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Tropisetron-containing composition for injection

A technology of tropisetron and composition, which is applied in the field of injection composition containing tropisetron and its preparation, can solve problems such as unqualified clarity, poor resolubility, and lower pH value, and the method is simple , Stabilize the pH value environment, increase the effect of stability

Inactive Publication Date: 2017-11-24
天津双硕医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are tropisetron hydrochloride powder injections and injections on the market in China. The powder injections are all freeze-dried, but the resolubility is not good. After reconstitution, the content of tropisetron hydrochloride in the aqueous solution decreases rapidly, and the acidity changes significantly. The clarity of the injection is unqualified after long-term storage, the pH value is lowered, and the stability is poor

Method used

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  • Tropisetron-containing composition for injection
  • Tropisetron-containing composition for injection
  • Tropisetron-containing composition for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0104] Example 1 Preparation of 2mg / 2ml Tropisetron Hydrochloride Injection

[0105]

[0106] The preparation method is as follows:

[0107] 1) Take the tropisetron raw material, grind it into fine powder, and set aside;

[0108] 2) Take 80% of the total volume of water for injection, dissolve sodium aspartate, glycerin, and 0.1M HCl in turn to adjust the pH value of the solution to 4.6-5.0;

[0109] 3) Take the solution obtained in step 2), add the tropisetron bulk drug powder obtained in step 1), stir, and dissolve to obtain the drug-containing solution ①;

[0110] 4) Take the drug-containing solution ① obtained in step 3), add water for injection to the full amount, and adjust the pH value to 4.6-5.0 with 0.1M HCl or NaOH aqueous solution to obtain the drug-containing solution ②;

[0111] 5) Take the drug-containing solution ② obtained in step 4), adsorb the pyrogen with 0.2% activated carbon, and filter to obtain the drug-containing solution ③;

[0112] 6) Take the d...

Embodiment 2

[0114] Preparation of Example 2 5mg / 5ml Tropisetron Hydrochloride Injection

[0115]

[0116] The preparation method is as follows:

[0117] 1) Take the tropisetron raw material, grind it into fine powder, and set aside;

[0118] 2) Take 80% of the total volume of water for injection, dissolve sodium aspartate, glycerin, and 0.1M HCl in turn to adjust the pH value of the solution to 4.6-5.0;

[0119] 3) Take the solution obtained in step 2), add the tropisetron bulk drug powder obtained in step 1), stir, and dissolve to obtain the drug-containing solution ①;

[0120] 4) Take the drug-containing solution ① obtained in step 3), add water for injection to the full amount, and adjust the pH value to 4.6-5.0 with 0.1M HCl or NaOH aqueous solution to obtain the drug-containing solution ②;

[0121] 5) Take the drug-containing solution ② obtained in step 4), adsorb the pyrogen with 0.2% activated carbon, and filter to obtain the drug-containing solution ③;

[0122] 6) Take the d...

Embodiment 3

[0124] Example 3 Preparation of 2mg / 2ml Tropisetron Citrate Injection

[0125]

[0126] The preparation method is as follows:

[0127] 1) Take the tropisetron raw material, grind it into fine powder, and set aside;

[0128] 2) Take 80% of the total volume of water for injection, dissolve sodium aspartate, glycerin, and 0.1M HCl in turn to adjust the pH value of the solution to 4.6-5.0;

[0129] 3) Take the solution obtained in step 2), add the tropisetron bulk drug powder obtained in step 1), stir, and dissolve to obtain the drug-containing solution ①;

[0130] 4) Take the drug-containing solution ① obtained in step 3), add water for injection to the full amount, and adjust the pH value to 4.6-5.0 with 0.1M HCl or NaOH aqueous solution to obtain the drug-containing solution ②;

[0131] 5) Take the drug-containing solution ② obtained in step 4), adsorb the pyrogen with 0.2% activated carbon, and filter to obtain the drug-containing solution ③;

[0132] 6) Take the drug-co...

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Abstract

The invention discloses a tropisetron-containing composition for injection, which can enhance the stability of Tropisetron Hydrochloride Injection in the long-term storage process and reduce the degradation of a raw material, namely tropisetron, in the storage process to generate an impurity A and an impurity B. By addition of aspartic acid and sodium salt thereof in the injection, the degradation of tropisetron is effectively inhibited. Meanwhile a stable pH environment is provided, and the storage stability of a final formulation is further enhanced. In the meantime, a problem that salt forms of drug substances are easily dissociated and separated out during long-term storage of the injection to generate insoluble particles, resulting in the unacceptance of visible particles is solved effectively by applying a crystallization inhibitor, namely glycerin, in the injection. At the same time, as a small molecule, the glycerol also plays a role in regulation of osmotic pressure. The obtained tropisetron injection is simple in preparation method, and capable of being produced by using a conventional preparation method, and has obvious advantages of being prone to industrialization, high in production efficiency, good in stability, controllable in quality, and the like.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a composition for injection containing tropisetron, a preparation method and application thereof. Background technique [0002] With the changes of human living environment, living standards and lifestyles and the advancement of medicine, the spectrum of diseases has undergone significant changes, general infectious diseases have been gradually controlled, and malignant tumors have become common major diseases that seriously affect human life and living standards one. According to the World Health Organization, there are more than 10 million new cancer patients and more than 6 million deaths in the world every year. In my country, more than 1.6 million new cases are added every year, and more than 1.3 million deaths are caused. At present, cancer has become another major cause of death in China and even in the world. [0003] In the past few decades, there have be...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K47/18A61K47/10A61K31/46A61P1/08
CPCA61K9/0019A61K9/08A61K31/46A61K47/10A61K47/183
Inventor 不公告发明人
Owner 天津双硕医药科技有限公司
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