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Venetoclaxnanocrystal oral solid medicinal composition

A technology of nanocrystals and venetola, applied in the field of medicine, can solve the problems of low bioavailability of final preparations, reduced patient compliance, and large tablet size.

Inactive Publication Date: 2018-11-20
天津双硕医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] But even so, the bioavailability of its final preparation product is still not high
And due to the use of solid dispersion technology and its own large size, the weight of the final product is relatively large, and the weight of each 100mg tablet exceeds 1.0g
Restricts the medication of elderly patients and other people who have difficulty swallowing, and seriously reduces the patient's compliance

Method used

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  • Venetoclaxnanocrystal oral solid medicinal composition
  • Venetoclaxnanocrystal oral solid medicinal composition
  • Venetoclaxnanocrystal oral solid medicinal composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0102] Example 1 Preparation of 50 mg venetoclax tablet (unit: g)

[0103] prescription:

[0104] .

[0105] The pharmaceutical composition of the venetora nanocrystals is further prepared into tablets by the following steps:

[0106] 1) Take the raw material of venetora and pulverize it, pass through a 200-mesh sieve, and set aside;

[0107] 2) Sodium cholate and hydroxypropyl cellulose were dissolved in purified water successively, with concentrations of 3% and 5%;

[0108] 3) dispersing the venetora crude drug obtained in step 1) in the solution obtained in step 1), with a concentration of 5%;

[0109] 4) Add the suspension obtained in step 3) into a high-pressure homogenizer, and circulate it 10 times under a pressure of 500 bar to obtain a suspension of venetora nanocrystals;

[0110] 5) taking step 4) obtained venetoclax nanocrystal suspension, and spray drying to obtain venetoclax nanocrystal;

[0111] 6) Take the venetoclax nanocrystals obtained in step 5), add ...

Embodiment 2

[0113] Example 2 Preparation of 100 mg venetoclax tablet (unit: g)

[0114] prescription:

[0115] .

[0116] The pharmaceutical composition of the venetora nanocrystals is further prepared into tablets by the following steps:

[0117] 1) Take the raw material of venetora and pulverize it, pass through a 200-mesh sieve, and set aside;

[0118] 2) Sodium cholate and hydroxypropyl cellulose were dissolved in purified water successively, with concentrations of 3% and 5%;

[0119] 3) dispersing the venetora crude drug obtained in step 1) in the solution obtained in step 1), with a concentration of 5%;

[0120] 4) Add the suspension obtained in step 3) into a high-pressure homogenizer, and circulate it 10 times under a pressure of 500 bar to obtain a suspension of venetora nanocrystals;

[0121] 5) taking step 4) obtained venetoclax nanocrystal suspension, and spray drying to obtain venetoclax nanocrystal;

[0122] 6) Take the venetoclax nanocrystals obtained in step 5), add...

Embodiment 3

[0124] Example 3 Preparation of 50 mg venetoclax hard capsules (unit: g)

[0125] prescription:

[0126]

[0127] .

[0128] The pharmaceutical composition of the venetora nanocrystals is further prepared into hard capsules through the following steps:

[0129] 1) Take the raw material of venetora and pulverize it, pass through a 200-mesh sieve, and set aside;

[0130] 2) Sodium cholate and hydroxypropyl cellulose were dissolved in purified water successively, with concentrations of 3% and 5%;

[0131] 3) dispersing the venetora crude drug obtained in step 1) in the solution obtained in step 1), with a concentration of 5%;

[0132] 4) Add the suspension obtained in step 3) into a high-pressure homogenizer, and circulate it 10 times under a pressure of 500 bar to obtain a suspension of venetora nanocrystals;

[0133] 5) taking step 4) obtained venetoclax nanocrystal suspension, and spray drying to obtain venetoclax nanocrystal;

[0134] 6) Take the venetoclax nanocrys...

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Abstract

The invention relates to a venetoclaxnanocrystal oral solid medicinal composition and a preparation method and application thereof. The inventor applies a nanotechnology to a venetoclax raw material to prepare a venetoclaxnanocrystal so as to prepare an oral solid preparation. Ultimately, a preparation technology of the venetoclaxnanocrystal is obtained and a venetoclaxnanocrystal raw material with high water solubility is obtained. The venetoclaxnanocrystal raw material is further prepared into an ordinary oral solid preparation. Tests prove that the dissolution behavior of the venetoclax oral solid preparation prepared by the technology is significantly improved, so that the bioavailability is also improved. The preparation technology is simple, the quality is controllable, and the preparation technology is suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a venetora nanocrystal oral solid pharmaceutical composition and a preparation method and application thereof. Background technique [0002] The Bcl-2 protein was first discovered in 1986 and is expressed by the Bcl-2 gene. The Bcl-2 gene is a proto-oncogene, and the protein it expresses is called the Bcl-2 family protein. The Bcl-2 family protein is an important protein in the apoptosis pathway, and plays a key role in the occurrence and metastasis of tumors. By forming dimers with Bax protein and self-dimerization, Bcl-2 protein plays an important role in the regulation of apoptosis: when Bcl-2 protein is inhibited, it dimerizes with Bax protein, which leads to Apoptosis: When Bcl-2 protein is overexpressed, the heterodimer formed by it and Bax protein increases, and cell apoptosis is inhibited. The balance between Bcl-2 and Bax proteins at cell death signaling ...

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K9/48A61K47/38A61K47/28A61K47/32A61K47/04A61K47/12A61K31/635A61P35/00C07D471/04
CPCA61K9/2009A61K9/2013A61K9/2027A61K9/2054A61K9/2095A61K9/2866A61K9/4808A61K9/485A61K9/4858A61K9/4866A61K31/635A61P35/00C07D471/04A61K31/496
Inventor 不公告发明人
Owner 天津双硕医药科技有限公司
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