Method for preparing medical composition of abiraterone or derivative thereof, and application of medical composition

An abiraterone and a technology for preparing medicines, which are applied in the field of pharmaceutical preparations and can solve problems such as differences in poor bioavailability between individuals

Pending Publication Date: 2020-09-04
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in terms of clinical efficacy, the commercially available Zeke Exhibits poor bioavailability and greater inter-individual variability

Method used

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  • Method for preparing medical composition of abiraterone or derivative thereof, and application of medical composition
  • Method for preparing medical composition of abiraterone or derivative thereof, and application of medical composition
  • Method for preparing medical composition of abiraterone or derivative thereof, and application of medical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0101]

[0102] 1) Preparation of nanosuspension

[0103] Add 19.2g of HPMC E5 LV to 739.6g of water to disperse and dissolve, then add 1.92g of SDS to dissolve, then add 75g of compound A to the above solution, stir to disperse.

[0104] Sand mill is installed (grinding chamber volume is 160ml, fills the 0.3mm grinding bead of 112ml, and feed rate is 160rpm, and grinding speed is 3000rpm), and dispersed suspension is added into grinder preparation tank, starts stirring, grinds to obtain Compound A nanosuspension D90 500nm, for future use.

[0105] 2) Fluidized bed granulation

[0106] Take 1003 g of the above-mentioned nano-suspension, add 90 g of the absorption-promoting agent SNAC into the above-mentioned nano-suspension, and stir and disperse. Add 144g of lactose and 28.8g of crospovidone XL into the fluidized bed for fluidized bed top spray granulation. After the granulation is completed, the granules are dried, and the drying can be stopped when the water content o...

Embodiment 2

[0115]

[0116] 1) Preparation of nanosuspension

[0117] Add 19.2g of HPMC E5 LV to 739.6g of water to disperse and dissolve, then add 1.92g of SDS to dissolve, then add 75g of compound A to the above solution, stir and disperse.

[0118] Sand mill is installed (grinding chamber volume is 160ml, fills the 0.3mm grinding bead of 112ml, and feed rate is 160rpm, and grinding speed is 3000rpm), and dispersed suspension is added into grinder preparation tank, starts stirring, grinds to obtain Compound A nanosuspension D90 is about 500nm, for future use.

[0119] 2) Fluidized bed granulation

[0120] Take 1170.2 g of the above-mentioned nano-suspension, add 105 g of the absorption-promoting agent SNAC into the above-mentioned nano-suspension, and stir and disperse. Add 168g of lactose and 33.6g of crospovidone XL into the fluidized bed for fluidized bed top spray granulation. After the granulation is completed, the granules are dried, and the drying can be stopped when the wa...

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Abstract

The invention relates to a method for preparing a medical composition of abiraterone or a derivative thereof, and an application of the medical composition. Specifically, the method comprises the steps of mixing nanometer suspension containing the abiraterone or the derivative thereof with an absorption enhancer and one or more arbitrarily-chosen excipients, and performing granulation in a fluidized bed, wherein the particle diameter D90 value of the abiraterone or the derivative thereof is smaller than 1000nm, and is preferably 400-600nm. Compared with preparations sold in the market, the medical composition has the advantages that the biological availability is improved, and individual differences and the like of medicine administration patients are improved.

Description

technical field [0001] The disclosure belongs to the field of pharmaceutical preparations, and in particular relates to a method for preparing abiraterone or its derivative pharmaceutical composition and its application. Background technique [0002] Abiraterone is a CYP17 inhibitor used to inhibit the biosynthesis of androgens and estrogens. . The acetate ester of this compound is approved in the United States for the treatment of castration-resistant prostate cancer. However, in terms of clinical efficacy, the commercially available Zeke Exhibits poor bioavailability and greater inter-individual variability. Meanwhile, abiraterone acetate also belongs to a class of compounds with poor water solubility. [0003] There are two main ways to improve the oral bioavailability of drugs. One is to change the physical and chemical properties of drugs, improve their membrane penetration ability or improve their dissolution characteristics, such as micronization technology, soli...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/18A61K31/58A61P35/00
CPCA61K47/18A61K31/58A61P35/00
Inventor 潘彩云陈爱玲潘凯刘凯莫志荣
Owner JIANGSU HENGRUI MEDICINE CO LTD
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