Exemestane orally disintegrating tablet and preparation method thereof

A technology of orally disintegrating tablets and exemestane, applied in the field of exemestane orally disintegrating tablets and its preparation, can solve the problem that formestane can only be administered by injection

Inactive Publication Date: 2014-08-06
赵辉
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the aromatase inhibitor with better curative effect is formestane, which has been used clinically a...

Method used

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  • Exemestane orally disintegrating tablet and preparation method thereof
  • Exemestane orally disintegrating tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Weight ratio of raw and auxiliary materials:

[0027] Exemestane 250g, lactose 150g, sorbitol 500g, microcrystalline cellulose 250g, low-substituted hydroxypropyl cellulose 50g, sodium saccharin 5g, magnesium stearate 10g

[0028] Tablets were produced in 10,000 tablets.

[0029] Preparation:

[0030] (a) Exemestane, microcrystalline cellulose, low-substituted hydroxypropyl cellulose, sorbitol, and magnesium stearate were dried at 105°C for 1 hour, pulverized through a 100-mesh sieve, and lactose and saccharin sodium were pulverized through a 100-mesh sieve for later use ;

[0031] (b) weighing exemestane, sorbitol, lactose, sodium saccharin, 1 / 3 amount of low-substituted hydroxypropyl cellulose, and 1 / 3 amount of microcrystalline cellulose and mixing them to obtain a mixed material;

[0032] (c) Add 50% ethanol solution to the mixed material obtained in step (b) to make a suitable soft material, granulate with a 32-mesh sieve, dry the wet granules at 45±5°C, and gra...

Embodiment 2

[0037] Weight ratio of raw and auxiliary materials:

[0038] Exemestane 250g, lactose 150g, sorbitol 500g, microcrystalline cellulose 250g, low-substituted hydroxypropyl cellulose 50g, sodium saccharin 5g, magnesium stearate 10g

[0039] Tablets were produced in 10,000 tablets.

[0040] Preparation:

[0041] (a) Exemestane, microcrystalline cellulose, low-substituted hydroxypropyl cellulose, sorbitol, and magnesium stearate were dried at 105°C for 1 hour, pulverized through a 100-mesh sieve, and lactose and saccharin sodium were pulverized through a 100-mesh sieve for later use ;

[0042] (b) weighing exemestane, sorbitol, lactose, sodium saccharin, 1 / 3 amount of low-substituted hydroxypropyl cellulose, and 1 / 3 amount of microcrystalline cellulose and mixing them to obtain a mixed material;

[0043] (c) Add 50% ethanol solution to the mixed material obtained in step (b) to make a suitable soft material, granulate with a 32-mesh sieve, dry the wet granules at 45±5°C, and gra...

Embodiment 3

[0048] Weight ratio of raw and auxiliary materials

[0049] Exemestane 250g, lactose 350g, sorbitol 100g, microcrystalline cellulose 315g, low-substituted hydroxypropyl cellulose 60g, sodium saccharin 10g, magnesium stearate 30g

[0050] Tablets were produced in 10,000 tablets.

[0051] Preparation:

[0052] (a) Exemestane, microcrystalline cellulose, low-substituted hydroxypropyl cellulose, sorbitol, and magnesium stearate were dried at 105°C for 1 hour, pulverized through a 100-mesh sieve, and lactose and saccharin sodium were pulverized through a 100-mesh sieve for later use ;

[0053] (b) weighing exemestane, sorbitol, lactose, sodium saccharin, 1 / 3 amount of low-substituted hydroxypropyl cellulose, and 1 / 3 amount of microcrystalline cellulose and mixing them to obtain a mixed material;

[0054] (c) Add 50% ethanol solution to the mixed material obtained in step (b) to make a suitable soft material, granulate with a 32-mesh sieve, dry the wet granules at 45±5°C, and gra...

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Abstract

The invention provides an exemestane orally disintegrating tablet and a preparation method thereof. The exemestane orally disintegrating tablet comprises a principal ingredient of exemestane and auxiliary ingredients of disintegrating agents, fillers and corrective agents. The preparation method comprises the following steps: mixing, directly tabletting, coating and the like. Exemestane orally disintegrating tablets have the following advantages: the tablets can disintegrate or be soluble in mouth without water and enter digestive tracts with a swallowing act, and the behavior in vivo is consistent with that of common tablets; the exemestane orally disintegrating tablets have the characteristics of convenience for taking, quick absorption, high bioavailability and the like; patient adaptabilities can be improved and clinical medicine choices for doctors and patients can be increased.

Description

field of invention [0001] The invention relates to an orally disintegrating exemestane tablet and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background of the invention [0002] Breast cancer is one of the most common malignant tumors among women in the world. The incidence rate is increasing year by year. In today's elderly population, women over 65 years old, about 26% suffer from breast cancer, and about 1 / 3 of the tumor growth requires high estrogen levels to maintain, that is, estrogen dependence Characteristics. Estrogen-dependent breast cancer occurs more frequently in postmenopausal women. Antiestrogens are commonly used in patients with estrogen-dependent breast cancer. Tamoxifen has been used as the first-line treatment drug, but the effect of tamoxifen is better when it is first used, and long-term use is prone to drug resistance, leading to disease recurrence. Another class of aromatase inhibitors whose mecha...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/5685A61K47/38A61P15/14A61P35/00
Inventor 赵辉赵冠淇郭涛胡晓川
Owner 赵辉
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