Hydrochloric-acid tropisetron freeze-dried powder injection for injection and preparation method thereof

A technology of tropisetron hydrochloride and freeze-dried powder injection, which is applied in freeze-dried delivery, powder delivery, digestive system and other directions, can solve the problem that the safety of stabilizer medication is not fully guaranteed, and affects the oxidation rate, solubility, and product quality of the product. problems such as poor stability, to achieve the effect of good resolubility, suitable for industrial production, and improved drug safety

Active Publication Date: 2015-12-09
REYOUNG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] During the long-term storage of the existing tropisetron hydrochloride injections on the market, tropisetron hydrochloride is prone to oxidative degradation, resulting in a decrease in the content of the preparation, an increase in related substances, and a deepening of the color. The reason for this phenomenon is that this product is Indole derivatives, indole is converted into indigo by oxygen in the air when exposed to light (blue fluorescence will appear after the finished product is reconstituted), and continues to become indole quinone
The stability of this product is related to its own pH. This product is hydrochloride, and its stability is better when the pH is between 4.6 and 5.2. Low or high pH can affect the oxidation rate and solubility of the product. The manufacturer added glycine as a stabilizer to the injection, but the drug safety of the stabilizer is not fully guaranteed. At the same time, due to the need for high-temperature sterilization, the stability of the product is not good, and the related substances increase significantly after sterilization. In, the drug undergoes hydrolysis

Method used

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  • Hydrochloric-acid tropisetron freeze-dried powder injection for injection and preparation method thereof
  • Hydrochloric-acid tropisetron freeze-dried powder injection for injection and preparation method thereof
  • Hydrochloric-acid tropisetron freeze-dried powder injection for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] The formula of the tropisetron hydrochloride freeze-dried powder for injection consists of:

[0033]

[0034] Its preparation method:

[0035] (1) Measure 1500mL of water for injection and add it to the ingredient preparation container, add 30g of mannitol, 1g of citric acid, 2.6g of sodium citrate, and 0.5g of sodium chloride in sequence, stir until completely dissolved, and cool down to below 25°C;

[0036] (2) Add Tropisetron Hydrochloride 5.64g, stir until fully dissolved, and test its pH to be 4.8;

[0037] (3) Filling after sterilization and filtration, the filling volume is 2mL;

[0038] (4) Put the drug into the lyophilizer for pre-freezing at -42°C, maintain for 1h, raise the medium to -5°C, take 1h to rise to 40°C, maintain for 12h, raise the medium to 40°C, maintain for 3.5h, stop the machine after drying, and pass through aseptic Nitrogen, plugging;

[0039] (5) Capping, packaging, full inspection, and storage.

Embodiment 2

[0041]

[0042]

[0043] Its preparation method:

[0044] (1) Measure 1500mL of water for injection and add it to the ingredient preparation container, add 38g of mannitol, 1.2g of citric acid, 2.5g of sodium citrate, and 0.7g of sodium chloride in sequence, stir until completely dissolved, and cool down to below 25°C;

[0045] (2) Add Tropisetron Hydrochloride 5.64g, stir until fully dissolved, and test its pH to be 5.1;

[0046] (3) Filling after sterilization and filtration, the filling volume is 2mL;

[0047] (4) Put the drug into the lyophilizer for pre-freezing at -42°C, maintain it for 0.5h, raise the medium to -5°C, take 1.5h to raise it, then maintain it for 10h, raise the medium to 40°C, maintain it for 3h, stop the machine after drying, and pass without Bacterial nitrogen, plugging;

[0048] (5) Capping, packaging, full inspection, and storage.

Embodiment 3

[0050]

[0051] Its preparation method:

[0052] (1) Measure 1500mL of water for injection and add it to the ingredient preparation container, add 48g of mannitol, 1g of citric acid, 2.6g of sodium citrate, and 1g of sodium chloride in sequence, stir until completely dissolved, and cool down to below 25°C;

[0053] (2) Add Tropisetron Hydrochloride 5.64g, stir until fully dissolved, and test its pH to be 5.0;

[0054] (3) Filling after sterilization and filtration, the filling volume is 2mL;

[0055] (4) Put the drug into the lyophilizer for pre-freezing at -42°C, maintain for 1.5h, raise the medium to -5°C, take 1.5h to rise to and then maintain for 12h, raise the medium to 40°C, maintain for 4h, stop the machine after drying, pass without Bacterial nitrogen, plugging;

[0056] (5) Capping, packaging, full inspection, and storage.

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a hydrochloric-acid tropisetron freeze-dried powder injection for injection and a preparation method thereof. The hydrochloric-acid tropisetron freeze-dried powder injection comprises a medicinal active ingredient, excipients and pH (potential of hydrogen) stabilizers, wherein the medicinal active ingredient is hydrochloric-acid tropisetron, the excipients include mannitol and sodium chloride, and the pH stabilizers include citric acid and sodium citrate. According to the hydrochloric-acid tropisetron freeze-dried powder injection, the mannitol and the sodium chloride serve as the excipients, the pH value of a midbody solution is controlled to be stabilized within 4.6-5.2 by citric acid and sodium citrate buffer solutions, oxidation of a main drug is inhibited, and stability of the main drug is improved; in six months of an acceleration test, the injection is stable in content, changes of related substances are small, and the storage period of the injection is prolonged. The preparation method is simple in process and suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a tropisetron hydrochloride freeze-dried powder for injection and a preparation method thereof. Background technique [0002] Tropisetron hydrochloride is a commonly used drug for the prevention and treatment of nausea and vomiting caused by cancer chemotherapy and postoperative nausea and vomiting. A potent and highly selective competitive antagonist of systemic serotonin 3 (5-HT3) receptors, inhibits the gag reflex primarily by selectively blocking presynaptic 5-HT3 receptors in peripheral neurons. [0003] Intravenous injection of tropisetron hydrochloride in healthy volunteers, the elimination half-life (t1 / 2β) is about 7.3 to 30.3 hours, the apparent volume of distribution (V) is about 400 to 600 liters, and the protein binding rate is about 59 to 71%. The metabolism of tropisetron is related to spartine / polyisoquine (cytochrome P450 2D6), which is defic...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/46A61P1/08
Inventor 苗得足张光明艾全陈付杰张国明黄芳生王元英
Owner REYOUNG PHARMA
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