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Composition with 3-n-butylphthalide derivative and preparation method of composition

A technology for n-butylphthalide and derivatives, which is applied to the composition of 3-n-butylphthalide derivatives and the field of preparation thereof, and can solve problems such as no clear active ingredients and the like

Inactive Publication Date: 2019-03-01
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it is worth noting that, except that CN1523003A clearly states that the active ingredient used in its composition is 2-(α-hydroxypentyl)benzoate N,N-dibenzylethylenediamine salt, there is no clear activity even in the remaining inventions. What are the ingredients, and none of the above inventions has made further research on the composition of the disclosed active compound, such as for oral tablet, granule or capsule, its stability, in vitro disintegration or dissolution, and these pharmaceutical properties , directly determines whether the active compound can be prepared into a preparation suitable for clinical use

Method used

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  • Composition with 3-n-butylphthalide derivative and preparation method of composition
  • Composition with 3-n-butylphthalide derivative and preparation method of composition
  • Composition with 3-n-butylphthalide derivative and preparation method of composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-3

[0030] Embodiment 1-3 powder-coated tablet (1000 preparation units)

[0031] Element

[0032] The preparation process is as follows.

[0033] Coating solution configuration: Add the prescribed amount of Opadry AMB coating powder into distilled water under stirring, with a solid content of about 10%, and stir for 45 minutes to fully dissolve it to obtain a uniform coating solution for later use.

[0034] Coating: Put the main ingredient in the fluidized bed, spray the coating on the top of the fluidized bed, make the distance between the nozzle and the material 10-11cm, feed compressed air to suspend the material, preheat for 5 minutes, increase the air volume and start spraying Liquid coating, the temperature of the material is controlled during the coating process, and after the coating is completed, it is dried for 5-10 minutes. The coating weight gain is controlled at 10-40%, and the detailed coating parameters are shown in the table below:

[0035] The...

Embodiment 4-6

[0037] Embodiment 4-6 granule-coated tablet (1000 preparation units)

[0038] Element

[0039] The preparation process is as follows.

[0040] Preparation of granules: mix the main drug, microcrystalline cellulose and hypromellose evenly, use 95% ethanol to make a soft material, granulate with a 32-mesh sieve, dry, and granulate with a 30-mesh sieve.

[0041] Coating solution configuration: Add the prescribed amount of Opadry AMB coating powder into distilled water under stirring, with a solid content of about 10%, and stir for 45 minutes to fully dissolve it to obtain a uniform coating solution for later use.

[0042] Coating: Put the above granules in a fluidized bed, spray coating on the top of the fluidized bed, make the distance between the nozzle and the material 10-11cm, feed compressed air to suspend the material, preheat for 5 minutes, increase the air volume and start spraying Liquid coating, the temperature of the material is controlled during the coating...

Embodiment 7-9

[0045] Example 7-9 Tablet Core Coating (1000 formulation units)

[0046] Element

Example 7

Example 8

Example 9

2-(α-Hydroxypentyl)benzoic acid potassium salt

200g

200g

200g

microcrystalline cellulose

50g

50g

50g

hypromellose

8g

8g

8g

Magnesium stearate

2g

2g

2g

Opadry AMB

2.6g

7.2g

13g

[0047] The preparation process is as follows.

[0048] Tablet core preparation: mix the main drug, microcrystalline cellulose and hypromellose evenly, use 95% ethanol to make a soft material, granulate with a 32-mesh sieve, dry, granulate with a 30-mesh sieve, mix the above-mentioned granules with stearin Magnesium acid is mixed evenly and pressed into tablets with a hardness of 50-120N.

[0049]Coating solution configuration: Add the prescribed amount of Opadry AMB coating powder into distilled water under stirring, with a solid content of about 10%, and stir for 45 minutes to fully diss...

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PUM

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Abstract

The invention discloses a composition with a 3-n-butylphthalide derivative and a preparation method of the composition. The composition is prepared from the 3-n-butylphthalide derivative, a dampproofcoating layer and other pharmaceutical excipients, wherein the dampproof coating layer contains AMB-type Opadry. The invention further provides the preparation method of the composition with the 3-n-butylphthalide derivative, and the preparation method is characterized in that powder coating, particle coating or tablet coating are adopted, AMB-type Opadry coating powder needs to be dissolved intodistilled water before coating, and a uniform coating solution is formed after full dissolving.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a composition of 3-n-butylphthalide derivatives and a preparation method thereof. Background technique [0002] Acute ischemic stroke, coronary heart disease, and myocardial infarction are all diseases caused by atherosclerosis until thrombosis leads to ischemic injury. These diseases bring great pain to patients and even endanger their lives. At present, this type of drug has always been the hot spot and frontier of drug research and development. [0003] Chinese patent CN1382682A discloses 2-(α-hydroxypentyl) benzoate and its preparation method and application, relates to salts of monovalent metal ions, divalent metal ions and organic bases, specifically discloses potassium, sodium, Salts of calcium, magnesium, zinc, aniline, benzylamine, morpholine, diethylamine. It also discloses the effect of potassium salt on cerebral infarct size and rat platelet aggregation in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K9/14A61K9/16A61K31/192A61K47/38A61P9/10A61P7/02A61P9/06
Inventor 陈亚平王世霞赫玉霞金晓利吴欢欢刘英帝杨敏
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD