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Abiraterone pharmaceutical composition with high drug loading capacity as well as preparation method and application of abiraterone pharmaceutical composition

A technology of abiraterone and abiraterone acetate, applied in the field of abiraterone pharmaceutical composition and preparation thereof, can solve the problems of product stability and curative effect, insufficient bioavailability, inconvenient administration, etc. Improve bioavailability and drug loading, realize large-scale industrial production, and eliminate the effect of blood drug concentration differences

Pending Publication Date: 2022-07-19
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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  • Abiraterone pharmaceutical composition with high drug loading capacity as well as preparation method and application of abiraterone pharmaceutical composition
  • Abiraterone pharmaceutical composition with high drug loading capacity as well as preparation method and application of abiraterone pharmaceutical composition
  • Abiraterone pharmaceutical composition with high drug loading capacity as well as preparation method and application of abiraterone pharmaceutical composition

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Effect test

Embodiment 1

[0088] The present 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:

[0089] Name Proportion (mass ratio)

[0090] Abiraterone acetate 28.6%

[0091] Oleic acid 71.4%

[0092] Preparation method: Add abiraterone acetate to oleic acid, stir or sonicate to dissolve it completely to form a homogeneous and clear solution.

[0093] The human body also secretes a large amount of bile salts in the gastrointestinal tract, and the phospholipids in the human body can self-emulsify oil-soluble substances. This embodiment is the simplest combination of the embodiments of the present invention.

Embodiment 2

[0095] The present 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:

[0096]

[0097] Preparation method: Mix oleic acid, polyoxyethylene 40 hydrogenated castor oil and propylene glycol evenly, then add abiraterone acetate, stir or sonicate to dissolve it completely to form a homogeneous and clear solution.

Embodiment 3

[0099] The present 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:

[0100]

[0101]

[0102] Preparation method: mix oleic acid, polyoxyethylene 35 castor oil and propylene glycol evenly, then add abiraterone acetate, stir or ultrasonicate to dissolve it completely to form a homogeneous and clear solution.

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Abstract

The invention discloses an abiraterone pharmaceutical composition with high drug loading capacity as well as a preparation method and application thereof. The abiraterone pharmaceutical composition comprises the following components in parts by weight: 1-80 parts of an active ingredient, 1-50 parts of fatty acid, 5-75 parts of grease, 10-70 parts of a surfactant and 1-50 parts of a cosurfactant, the active component is abiraterone acetate and/or abiraterone, preferably abiraterone acetate. According to the preparation disclosed by the invention, the abiraterone acetate and the fatty acid are compounded, so that the drug loading capacity of the abiraterone acetate is increased, the bioavailability of the abiraterone acetate pharmaceutical preparation is improved, the plasma concentration difference before and after meals can be reduced, and the preparation is convenient to take. Meanwhile, the abiraterone acetate pharmaceutical preparation is few in component, good in stability, simple in preparation process, capable of achieving large-scale industrial production and convenient to produce and transport.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to an abiraterone pharmaceutical composition and a preparation method and application thereof. Background technique [0002] Abiraterone acetate is a derivative of steroid progesterone developed by Johnson & Johnson, 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 testis, adrenal and prostate tumor tissues and is required for androgen biosynthesis. The drug molecule has been approved in many countries for metastatic castration-resistant prostate cancer (CRPC), 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 33 NO 2 , and the molecu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/58A61K47/12A61K9/08A61K9/48A61K47/10A61K47/14A61K47/44A61P35/00A61P35/04
CPCA61K31/58A61K47/12A61K9/08A61K47/44A61K47/10A61K47/14A61K9/4866A61P35/00A61P35/04
Inventor 唐珊石凯荣黄依娟赵小芳张丽月陈礼莉李英富
Owner CHENGDU HYPERWAY PHARM CO LTD
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