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Solid dispersion and preparation method thereof

A technology of solid dispersion and carrier material, which can be applied to medical preparations without active ingredients, medical preparations containing active ingredients, pharmaceutical formulas, etc. And other issues

Active Publication Date: 2018-11-13
SUNCADIA PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

CN103070828B also discloses a solid dispersion containing abiraterone acetate and povidone, wherein the mass ratio of abiraterone acetate to povidone is 1:0.5-4, the preparation method of the solid dispersion is relatively complicated, and the solid dispersion Drug formulations do not have good bioavailability
[0005] However, in the process of administering abiraterone acetate to treat prostate cancer, there are problems such as large individual differences between patients and large differences in oral drug absorption on an empty and full stomach. Researchers need to study in depth and solve the problems encountered

Method used

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  • Solid dispersion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Embodiment 1: preparation of solid dispersion

[0046] Compound A and different types of carrier materials were used to prepare solid dispersions. The specific formula is shown in Table 2:

[0047] Table 2

[0048]

[0049] Preparation:

[0050] 1) Pass the abiraterone acetate and the carrier material through a 40-80 mesh screen respectively, weigh the abiraterone acetate and the carrier material in a ratio of 1:3 by weight percentage, and fully mix them uniformly;

[0051] 2) Preset the extrusion temperature of each heating zone of twin-screw hot melt extruder 1-8 to 120°C-145°C, when the preset temperature is reached, start the screw to slowly add the mixture obtained in step 1) from the feeding hopper to the extruder In the machine, hot melt extrusion is carried out at a speed of 150-300RPM;

[0052] 3) The solid extrudate obtained in step 2) is pulverized and passed through a 60-100 mesh sieve to obtain a uniform solid dispersion of particles.

Embodiment 2

[0054] Compound A and different types of carrier materials were used to prepare solid dispersions. The specific formula is shown in Table 3:

[0055] table 3

[0056]

[0057] Preparation:

[0058] Dissolve abiraterone acetate and carrier material in dichloromethane / methanol mixed solvent, according to the ratio in Table 3, fully stir evenly, prepare the solution, use spray drying equipment to carry out spray drying, and the spray-dried product is dried in a vacuum oven. The obtained product is an amorphous solid dispersion of abiraterone acetate.

Embodiment 3

[0060] Compound A and different types of carrier materials were used to prepare solid dispersions. The specific formula is shown in Table 4:

[0061] Table 4

[0062]

[0063] Preparation:

[0064] The abiraterone acetate and the carrier material are dissolved together in the dichloromethane / methanol mixed solvent, and the organic solvent is evaporated to allow the drug and the carrier material to be precipitated at the same time, that is, a coprecipitate formed by mixing the abiraterone acetate and the carrier material is obtained. After drying, the solid dispersion of abiraterone acetate was obtained.

[0065] Appearance and Yield

[0066] The solid dispersions of Examples 1-3 and Comparative Examples 1-6 were compared for appearance and recovery data.

[0067] table 5

[0068] Element

Exterior

Recovery rate(%)

Experimental example 1

dry dispersion

82

Experimental example 2

dry dispersion

80

Experimental example 3

...

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Abstract

The invention relates to a solid dispersion and a preparation method of the solid dispersion, in particular to the solid dispersion. The solid dispersion contains abiraterone or a derivative of the abiraterone and a carrier material HPMCAS, wherein DS<Ac> in HPMCAS is not greater than 0.50, and DS<Ac>+DS<s> is not smaller than 0.83, The preparation prepared by the solid dispersion system has gooddissolution and stability, and can eliminate individual differences after patients take medicines and food effects and the like caused by fasting and satiety administration to some extent.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a solid dispersion of abiraterone or its derivatives, the preparation containing the solid dispersion has good dissolution rate, stability and the ability to eliminate drug reactions of abiraterone or its derivatives Individual differences, etc. Background technique [0002] Prostate cancer is a common malignant and fatal cancer. It is the second leading cause of cancer-related male death after lung cancer. In recent years, the market demand has grown rapidly. Abiraterone acetate is a prodrug of abiraterone , is a CYP17 enzyme inhibitor that was approved for marketing in the United States in 2011 and is suitable for the treatment of prostate cancer patients. [0003] Abiraterone acetate is a lipophilic compound, with an octanol-water partition coefficient of 5.12 (Log P), and is almost insoluble in water. The BCS classification belongs to four categories, so it is key ...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/20A61K9/48A61K31/58A61K47/38A61P13/08A61P35/00
CPCA61K9/1652A61K9/2054A61K9/4866A61K31/58A61K47/38A61P13/08A61P35/00
Inventor 王立坤王伟张凤娥钱雯
Owner SUNCADIA PHARM CO LTD
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