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Letrozole tablet with high dissolubility and preparation method thereof

A technology for letrozole tablets and dissolution rate is applied in the directions of pharmaceutical formulations, medical preparations without active ingredients, medical preparations containing active ingredients, etc. Achieve the effect of improving bioavailability, saving energy and increasing absorption

Active Publication Date: 2012-06-06
SHENZHEN NEPTUNUS PHARM CO LTD
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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
However, the solid dispersion preparation process is difficult to scale up, and industrial production is difficult

Method used

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  • Letrozole tablet with high dissolubility and preparation method thereof
  • Letrozole tablet with high dissolubility and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] [Example 1] Prescription composition and preparation of letrozole tablets with high dissolution rate

[0034] Prescription A total of 8000 tablets

[0035] Letrozole 20g

[0036] Polyvinylpyrrolidone K30 35g

[0037] Tween 80 15g

[0038] Mannitol 30g

[0039] Lactose 500g

[0040] Microcrystalline Cellulose 450g

[0041] Cross-linked polyvinylpolypyrrolidone 40g

[0042] Magnesium Stearate 5g

[0043] Preparation method: Add the prescribed amount of polyvinylpyrrolidone K30 (PVP K30), Tween 80, and mannitol into 400ml of water, stir to form a uniform solution, add letrozole into the solution, and disperse it uniformly for 5 minutes with ultrasonic to obtain a suspension ; Lactose, microcrystalline cellulose, and cross-linked polyvinylpolypyrrolidone (PVPP) of the above-mentioned prescription quantity are mixed uniformly, and the above-mentioned suspension is sprayed into the mixed auxiliary material by a spray gun with a peristaltic pump, and stirred while spray...

Embodiment 2

[0044] [Example 2] Prescription Composition and Preparation of High Dissolution Letrozole Tablets

[0045] Prescription A total of 8000 tablets

[0046] Letrozole 20g

[0047] Polyvinylpyrrolidone K30 20g

[0048] Tween 80 20g

[0049] Mannitol 20g

[0050] Lactose 600g

[0051] Microcrystalline Cellulose 350g

[0052] Cross-linked polyvinylpolypyrrolidone 30g

[0053] Magnesium Stearate 5g

[0054] Preparation method: Add the prescribed amount of polyvinylpyrrolidone K30 (PVP K30), Tween 80, and mannitol into 400ml of water, stir to form a uniform solution, add letrozole to the solution, and disperse it evenly for 10 minutes by ultrasonication to obtain a suspension ; Lactose, microcrystalline cellulose, and cross-linked polyvinylpolypyrrolidone (PVPP) of the above-mentioned prescription quantity are mixed uniformly, and the above-mentioned suspension is sprayed into the mixed auxiliary material by a spray gun with a peristaltic pump, and stirred while spraying, to mak...

Embodiment 3

[0055] [Example 3] Prescription Composition and Preparation of High Dissolution Letrozole Tablets

[0056] Prescription A total of 8000 tablets

[0057] Letrozole 20g

[0058] Polyvinylpyrrolidone K30 25g

[0059] Tween 80 20g

[0060] Mannitol 25g

[0061] Lactose 600g

[0062] Microcrystalline Cellulose 350g

[0063] Cross-linked polyvinylpolypyrrolidone 25g

[0064] Magnesium Stearate 5g

[0065]Preparation method: Add the prescribed amount of polyvinylpyrrolidone K30 (PVP K30), Tween 80, and mannitol into 500ml of water, stir to form a uniform solution, add letrozole into the solution, and disperse it evenly for 10 minutes with ultrasonic to obtain a suspension ; Lactose, microcrystalline cellulose, and cross-linked polyvinylpolypyrrolidone (PVPP) of the above-mentioned prescription quantity are mixed uniformly, and the above-mentioned suspension is sprayed into the mixed auxiliary material by a spray gun with a peristaltic pump, and stirred while spraying, to make ...

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Abstract

The invention discloses a Letrozole tablet with high dissolubility and a preparation method thereof. An effective component of the tablet is Letrozole, and polyvinylpyrrolidone K30, tween 80, mannitol, lactose, microcrystalline cellulose, cross-linked polyvinylpolypyrrolidone and magnesium stearate are used as accessories. The product of the tablet has stable quality and high dissolubility, enables absorption of Letrozole in a human body to be increased and bioavailability to be effectively improved and is easy to prepare and applicable to industrial production.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a letrozole tablet with high dissolution rate and a preparation method thereof. Background technique [0002] Letrozole is a new-generation aromatase inhibitor, which is a synthetic benzyltriazole derivative. Letrozole reduces the level of estrogen by inhibiting aromatase, thereby eliminating the stimulating effect of estrogen on tumor growth. The indication is postmenopausal advanced breast cancer, and it is mostly used for second-line treatment after failure of anti-estrogen therapy. Letrozole has no potential toxicity to the system and target organs of the whole body, and has the characteristics of good tolerance and strong pharmacological effects. Compared with other aromatase inhibitors and anti-estrogen drugs, letrozole has stronger antitumor effect. [0003] Its structural formula is as follows: [0004] [0005] Letrozole has poor water solubility, and the...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/4196A61K47/38A61P35/00
Inventor 叶冠豪冯汉林王志国任新荣严启新李勇
Owner SHENZHEN NEPTUNUS PHARM CO LTD
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