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Abiraterone oral spray and use and preparation methods thereof

The technology of oral spray and abiraterone, which is applied in the field of pharmaceutical preparations, can solve problems such as difficulty in forming microemulsion, and achieve the effects of improving bioavailability and reducing the risk of toxic and side effects.

Inactive Publication Date: 2015-11-18
HANGZHOU ANDE TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Simultaneously, the oral spray of abiraterone acetate of the present invention also solves the problem that it is not easy to form microemulsions due to the insolubility of abiraterone acetate and its unique properties from the formula

Method used

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  • Abiraterone oral spray and use and preparation methods thereof

Examples

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Comparison scheme
Effect test

Embodiment 1

[0039] An oral spray of abiraterone, comprising the following components by weight percentage, abiraterone acetate 0.44%; oil phase (medium chain triglyceride, ethyl oleate or oleic acid) 9.05%; Co-surfactant (ethanol, n-butanol or propylene glycol) 4.42%; surfactant (polyoxyethylene 40 hydrogenated castor oil or polyoxyethylene 35 castor oil) 19.18%; balance of water.

[0040] A preparation method of abiraterone oral spray, specifically comprising the following steps:

[0041] (1) Weigh the oil phase, co-surfactant, and surfactant of the formula respectively and stir them evenly;

[0042] (2) Weigh the formula amount of abiraterone acetate and stir in it, and then place it in a water bath at 40-50°C;

[0043] (3) Stir the mixture in step (2) at a speed of 210rpm for 30 minutes to form a microemulsion;

[0044] (4) Cool the microemulsion in step (3) naturally, filter and fill it in a spray bottle with a quantitative valve to prepare the oral spray of abiraterone acetate. The t...

Embodiment 2

[0046] An oral spray of abiraterone, by weight percentage, comprising the following components, abiraterone acetate 2.17%; oil phase (medium chain triglyceride, ethyl oleate or oleic acid) 5.01%; Co-surfactant (ethanol, n-butanol or propylene glycol) 5.46%; surfactant (polyoxyethylene 40 hydrogenated castor oil or polyoxyethylene 35 castor oil) 11.07%; balance of water.

[0047] A preparation method of abiraterone oral spray, specifically comprising the following steps:

[0048] (1) Weigh the oil phase, co-surfactant, and surfactant of the formula respectively and stir them evenly;

[0049] (2) Weigh the formula amount of abiraterone acetate and stir in it, and then place it in a water bath at 40-50°C;

[0050] (3) Stir the mixture in step (2) at a speed of 210rpm for 30 minutes to form a microemulsion;

[0051] (4) Cool the microemulsion in step (3) naturally, filter and fill it in a spray bottle with a quantitative valve to prepare the oral spray of abiraterone acetate. Th...

Embodiment 3

[0053] A kind of oral spray of abiraterone, by weight percentage, comprises following component, abiraterone acetate 0.51%; Abiraterone acetate is 3 / 50 of oily phase, and oily phase (medium chain triglyceride ester, ethyl oleate or oleic acid) specifically 8.5%; co-surfactant (ethanol, n-butanol or propylene glycol) co-surfactant is 1 / 3 of the surfactant, specifically 4.56%; surfactant (polyoxyethylene 40 hydrogenated castor oil or polyoxyethylene 35 castor oil) 13.68%; flavoring agent 2.65% (sucrose 1.77%, banana powder 0.88%); antibacterial agent potassium sorbate 0.19%; water balance.

[0054] A preparation method of abiraterone oral spray, specifically comprising the following steps:

[0055] (1) Weigh the oil phase, co-surfactant, and surfactant of the formula respectively and stir them evenly;

[0056] (2) Weigh the formula amount of abiraterone acetate and stir in it, and then place it in a water bath at 40-50°C;

[0057] (3) First, dissolve the flavoring agent and po...

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Abstract

The invention relates to the technical field of pharmaceutical preparations and particularly relates to an abiraterone oral spray. The abiraterone oral spray comprises the following components in percent by weight: abiraterone acetate, an oil phase, a surfactant, a co-surfactant and the balance of water, wherein the oil phase is used as a carrier for prompting system micro-emulsification, and the oil phase is medium chain triglyceride, ethyl oleate or oleic acid; the surfactant is used for improving the performance of the abiraterone oral spray, expanding the range of application and realizing solubilization, and the surfactant is polyoxyethylene 40 hydrogenated castor oil or polyoxyethylene 35 castor oil; and the co-surfactant is used for reducing the surface tension of liquid and enhancing the emulsifying, moistening and blistering effects, and the co-surfactant is ethanol, n-butyl alcohol or propylene glycol. The spray has the advantages that the taking dose is reduced, so that the manufacturing cost is lowered; the formation of invalid metabolites is reduced, so that adverse reactions are effectively reduced; and the drug effect of the spray is longer than that of an oral drug.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to an oral spray of abiraterone. Background technique [0002] Abiraterone acetate, also known as abiraterone acetate, abiraterone acetate, English name Abirateroneacetate, chemical name: (3beta)-17-(3-pyridyl)-androster-5,16- Diene-3-acetate, the English chemical name is 17-(3-pyridinyl)-5,16-androstadien-3beta-acetate or (3beta)-17-(3-pyridinyl)-Androsta-5,16-dien -3-olacetate (ester); its chemical structure is shown below: [0003] [0004] Abiraterone acetate is a white to off-white, non-hygroscopic crystalline powder. Its molecular formula is C 26 h 33 NO 2 , molecular weight 391.55. Abiraterone acetate is a lipophilic compound with an octanol-water partition coefficient of 5.12 (LogP), and is particularly insoluble in water. [0005] Abiraterone acetate, a prodrug of abiraterone, is rapidly converted in vivo to abiraterone, a selective, irreversib...

Claims

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Application Information

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IPC IPC(8): A61K9/12A61K31/58A61P35/00
Inventor 周俊侨
Owner HANGZHOU ANDE TECH CO LTD
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