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Azasetron hydrochloride injection and preparation method thereof

A technology of azasetron hydrochloride and azasetron, which is applied in the direction of pharmaceutical formulations, medical preparations with no active ingredients, medical preparations containing active ingredients, etc., can solve the problem of unstable aqueous solution, affecting product quality, and light Sensitivity and other issues to achieve the effect of reducing adverse reactions, overcoming instability, and low production costs

Active Publication Date: 2013-11-06
ZHEJIANG WAN SHENG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Azasetron hydrochloride is a highly efficient, highly selective, new type of 5-HT 3 Receptor antagonist, via 5-HT on visceral afferents and central chemoreceptors 3 Significant inhibitory effect on the receptor, antagonizing the nausea and vomiting caused by tumor drugs and radiation therapy, and reducing the number of nausea and vomiting in tumor patients within 24 hours after routinely given high-dose cisplatin therapy, the preparation of azasetron hydrochloride is an infusion solution Dosage form, which can facilitate clinical medication and reduce drug-induced pollution, but there are chemical instability factors in azasetron hydrochloride injection itself
[0005] The shortcoming of Azaus hydrochloride injection in the prior art is that it is sensitive to light, high temperature has an impact on the pH of the injection, and the aqueous solution is unstable, which directly affects the quality of the product

Method used

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  • Azasetron hydrochloride injection and preparation method thereof
  • Azasetron hydrochloride injection and preparation method thereof
  • Azasetron hydrochloride injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Preparation of Azasetron Hydrochloride Injection: Weigh sodium chloride, thiourea and methionine respectively according to the batch production instructions, dissolve them in fresh and cooled water for injection in turn, stir and dissolve completely, then add to the instruction amount . Azasetron hydrochloride was weighed so that the weight ratio of azasetron, thiourea, methionine and sodium chloride was 20:3:6:36.

[0018] Add azasetron to the above solution, stir to dissolve, and the operation after adding azasetron hydrochloride needs to be protected from light. Adjust the pH to 3.5-4.5 with 0.1mol / L citric acid. The liquid medicine is filtered through a titanium rod filter and then poured into the fine filter tank. The medicinal liquid in the preparation tank is delivered to the fine filter tank through the infusion pump, and the medicinal liquid is filtered through a 0.45 μm cartridge filter, and the pH value and content are measured by sampling. Visible foreign...

Embodiment 2

[0022] This example detects the influence of different potting environments on the stability of azasetron hydrochloride. Experiments have proved that the use of linked line potting has a lower reject rate and higher yield than single-machine potting lamp inspection.

[0023] Potting environment

Embodiment 3

[0025] In this example, different antioxidants were added to the azasetron injection, and the contents of related substances were detected. The preparation method of azasetron injection is the same as that of Example 1. All the samples in this small test were filled and sealed with 1ml ampoule linkage line, and the number of each sample was 1000.

[0026] Sample number

antioxidant

pH

Sample No. 1

Thiourea + Methionine

pH after preparation is 4.07

No. 2 sample

Methionine+sodium metabisulfite

pH after preparation is 4.08

Sample No. 3

Thiourea + Methionine + Sodium Metabisulfite

pH after preparation is 4.09

[0027] The results proved that when sodium metabisulfite was added to the injection, the content of related substances in azasetron hydrochloride injection would increase or even exceed the standard.

[0028]

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PUM

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Abstract

The invention discloses an azasetron hydrochloride injection. The injection comprises the following active components: azasetron, an antioxidant and sodium chloride, wherein the weight ratio of azasetron: the antioxidant: sodium chloride is 20:9:36; and the antioxidant is a mixture of thiourea and methionine. The invention also provides a preparation method of the injection. By changing a buffer system, adjusting the selection and the proportion of the antioxidant and selecting an inert gas in the invention, a good antioxidation effect is reached, so the instable defect of the azasetron hydrochloride injection is overcome.

Description

technical field [0001] The invention belongs to the technical field of medicine preparation, and in particular relates to azasetron hydrochloride injection and a preparation method thereof. Background technique [0002] Azasetron hydrochloride, alias N-(1-azabicyclo2.2.2oct-8-yl)-6-chloro-4-methyl-3-oxo-3,4-dihydro-2H-1, 4-Benzoxazine-8-carboxamide hydrochloride, is a colorless or almost colorless clear aqueous solution, molecular formula: Cl7H20ClN303·HCI, suitable for nausea, vomiting and gynecological and surgical procedures caused by cytotoxic drugs Nausea and vomiting caused by surgery. Its structural formula is as follows: [0003] [0004] Azasetron hydrochloride is a highly efficient, highly selective, new type of 5-HT 3 Receptor antagonist, via 5-HT on visceral afferents and central chemoreceptors 3 Significant inhibitory effect on the receptor, antagonizing the nausea and vomiting caused by tumor drugs and radiation therapy, and reducing the number of nausea...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/08A61K31/538A61K47/20A61K47/02A61P1/08
Inventor 杜军鲍黎
Owner ZHEJIANG WAN SHENG PHARMA CO LTD
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