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Dispersible tablet containing letrozole and preparation method thereof

A technology of letrozole and dispersible tablets, which is applied in the field of technology and preparation of solid preparation dispersible tablets, can solve the problems of large loss of raw materials, inability to completely solve the rapid dissolution and absorption of letrozole, and unsuitability for industrial production

Inactive Publication Date: 2016-11-16
BEIJING VENTUREPHARM BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method only considers the disintegration of dispersible tablets, but ignores the insoluble characteristics of the drug itself in water, so it cannot completely solve the problem of rapid dissolution and absorption of the insoluble drug letrozole
[0005] Patent CN101099724 discloses a kind of micronized letrozole and its composition, mainly through jet milling, colloid mill, ball mill and other letrozole differentiation to increase the dissolution rate, but the micronization requires high equipment, and the raw materials in the micronization process drug loss
[0006] Patent CN201110270854 discloses a letrozole orally disintegrating tablet and its preparation method. It mainly improves the dissolution rate of the drug by preparing a solid dispersion. After heating and melting with polyethylene glycol 6000, it is mixed with the main drug to obtain letrozole The azole dispersion needs to be vacuum freeze-dried for 31 hours afterwards. Although it can achieve the effect of accelerating the dissolution rate, the preparation process is very cumbersome and time-consuming, and it requires high equipment, so it is not suitable for industrial production.

Method used

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  • Dispersible tablet containing letrozole and preparation method thereof
  • Dispersible tablet containing letrozole and preparation method thereof
  • Dispersible tablet containing letrozole and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013]

[0014] Preparation Process:

[0015] Letrozole was crushed through a 200-mesh sieve, then mixed with 10 times the weight of lactose through an 80-mesh sieve for 3 times, added the remaining lactose, microcrystalline cellulose and sodium carboxymethyl starch, passed through a 80-mesh sieve for 3 times and mixed evenly, 2% hydroxypropyl Base cellulose as a binder, granulate with a 24 mesh sieve, blow dry at 50 ℃, dry to 1~3% moisture, pass the dried granules through a 24 mesh sieve for granulation, weigh, convert the yield, and add carboxymethyl Starch sodium, silicon dioxide, aspartame, mint flavor and magnesium stearate, Φ8 flat punched tablets, tablet weight 200 mg, hardness 20-40 N.

Embodiment 2

[0017]

[0018] Preparation Process:

[0019] Letrozole was crushed through a 200-mesh sieve, then mixed with 10 times the weight of mannitol through an 80-mesh sieve for 3 times, and the remaining mannitol, microcrystalline cellulose and sodium carboxymethyl starch were mixed through an 80-mesh sieve for 3 times, 2% Hydroxypropyl cellulose is used as a binder, granulated with a 24-mesh sieve, blast-dried at 50 °C, and dried to a moisture content of 1-3%, and the dried granules are passed through a 24-mesh sieve for granulation, weighed, converted yield, and carboxylated Sodium methyl starch, silicon dioxide, aspartame, mint flavor and magnesium stearate, Φ8 flat punched tablets, tablet weight 200 mg, hardness 20-40 N.

Embodiment 3

[0021]

[0022] Preparation Process:

[0023] Letrozole was crushed through a 200-mesh sieve, then mixed with 10 times the weight of lactose through an 80-mesh sieve for 5 times, and the remaining lactose, microcrystalline cellulose and sodium carboxymethyl starch were mixed through an 80-mesh sieve for 3 times, and 2% hydroxypropyl Base cellulose as a binder, granulate with a 24 mesh sieve, blow dry at 50 ℃, dry to 1~3% moisture, pass the dried granules through a 24 mesh sieve for granulation, weigh, convert the yield, and add carboxymethyl Starch sodium, silicon dioxide, aspartame, mint flavor and magnesium stearate, Φ8 flat punched tablets, tablet weight 200 mg, hardness 20-40 N.

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Abstract

The invention discloses a preparation method of a dispersible tablet containing a letrozole-hdrophilic material blend. The dispersible tablet contains a letrozole-hydrophilic material blend and other pharmaceutically acceptable excipients. A wet granulation and tablet compression method is employed for the preparation of the dispersible tablet. The dispersible tablet has good dispersion uniformity, and can effectively improve the dissolution rate of a letrozole solid preparation, improve the compliance for patient administration and bioavailability of the drug. The dispersible tablet can be used for the treatment of breast cancer in postmenopausal women; and the method is simple and applicable to industrialized production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a technology for improving the dissolution rate of letrozole in solid preparations and a preparation method for solid preparation dispersible tablets thereof. Background technique [0002] The chemical name of Letrozole is 4,4'-(1H-1,2,4-triazole-1-1methine)dibenzonitrile (1), which belongs to the synthetic benzyltriazoles Derivatives, the mechanism of action is to reduce the level of estrogen by inhibiting aromatase, thereby eliminating the stimulating effect of estrogen on tumor growth. It is quickly and safely absorbed orally, and is quickly and widely distributed in tissues. The clinical effect of letrozole for patients with advanced breast cancer is better than that of tamoxifen, megestrol, and aminoglutethimide, and its in vivo activity is 150-250 times higher than that of aminoglutethimide and the incidence of adverse reactions Lower than a...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/4196A61K47/26A61P35/00
CPCA61K9/0056A61K9/2018A61K9/2059A61K31/4196
Inventor 刘英甜马莉
Owner BEIJING VENTUREPHARM BIOTECH
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