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A kind of letrozole tablet and preparation method thereof

A technology of letrozole tablets and parts by weight, which is applied in the field of medicine, can solve the problems of poor water solubility and easy sticking, and achieve the effects of good dissolution rate, less impurities and strong operability

Active Publication Date: 2020-04-14
JIANGSU SUNAN PHARMA IND CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, compared with other aromatase inhibitors and antihormonal drugs, letrozole has a stronger antitumor effect, but its water solubility is poor, and it is prone to sticking phenomenon during preparation

Method used

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  • A kind of letrozole tablet and preparation method thereof
  • A kind of letrozole tablet and preparation method thereof
  • A kind of letrozole tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Raw materials: 40 parts of letrozole, 70 parts of starch, 50 parts of carrageenan, 180 parts of starch slurry, 18 parts of disintegrant, 25 parts of magnesium stearate, 12 parts of talcum powder, 5 parts of white oil, 20 parts of magnesium hydrogen phosphate And 12 parts of glycerin. Wherein, the disintegrating agent is sodium carboxymethyl starch and cross-linked sodium carboxymethyl cellulose with a ratio of parts by weight of 8:1.

[0016] Preparation method: After mixing letrozole and starch slurry, add glycerin, evaporate to dryness, pass through an 80-mesh sieve, add starch, carrageenan, disintegrant, magnesium stearate, talcum powder, magnesium hydrogen phosphate and white oil, and mix well Then press the tablet.

Embodiment 2

[0018] Raw materials: 38 parts of letrozole, 65 parts of starch, 54 parts of carrageenan, 200 parts of ethanol, 20 parts of disintegrant, 20 parts of magnesium stearate, 10 parts of talcum powder, 8 parts of white oil, 25 parts of magnesium hydrogen phosphate and 8 parts of glycerin. Wherein, the disintegrating agent is sodium carboxymethyl starch and cross-linked sodium carboxymethyl cellulose with a ratio of parts by weight of 12:1.

[0019] Preparation method: After mixing letrozole and ethanol, add glycerin, evaporate to dryness, pass through an 80-mesh sieve, add starch, carrageenan, disintegrant, magnesium stearate, talcum powder, magnesium hydrogen phosphate and white oil, and mix well Just press the tablet.

Embodiment 3

[0021] Raw materials: 30 parts of letrozole, 80 parts of starch, 45 parts of carrageenan, 210 parts of hydroxypropyl cellulose, 15 parts of disintegrant, 32 parts of magnesium stearate, 8 parts of talcum powder, 9 parts of white oil, hydrogen phosphate 16 parts of magnesium and 15 parts of glycerin. Wherein, the disintegrating agent is sodium carboxymethyl starch and cross-linked sodium carboxymethyl cellulose with a ratio of parts by weight of 5:1.

[0022] Preparation method: After mixing letrozole and hydroxypropyl cellulose, add glycerin, evaporate to dryness, pass through an 80-mesh sieve, add starch, carrageenan, disintegrant, magnesium stearate, talcum powder, magnesium hydrogen phosphate and white oil , mix well and press into tablets.

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Abstract

The invention discloses a letrozole tablet and a preparation method. The lzoxazole tablet comprises 30 to 50 parts of letrozole, 60 to 80 parts of starch, 45 to 57 parts of carrageenan, 150 to 210 parts of a binder, 15 to 22 parts of a disintegrant, 17 to 32 parts of magnesium stearate, 8 to 15 parts of talcum powder, 3 to 9 parts of white oil, 16 to 27 parts of magnesium hydrogen phosphate and 6 to 15 parts of glycerin. The preparation method comprises mixing the letrozole and the binder, adding glycerin into the mixture, carrying out distillation drying, carrying out screening, adding the starch, carrageenan, disintegrating agent, magnesium stearate, talcum powder, magnesium hydrogen phosphate and white oil into the powder, carrying out uniform mixing and carrying out tabletting. The letrozole tablet has the advantages of poor dissolution degree, strong stability and few impurities after long term storage. The preparation method can effectively reduce sticking, can realize smooth, flat and no defect surface and has simple processes, strong operability, safety and environmental friendliness.

Description

technical field [0001] The invention belongs to the field of medicine, in particular to a letrozole tablet and a preparation method thereof. Background technique [0002] Breast cancer is one of the main tumors that threaten women's health, its incidence rate accounts for about 30% of malignant tumors, and its mortality rate accounts for about 15%. In recent years, the incidence of breast cancer in my country has gradually increased, and there is a trend of younger and urbanized development. The prevention and treatment work has a long way to go. As one of the important treatments for breast cancer, endocrine therapy has undergone adrenalectomy, oophorectomy, androgen, estrogen, progesterone, anti-estrogen, and aromatase inhibitor therapy. Letrozole is a new generation of aromatase inhibitors. It is a synthetic benzyltriazole derivative. It can reduce the level of estrogen E2 by inhibiting aromatase, thereby eliminating the stimulating effect of estrogen on tumor growth. H...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K31/4196A61K47/36A61K47/06A61K47/10A61K47/38A61P35/00
CPCA61K9/2013A61K9/2054A61K9/2059A61K31/4196
Inventor 俞洋徐明陈军王俊
Owner JIANGSU SUNAN PHARMA IND CO LTD
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