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Tropisetron preparation for injection and preparation method thereof

A technology of tropisetron and tropisetron hydrochloride, which is applied in the direction of digestive system, non-active ingredients of high molecular compounds, active ingredients of heterocyclic compounds, etc., can solve the problem of general solubility of tropisetron, inconvenient use, Affect convenience and other issues, achieve good marketing effect, smooth surface, and stable product quality

Inactive Publication Date: 2010-10-27
海南瑞基药物研究有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, according to the nurses in the hospital, the solubility of tropisetron for injection currently on the market is average. After adding water for injection, it needs to be shaken for a few minutes before it can be completely dissolved, which affects the convenience of use, and the solution is slightly cloudy, which affects the safety of use. And it's not very convenient to use

Method used

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  • Tropisetron preparation for injection and preparation method thereof
  • Tropisetron preparation for injection and preparation method thereof
  • Tropisetron preparation for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Preparation composition (based on 2mg tropisetron) 1000 bottles

[0013] Tropisetron 2g

[0014] β-cyclodextrin 20g

[0015] Mannitol 40g

[0016] Water for injection 1000ml

[0017] Preparation Process

[0018] 1. Weigh tropisetron and β-cyclodextrin, add 80% water for injection and stir to dissolve, then add mannitol, stir to dissolve completely, and use citric acid-disodium hydrogen phosphate buffer (pH4.0 ) to adjust the pH value to 4.0-6.0, add water for injection to the full amount, add needles with a total volume of 0.05-0.1% (g / ml), stir and adsorb with carbon for 20 minutes, and decarburize by filtration.

[0019] 2. Fine filter with 0.22μm microporous membrane.

[0020] 3. Inspection of semi-finished products

[0021] 4. Filling, press half stopper.

[0022] 5. Freeze-drying: first cool down the freeze-drying box to -40°C~-50°C, then put in the sample to make it freeze quickly, the time is 100 minutes to 150 minutes, the sublimation temperature is -40°C...

Embodiment 2

[0024] Preparation composition (based on 2mg tropisetron) 1000 bottles

[0025] Tropisetron 2g

[0026] Hydroxypropyl-β-cyclodextrin 30g

[0027] Mannitol 30g

[0028] Water for injection 1000ml

[0029] Preparation Process

[0030] 1. Weigh tropisetron and hydroxypropyl-β-cyclodextrin, add 80% water for injection and stir to dissolve, then add mannitol, stir to dissolve completely, and use citric acid-disodium hydrogen phosphate buffer solution (pH4.0) adjust the pH value to 4.0-6.0, add water for injection to the full amount, add needles with a total volume of 0.05-0.1% (g / ml), stir and adsorb with charcoal for 20 minutes, and decarburize by filtration.

[0031] 2. Fine filter with 0.22μm microporous membrane.

[0032] 3. Inspection of semi-finished products

[0033] 4. Filling, press half stopper.

[0034] 5. Freeze-drying: first cool down the freeze-drying box to -40°C ~ -50°C, then put the sample into it to make it freeze quickly, the time is 100 minutes to 150 min...

Embodiment 3

[0036] Preparation composition (based on 5mg tropisetron) 1000 bottles

[0037] Tropisetron 5g

[0038] β-cyclodextrin 40g

[0039] Mannitol 100g

[0040] Water for injection 2000ml

[0041] Preparation Process

[0042] 1. Weigh tropisetron and β-cyclodextrin, add 80% water for injection and stir to dissolve, then add mannitol, stir to dissolve completely, and use citric acid-disodium hydrogen phosphate buffer (pH4.0 ) to adjust the pH value to 4.0-6.0, add water for injection to the full amount, add needles with a total volume of 0.05-0.1% (g / ml), stir and adsorb with carbon for 20 minutes, and decarburize by filtration.

[0043] 2. Fine filter with 0.22μm microporous membrane.

[0044] 3. Inspection of semi-finished products

[0045] 4. Filling, press half stopper.

[0046] 5. Freeze-drying: first cool down the freeze-drying box to -40°C ~ -50°C, then put the sample into it to make it freeze quickly, the time is 100 minutes to 150 minutes, the sublimation temperature ...

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Abstract

The invention provides a tropisetron preparation for injection. The main active components of the tropisetron preparation are tropisetron, beta-cyclodextrin or hydroxypropyl-beta-cyclodextrin and mannitol. The method comprises the following steps: dissolving tropisetron hydrochloride and the beta-cyclodextrin or the hydroxypropyl-beta-cyclodextrin, then adding the mannitol for dissolving, adjusting the pH value with citric acid-disodium hydrogen phosphate buffer solution to obtain a liquid medicine, quickly prefreezing the liquid medicine after filling, and then lyophilizing to obtain the tropisetron preparation. The tropisetron preparation for injection has flat surface, is fine and smooth and uniform, and is free from crack, breakage and sticking to bottles. The tropisetron preparation is a white loose block which is well formed and very easily dissolved, has good redissolution performance, clean and transparent solution, stable product quality, and practicability.

Description

technical field [0001] The present invention relates to pharmaceutical preparations, and particularly provides a freeze-dried preparation that can be used as anti-nausea and vomiting, which contains endo-1H-indole-3-carboxylic acid-8-methyl-8-azabicyclo[3.2. 1] Oct-3-yl ester (ie tropisetron). Background technique [0002] According to literature reports, tropisetron hydrochloride is unstable in aqueous solution, and if it is placed for a long time, part of the hydrochloride will be hydrolyzed and separated, resulting in insoluble visible foreign matter, which will affect the quality of the drug and reduce the curative effect, so it is suitable to be made into a freeze-dried agent. However, according to the nurses in the hospital, the solubility of tropisetron for injection currently on the market is average. After adding water for injection, it needs to be shaken for a few minutes before it can be completely dissolved, which affects the convenience of use, and the solution ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/46A61K47/40A61P1/08
Inventor 陶灵萍
Owner 海南瑞基药物研究有限公司
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