A kind of letrozole tablet and preparation method thereof

A technology for letrozole tablets and azole tablets, which is applied in the field of letrozole tablets and its preparation, can solve the problems that the dissolution rate cannot be effectively controlled, and achieve the effect of dissolution rate guarantee

Active Publication Date: 2020-09-01
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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  • 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

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preparation example Construction

[0029] In order to further increase the uniformity of the mixing of the various components, it is preferred that the above preparation method includes: step S1, mixing micronized silica gel with the first part of lactose to form the first mixture; step S2, mixing letrozole and the second part of lactose with 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, 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 tablet cores.

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

Embodiment 1

[0041] preprocessing

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

[0043] With 0.400kg letrozole and 1.520kg lactose (100 mesh), pass through the 40 mesh sieve of vortex vibrating sieve jointly 3 times, pack in the container of lining double-layer plastic bag, as the second material.

[0044] With 3.840kg lactose (100 order), pass the 40 order screen cloth of vortex vibrating sieve 1 time, pack in the container lined double-layer plastic bag, as the 3rd material.

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

[0046] 0.080 kg...

Embodiment 2

[0065] The amount of lactose in the first material is 1.968kg, the amount of lactose in the second material is 1.476kg, the amount of lactose in the third material is 3.936kg, and the amount of lactose in the fourth material is 2.460kg. All the other are with embodiment 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, which is a non-steroidal drug. Its structural formula is as follows: [0003] [0004] Letrozole binds to the iron atom in heme and competes with the endogenous substrate for the active site of aromatase, thereby reversibly inhibiting the activity of the enzyme and effectively reducing the level of plasma estrogen, thereby eliminating hormone-sensitive Tumor stimulation. Therefore, it is especially suitable for postmenopausal breast cancer patients. [0005] Compared with other aromatase inhibitors and anti-estrogen drugs, letrozole has a stronger anti-tumor effect, but its water solubility is poor, resulting in low dissolution rate after it is made into oral solid preparations. Letrozole is BCS Class II Compounds whose diss...

Claims

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Application Information

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Patent Type & Authority Patents(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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