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Abiraterone oral emulsion and preparation method thereof

A technology of abiraterone and abiraterone acetate, which is applied in the direction of pharmaceutical formulations, emulsion delivery, medical preparations of non-active ingredients, etc., can solve the problems of low bioavailability, achieve improved dissolution, improved bioavailability, The effect of emulsion stabilization

Pending Publication Date: 2020-04-17
SHENZHEN NEPTUNUS PHARMA RES INST CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0026] The object of the present invention is to provide a kind of abiraterone emulsion and preparation method thereof, solve the technical problem that abiraterone or abiraterone acetate bioavailability are low

Method used

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  • Abiraterone oral emulsion and preparation method thereof
  • Abiraterone oral emulsion and preparation method thereof
  • Abiraterone oral emulsion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1: Excipient investigation

[0040] Table 1: Solubility investigation of excipients

[0041]

[0042]

[0043] Table 2: Investigation of emulsifying properties of excipients

[0044]

[0045]

[0046] Table 3: Investigation on the Stability of Excipients

[0047]

[0048]

[0049] The results showed that: (1) Abiraterone acetate was easily degraded after being dissolved in ester excipients; (2) Adding antioxidants could effectively improve the stability of abiraterone acetate in the emulsion.

Embodiment 2

[0050] Embodiment 2: the preparation of abiraterone oral emulsion

[0051] A preparation method of abiraterone emulsion comprises the following steps:

[0052] (1) After heating the solubilizer and emulsifier to 60°C, stir evenly to obtain solution 1;

[0053] (2) Add antioxidant to solution 1, stir and dissolve to obtain solution 2;

[0054] (3) Add the active ingredient into solution 2, stir to dissolve, and obtain the emulsion.

Embodiment 3

[0055] Example 3: Emulsion Evaluation

[0056] The emulsion was prepared according to the method described in Example 2 according to the proportion of the components. Weigh 1g of the emulsion, add it to 9ml of purified water, stir to dissolve, and observe the properties of the emulsion.

[0057] (1) Simulated gastric digestion evaluation:

[0058] According to the literature Koziolek, M., et al. (2019). "The mechanisms of pharmacokinetic food-drug interactions–A perspective from the UNGAP group." European Journal of Pharmaceutical Sciences 134:31-59. The amount of fluid in the stomach is affected by the state of eating The impact is relatively large. In the fasting state, the amount of fluid in the stomach is about 35ml, and the pH is about 1. Firstly, 5g of emulsion was diluted into 50ml of emulsion, then mixed with 35ml of artificial gastric juice (Chinese Pharmacopoeia, containing pepsin), and simulated gastric digestion at 37°C for 1 hour. After digestion, the sample is...

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Abstract

The invention discloses an abiraterone oral emulsion and a preparation method thereof. The preparation comprises an active component, a solubilizer, an emulsifier and an antioxidant; the active component is abiraterone acetate or abiraterone; and the preparation comprises, by weight, 2%-10% of abiraterone acetate or abiraterone, 20%-70% of the solubilizer, 20%-40% of the emulsifier and 0.01%-1% ofthe solubilizer. According to the invention, the drug loading capacity and the stability of the abiraterone oral emulsion are high; and the abiraterone oral emulsion can be spontaneously emulsified to form an emulsion when meeting water. And the formed emulsion is stable; the digestion influence is low; the dissolution of medicines in gastrointestinal tracts is improved; the absorption of the medicines is promoted; and the bioavailability is improved.

Description

technical field [0001] The invention relates to an abiraterone oral emulsion and a preparation method thereof. Background technique [0002] Abiraterone (17-(3-pyridyl)-androst-5,16-dien-3-ol, CAS number: 154229-19-3, molecular formula: C24H31NO, molecular weight: 349.5g / mol) structure is as follows Show. [0003] [0004] Abiraterone acetate (17-(3-pyridyl)-androst-5,16-diene-3β-acetate, CAS number: 154229-18-2, molecular formula: C26H33NO2, molecular weight: 391.55g / mol) , the structure is as follows. [0005] [0006] Abiraterone acetate is a prodrug of abiraterone, which is converted into abiraterone in the body. Abiraterone acetate tablets are currently used clinically, and the trade name is: Imported drug registration number: H20150264, originally developed by Johnson & Johnson, and approved by the U.S. Food and Drug Administration in 2011 for the treatment of metastatic castration-resistant prostate cancer in combination with prednisone or prednisolone, and...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/58A61K47/14A61K47/10A61P35/04
CPCA61K9/107A61K9/0053A61K31/58A61K47/14A61K47/10A61P35/04
Inventor 周子岚杨经安王志国郭青石涛冯汉林于琳
Owner SHENZHEN NEPTUNUS PHARMA RES INST CO LTD
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