Abiraterone inclusion compound tablet and preparation method thereof

A technology of abiraterone and inclusion compound, applied in the field of abiraterone inclusion compound tablet and preparation thereof, can solve the problems of poor compressibility of abiraterone, troubles in preparation development, poor water solubility of abiraterone, etc. The effect of poor solubility, accurate dosage and stable quality

Active Publication Date: 2019-08-20
李建恒
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore need to find a kind of technology to solve and improve the technical problem of the poor water solubility of abiraterone
[0007] In addition, tablet refers to a solid preparation that is compressed into a round or oval shape after the drug is evenly mixed with suitable excipients. It is the most common of all solid preparations and is the first major dosage form; Poor physical properties have also brought serious troubles to formulation development

Method used

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  • Abiraterone inclusion compound tablet and preparation method thereof
  • Abiraterone inclusion compound tablet and preparation method thereof
  • Abiraterone inclusion compound tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] The preparation of embodiment 1 abiraterone clathrate

[0042] Precisely weigh 1 mol of abiraterone crude drug and put it into a 50ml reaction bottle, add 10ml of absolute ethanol, put it into an ultrasonic generator and ultrasonically oscillate for 30min until it is completely dissolved. Put it into a constant temperature magnetic stirrer with a set temperature of 75°C, weigh 3mol 2-HP-β-CD, and weigh 0.3mol polyvinylpyrrolidone into a 10ml stoppered test tube, add 5ml distilled water to dissolve it completely. Set the stirring speed of the constant temperature magnetic stirrer to 900r / min, slowly add the above-mentioned Abiraterone aqueous phase into the 2-HP-β-CD organic phase, stir for 6 hours, take it out, cool naturally, and remove the excess by rotary evaporation of the cooling liquid Absolute ethanol, put the suspension in the refrigerator at -10°C for 24 hours, fully analyze the clathrate, and then freeze-dry it in a freeze dryer at -50°C for 24 hours to obtain...

Embodiment 2

[0043] The characterization of embodiment 2 Abiraterone inclusion compound

[0044] 1.1 Determination of Encapsulation Efficiency

[0045] The inclusion compound yield was calculated by weighing, and the content of the inclusion compound was measured by ultraviolet light, so as to finally determine the encapsulation efficiency of the inclusion compound.

[0046] According to the preparation method of Example 1, four batches of Abiraterone inclusion compounds were prepared, and the encapsulation efficiency and drug content were shown in Table 1. The results showed that the Abiraterone inclusion compound encapsulated by the preparation method of Example 1 The ratio is between 52.72%-56.28%, and the drug content in the clathrate is between 19.26%-20.76wt%.

[0047] Table 1

[0048] batch number Encapsulation rate (%) Drug content (wt%) 1 56.28 19.91 2 54.94 20.18 3 52.72 20.76 4 54.78 19.26

[0049] 1.2 Solubility

[0050] For the det...

Embodiment 3～6

[0078] The preparation of embodiment 3~6 abiraterone inclusion compound tablet

[0079] Take Abiraterone inclusion complex and pharmaceutical excipients in proportion, and its specific ratio is shown in Table 5,

[0080] table 5

[0081] Abiraterone clathrate, % Thinner, % Disintegrant, % Binder, % Example 3 5 80 5 10 Example 4 25 59 15 1 Example 5 20 76 1 3 Example 6 20 70 5 5

[0082] Preparation:

[0083] (1) Weigh each component according to the above ratio, pass the abiraterone inclusion compound, diluent, and disintegrant through an 80-mesh sieve, and mix uniformly by the equal-volume incremental method;

[0084](2) Add binder to make soft material, pass the obtained soft material through a 14-mesh sieve to make wet granules, put it into a 60°C oven and dry until the moisture is 1-2%, pass through a 16-mesh sieve, and weigh the weight of the dry granules;

[0085] (3) Add 1% lubricant by weight of dry granules,...

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Abstract

The invention discloses an abiraterone inclusion compound tablet and a preparation method thereof, and belongs to the technical field of pharmaceutical preparations. The tablet contains an abirateroneinclusion compound and medicinal auxiliary materials. The preparation method comprises the following steps: sieving the abiraterone inclusion compound, a diluent and a disintegrant with a 80-mesh sieve, and performing uniform mixing by an equal-amount increment method; adding an adhesive to prepare a soft material, sieving the obtained soft material with a 14-mesh sieve, preparing wet particles,putting the wet particles into a 60 DEG C oven, performing drying until the moisture content is 1-2%, performing sieving with a 16-mesh sieve, and weighing the dry particles; and adding a lubricant which is 1% by weight of the dry particles, and performing uniform mixing and tabletting. The method prepares the abiraterone inclusion compound into a tablet. The tablet has the advantages of accuratedosage, stable quality, low cost, convenient carrying and the like, is a preferred dosage form of the pharmaceutical preparation, and solves and improves the technical problems of compressibility andsolubility of the abiraterone tablet.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an abiraterone inclusion compound tablet and a preparation method thereof. Background technique [0002] There is currently a significant increase in the number of people diagnosed with cancer worldwide, with particular concern being diagnosed with androgen-dependent diseases such as prostate cancer, which is the second leading cause of cancer-related death in men after lung cancer . Abiraterone, invented by researchers at the Royal Marsden Hospital in Southwest London, is a key enzyme in androgen synthesis 17α~hydroxylase~C17, 2~lyase 17α~monooxygenase inhibitors or human cytochrome P450 17 An effective selective oral inhibitor of α, which reduces androgen levels by inhibiting the key enzyme in androgen synthesis - CYP450c17, and has inhibitory effects on androgen in the testis and other parts of the body. [0003] The structure of abiraterone is shown in Formula I....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/58A61K47/69A61K47/26A61K47/38A61K47/32A61K47/12A61P35/00A61P5/28
CPCA61K9/2013A61K9/2018A61K9/2027A61K9/2054A61K31/58A61K47/6951A61P5/28A61P35/00
Inventor 李建恒
Owner 李建恒
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