Letrozole troche and preparation method of letrozole troche

Abstract

The invention discloses a letrozole troche and a preparation method of the letrozole troche. The letrozole troche disclosed by the invention is prepared from the following original auxiliary materials in parts by weight: 1-5 parts of letrozole, 0-56.5 parts of microcrystalline cellulose, 30-70 parts of lactose, 0-50 parts of pregelatinized starch, 0-10 parts of croscarmellose sodium, 0-10 parts of polyvinylpolypyrrolidone, and 0.5-2.0 parts of stearic acid, wherein coating powder is a film coating premixed agent. The preparation method of the letrozole troche comprises the following steps of taking letrozole bulk drug, and putting the letrozole bulk drug in crushing equipment to crush; uniformly mixing the crushed letrozole bulk drug with a filling agent and a disintegrating agent according to the amount; adding magnesium stearate according to the amount, and uniformly mixing; pressing mixed powder on a tablet press to prepare the troche, thereby obtaining streptomycin; and coating streptomycin on a high-efficiency coating machine, and packaging after the coated troche is qualified. The letrozole troche disclosed by the invention has the advantages of high dissolution rate, simple process, low production cost and the like.

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 is a new generation of aromatase inhibitors, which can reduce the level of estrogen by inhibiting aromatase, thereby eliminating the stimulating effect of estrogen on tumor growth. Compared with other aromatase inhibitors and anti-estrogen drugs, letrozole The anti-tumor effect of letrozole is stronger, but its water solubility is poor, resulting in a low dissolution rate after it is made into oral solid preparations. Letrozole is a BCS Class II compound, and its dissolution rate is related to its bioavailability in vivo. [0003] Patent CN101467971 discloses a dispersible tablet containing letrozole, using solid dispersion technology to solve the problem of slow dissolution, but the process is difficult and cumbersome, the cost is high, and it is not suitable for industrial pro...

AI Technical Summary

Problems solved by technology

[0002] Letrozole is a new generation of aromatase inhibitors, which can reduce the level of estrogen by inhibiting aromatase, thereby eliminating the stimulating effect of estrogen on tumor growth. Compared with other aromatase inhibitors and anti-estrogen drugs, letrozole The anti-tumor effect of letrozole is stronger, but its water solubility is poor, resulting in a low dissolution rate after it is made into oral solid preparations. Letrozole is a BCS Class II compound, and its dissolution rate is related to the bioavailability in vivo

[0003] Patent CN101467971 discloses a dispersible tablet containing letrozole, using solid dispersion technology to solve the problem of slow dissolution, but the process is difficult and cumbersome, the cost is high, and it is not suitable for industrial production; patent CN101669942 discloses a combination of insoluble drugs It is characterized in that surfactants are added as solubilizers to increase the dissolution rate, but the addition of surfactants will increase the risk of cytotoxicity and hemolysis; patent CN101884791A discloses a letrozole co-grind and its preparation method and its The drug-containing composition improves the dissolution rate by co-grinding with hydrophilic excipients. However, first, the main drug and auxiliary materials are ground together and then transferred out for feeding. There may be a loss of the main drug during the material transfer process, and due to the grinding process Mixed with auxiliary materials, the loss may not be accurately quantified. Second, the particle size is detected after the main drug and auxiliary materials are jointly ground. The particle size result is the particle size of the mixture of the main drug and the auxiliary material, which cannot represent the particle size of the main drug; A combination of aromatase inhibitors and bisphosphonates, the disclosed letrozole tablet core contains 6 kinds of excipients, many types of excipients, and the cost is relatively high

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