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Enzalutamide nano crystal oral solid pharmaceutical composition

A technology for enzalutamide and nanocrystals, which is applied in the field of enzalutamide nanocrystal oral solid pharmaceutical compositions and the preparation thereof, can solve the problems of easy adhesion, high labor intensity, affecting product quality and yield, etc.

Inactive Publication Date: 2018-11-16
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

Finally, the production of soft capsules is a continuous process with high labor intensity. The resulting pre-packaged products are prone to adhesion and leakage, which affects the quality and yield of the final product.

Method used

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  • Enzalutamide nano crystal oral solid pharmaceutical composition
  • Enzalutamide nano crystal oral solid pharmaceutical composition
  • Enzalutamide nano crystal oral solid pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0110] Example 1 Preparation of 40 mg Enzalutamide Tablets (Unit: g)

[0111] prescription:

[0112]

[0113] The pharmaceutical composition of the enzalutamide nanocrystals is further prepared into tablets by the following steps:

[0114] 1) Take the enzalutamide bulk drug and pulverize it, pass it through a 200-mesh sieve, and set aside;

[0115] 2) Take tyloxapol and polyvinyl alcohol and dissolve them in purified water successively, the concentrations are 2% and 10%;

[0116] 3) Disperse the enzalutamide bulk drug obtained in step 1) in the solution obtained in step 1), with a concentration of 5%;

[0117] 4) Add the suspension obtained in step 3) into a high-pressure homogenizer, and circulate it 7 times under a pressure of 100 bar to obtain a suspension of enzalutamide nanocrystals;

[0118] 5) Take the enzalutamide nanocrystal suspension obtained in step 4), and spray dry to obtain the enzalutamide nanocrystal;

[0119] 6) Take the enzalutamide nanocrystals obtai...

Embodiment 2

[0121] Example 2 Preparation of 80 mg Enzalutamide Tablets (Unit: g)

[0122] prescription:

[0123]

[0124]

[0125] The pharmaceutical composition of the enzalutamide nanocrystals is further prepared into tablets by the following steps:

[0126] 1) Take the enzalutamide bulk drug and pulverize it, pass it through a 200-mesh sieve, and set aside;

[0127] 2) Take tyloxapol and polyvinyl alcohol and dissolve them in purified water successively, the concentrations are 2% and 10%;

[0128] 3) Disperse the enzalutamide bulk drug obtained in step 1) in the solution obtained in step 1), with a concentration of 5%;

[0129] 4) Add the suspension obtained in step 3) into a high-pressure homogenizer, and circulate it 7 times under a pressure of 100 bar to obtain a suspension of enzalutamide nanocrystals;

[0130] 5) Take the enzalutamide nanocrystal suspension obtained in step 4), and spray dry to obtain the enzalutamide nanocrystal;

[0131] 6) Take the enzalutamide nanocr...

Embodiment 3

[0133] Example 3 Preparation of 160 mg Enzalutamide Tablets (Unit: g)

[0134] prescription:

[0135]

[0136] The pharmaceutical composition of the enzalutamide nanocrystals is further prepared into tablets by the following steps:

[0137] 1) Take the enzalutamide bulk drug and pulverize it, pass it through a 200-mesh sieve, and set aside;

[0138] 2) Take tyloxapol and polyvinyl alcohol and dissolve them in purified water successively, the concentrations are 2% and 10%;

[0139] 3) Disperse the enzalutamide bulk drug obtained in step 1) in the solution obtained in step 1), with a concentration of 5%;

[0140] 4) Add the suspension obtained in step 3) into a high-pressure homogenizer, and circulate it 7 times under a pressure of 100 bar to obtain a suspension of enzalutamide nanocrystals;

[0141] 5) Take the enzalutamide nanocrystal suspension obtained in step 4), and spray dry to obtain the enzalutamide nanocrystal;

[0142] 6) Take the enzalutamide nanocrystals obta...

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Abstract

The invention relates to an enzalutamide nano crystal oral solid pharmaceutical composition, and a preparation method and applications thereof. The raw materials of enzalutamide are processed by a nano technology to prepare enzalutamide nano crystals, and then an oral solid preparation is prepared from the enzalutamide nano crystals. The test results show that the effect is good. Through a seriesof tests, an enzalutamide nano crystal preparation technology is obtained finally, and enzalutamide nano crystals with good water solubility are obtained. By selecting the adjuvants, the degradation of amido bonds and lactam bonds of bulk drugs is inhibited, and the enzalutamide nano crystals are made into a common oral solid preparation. The test results show that the dissolving-out behavior of the oral solid preparation prepared by the technology is obviously improved and the bioavailability is enhanced at the same time. At the same time, the hydrolysis impurities are inhibited, the stability is improved, the preparation technology is simple and suitable for industrial production, and the quality is controllable.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an enzalutamide nano-crystal oral solid pharmaceutical composition and a preparation method and application thereof. Background technique [0002] Prostate cancer refers to epithelial malignant tumors that occur in the prostate. According to the 2004 WHO "Pathology and Genetics of Tumors of the Urinary System and Male Genital Organs", the pathological types of prostate cancer include adenocarcinoma (acinar adenocarcinoma), ductal adenocarcinoma, urothelial carcinoma, squamous cell carcinoma, and adenosquamous carcinoma. Among them, prostate adenocarcinoma accounts for more than 95%. Therefore, what we usually call prostate cancer refers to prostate adenocarcinoma. [0003] Prostate cancer incidence has marked geographic and ethnic disparities, with highest rates in Australia / New Zealand, the Caribbean, and Scandinavia and lower rates in Asia and North Africa. World...

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K9/48A61K31/4166A61K47/32A61P13/08A61P35/00C07D233/86
CPCA61K9/2027A61K9/2866A61K9/4866A61K31/4166A61P13/08A61P35/00C07B2200/13C07D233/86
Inventor 不公告发明人
Owner 天津双硕医药科技有限公司
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