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Abiraterone acetate sublingual tablet and preparation method thereof

A technology of abiraterone acetate and sublingual tablet, applied in the field of medicine, can solve the problem of unsolved tablet dissolution rate and the like, achieve the effects of improving drug bioavailability, avoiding irritation, and ensuring drug efficacy

Active Publication Date: 2017-07-04
SHANDONG NEWTIME PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But did not solve the dissolution problem of the tablet

Method used

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  • Abiraterone acetate sublingual tablet and preparation method thereof
  • Abiraterone acetate sublingual tablet and preparation method thereof
  • Abiraterone acetate sublingual tablet and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0027]

[0028] Preparation Process:

[0029] Prescription quantity Weigh abiraterone acetate, polyethylene glycol 1000 vitamin E succinate, dissolve in dichloromethane, dry under reduced pressure at 40°C to remove dichloromethane, obtain a dry product, pass through a 100-mesh sieve, and mix with the prescription quantity of lactose , sodium carboxymethyl starch and magnesium stearate are mixed and compressed into tablets.

Embodiment 2

[0031]

[0032] Preparation Process:

[0033] Prescription quantity Weigh Abiraterone acetate, polyethylene glycol 1000 vitamin E succinate, dissolve in chloroform, dry under reduced pressure at 50°C to remove dichloromethane, obtain a dry product, pass through a 100-mesh sieve, and mix with the prescription quantity of lactose , crospovidone and magnesium stearate are mixed and compressed into tablets.

Embodiment 3

[0035]

[0036] Preparation Process:

[0037] Prescription quantity Weigh abiraterone acetate, polyethylene glycol 1000 vitamin E succinate, dissolve in dichloromethane, and dry under reduced pressure at 45°C to remove dichloromethane to obtain a dry product, pass through a 100-mesh sieve, and mix with the prescription quantity of lactose , sodium carboxymethyl starch and magnesium stearate are mixed and compressed into tablets.

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PUM

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Abstract

The present invention relates to a tablet, which uses water as a dissolution medium and has characteristics of rapid dissolution and good absorption. The preparation method comprises: dissolving abiraterone acetate and D-alpha-tocopheryl polyethylene glycol 1000 succinate in an organic solvent, carrying out pressure reducing drying to remove the organic solvent, mixing the obtained dried product, a filler and a disintegrant, adding a lubricant, mixing, and tableting to obtain the abiraterone acetate sublingual tablet. Compared to the abiraterone acetate sublingual tablet in the prior art, the abiraterone acetate sublingual tablet of the present invention has the following advantages that the abiraterone acetate sublingual tablet can be subjected to complete dissolution within 15 min so as to ensure the efficacy of the medicine, the complex micro-powder treatment does not required, and the bioavailability of the medicine is substantially improved.

Description

technical field [0001] The invention belongs to the technical field of medicines, in particular to an abiraterone acetate sublingual tablet and a preparation method thereof. Background technique [0002] Abiraterone acetate is an oral cytochrome oxidase P450 (CYP450) c17 inhibitor, which reduces androgen levels by inhibiting the key enzyme in androgen synthesis - CYP450c17, and has no effect on androgens in the testis and other parts of the body. It has inhibitory effect and is used in the treatment of advanced prostate cancer. Its structural formula is: [0003] [0004] Abiraterone acetate is a lipophilic compound, easily soluble in organic solvents such as tetrahydrofuran, dichloromethane, especially alcohols; almost insoluble in water at pH2-12 at 20°C; slightly soluble in 0.1N hydrochloric acid, BCS classification belongs to Four types, so improving its dissolution rate and bioavailability is the key of the present invention when carrying out pharmaceutical prepara...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/58A61K47/22A61P35/00
CPCA61K9/006A61K9/2031A61K31/58
Inventor 张贵民郝贵周高西蒙
Owner SHANDONG NEWTIME PHARMA
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