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Carbazole sulfonamide antineoplastic agent capsules and preparation method

An anti-tumor drug, carbazole sulfonamide technology, applied in the direction of anti-tumor drugs, drug combination, capsule delivery, etc., can solve problems such as insoluble in water, capsule dissolution rate cannot reach, and achieve the effect of quality assurance

Active Publication Date: 2012-09-05
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 anti-tumor activity, but the compound is difficult to dissolve in water. According to the general capsule preparation process, the dissolution rate of the capsule is far from meeting the requirements of the Pharmacopoeia.

Method used

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  • Carbazole sulfonamide antineoplastic agent capsules and preparation method
  • Carbazole sulfonamide antineoplastic agent capsules and preparation method
  • Carbazole sulfonamide antineoplastic agent capsules and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0051] Prescription: (1000 capsules)

[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 50g of N-(2,6-dimethoxypyridine-3-substituted)-9-methylcarbazole-3-sulfonamide and 100g of β-cyclodextrin, grind it 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 14-mesh sieve, 50°C-60°C Dry and sieve through a 14-mesh sieve.

[006...

Embodiment 2

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

[0063] Prescription: (1000 capsules)

[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 6g

[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, and continue to grind until fine powder. 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 14-mesh sieve, dry at 50°C to 60°C, and dry for 14 Mesh sieve for whole grains.

[0073]...

Embodiment 3

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

[0075] Prescription: (1000 capsules)

[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] Micronized silica gel 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 12g 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 14-mesh sieve, 50°C-60°C Dry and sieve through a 14-mesh sieve...

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Abstract

The invention belongs to the field of pharmaceutic preparations and relates to a preparation method of the antineoplastic agent, in particular to carbazole sulfonamide antineoplastic agent capsules and a preparation method thereof. The carbazole sulfonamide antineoplastic agent capsules are characterized in that: lactose and beta-cyclodextrin are added into a carbazole sulfonamide medicine, namely N-(2,6-dimethypyridine-3-yl)-9-methylcarbazole-3-sulfamide; the materials are mixed and ground into micro powder; the micro powder is granulated, and the granulates are formed into capsules; and thedissolution rate of the capsules are improved.

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 capsule 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 seri...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/48A61K31/4439A61K47/40A61P35/00
Inventor 解晓荣李立忠李润宝王勇高文胡成伟
Owner SHANXI PUDE PHARMA CO LTD