Oral abiraterone pharmaceutical composition and preparation method and use thereof

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 ...

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.

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