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Letrozole tablet and preparation method thereof

A letrozole tablet and auxiliary material technology, applied in the field of letrozole tablet and its preparation, can solve the problems of poor dissolution rate, poor water solubility, dust pollution, etc., and achieve the effect of increased dissolution rate and improved stability

Active Publication Date: 2013-10-23
HAINAN LINHENG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the poor water solubility of letrozole, it is necessary to solve the problem of poor dissolution rate through preparation technology when preparing solid preparations
Chinese patent CN101099724 discloses a micronized letrozole and its composition. The method is to micronize letrozole into a particle size of 10-100 microns and then combine with a carrier to prepare a preparation with suitable dissolution rate. However, the micronized process It needs a lot of energy, and there is a risk of particle aggregation, and the particle size is too small, and the powder floating during the preparation process will cause material loss and dust pollution, which is not conducive to industrial scale-up production

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

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Embodiment 1: the preparation of letrozole tablet

[0019] Letrozole prescription:

[0020] Letrozole 2.5g

[0021] Microcrystalline Cellulose 12.5g

[0022] Lactose 90g

[0023] Sodium starch glycolate 2.5g

[0024] L-HPC 0.5g

[0025] Sodium Lauryl Sulfate 1.0g

[0026] Tween 80 0.5g

[0027] Magnesium Stearate 1.5g

[0028] Appropriate amount of starch

[0029] A total of 1000 pieces were made

[0030] Preparation:

[0031] Adhesive preparation: take starch, add appropriate amount of water, stir well, add water and boil to obtain starch slurry with a concentration of about 2.5%, add Tween-80 and mix well;

[0032] Crush and sieve: take the letrozole raw material, ultrafinely pulverize, and pass the auxiliary materials microcrystalline cellulose, lactose, sodium starch glycolate, L-HPC, and sodium lauryl sulfate through an 80-mesh sieve;

[0033] Mixing and granulation: Take the pulverized letrozole and mix it with lactose in equal increments, pass th...

Embodiment 1

[0036] Comparative example 1: the preparation of letrozole tablet

[0037] Letrozole prescription:

[0038] Letrozole 2.5g

[0039] Polyvinylpyrrolidone K30 4.375g

[0040] Tween 80 1.875g

[0041] Mannitol 3.75g

[0042] Lactose 62.5g

[0043] Microcrystalline Cellulose 56.25g

[0044] Cross-linked polyvinylpolypyrrolidone 5g

[0045] Magnesium stearate 0.625g, made into 1000 tablets.

[0046] Preparation:

[0047] Add polyvinylpyrrolidone K30 (PVP K30), polysorbate 80, and mannitol of prescription quantity into 400ml water, stir to form a uniform solution, add letrozole in the solution, and ultrasonically disperse it for 5 minutes to obtain a suspension; Mix the prescribed amount of lactose, microcrystalline cellulose, and cross-linked polyvinylpolypyrrolidone (PVPP) evenly, spray the above suspension into the mixed auxiliary materials through a spray gun with a peristalt...

Embodiment 2

[0048] Comparative example 2: the preparation of letrozole tablet

[0049] Letrozole 2.5g

[0050] Sorbitol 12 g

[0051] Dextrin 57.4g

[0052] Aspartame 1.7 g

[0053] Cross-linked polyvinylpyrrolidone 7.5 g

[0054] Polysorbate 80 0.1 g

[0055]Hypromellose 0.6 g

[0056] Orange essence 1.0 g, made into 1000 pieces.

[0057] Preparation:

[0058] (1) Letrozole is pulverized through a 170 mesh sieve for subsequent use;

[0059] (2) All auxiliary materials are passed through an 80-mesh sieve for subsequent use;

[0060] (3) Sorbitol, dextrin, aspartame, and cross-linked polyvinylpyrrolidone are weighed and mixed uniformly to obtain material I. Letrozole is taken in an equal amount and added to material I in equal amounts, mixed uniformly to obtain material II;

[0061] (4) Add polysorbate 80 to 2% hypromellose aqueous solution to make a binder, add an appropri...

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PUM

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Abstract

The invention relates to a letrozole tablet and a preparation method thereof. The letrozole tablet comprises the following main auxiliary materials: microcrystalline cellulose, lactose, sodium starch glycolate, L-HPC (low-substituted hydroxypropyl cellulose), sodium lauryl sulfate, Tween 80, magnesium stearate and starch; the preferable sodium lauryl sulfate:Tween 80 ratio is 2:1, and the sodium starch glycolate:L-HPC ratio is 5:1. The tablet has stable product quality, obviously enhances the letrozole dissolution, and effectively enhances the bioavailability; and the tablet preparation technique is simple, does not need special equipment, and is convenient to operate and suitable for industrial production.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a letrozole tablet and a preparation method thereof. Background technique [0002] Letrozole (Letrozole) chemical name is 1-[bis(4-cyanophenyl)methyl]-1,2,4-triazole, which is a synthetic benzyltriazole derivative and is an oral It is a highly specific non-steroidal third-generation aromatase inhibitor, which has become the first-line treatment drug for postmenopausal breast cancer. Letrozole was developed by the Swiss Ciba Pharmaceutical Company. It was first launched in the UK in 1996 and in the United States in 1997. It has been listed in more than 30 countries and regions for the first-line treatment of advanced breast cancer and is widely used as a second-line drug for breast cancer. . Domestic Jiangsu Hengrui Pharmaceutical Co., Ltd. obtained the production approval in 1999, and the trade name is "Furui". Letrozole of Novartis was also listed in China in 2003, ...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/4196A61K47/38A61K47/36A61K47/26A61K47/20A61P35/00
Inventor 林尤仁何瑞卿陈梅
Owner HAINAN LINHENG PHARMA
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