical composition and preparation method thereof
  • A kind of pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] prescription:

[0036]

[0037] Taking materials according to the above prescription, mixing the active substance, lactose, microcrystalline cellulose and crospovidone to obtain an intermediate mixture, adding silicon dioxide and magnesium stearate and mixing to obtain a final mixture.

[0038] Directly observe the electrostatic state of each mixture powder in the whole process with the naked eye, and find that the intermediate mixtures are all electrostatically charged, but the electrostatic state of the final mixture of each prescription is different, and the measured particle content is different. The results are shown in Table 1 below.

[0039] Table 1 Experimental related results of Example 1

[0040] combination A B C D E character 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 refers to the measured value / theoret...

Embodiment 2

[0044] Taking the composition C of Example 1 as an object, explore the impact of different mixing processes on the composition and the final tablet (directly made from composition C tablet compression), the technological scheme is summarized as follows:

[0045]

[0046] Note: Premix I, premix II, and final mixing are steps carried out in sequence, that is, add all the materials to the mixture obtained in the previous step, and then mix.

[0047] Result: 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 from the premixing of scheme 1 had static electricity, while the intermediate mixture obtained from scheme 2 premix I and premix II had no static electricity. Static electricity; take 6 samples of the mixture obtained in each step, measure the particle content and calculate the deviation RSD, the results are shown in Table 2.1 and 2.2.

[0048] Table 2.1 Mixing Uniformity ...

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％ 98％ 30 98％ 99％

[0075] Dissolution curve comparison see figure 1 .

[0076] Clea...

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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 invention relates to the field of pharmacy, in particular 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, usually obtained by direct synthesis, the active ingredient (API) is needle-shaped, which leads to: [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, [0005] 3. Tablet capping or lamination during the direct compression process caused by too much air trapped 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 the dry granulation process and...

Claims

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Application Information

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Patent Type & Authority Patents(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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