Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Abiraterone acetate soft capsule and preparation method thereof

A technology of abiraterone acetate and soft capsules, which is applied in capsule delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., and can solve problems such as low solubility, precipitation of abiraterone, and poor oral bioavailability

Pending Publication Date: 2021-11-09
HANGZHOU HEZE PHARMA TECH +1
View PDF7 Cites 4 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the co-emulsifiers ethanol and propylene glycol used in this patent can be released from the contents during storage, resulting in a serious reduction in the content of ethanol or propylene glycol in the contents, which may cause the precipitation of abiraterone during long-term storage
[0011] In summary, it can be seen that abiraterone acetate has the characteristics of low solubility and poor osmotic pressure. By pulverizing abiraterone acetate and controlling the particle size in a small range, the problem of poor oral bioavailability cannot be significantly solved. However, the preparation of abiraterone acetate into liquid capsules can obviously improve the oral bioavailability of abiraterone acetate and eliminate the influence of food in theory, but the content of the liquid capsules consists of propylene glycol or ethanol, which is volatile and may cause Abiraterone can precipitate during long-term storage

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Abiraterone acetate soft capsule and preparation method thereof
  • Abiraterone acetate soft capsule and preparation method thereof
  • Abiraterone acetate soft capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] The present embodiment provides a kind of abiraterone acetate soft capsule (batch: 1000), and its content comprises following component:

[0063]

[0064]

[0065] The above pharmaceutical composition is filled in the soft capsule shell as the content, and the components of the soft capsule shell include: gelatin, water, glycerin, sorbitol and sorbitan solution MDF85, and the ratio of each component is 1:0.74:0.35:0.35.

[0066] The preparation method is provided as follows:

[0067] 1) Chemical glue: Add the prescribed amount of glycerin, sorbitol and water into the chemical glue barrel, start stirring, seal and heat to 75°C, after the materials are evenly mixed, add the prescribed amount of gelatin, and simultaneously vacuumize to -0.05~ -0.06MPa, keep stirring under negative pressure for 25-35min, open the capping respirator until the vacuum disappears, keep warm and degas at 55-60°C, and wait for use; 2) Preparation of contents: Dissolve abiraterone acetate in...

Embodiment 2

[0069] The present embodiment provides a kind of abiraterone acetate soft capsule (batch: 1000), and its content comprises following component:

[0070]

[0071] The above pharmaceutical composition is filled in the soft capsule shell as the content, and the components of the soft capsule shell include: gelatin, water, glycerin, sorbitol and sorbitan solution MDF85, and the ratio of each component is 1:0.74:0.35:0.35.

[0072] The preparation method is provided as follows:

[0073] 1) Chemical glue: Add the prescribed amount of glycerin, sorbitol and water into the chemical glue barrel, start stirring, seal and heat to 75°C, after the materials are evenly mixed, add the prescribed amount of gelatin, and simultaneously vacuumize to -0.05~ -0.06MPa, keep stirring under negative pressure for 25-35min, open the capping respirator until the vacuum disappears, keep warm and degas at 55-60°C, and wait for use; 2) Preparation of contents: Dissolve abiraterone acetate in In the mix...

Embodiment 3

[0075] The present embodiment provides a kind of abiraterone acetate soft capsule (batch: 1000), and its content comprises following component:

[0076]

[0077]

[0078] The above pharmaceutical composition is filled in the soft capsule shell as the content, and the components of the soft capsule shell include: gelatin, water, glycerin, sorbitol and sorbitan solution MDF85, and the ratio of each component is 1:0.74:0.35:0.35.

[0079] The preparation method is provided as follows:

[0080] 1) Chemical glue: Add the prescribed amount of glycerin, sorbitol and water into the chemical glue barrel, start stirring, seal and heat to 75°C, after the materials are evenly mixed, add the prescribed amount of gelatin, and simultaneously vacuumize to -0.05~ -0.06MPa, keep stirring under negative pressure for 25-35min, open the capping respirator until the vacuum disappears, keep warm and degas at 55-60°C, and wait for use; 2) Preparation of contents: Dissolve abiraterone acetate in...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Concentrationaaaaaaaaaa
Login to View More

Abstract

The invention discloses an abiraterone acetate soft capsule and a preparation method thereof. The abiraterone acetate soft capsule consists of a content and a capsule shell, wherein the content comprises abiraterone acetate, caprylic / capric acid mono / diglyceride, Tween 80, Span 80 and butylated hydroxyanisole; and the capsule shell is made of soft capsule materials and comprises gelatin, water, glycerol and a sorbitol and sorbitan solution, wherein the ratio of the gelatin to the water to the glycerol to the sorbitol and sorbitan solution is 1: 0.74: 0.35: 0.35. After the abiraterone acetate soft capsule provided by the invention is orally taken on the empty stomach, compared with an original research medicine Zytiga (the specification is 250mg), the step of dissolving out the original research medicine Zytiga in the digestive tract is not required, the oral bioavailability is improved to 12.5 times, variability among individuals is low, and the phenomenon that the exposure quantity of abiraterone is obviously increased due to postprandial administration of the original research medicine Zytiga is eliminated.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to an abiraterone acetate soft capsule and a preparation method thereof. Background technique [0002] Abiraterone Acetate is a white to off-white, non-hygroscopic crystalline powder. Abiraterone acetate is a prodrug of abiraterone, a selective irreversible inhibitor of 17α-hydroxylase / C17,20-lyase (CYP17). The enzyme is expressed in testis and adrenal gland tissues and catalyzes the conversion of pregnene and nandrolone and progesterone to testosterone precursors, DHEA and androstenedione, respectively, through 17α hydroxylation and cleavage of C17,20 bonds. Abiraterone can inhibit the activity of CYP17 to prevent testosterone synthesis in testes, adrenal glands and tumors. Prostate cancer is an androgen-dependent disease, and testosterone suppression is a key pharmacological tool in controlling prostate cancer development. The chemical structure of abiraterone acetate...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K9/48A61K47/14A61K47/44A61K47/22A61K47/28A61K31/58A61P35/00
CPCA61K9/4808A61K9/4858A61K9/4866A61K31/58A61P35/00
Inventor 倪晟王振环夏金强廖志雄赵航徐兵勇王思敏周亮陈鸿翔
Owner HANGZHOU HEZE PHARMA TECH
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com