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

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...

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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