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Carbazole sulfamide-derived anti-tumor medicine tablets and preparation method thereof

An anti-tumor drug, carbazole sulfonamide technology, applied in the field of carbazole sulfonamide anti-tumor drug tablets and its preparation, anti-tumor preparations, can solve the problem of insoluble in water, tablet dissolution rate cannot reach And other issues

Active Publication Date: 2012-02-15
SHANXI PUDE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The compound has significant antitumor activity, but the compound is difficult to dissolve in water. According to the general tablet preparation process, the dissolution rate of the tablet is far from meeting the requirements of the Pharmacopoeia.

Method used

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  • Carbazole sulfamide-derived anti-tumor medicine tablets and preparation method thereof
  • Carbazole sulfamide-derived anti-tumor medicine tablets and preparation method thereof
  • Carbazole sulfamide-derived anti-tumor medicine tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Example 1 Preparation of N-(2,6-dimethoxypyridine-3-substituted)-9-methylcarbazole-3-sulfonamide tablets

[0051] Prescription: (1000 tablets)

[0052] N-(2,6-dimethoxypyridine-3-substituted)-9-methylcarbazole-3-sulfonamide 50g

[0053] β-cyclodextrin 100g

[0054] Lactose 250g

[0055] Low-substituted hydroxypropyl cellulose 10g

[0056] Magnesium Stearate 4g

[0057] Preparation Process:

[0058] (1) After mixing 50 g of N-(2,6-dimethoxypyridine-3-substituted)-9-methylcarbazole-3-sulfonamide and 100 g of β-cyclodextrin, it was ground to fine powder.

[0059] (2) Add 250 g of lactose to the above-mentioned fine powder, continue to grind to fine powder, and pass through a 200-mesh sieve.

[0060] (3) Mix the micropowder prepared in (2) and 10 g of low-substituted hydroxypropyl cellulose passed through a 100-mesh sieve evenly, add 50% ethanol aqueous solution to make a soft material, granulate with a 20-mesh sieve, and dry at 60-80°C , 18-mesh sieve for granulation....

Embodiment 2

[0062] Example 2 Preparation of N-(2,6-dimethoxypyridine-3-substituted)-9-methylcarbazole-3-sulfonamide tablets

[0063] Prescription: (1000 tablets)

[0064] N-(2,6-dimethoxypyridine-3-substituted)-9-methylcarbazole-3-sulfonamide 100g

[0065] β-cyclodextrin 100g

[0066] Lactose 100g

[0067] Microcrystalline Cellulose 15g

[0068] Magnesium Stearate 7g

[0069] Preparation Process:

[0070] (1) After mixing 100g of N-(2,6-dimethoxypyridine-3-substituted)-9-methylcarbazole-3-sulfonamide and 100g of β-cyclodextrin, grind it to fine powder.

[0071] (2) Add 100 g of lactose to the above-mentioned fine powder, continue to grind to fine powder, and pass through a 200-mesh sieve.

[0072] (3) Mix the micropowder prepared in (2) and 15 g of microcrystalline cellulose passed through a 100-mesh sieve evenly, add 50% ethanol aqueous solution to make a soft material, granulate with a 20-mesh sieve, dry at 60-80 ° C, 18-mesh Sieve whole grains.

[0073] (4) The granules prepare...

Embodiment 3

[0074] Example 3 Preparation of N-(2,6-dimethoxypyridine-3-substituted)-9-methylcarbazole-3-sulfonamide tablets

[0075] Prescription: (1000 tablets)

[0076] N-(2,6-dimethoxypyridine-3-substituted)-9-methylcarbazole-3-sulfonamide 50g

[0077] β-cyclodextrin 150g

[0078] Lactose 350g

[0079] Low-substituted hydroxypropyl cellulose 12g

[0080] Magnesium Stearate 6g

[0081] Preparation Process:

[0082] (1) After mixing 50g of N-(2,6-dimethoxypyridine-3-substituted)-9-methylcarbazole-3-sulfonamide and 150g of β-cyclodextrin, grind it to fine powder.

[0083] (2) Add 350 g of lactose to the above-mentioned fine powder, and continue to grind until fine powder. Pass through a 200 mesh sieve.

[0084] (3) Mix the micropowder prepared in (2) and 12 g of low-substituted hydroxypropyl cellulose passing through a 100-mesh sieve evenly, add 50% ethanol aqueous solution to make a soft material, granulate with a 20-mesh sieve, and dry at 60-80°C , 18-mesh sieve for granulation....

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Abstract

The invention belongs to the field of pharmaceutic preparation and relates to a method for preparing anti-tumor preparations, in particular to carbazole sulfamide-derived anti-tumor medicine tablets and a preparation method thereof. The invention is characterized in that lactose and beta-cyclodextrin are added to a carbazole sulfamide-derived medicine, i.e. N-(2,6-dimethoxypyridine-3-substitution)-9-methyl carbazole-3-sulfamide, for mixing, and the mixture is ground to micro powder and prepared into the tablets. Therefore, the dissolution rate of the tablets can be increased.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a preparation method of an antitumor preparation, in particular to a carbazole sulfonamide antitumor drug tablet and a preparation method thereof. Background technique [0002] Tubulin inhibitors are a class of effective anti-tumor drugs. With the wide application of paclitaxel in clinical practice and the in-depth understanding of the structure and function of microtubules, the research on anti-tumor drugs targeting tubulin and development are increasingly attracting the attention of pharmaceutical companies worldwide. [0003] At present, paclitaxel and vinblastine tubulin inhibitors have been successfully used in the clinical treatment of various tumors, but as a natural product of macromolecules, their synthesis is difficult, their bioavailability is low, and they have toxic side effects. In particular, multiple The emergence of drug-resistant glycoproteins has serio...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4439A61K47/26A61K47/40A61K9/20A61P35/00
Inventor 解晓荣李立忠李润宝王勇高文胡成伟
Owner SHANXI PUDE PHARMA CO LTD