Compound medicine containing letrozole and preparation method of compound medicine

Abstract

The invention discloses a compound medicine containing letrozole and a preparation method of the compound medicine. The medicine contains the letrozole, copovidone, mannitol, cellulose, crosslinked povidone, magnesium stearate, polyethylene glycol, lactose and starch. The formula of the medicine consists of 8-20 parts of the letrozole, 80-150 parts of the copovidone, 1-3 parts of the mannitol, 4-6 parts of the cellulose, 1-2 parts of the crosslinked povidone, 1-2 parts of the magnesium stearate, 1-3 parts of the polyethylene glycol, 0.5-1 part of the lactose and 1-2 parts of the starch. The compound medicine provided by the invention can significantly improve a letrozole dissolution rate and can further improve bioavailability and clinical treatment effect of medicinal active ingredients; and in addition, a release speed can be reduced, so that the purpose of uniform administration is achieved; therefore, drug tolerance is enhanced.

Description

technical field [0001] The invention belongs to the technical field of medicine production, and in particular relates to a compound medicine of letrozole and a preparation method thereof. Background technique [0002] Letrozole is a synthetic benzyltriazole derivative, which is a new type of highly selective aromatase inhibitor. By inhibiting aromatase, the level of estrogen is reduced, thereby eliminating the stimulating effect of estrogen on tumor growth. Letrozole is 150-250 times more potent in vivo than the first-generation aromatase inhibitor, aminoglutethimide. Clinical studies have proved that letrozole has strong antitumor effect, high specificity, and less toxic and side effects. [0003] Letrozole is the third-generation aromatase inhibitor first developed by Novartis in Switzerland. It was first launched in the UK in 1996, and then in the United States in 1997. It is currently on the market in more than 30 countries and regions For the first-line treatment of a...

AI Technical Summary

Problems solved by technology

[0004] However, letrozole is almost insoluble in water, and the dissolution rate of the preparation is low, which will affect the bioavailability and thus affect the efficacy

A kind of micronized letrozole disclosed in Chinese patent CN101099724 and its composition, its method is to improve its dissolution rate from the preparation by micronizing letrozole, but the degree of improvement is not large, which is comparable to the dissolution rate of Novartis products. There is also a large gap; CN101467971 discloses a dispersible tablet containing letrozole, which adopts the method of solid dispersion to improve the dissolution rate of letrozole from the preparation, but the process is complicated and is not suitable for suitability for industrialized production; CN101669942 discloses a difficult Soluble drug composition, the method of adding a certain amount of surfactant in the composition as a solubilizer can obviously improve the dissolution rate of the drug, but in the field of pharmaceuticals, even non-ionic surfactants have certain cytotoxicity and hemolysis. cause allergic reaction