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A kind of crystalline substance, its preparation method, its pharmaceutical composition and application

A composition and drug technology, applied in the direction of drug combination, pharmaceutical formula, anti-tumor drugs, etc., can solve the problem of little anti-tumor activity

Active Publication Date: 2019-10-11
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are few studies on the antitumor activity of these compounds

Method used

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  • A kind of crystalline substance, its preparation method, its pharmaceutical composition and application
  • A kind of crystalline substance, its preparation method, its pharmaceutical composition and application
  • A kind of crystalline substance, its preparation method, its pharmaceutical composition and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Preparation method 1 of 990207-22-1 crystal type II sample:

[0041] After 500 mg of the 990207-22-1 sample was completely dissolved at room temperature using 60 mL of tetrahydrofuran solvent, 60 mL of ethyl acetate was added, and recrystallized at room temperature to obtain the 990207-22-1 crystal type II sample, and its powder X-ray diffraction Atlas and figure 1 unanimous.

[0042] Preparation method 2 of 990207-22-1 crystal type II sample:

[0043]After completely dissolving 500 mg of the 990207-22-1 sample at 40°C using a mixed solvent of tetrahydrofuran:ethyl acetate at a ratio of 2:1, recrystallize at 40°C to obtain a 990207-22-1 crystal type II sample, Its powder X-ray diffraction pattern and figure 1 unanimous.

Embodiment 2

[0045] The preparation method 1 (tablet) of combination pharmaceutical preparation:

[0046] A method for preparing a combined drug preparation, which is characterized in that several excipients are used to prepare 990207-22-1 crystal type II pure product or a mixed crystal solid substance containing crystal type II in any proportion as the raw material drug of the combined drug. Form into tablets with a drug content of 10-300 mg per tablet, and Table 2 provides the tablet formulation:

[0047] Table 2 The preparation formula of 990207-22-1 combination medicine tablet

[0048]

[0049]

[0050] The method for preparing 990207-22-1 crystal type II pure product or mixed crystal bulk drug containing crystal type II in any proportion into tablet preparations is as follows: mix several excipients with the bulk drug evenly, and add 1% hydroxymethyl Appropriate amount of sodium cellulose solution is made into a soft material, granulated by sieving, wet granules are dried, siev...

Embodiment 3

[0052] The preparation method 2 (capsule) of combined pharmaceutical preparation:

[0053] A method for preparing a combined drug preparation, which is characterized in that several excipients are used to prepare 990207-22-1 crystal type II pure product or a mixed crystal solid substance containing crystal type II in any proportion as the raw material drug of the combined drug. Form into capsules with a drug content of 10-300 mg per grain, and the capsule formula is given in Table 3:

[0054] Table 3 Preparation formula of 990207-22-1 combination drug capsule

[0055]

[0056] The method of preparing 990207-22-1 crystal type II pure product or mixed crystal bulk drug containing crystal type II in any proportion into capsule preparations is as follows: mix several excipients with the bulk drug evenly, and add 1% hydroxymethyl Appropriate amount of sodium cellulose solution is made into wet granules, dried, sieved and granulated, added with magnesium stearate, mixed evenly, ...

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Abstract

The invention discloses a type II crystal substance of the compound 990207-22-1 (having a chemical name of 1-piperazinedithiocarbamoto-3-cyano-3,3-diphenylpropyl ester hydrochloride), a preparation method thereof, and a pharmaceutical composition and application thereof. In particular, the invention discloses a type II crystal solid substance form of the compound 990207-22-1 in solid state, a preparation method of the type II crystal sample, and application of the crystal substance of 990207-22-1 as an active ingredient in the preparation of antitumor and tumor-preventive drugs.

Description

technical field [0001] The present invention relates to the discovery of a new crystal type II substance state form of 990207-22-1 compound in a solid state; relates to the invention of a preparation method for 990207-22-1 crystal type II; relates to the invention of a compound containing 990207- 22-1 Pharmaceutical composition of crystal type II or a mixed crystal form containing any non-zero ratio of crystal type II; the present invention also relates to the use of 990207-22-1 crystal form substance as an active ingredient in the preparation of anti-tumor and tumor-preventive disease medicines application. Background technique [0002] 990207-22-1 (chemical name: 1-piperazine dithioformate-3-cyano-3,3-diphenylpropyl hydrochloride) [0003] [0004] Carbamate compounds are widely used in many fields, especially as fungicides in the field of pesticides. However, there are few studies on the antitumor activity of these compounds. [0005] Gerhauser C et al. isolated Bra...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D295/21A61K31/495A61P35/00
Inventor 李润涛吕扬崔景荣杜冠华葛泽梅杨世颖
Owner PEKING UNIV