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Ultra-fine bicalutamide oral tablet and preparation method thereof

A technology for oral calutamide tablets and bicalutamide, which is applied in the directions of pill delivery, pharmaceutical formulations, and medical preparations of inactive ingredients, etc., can solve problems such as low dissolution rate, drug pollution, drug loss, etc. The effect of convenient control, simplified production process and improved dissolution rate

Active Publication Date: 2012-07-18
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this method has the following three disadvantages: First, this method uses mechanical grinding to micronize bicalutamide, the loss of the drug is serious during the mechanical grinding process, and the long-term contact between the grinding medium and the drug may also cause contamination of the drug
After mechanical grinding, the particle size of bicalutamide is about 25 μm, and the particle size is uneven; secondly, the high-speed wet granulator used in this method stirs the drug and excipients, the equipment used consumes a lot of energy, and the wet granules need to be dried Dry, with a wide range of particle size distribution and unevenness. Generally, it needs to be granulated twice to meet the requirements.
In addition, the formula bicalutamide drug mass content of the patent preparation is less than 30%, the drug content is low
[0009] PCT patent application WO 2008 / 099160A1 discloses a formulation of bicalutamide tablets, the formulation uses microcrystalline cellulose as the main auxiliary material to prepare bicalutamide tablets, but the dissolution rate of the tablet is low, the first 30min The dissolution rate within the drug is only 80%, and the content of the drug is also low, only about 30%

Method used

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  • Ultra-fine bicalutamide oral tablet and preparation method thereof
  • Ultra-fine bicalutamide oral tablet and preparation method thereof
  • Ultra-fine bicalutamide oral tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Take 5g of bicalutamide bulk drug, dissolve it in 50ml of N-N dimethylacetamide, pour the solution into 1000ml of deionized water containing 3.5g of lactose, stir at high speed for 30min, wherein the rotating speed of high-speed stirring is 10000rpm, and the reaction temperature at 15°C to obtain a suspension containing bicalutamide nanoparticles, spray-dry, and set the spray-drying temperature to 140°C, uniformly mix the obtained powder with various pharmaceutical excipients, pass through a 100-mesh molecular sieve, and press into tablets. The contents of various drugs are shown in Table 4:

[0042] Table 4 Example 1 sample bicalutamide tablet formula

[0043] Raw materials

Embodiment 2

[0045] Take 5g of bicalutamide raw material, dissolve it in 50ml of N-N dimethylacetamide, pour the solution into 500ml of deionized water containing 5g of polyvinylpyrrolidone, stir at high speed for 30min, control the reaction temperature at 25°C, and rotate at 8000rpm. A suspension containing bicalutamide nanoparticles was obtained, and the mixed suspension was spray-dried, and the spray-drying temperature was set at 130° C., the obtained powder was uniformly mixed with pharmaceutical excipients, passed through a 100-mesh molecular sieve, and compressed into tablets. The contents of various drugs are shown in Table 5:

[0046] Table 5. Example 2 sample bicalutamide tablet formula

[0047] Raw materials

Embodiment 3

[0049] Take 5g of bicalutamide raw material, dissolve it in 40ml of dimethyl sulfoxide, pour the solution into 400ml of deionized water containing 2.5g of lactose and 2.5g of polyvinylpyrrolidone, stir at high speed for 35min, and the reaction temperature is 20°C , rotate at 8000rpm, and spray dry the mixed solution. The spray drying temperature is set at 130°C. The obtained powder is uniformly mixed with pharmaceutical excipients, passed through a 100-mesh molecular sieve, and compressed into tablets. The contents of various drugs are as shown in Table 6:

[0050] Table 6 Example 3 sample bicalutamide tablet formula

[0051] Raw materials

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Abstract

The invention relates to an ultra-fine bicalutamide oral tablet and a preparation method thereof. The bicalutamide with small granule is prepared by a simple antisolvent recrystallization method; in addition, by improving the formula of the medicament, the content of effective elements of the medicament is increased, and the dissolution degree of the medicament is greatly improved. The invention simplifies the production process and reduces the production energy consumption by utilizing a new production process flow.

Description

Technical field: [0001] The invention relates to a superfine bicalutamide oral tablet and a preparation method thereof. Background technique: [0002] Prostate cancer (PCA) is a common malignant tumor of the male reproductive system, and it is also the second most common malignant tumor in males worldwide after lung cancer, and its incidence is on the rise worldwide. Endocrine therapy is one of the main treatment methods for prostate cancer and has been applied to various stages of prostate cancer. [0003] The pharmacology of bicalutamide is: pure androgen receptor (AR) antagonist, Furr (Furr) endocrine test shows that the affinity of bicalutamide to mouse androgen receptor is better than the active metabolism of flutamide in vivo The product is 4 times stronger and can competitively inhibit androgen. This product has peripheral selectivity, has pure antiandrogen effect, has no androgen, estrogen, glucocorticoid or mineralocorticoid activity, and hardly affects serum lute...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K31/167A61K47/26A61K47/32A61K47/36A61P35/00A61P13/08
Inventor 陈建峰李婵乐园王洁欣
Owner BEIJING UNIV OF CHEM TECH