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Micronization femara and its composition

A technology of letrozole and micronization, applied in the field of pharmacy, can solve problems such as being unsuitable for large-scale preparation production

Inactive Publication Date: 2008-01-09
上海复旦复华药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The test found that some studies have made letrozole and PEG into dispersed granules for administration. This method is only used for laboratory preparation and is not suitable for large-scale preparation production.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1: Letrozole tablet preparation

[0028] Letrozole (80% particle size less than or equal to 10 microns) 2.5g

[0029] Lactose 80g

[0030] Sodium carboxymethyl starch 2.5g

[0031] 10% ethanol solution of povidone K30 25ml

[0032] Magnesium stearate 0.4g

[0033] A total of 1000 pieces were made

[0034] Preparation process: Mix the micronized letrozole powder with lactose in an equal amount addition method, and then mix it with carboxymethyl starch sodium evenly, add 25ml of ethanol solution containing 10% povidone K30 to make granules, and ventilate and dry at 65°C , whole grain, add the remaining magnesium stearate, mix evenly, and compress into tablets.

Embodiment 2

[0035] Embodiment 2: Preparation of Letrozole Capsules

[0036] Letrozole (80% particle size less than or equal to 10 microns) 2.5g

[0037] Lactose 60g

[0038] Microcrystalline Cellulose 22.5g

[0039] 10% ethanol solution of povidone K30 30ml

[0040] Magnesium stearate 0.4g

[0041] A total of 1000 capsules were made

[0042] Preparation process: mix the micronized letrozole powder with lactose by equal amount addition method, and then mix it with microcrystalline cellulose evenly, prepare granules with 30ml ethanol solution containing 10% povidone K30, ventilate and dry at 65°C, Whole grains, add the remaining magnesium stearate, mix evenly, fill in No. 3 capsules, and get ready.

Embodiment 3

[0044] Each micronized letrozole tablet (embodiment 1) contains 25 mg of letrozole, and each micronized letrozole capsule (embodiment 2) contains 25 mg of letrozole, and each commercially available letrozole tablet contains Letrozole is 25 mg, and the dissolution rate is expressed as a percentage of the labeled amount.

[0045] The mensuration of dissolution rate: get micronized letrozole tablet, micronized letrozole capsule, each 6 pieces of commercially available letrozole sheet respectively, according to dissolution assay (Chinese Pharmacopoeia 2005 edition two appendix XC (second method) )), with 1000ml of 0.1mol / L hydrochloric acid as the solvent, the rotating speed is 75rpm, according to the law. Samples were taken at 5, 10, 15, 30, 45, and 60 minutes for measurement, and the results are as follows:

[0046] 5min

[0047] The dissolution rate of poorly soluble drugs is directly related to its bioavailability. In the case of micronization, it can ensure that ...

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Abstract

The present invention discloses a kind of micronized letrozole and its composite. Said invention utilizes a micronization process to micronize said letrozole and make the micronized letrozole be combined with a proper carrier so as to obtain a micronized letrozol preparation with proper dissolubility. Said preparation can be used for effectively curing mammary cancer.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to micronized letrozole and its composition for treating breast cancer. Background technique [0002] Letrozole is a new generation of aromatase inhibitors, which can reduce the level of estrogen by inhibiting aromatase, thereby eliminating the inhibitory effect of estrogen on tumor growth. Letrozole can effectively inhibit the conversion of estrogen to androgen, and postmenopausal women's estrogen mainly comes from the aromatization of androgen precursors in peripheral tissues, so it is especially suitable for postmenopausal breast cancer patients. [0003] Studies have shown that the in vivo activity of letrozole is 150-250 times stronger than that of the first-generation aromatase inhibitor aminoglutethimide, and the ability of letrozole to reduce plasma estrogen levels in vivo is 8 times that of fadrozole, even in At low doses, it also almost completely inhibits estradiol and estrone in...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/4196A61P35/00
Inventor 马国宏
Owner 上海复旦复华药业有限公司
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