Oral abiraterone pharmaceutical composition and preparation method and use thereof

A technology of abiraterone and abiraterone acetate, applied in the field of oral abiraterone pharmaceutical composition and its preparation, can solve the problems of product stability and curative effect, insufficient bioavailability, inconvenient administration, etc. , to achieve the effects of improving bioavailability and drug loading, realizing large-scale industrial production, and eliminating differences in blood drug concentration

Pending Publication Date: 2021-12-07
CHENGDU HYPERWAY PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But this technology also has two problems: (1) The patented formula contains ethanol, because ethanol plays an important role in increasing the solubility of API and reducing the particle size of milk particles in the formula, and ethanol is very volatile, which will stabilize the product sex and curative effect
(2) The drug loading amount in this technology is still limited, and the drug loading amount is 20-100 mg / mL. If it is converted from the example of CN10728152A beagle dog 11 times and human body 4 times, the drug may be in the human body The bioavailability is increased by 3.5 times, so the dose of each dose is 286mg. According to the calculation of the drug load, the oil content in each soft capsule is 14.3mL-2.86mL, and the 0# capsule can only be filled with 0.5mL / capsule. This means that the patient needs to take 25-6 large capsules orally every time, which is poor in clinical practice
[0015] It can be seen that the existing abiraterone preparations have problems such as insufficient bioavailability, low drug loading, inconvenient administration, poor stability, inconvenient transportation, complex production process and large environmental pollution, which greatly affect its commercial development. Therefore, it is of great significance for the clinical application of abiraterone or abiraterone acetate to develop an abiraterone preparation that can improve bioavailability and drug loading, reduce the difference in blood drug concentration before meals, have a simple and stable prescription process, and be convenient for transportation.

Method used

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  • Oral abiraterone pharmaceutical composition and preparation method and use thereof
  • Oral abiraterone pharmaceutical composition and preparation method and use thereof
  • Oral abiraterone pharmaceutical composition and preparation method and use thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0163] This embodiment provides a pharmaceutical composition containing abiraterone acetate, and the proportion of each component in the combination is calculated by mass fraction, including the following components:

[0164] Name Proportion (mass ratio)

[0165] Abiraterone Acetate 28.6%

[0166] Oleic acid 71.4%

[0167] Preparation method: Add abiraterone acetate to oleic acid, stir or ultrasonically dissolve it completely to form a uniform and clear solution.

[0168] A large amount of bile salt is also secreted in the gastrointestinal tract of the human body, and the phospholipids in the human body can self-emulsify oil-soluble substances. This embodiment is the most simplified combination of the embodiments of the present invention.

Embodiment 2

[0170] This embodiment provides a pharmaceutical composition containing abiraterone acetate, and the proportion of each component in the combination is calculated by mass fraction, including the following components:

[0171]

[0172] Preparation method: Mix oleic acid, polyoxyethylene 40 hydrogenated castor oil, and propylene glycol evenly, then add abiraterone acetate, stir or ultrasonically dissolve it completely, and form a uniform and clear solution.

Embodiment 3

[0174] This embodiment provides a pharmaceutical composition containing abiraterone acetate, and the proportion of each component in the combination is calculated by mass fraction, including the following components:

[0175]

[0176] Preparation method: Mix oleic acid, polyoxyethylene 35 castor oil, and propylene glycol evenly, then add abiraterone acetate, stir or ultrasonically dissolve it completely, and form a uniform and clear solution.

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Abstract

The invention discloses an oral abiraterone pharmaceutical composition and a preparation method and use thereof. The oral abiraterone pharmaceutical composition comprises an active component and fatty acid. The active component is abiraterone acetate and/or abiraterone. The abiraterone acetate and the fatty acid are compounded, such that the drug loading capacity of the abiraterone acetate is increased, the bioavailability of the abiraterone pharmaceutical preparation is improved, plasma concentration differences before and after meals can be reduced, and the oral abiraterone pharmaceutical composition is convenient to take. Meanwhile, the abiraterone pharmaceutical preparation has few components, good stability and a simple preparation process, and is capable of realizing large-scale industrial production and convenient to produce and transport.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to an oral abiraterone pharmaceutical composition and a preparation method and application thereof. Background technique [0002] Abiraterone acetate is a derivative of steroidal progesterone developed by Johnson & Johnson, and is a prodrug of abiraterone, which can be rapidly hydrolyzed and deacetylated into abiraterone in vivo. Abiraterone inhibits 17α-hydroxylase / C17,20-lyase (CYP17), which is expressed in testicular, adrenal, and prostate tumors and is required for androgen biosynthesis. The drug molecule has been approved for metastatic castration-resistant prostate cancer (CRPC) in many countries, and abiraterone acetate has also been included in the World Health Organization's "Essential Medicines List". [0003] The chemical name of abiraterone acetate is (3β)-17-(3-pyridyl)androst-5,16-dien-3-yl acetate, and the molecular formula is C 26 h ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/58A61K47/12A61K47/26A61K47/44A61K47/10A61K47/28A61K47/02A61K9/20A61K9/48A61K9/08A61K9/107A61P35/00A61P13/08
CPCA61K9/0053A61K31/58A61K47/12A61K47/26A61K47/44A61K47/10A61K47/28A61K47/02A61K9/2013A61K9/4858A61K9/4875A61K9/4866A61K9/08A61K9/1075A61P35/00A61P13/08
Inventor 唐珊黄依娟石凯荣张丽月赵小芳陈礼莉李英富
Owner CHENGDU HYPERWAY PHARM CO LTD
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