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Letrozole tablet and preparation method thereof

A technology for letrozole tablets and tablet cores, which can be used in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. Effect

Active Publication Date: 2020-04-17
瀚晖制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The main purpose of the present invention is to provide a kind of letrozole tablet and preparation method thereof, to solve the problem that its dissolution rate cannot be effectively controlled when the letrozole tablet in the prior art uses micropowder silica gel as lubricant

Method used

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  • Letrozole tablet and preparation method thereof
  • Letrozole tablet and preparation method thereof
  • Letrozole tablet and preparation method thereof

Examples

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preparation example Construction

[0029] In order to further increase the uniformity of the mixing of the components, the above preparation method preferably includes: step S1, mixing the micronized silica gel with the first part of lactose to form a first mixture; step S2, mixing the first mixture of terazole, the second part of lactose and the first mixture to form The second mixture; step S3, mixing the third part of lactose with the second mixture to form a third mixture; step. S4, mixing the microcrystalline cellulose, disintegrant, the fourth part of lactose and the third mixture to form a fourth mixture; Step S5, mixing magnesium stearate with the fourth mixture to form a fifth mixture; and step S6, compressing the fifth mixture to obtain a tablet core.

[0030] In the above preparation method, the lactose is divided into four parts and added separately, and the micropowdered silica gel and the first part of lactose are mixed to remove the static electricity of the mixing equipment and reduce the adsorption...

Embodiment 1

[0041] Pretreatment

[0042] 1.760 kg of lactose (100 mesh) and 0.160 kg of silicon dioxide were jointly passed through a 40-mesh vortex vibrating screen once, and put into a container lined with a double-layer plastic bag as the first material.

[0043] 0.400 kg of letrozole and 1.520 kg of lactose (100 mesh) were passed through a 40-mesh vortex vibrating sieve 3 times, and put into a container lined with a double-layer plastic bag as the second material.

[0044] 3.840 kg of lactose (100 mesh) was passed through a 40-mesh vortex vibrating screen once and put into a container lined with a double-layer plastic bag as the third material.

[0045] Pass 2.720kg of lactose (100 mesh), 3.200kg of microcrystalline cellulose 102, 0.800kg of sodium carboxymethyl starch, 1.520kg of corn starch, together through a vortex vibrating sieve 40 mesh screen twice, and put them into a double-layer plastic bag lined In the container, as the fourth material.

[0046] Pass 0.080 kg of magnesium stearate t...

Embodiment 2

[0065] The amount of lactose in the first material was 1.968 kg, the amount of lactose in the second material was 1.476 kg, the amount of lactose in the third material was 3.936 kg, and the amount of lactose in the fourth material was 2.460 kg. The rest is the same as in Example 1.

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Abstract

The invention provides a letrozole tablet and a preparation method thereof. The letrozole tablet comprises a tablet core comprising the following components, by weight: 1-4% of letrozole, 20 to 40% ofmicrocrystalline cellulose, 40 to 65% of lactose, 11.5%-16.5% of a disintegrating agent, and 1 to 1.5% of a lubricating agent. On the basis of the total weight of the tablet core, the lubricating agent comprises 0.3%-0.5% of magnesium stearate and 0.7%-1.0% of superfine silica powder; and the disintegrating agent comprises 3%-7% of sodium carboxymethyl starch and 8.5%-9.5% of corn starch. After controlling of the use amounts of the corn starch and the sodium carboxymethyl starch, on the one hand, the disintegration time of the letrozole tablet is regulated and controlled;and on the other hand, the mixing uniformity of the superfine silica powder in the mixing and tabletting processes is ensured and the demixing phenomenon is avoided. The dosage ratio of the superfine silica powder, the lactose and the corn starch is strictly controlled, so that the mixing uniformity of the materials and the dissolution rate of the letrozole are guaranteed. The clinical application requirements are met.

Description

Technical field [0001] The invention relates to the field of preparation of letrozole tablets, in particular to a letrozole tablet and a preparation method thereof. Background technique [0002] Letrozole is a third-generation aromatase inhibitor and a non-steroidal drug. Its structural formula is as follows: [0003] [0004] Letrozole binds to the iron atoms in heme and competes with endogenous substrates for the active site of aromatase, thereby reversibly inhibiting enzyme activity, effectively reducing plasma estrogen levels, and eliminating hormone sensitivity Tumor stimulation. So it is especially suitable for breast cancer patients after menopause. [0005] Compared with other aromatase inhibitors and anti-estrogen drugs, letrozole has a stronger anti-tumor effect, but its poor water solubility results in low dissolution after being made into oral solid preparations. Letrozole is classified as BCS Class II The dissolution rate of a compound is related to its bioavailabili...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/4196A61K47/36A61K47/26A61K47/04A61K47/12A61K47/38A61P35/00
CPCA61K9/2009A61K9/2013A61K9/2018A61K9/2054A61K9/2059A61K9/2095A61K31/4196A61P35/00
Inventor 杜加秋董福霞蔡邱华易芬芬邵婷婷
Owner 瀚晖制药有限公司
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