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Solid dispersion and tablets comprising abiraterone acetate, and preparation methods thereof

A technology of abiraterone acetate and solid dispersion, which is applied in the direction of medical preparations containing active ingredients, medical preparations with non-active ingredients, pill delivery, etc., to achieve the effects of convenient operation, improved water solubility, and simple preparation process

Active Publication Date: 2013-05-01
SHANDONG NEWTIME PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no bibliographical report of a kind of abiraterone acetate tablet with higher dissolution rate in the prior art

Method used

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  • Solid dispersion and tablets comprising abiraterone acetate, and preparation methods thereof
  • Solid dispersion and tablets comprising abiraterone acetate, and preparation methods thereof
  • Solid dispersion and tablets comprising abiraterone acetate, and preparation methods thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1 Abiraterone acetate tablet preparation

[0026] 1.1 Solid dispersion ratio and preparation process

[0027] 1 part abiraterone acetate

[0028] Povidone K30 1.5 parts

[0029] 3 parts chloroform

[0030] Abiraterone acetate and povidone were dissolved in chloroform and dried under reduced pressure to obtain solid dispersion A.

[0031] 1.2 Micropowder grinding ratio and preparation process

[0032] 1 part of solid dispersion A

[0033] 1 part water

[0034] Disperse the solid dispersion A in water, carry out micropowder grinding, the grinding time is 1h, D (0.9) is less than 50 microns, and obtain the suspension B.

[0035] 1.3 Preparation of Abiraterone Acetate Tablets

[0036]

[0037] Preparation Process:

[0038] (1) Prescription quantity takes lactose and crospovidone that have passed through a 100-mesh sieve, mixes them evenly, and sets aside;

[0039] (2) Add all the suspension B into (1), granulate, dry, add magnesium stearate, and compr...

Embodiment 2

[0040] Embodiment 2 Abiraterone acetate tablet preparation

[0041] 2.1 Solid dispersion ratio and preparation process

[0042] 1 part abiraterone acetate

[0043] Povidone K30 1.5 parts

[0044] 3 parts chloroform

[0045] Abiraterone acetate and povidone were dissolved in chloroform and dried under reduced pressure to obtain solid dispersion A.

[0046] 2.2 Micropowder grinding ratio and preparation process

[0047] 1 part of solid dispersion A

[0048] 1 part water

[0049] Disperse the solid dispersion A in water, carry out micropowder grinding for 3 hours, D (0.9) is less than 15 microns, and obtain the suspension B.

[0050] 2.3 Preparation of Abiraterone Acetate Tablets

[0051]

[0052] Preparation Process:

[0053] (1) Prescription quantity takes lactose and crospovidone that have passed through a 100-mesh sieve, mixes them evenly, and sets aside;

[0054] (2) Add all the suspension B into (1), granulate, dry, add magnesium stearate, and compress into tabl...

Embodiment 3

[0055] Embodiment 3 Abiraterone acetate tablet preparation

[0056] 3.1 Solid dispersion ratio and preparation process

[0057] 1 part abiraterone acetate

[0058] Povidone K30 1.5 parts

[0059] 3 parts chloroform

[0060] Abiraterone acetate and povidone were dissolved in chloroform and dried under reduced pressure to obtain solid dispersion A.

[0061] 3.2 Micropowder grinding ratio and preparation process

[0062] 1 part of solid dispersion A

[0063] 1 part water

[0064] Disperse the solid dispersion A in water, perform micropowder grinding for 6 hours, D (0.9) is less than 3 microns, and obtain the suspension B.

[0065] 3.3 Preparation of Abiraterone Acetate Tablets

[0066]

[0067] Preparation Process:

[0068] (1) Prescription quantity takes lactose and crospovidone that have passed through a 100-mesh sieve, mixes them evenly, and sets aside;

[0069] (2) Add all the suspension B into (1), granulate, dry, add magnesium stearate, and compress into tablets t...

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Abstract

The invention relates to a solid dispersion and tablets comprising abiraterone acetate, and preparation methods thereof. The solid dispersion is prepared through the steps that: abiraterone acetate and povidone with a weight ratio of 1:0.5-4 are dissolved in chloroform; and reduced-pressure drying is carried out, such that the solid dispersion is obtained. The tablets comprises 1 part of the abiraterone acetate solid dispersion, 2-8 parts of a filling agent, 0.2-0.8 parts of a disintegrating agent, and 0.05-0.1 parts of a lubricant. According to the invention, a micronization technology and a solid dispersion technology are creatively combined, such that abiraterone acetate water solubility is greatly improved. Therefore, abiraterone acetate can be rapidly dissolved in gastrointestinal tract body fluids.

Description

technical field [0001] The invention belongs to the technical field of western medicine preparations, in particular to a solid preparation of abiraterone acetate, in particular to a solid dispersion containing abiraterone acetate, a tablet and a preparation method thereof. Background technique [0002] The number of people diagnosed with cancer has increased significantly, with particular concern being diagnosed with androgen-dependent diseases such as prostate cancer, which is the second leading cause of cancer-related death in men after lung cancer. Abiraterone, invented by researchers at the Royal Marsden Hospital in Southwest London, is a key enzyme in androgen synthesis, 17α-hydroxylase-C17, 2-lyase 17α-monooxygenase inhibitors or human cytochrome P450 17 An effective selective oral inhibitor of α, which reduces androgen levels by inhibiting the key enzyme in androgen synthesis - CYP450c17, and has inhibitory effects on androgen in the testis and other parts of the bod...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/20A61K31/58A61K47/32A61P5/28
Inventor 赵志全郝贵周丁兵韩忠丽
Owner SHANDONG NEWTIME PHARMA
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