Preparation and inclusion method of albendazole inclusion complex tablets

A technology of albendazole and inclusion complex, applied in the field of pharmaceutical preparations, can solve the problems of low bioavailability, poor solubility of albendazole and the like, and achieve the effects of simple preparation process, improved in-vitro performance, and high stability

Inactive Publication Date: 2018-02-09
NANJING UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Aiming at the problem of poor solubility of albendazole, the present invention uses β-cyclodextrin as an inclusion material to prepare clathrates, so that the drug dissolution and absorption of the drug in the gastrointestinal tract are increased, and the problem of poor solubility of albendazole is solved. The problem of low utilization

Method used

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  • Preparation and inclusion method of albendazole inclusion complex tablets
  • Preparation and inclusion method of albendazole inclusion complex tablets
  • Preparation and inclusion method of albendazole inclusion complex tablets

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] prescription:

[0030] Albendazole

20g

β-cyclodextrin

85.4g

microcrystalline cellulose

100g

Croscarmellose Sodium

60g

Magnesium stearate

5g

[0031] Made in 1000 pieces.

[0032] Preparation method: After dissolving albendazole in formic acid, add it to the mixed solution of acetone: ethanol = 1:1. Dissolve β-cyclodextrin in water and add it dropwise to the mixed solution of albendazole, stir at 55°C for 6h, then put it in the refrigerator for 1h, filter, wash the solid with pure water, and dry it in a blast oven at 50°C Dry to obtain clathrate. Albendazole clathrate and filler microcrystalline cellulose, disintegrating agent croscarmellose sodium and lubricant magnesium stearate are mixed again, and then directly powdered into tablets with a tablet machine. The weight of the dose should be within 3~4kg, and the disintegration time should be within 1~2min.

Embodiment 2

[0034] prescription:

[0035] Albendazole

20g

β-cyclodextrin

170.8g

microcrystalline cellulose

100g

Croscarmellose Sodium

60g

Magnesium stearate

5g

[0036] Made in 1000 pieces.

[0037] Preparation method: After dissolving albendazole in formic acid, add it to the mixed solution of acetone: ethanol = 1:1. Dissolve β-cyclodextrin in water and add it dropwise to the mixed solution of albendazole, stir at 55°C for 6h, then put it in the refrigerator for 1h, filter, wash the solid with pure water, and dry it in a blast oven at 50°C Dry to obtain clathrate. Albendazole clathrate and filler microcrystalline cellulose, disintegrating agent croscarmellose sodium and lubricant magnesium stearate are mixed again, and then directly powdered into tablets with a tablet machine. The weight of the dose should be within 3~4kg, and the disintegration time should be within 1~2min.

Embodiment 3

[0039] prescription:

[0040] Albendazole

20g

β-cyclodextrin

256.2g

microcrystalline cellulose

100g

Croscarmellose Sodium

60g

Magnesium stearate

5g

[0041] Made in 1000 pieces.

[0042] Preparation method: After dissolving albendazole in formic acid, add it to the mixed solution of acetone: ethanol = 1:1. Dissolve β-cyclodextrin in water and add it dropwise to the mixed solution of albendazole, stir at 55°C for 6h, then put it in the refrigerator for 1h, filter, wash the solid with pure water, and dry it in a blast oven at 50°C Dry to obtain clathrate. Albendazole clathrate and filler microcrystalline cellulose, disintegrating agent croscarmellose sodium and lubricant magnesium stearate are mixed again, and then directly powdered into tablets with a tablet machine. The weight of the dose should be within 3~4kg, and the disintegration time should be within 1~2min.

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Abstract

The invention belongs to the field of pharmaceutical preparations, and relates to the preparation of albendazole inclusion complex tablets and the inclusion method thereof. Main feature of the present invention is to take albendazole as main component, with ethanol, acetone, formic acid and glacial acetic acid as solvent, with β-cyclodextrin as clathrate material albendazole is prepared into clathrate, then The albendazole inclusion compound is fully mixed with a fixed amount of filler, disintegrant, and lubricant to prepare tablets directly. The albendazole inclusion compound tablet prepared by the invention solves the problem of poor solubility of albendazole, and finally improves its bioavailability in vivo.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations and relates to an inclusion method for preparing albendazole inclusion compounds. Background technique [0002] Albendazole (Albendazole, ABZ, Formula 1), also known as albendazole, belongs to fat-soluble benzimidazole derivatives. It is one of the first-choice drugs for coccidiosis, but its poor water solubility, low intestinal absorption rate, low blood concentration in vivo, and low bioavailability limit the clinical effect to a certain extent. Moreover, its curative effect is positively correlated with its solubility. Therefore, improving the solubility and dissolution rate of ABZ is an effective way to treat echinococcosis at present. The current clinical common dosage forms have a cure rate of only about 30% for non-intestinal parasitic diseases. [0003] [0004] Albendazole structural formula. [0005] Commonly used preparation techniques for solving the poor water solubili...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/69A61K31/4184A61P33/02A61P33/10
CPCA61K9/2054A61K31/4184
Inventor 任丽莉王瑾陈国广
Owner NANJING UNIV OF TECH
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